GUILFORD PHARMACEUTICALS INC
S-3/A, 1997-04-07
PHARMACEUTICAL PREPARATIONS
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<PAGE>   1
 
   
     AS FILED WITH THE SECURITIES AND EXCHANGE COMMISSION ON APRIL 7, 1997
    
 
                                                      REGISTRATION NO. 333-23001
================================================================================
 
                       SECURITIES AND EXCHANGE COMMISSION
                             WASHINGTON, D.C. 20549
                               ------------------
 
   
                                AMENDMENT NO. 3
    
 
                                       TO
 
                                    FORM S-3
                             REGISTRATION STATEMENT
 
                                     UNDER
 
                           THE SECURITIES ACT OF 1933
                               ------------------
 
                         GUILFORD PHARMACEUTICALS INC.
             (EXACT NAME OF REGISTRANT AS SPECIFIED IN ITS CHARTER)
 
<TABLE>
<S>                                                   <C>
                       DELAWARE                                             52-1841960
           (STATE OR OTHER JURISDICTION OF                               (I.R.S. EMPLOYER
            INCORPORATION OR ORGANIZATION)                            IDENTIFICATION NUMBER)
</TABLE>
 
                               ------------------
 
                             6611 TRIBUTARY STREET
                           BALTIMORE, MARYLAND 21224
                                 (410) 631-6300
  (ADDRESS, INCLUDING ZIP CODE, AND TELEPHONE NUMBER, INCLUDING AREA CODE, OF
                   REGISTRANT'S PRINCIPAL EXECUTIVE OFFICES)
 
                              CRAIG R. SMITH, M.D.
                            CHIEF EXECUTIVE OFFICER
                         GUILFORD PHARMACEUTICALS INC.
                             6611 TRIBUTARY STREET
                           BALTIMORE, MARYLAND 21224
                                 (410) 631-6300
 (NAME, ADDRESS, INCLUDING ZIP CODE, AND TELEPHONE NUMBER, INCLUDING AREA CODE,
                             OF AGENT FOR SERVICE)
                               ------------------
 
                                   Copies to:
<TABLE>
<S>                                                         <C>
                     MICHAEL J. SILVER                                            GREGORY C. SMITH
                   HOGAN & HARTSON L.L.P.                                           JAMIE CHUNG
             111 S. CALVERT STREET, SUITE 1600                                      TAMARA HINDS
                 BALTIMORE, MARYLAND 21202                                       COOLEY GODWARD LLP
                       (410) 659-2700                                      ONE MARITIME PLAZA, 20TH FLOOR
                                                                          SAN FRANCISCO, CALIFORNIA 94111
                                                                                   (415) 693-2000
</TABLE>
 
        APPROXIMATE DATE OF COMMENCEMENT OF PROPOSED SALE TO THE PUBLIC:
 
    As soon as practicable following the effective date of this Registration
                                   Statement.
 
     If the only securities being registered on this Form are being offered
pursuant to dividend or interest reinvestment plans, please check the following
box. [ ]
 
     If any of the securities being registered on this form are to be offered on
a delayed or continuous basis pursuant to Rule 415 under the Securities Act of
1933, other than securities offered only in connection with dividend or interest
reinvestment plans, check the following box. [ ]
 
     If this Form is filed to register additional securities for an offering
pursuant to Rule 462(b) under the Securities Act, please check the following box
and list the Securities Act registration statement number of the earlier
effective registration statement for the same offering. [ ]
 
     If this Form is a post-effective amendment filed pursuant to Rule 462(c)
under the Securities Act, check the following box and list the Securities Act
registration statement number of the earlier effective registration statement
for the same offering. [ ]
 
     If delivery of the prospectus is expected to be made pursuant to Rule 434,
please check the following box. [ ]
                               ------------------
 
     THE REGISTRANT HEREBY AMENDS THIS REGISTRATION STATEMENT ON SUCH DATE OR
DATES AS MAY BE NECESSARY TO DELAY ITS EFFECTIVE DATE UNTIL THE REGISTRANT SHALL
FILE A FURTHER AMENDMENT WHICH SPECIFICALLY STATES THAT THIS REGISTRATION
STATEMENT SHALL THEREAFTER BECOME EFFECTIVE IN ACCORDANCE WITH SECTION 8(a) OF
THE SECURITIES ACT OF 1933 OR UNTIL THIS REGISTRATION STATEMENT SHALL BECOME
EFFECTIVE ON SUCH DATE AS THE SECURITIES AND EXCHANGE COMMISSION, ACTING
PURSUANT TO SAID SECTION 8(a), MAY DETERMINE.
================================================================================
<PAGE>   2
 
     Information contained herein is subject to completion or amendment. A
     registration statement relating to these securities has been filed with the
     Securities and Exchange Commission. These securities may not be sold nor
     may offers to buy be accepted prior to the time the registration statement
     becomes effective. This prospectus shall not constitute an offer to sell or
     the solicitation of an offer to buy nor shall there be any sale of these
     securities in any State in which such offer, solicitation or sale would be
     unlawful prior to registration or qualification under the securities laws
     of any such State.
 
   
                   SUBJECT TO COMPLETION, DATED APRIL 7, 1997
    
 
                                3,250,000 SHARES
 
                                 [GUILFORD LOGO]
 
                                  COMMON STOCK
                            ------------------------
 
     All of the shares of Common Stock offered hereby are being sold by Guilford
Pharmaceuticals Inc. The Company's Common Stock is listed on the Nasdaq National
Market under the symbol "GLFD." On March 12, 1997, the last reported sale price
of the Common Stock on the Nasdaq National Market was $27.25 per share.
 
        THE COMMON STOCK OFFERED HEREBY INVOLVES A HIGH DEGREE OF RISK.
                    SEE "RISK FACTORS" BEGINNING ON PAGE 7.
                            ------------------------
   THESE SECURITIES HAVE NOT BEEN APPROVED OR DISAPPROVED BY THE SECURITIES
      AND EXCHANGE COMMISSION OR ANY STATE SECURITIES COMMISSION NOR HAS
        THE SECURITIES AND EXCHANGE COMMISSION OR ANY STATE SECURITIES
           COMMISSION PASSED UPON THE ACCURACY OR ADEQUACY OF THIS
             PROSPECTUS. ANY REPRESENTATION TO THE CONTRARY IS A
                               CRIMINAL OFFENSE.
<TABLE>
<CAPTION>
=======================================================================================================
                                                    PRICE           UNDERWRITING         PROCEEDS TO
                                                  TO PUBLIC          DISCOUNT(1)         COMPANY(2)
<S>                                           <C>                 <C>                 <C>
- -------------------------------------------------------------------------------------------------------
Per Share...................................          $                   $                   $
Total(3)....................................          $                   $                   $
=======================================================================================================
</TABLE>
 
(1) See "Underwriting" for information concerning indemnification of the
    Underwriters and other information.
 
(2) Before deducting expenses of the offering payable by the Company estimated
    at $300,000.
 
(3) The Company has granted the Underwriters an option, exercisable within 30
    days of the date hereof, to purchase up to 487,500 additional shares of
    Common Stock at the Price to Public per share, less the Underwriting
    Discount, for the purpose of covering over-allotments, if any. If the
    Underwriters exercise such option in full, the total Price to Public,
    Underwriting Discount and Proceeds to Company will be $          ,
    $          and $          , respectively. See "Underwriting."
                            ------------------------
 
     The shares of Common Stock are offered severally by the Underwriters when,
as and if delivered to and accepted by them, subject to their right to withdraw,
cancel or reject orders in whole or in part and subject to certain other
conditions. It is expected that delivery of the certificates representing the
shares will be made against payment on or about           , 1997 at the office
of Oppenheimer & Co., Inc., Oppenheimer Tower, World Financial Center, New York,
New York 10281.
                            ------------------------
 
OPPENHEIMER & CO., INC.
                                 ALEX. BROWN & SONS
                                       INCORPORATED
                                                     HAMBRECHT & QUIST
 
                  The date of this Prospectus is        , 1997
<PAGE>   3
 
                INCORPORATION OF CERTAIN DOCUMENTS BY REFERENCE
 
   
     The following documents filed by the Company with the Securities and
Exchange Commission (the "Commission") pursuant to the Securities Exchange Act
of 1934, as amended (the "Exchange Act") are incorporated herein by reference
and made a part hereof: the Company's Annual Report on Form 10-K for the year
ended December 31, 1996, and the amendment thereto filed on March 14, 1997, and
the description of the Company's Common Stock set forth in the Company's
Registration Statement on Form 8-A filed under the Exchange Act on March 25,
1994 and all amendments and reports filed for the purpose of updating such
description including without limitation a Form 8-K filed on April 4, 1997. All
documents filed by the Company with the Commission pursuant to Sections 13(a) of
the Exchange Act and any definitive proxy statement so filed pursuant to Section
14 of the Exchange Act and any reports filed pursuant to Section 15(d) of the
Exchange Act after the date of this Prospectus and prior to the termination of
the offering of the Common Stock shall be deemed to be incorporated by reference
into this Prospectus and to be a part hereof from the date of filing of such
documents. Any statement contained in a document incorporated by reference
herein shall be deemed to be modified or superseded for purposes of this
Prospectus to the extent that a statement contained herein or in any other
subsequently filed document which is incorporated by reference herein modifies
or supersedes such earlier statement. Any such statement so modified or
superseded shall not be deemed, except as so modified or superseded, to
constitute a part of this Prospectus. Copies of all documents incorporated by
reference herein (other than exhibits to such documents which are not
specifically incorporated by reference into such documents) will be provided
without charge to each person who receives a copy of this Prospectus, upon
request of such person, directed to Thomas C. Seoh, Vice President, General
Counsel and Secretary, Guilford Pharmaceuticals Inc., 6611 Tributary Street,
Baltimore, Maryland 21224 (telephone (410) 631-6300).
    
 
     To the extent that any proxy statement is incorporated by reference herein,
such incorporation shall not include any information contained in such proxy
statement that is not, pursuant to the Commission's rules, deemed to be "filed"
with the Commission or subject to the liabilities of Section 18 of the Exchange
Act.
 
     GLIADEL(R) and DOPASCAN(R) are registered trademarks of the Company. All
other brand names or trademarks appearing in this Prospectus are the property of
their respective holders. Guilford was incorporated in Delaware on July 14,
1993. The Company's executive offices are located at 6611 Tributary Street,
Baltimore, Maryland 21224, and its telephone number is (410) 631-6300. As used
herein, unless the context otherwise requires, Guilford Pharmaceuticals Inc.
("Guilford" or the "Company") shall include Guilford and its subsidiaries.
 
   
     IN CONNECTION WITH THIS OFFERING, THE UNDERWRITERS AND OTHER SELLING GROUP
MEMBERS MAY ENGAGE IN PASSIVE AND OTHER MARKET MAKING TRANSACTIONS IN THE COMMON
STOCK ON THE NASDAQ NATIONAL MARKET IN ACCORDANCE WITH RULE 103 OF REGULATION M
UNDER THE EXCHANGE ACT AND OTHERWISE. SEE "UNDERWRITING."
    
 
     CERTAIN PERSONS PARTICIPATING IN THIS OFFERING MAY ENGAGE IN TRANSACTIONS
THAT STABILIZE, MAINTAIN, OR OTHERWISE AFFECT THE PRICE OF THE COMMON STOCK,
INCLUDING BY ENTERING STABILIZING BIDS OR EFFECTING SYNDICATE COVERING
TRANSACTIONS. FOR A DESCRIPTION OF THESE ACTIVITIES, SEE "UNDERWRITING."
 
                                        2
<PAGE>   4
 
                               PROSPECTUS SUMMARY
 
     The following summary is qualified in its entirety by the more detailed
information and the Consolidated Financial Statements and Notes thereto
appearing elsewhere in this Prospectus. Investment in the securities offered
hereby involves a high degree of risk. See "Risk Factors." Unless otherwise
noted, all information in this Prospectus assumes no exercise of the
Underwriters' over-allotment option. This Prospectus contains forward-looking
statements, including, but not limited to, those concerning the commencement and
completion of clinical trials, the Company's strategic plans, anticipated
expenditures and the need for additional funds, which involve risks and
uncertainties. The Company's actual results may differ significantly from the
results discussed in the forward-looking statements. Factors that could cause or
contribute to such differences include, but are not limited to, those discussed
in "Risk Factors" as well as those discussed elsewhere in this Prospectus.
 
                                  THE COMPANY
 
     Guilford is a biopharmaceutical company engaged in the development and
commercialization of novel products in two principal areas: (i) targeted and
controlled drug delivery systems using proprietary biodegradable polymers for
the treatment of cancer and other diseases; and (ii) therapeutic and diagnostic
products for neurological diseases and conditions.
 
     The Company's first product in its drug delivery business is GLIADEL(R)
Wafer ("GLIADEL"), a novel treatment for glioblastoma multiforme, the most
common and rapidly fatal form of brain cancer. GLIADEL was cleared for marketing
by the United States Food and Drug Administration (the "FDA") in September 1996
for use as an adjunct to surgery to prolong survival in patients with recurrent
glioblastoma multiforme for whom surgical resection is indicated. GLIADEL was
commercially launched in the United States on February 25, 1997 by the Company's
marketing partner, Rhone-Poulenc Rorer Pharmaceuticals, Inc. (collectively with
its parent, Rhone-Poulenc Rorer, Inc., "RPR"). The Company's lead neurological
product candidate is DOPASCAN(R) Injection ("DOPASCAN"), a radiolabeled tropane
derivative that is being developed for the diagnosis and monitoring of
Parkinson's disease. The Company has completed enrollment in a multi-center
Phase II clinical trial of DOPASCAN in the United States and is preparing to
commence Phase III clinical trials later this year. The Company also is
developing other neurological product candidates, including: (i) neurotrophic
drugs to promote nerve growth and repair, which may have applications for spinal
cord injuries, peripheral neuropathies and neurodegenerative diseases, such as
Alzheimer's disease and Parkinson's disease; (ii) neuroprotective drugs to
reduce neuronal damage due to stroke or severe head trauma; and (iii) drugs to
treat addictive disorders.
 
DRUG DELIVERY BUSINESS
 
     The Company's drug delivery business currently involves the use of
biodegradable polymers for targeted and controlled delivery of chemotherapeutic
drugs to treat cancer. The Company believes that delivering high drug
concentrations locally for a sustained period of time will increase the efficacy
of chemotherapy in controlling tumor growth and will decrease the side effects
associated with systemic drug administration. Guilford has developed expertise
in the product development, clinical development and manufacturing of
polymer-based drug delivery products.
 
     GLIADEL.  GLIADEL is a novel drug delivery system consisting of a patented
biodegradable polymer that contains the chemotherapeutic drug BCNU (carmustine).
GLIADEL is a targeted and controlled drug delivery system that is implanted in
the surgical cavity following brain tumor resection. This route of
administration overcomes limitations of systemic chemotherapy with BCNU by
delivering high concentrations of the drug directly to the tumor site for an
extended period without exposing the rest of the body to the toxic effects of
the drug. GLIADEL is used to complement standard therapy with surgery, radiation
therapy and systemic chemotherapy in patients with recurrent glioblastoma
multiforme. GLIADEL was shown in a North American Phase III clinical trial to
increase the six-month survival rate by more than 50% in these patients.
 
                                        3
<PAGE>   5
 
     In June 1996, the Company entered into a strategic agreement with RPR
granting RPR the worldwide (excluding Scandinavia) rights to market, sell and
distribute GLIADEL. During 1996, RPR paid Guilford $27.5 million in rights and
milestone payments, made a $7.5 million equity investment in Guilford Common
Stock and extended to the Company a $7.5 million line of credit. Under the
agreements with RPR, Guilford receives a combined transfer price and royalty of
35% to 40% of the net sales of GLIADEL. Guilford could earn additional payments
totaling up to $40.0 million, subject to achievement of certain milestone
events.
 
     GLIADEL was cleared for marketing by the FDA in September 1996 and launched
commercially in the United States in February 1997 by RPR through its existing
oncology sales force. Prior to launch, GLIADEL was available to neurosurgeons in
the United States under a Treatment Investigational New Drug Application
("Treatment IND") cleared by the FDA. The Treatment IND protocol was approved in
over 170 hospitals in the United States and more than 450 treatments were
distributed.
 
     Guilford and RPR have initiated a series of new clinical trials for the
purpose of seeking to expand the market for GLIADEL. A Phase III randomized,
double-blind, placebo-controlled trial in patients undergoing initial surgery
for malignant glioma is planned to commence in mid-1997. In addition, Guilford
has initiated a Phase I clinical trial to test the safety of escalating the
concentration of BCNU in GLIADEL from 3.85% to 20%, following preclinical
studies suggesting that higher concentrations of BCNU in GLIADEL may be even
more effective and appear to be safe.
 
     Other Polymer-Based Drug Delivery Products.  The Company intends to broaden
its line of polymer-based drug delivery products and has research and
preclinical studies underway. These programs include new polymer configurations
and the use of other chemotherapeutic agents such as paclitaxel (Taxol(R)) and
camptothecin in a variety of polymer systems. The Company has entered into
collaborations with scientists at The Johns Hopkins University ("Johns Hopkins")
and The Massachusetts Institute of Technology ("MIT") to discover new polymers
and to advise the Company on new product development. In addition, Guilford and
RPR are evaluating the opportunity to incorporate RPR's proprietary
chemotherapeutics in Guilford's proprietary polymer systems.
 
NEUROLOGICAL PRODUCTS PROGRAM
 
     DOPASCAN.  DOPASCAN is a radiolabeled tropane derivative that the Company
is developing for the diagnosis and monitoring of Parkinson's disease.
Parkinson's disease is a common neurodegenerative disorder afflicting more than
600,000 patients in the United States. Distinguishing Parkinson's disease from
other conditions is typically difficult in the early stages of the disease and
frequently requires observation over months or years. By improving the ability
of physicians to distinguish Parkinson's disease from similar disorders at an
early stage and enabling physicians to monitor the progression of the disease,
DOPASCAN may improve therapy by allowing for more appropriate drug selection and
dosing. To date, over 1,000 patients have been imaged in the United States and
Europe using DOPASCAN. In initial United States Phase II trials, DOPASCAN
accurately differentiated patients clinically diagnosed with Parkinson's disease
from those without the disease. The Company has completed enrollment in a
multi-center Phase II clinical trial of DOPASCAN in the United States and the
study report is expected to be available in the second quarter of 1997. Guilford
expects to commence Phase III clinical trials of DOPASCAN in North America prior
to the end of 1997. The Company has entered into an agreement with Daiichi
Radioisotope Laboratories Ltd. ("DRL"), a leading Japanese radiopharmaceutical
company, to develop and commercialize DOPASCAN in Japan, Korea and Taiwan. The
Company intends to seek partners for distribution of this product in other
territories, including the United States and Europe.
 
     Neurotrophic Drugs.  Guilford is developing small molecule, orally
bioavailable compounds to promote nerve growth and repair for the treatment of
neurodegenerative disorders (such as Alzheimer's disease and Parkinson's
disease), multiple sclerosis, spinal cord injuries, stroke, and peripheral
neuropathies. Scientists at Johns Hopkins discovered that commonly used
immunosuppressive drugs such as tacrolimus (FK-506) and cyclosporin A can
promote nerve growth. Guilford and Johns Hopkins scientists further discovered
that the mechanism of nerve growth promotion is independent of the mechanism
responsible for immunosuppression. The Company has synthesized multiple series
of proprietary small molecule neuroimmunophilin ligands that
 
                                        4
<PAGE>   6
 
promote nerve growth without being immunosuppressive. The Company has filed
numerous patent applications in the United States and internationally relating
to both novel compositions and methods of treating neurological disorders
utilizing these compounds and has been issued one United States patent for the
compositions and uses of a series of neuroimmunophilin ligands as neurotrophic
agents for the treatment of neurodegenerative disorders. Results from in vivo
experiments with GPI-1046, one of the Company's lead neurotrophic compounds,
were published in the March 4, 1997 issue of the Proceedings of the National
Academy of Sciences. These experiments demonstrated that GPI-1046 induced
significant nerve regeneration and functional recovery in animal models of both
central neuronal degeneration and peripheral nerve damage. In addition, these
compounds exhibited systemic activity, oral bioavailability and the ability to
cross the blood-brain barrier, unlike many naturally-occurring nerve growth
factors. The Company is engaged in preclinical development of its neurotrophic
compounds and intends to commence preliminary clinical trials with one of its
lead compounds in late 1997 or early 1998. The Company is currently in
discussions with several multinational pharmaceutical companies regarding a
collaboration for this program.
 
     Neuroprotective Drugs.  Guilford is developing novel compounds to protect
brain cells against damage from ischemia (the lack of oxygen delivery from
reduced blood flow) and other disorders which cause damage due to massive
release of excitatory amino acid neurotransmitters such as glutamate. The
Company's approach is to identify and clinically test compounds that have the
ability to intervene at three distinct steps in a biochemical pathway leading to
neuronal damage: (i) pre-synaptic inhibition of glutamate; (ii) inhibition of
nitric oxide synthase ("NOS"); and (iii) inhibition of poly-ADP-ribosyl
synthetase ("PARS"). Guilford has discovered a novel mechanism for the
pre-synaptic inhibition of the neurotransmitter glutamate and is currently
testing compounds in animal models of stroke and neurological disorders believed
to be associated with glutamate toxicity, such as amyotrophic lateral sclerosis
("ALS"), epilepsy, severe head trauma and Parkinson's disease. Certain of these
compounds have shown significant neuroprotective activity in these preclinical
models.
 
     Addiction Therapeutics.  Through the Company's subsidiary, Gell
Pharmaceuticals Inc. ("Gell"), the Company is focusing on the development of
therapeutics for cocaine addiction and other addictive behaviors. The Company's
scientists have identified and synthesized novel compounds with specificity for
the cocaine recognition site in the brain and filed patent applications covering
several classes of such compounds. These compounds block certain physiological
effects of cocaine and cocaine-seeking behavior in animals addicted to cocaine.
The Company is currently investigating whether this approach can be applied to
other forms of addictive behavior, such as nicotine addiction.
 
STRATEGY
 
     Guilford's strategy in its drug delivery business is to capitalize on the
FDA clearance and commercial launch of GLIADEL and the Company's relationship
with RPR, Johns Hopkins and MIT, by seeking to broaden the treatment indications
of GLIADEL and introducing new polymer-based drug delivery products. The Company
believes that its expertise in the discovery, development and manufacturing of
polymer-based drug delivery products positions Guilford to develop or acquire
new drug delivery technologies that could be complementary to GLIADEL. In its
neurological products business, Guilford plans to continue to develop novel
diagnostic and therapeutic product candidates that offer unique advantages over
competing products and technologies. Guilford will actively seek corporate
partners for these programs in order to minimize the costs and risks associated
with clinical development, capitalize on the capabilities of its partners and
enhance commercialization opportunities for its product candidates. Guilford
will seek to retain co-promotion rights for certain of its products in the
United States. At present, the Company does not intend to manufacture its small
molecule compounds.
 
                                        5
<PAGE>   7
 
                                  THE OFFERING
 
<TABLE>
<S>                                             <C>
Common Stock offered.........................   3,250,000 shares
Common Stock to be outstanding after the
  offering...................................   17,979,490 shares (1)
Use of proceeds..............................   Further clinical development of DOPASCAN; re-
                                                search, preclinical and clinical development
                                                of neurotrophic and neuroprotective product
                                                candidates; expansion of the Company's drug
                                                delivery business; working capital; and
                                                possible acquisitions of complementary
                                                businesses or technologies. See "Use of
                                                Proceeds."
Nasdaq National Market symbol................   GLFD
</TABLE>
 
                   SUMMARY CONSOLIDATED FINANCIAL INFORMATION
                     (IN THOUSANDS, EXCEPT PER SHARE DATA)
 
<TABLE>
<CAPTION>
                                                                           YEARS ENDED DECEMBER 31,
                                                                        ------------------------------
                                                                         1994        1995       1996
                                                                        -------    --------    -------
<S>                                                                     <C>        <C>         <C>
STATEMENT OF OPERATIONS DATA:
Total revenues.......................................................   $    --    $    586    $28,020
Expenses:
    Research and development.........................................     2,869       9,688     18,761
    General and administrative.......................................     2,369       4,367      6,736
    Compensation expense -- warrants.................................       991          --         --
                                                                        -------    --------    -------
         Total operating expenses....................................     6,229      14,055     25,497
                                                                        -------    --------    -------
    Income (loss) from operations....................................    (6,229)    (13,469)     2,523
    Other income, net................................................       332         832      2,550
                                                                        -------    --------    -------
Net income (loss)....................................................   $(5,897)   $(12,637)   $ 5,073
                                                                        =======    ========    ======= 
Primary earnings (loss) per common share (2).........................   $ (1.36)   $  (1.70)   $  0.35
                                                                        =======    ========    ======= 
Weighted average common and common equivalent shares used to compute
  earnings (loss) per common share (2)...............................     4,332       7,436     14,634
Fully diluted earnings (loss) per common share.......................   $ (1.36)   $  (1.70)   $  0.34
                                                                        =======    ========    ======= 
Weighted average common and common equivalent shares used to compute
  fully diluted earnings (loss) per common share (2).................     4,332       7,436     15,140
</TABLE>
 
<TABLE>
<CAPTION>
                                                                                DECEMBER 31, 1996
                                                                            --------------------------
                                                                            ACTUAL     AS ADJUSTED (4)
                                                                            -------    ---------------
<S>                                                                         <C>        <C>
BALANCE SHEET DATA:
Cash, cash equivalents and investments (3)...............................   $77,439       $ 161,052
Total assets (3).........................................................    93,659         177,272
Long-term debt...........................................................    10,905          10,905
Total stockholders' equity...............................................    75,877         159,490
</TABLE>
 
- ---------------
(1) Based upon the shares outstanding on December 31, 1996. Includes 750,000
    shares issued to The Abell Foundation, Inc. ("Abell") on March 5, 1997 upon
    exercise of its put right with respect to its ownership interest in Gell.
    Excludes: (i) 2,494,756 shares of Common Stock issuable upon the exercise of
    options outstanding on December 31, 1996 at a weighted average exercise
    price of $12.43 per share; and (ii) 312,934 shares of Common Stock issuable
    upon exercise of outstanding warrants at a weighted average exercise price
    of $7.19 per share.
 
(2) For information concerning the calculation of earnings (loss) per share, see
    Note 2 of Notes to Consolidated Financial Statements.
 
(3) Includes restricted investments of $10.1 million at December 31, 1996. See
    Note 6 of Notes to Consolidated Financial Statements.
 
(4) Adjusted to reflect the sale of 3,250,000 shares of Common Stock offered
    hereby at an assumed offering price of $27.25 per share and the receipt of
    the estimated net proceeds therefrom. See "Use of Proceeds" and
    "Capitalization."
 
                                        6
<PAGE>   8
 
                                  RISK FACTORS
 
     An investment in the shares of Common Stock offered hereby is speculative
in nature and involves a high degree of risk. In addition to the other
information contained in this Prospectus, the following factors should be
considered carefully in evaluating the Company and its business before
purchasing the shares of Common Stock offered hereby. This Prospectus contains,
in addition to historical information, forward-looking statements, including,
but not limited to, those concerning the commencement and completion of clinical
trials, the Company's strategic plans, anticipated expenditures and the need for
additional funds that involve risks and uncertainties. The Company's actual
results could differ materially. Factors that could cause or contribute to such
differences include, but are not limited to, those discussed below, as well as
those discussed elsewhere in this Prospectus.
 
     History of Losses; Uncertainty of Future Profitability.  The Company
incurred net operating losses from its inception through the first quarter of
1996 and for the fourth quarter of 1996 and, as of December 31, 1996, had an
accumulated deficit of $14.9 million. To date, substantially all of the
Company's revenues have been recognized as research and development or milestone
payments under the Company's collaborations. Except for GLIADEL, the Company's
product candidates are not expected to generate revenues for at least the next
several years, if at all, and whether GLIADEL sales will generate any
significant revenues is highly uncertain. While the Company reported net income
for the second and third quarters of 1996, this income was the result of
significant and non-recurring payments from RPR with respect to GLIADEL. The
Company does not anticipate that 1997 will be profitable, and there can be no
assurance that the Company will ever achieve or sustain profitability in the
future. Furthermore, the Company expects to experience quarter-to-quarter and
year-to-year fluctuations in its operating results due to a variety of factors,
including, but not limited to, the timing and amount of sales of GLIADEL, the
timing and realization of milestone and other payments under the Company's
collaborative agreements and expenses relating to the Company's research and
development, clinical and manufacturing activities. The Company's ability to
realize sustained profitability in the future will depend upon, among other
things, the successful marketing of GLIADEL by RPR, receipt of regulatory
clearance for additional indications for GLIADEL, and the successful completion
of clinical trials for and, if completed, receipt of regulatory clearance for
the marketing of, DOPASCAN. In addition, the Company must enter into
collaborative arrangements and license agreements on acceptable terms with
others with respect to its product candidates as they are developed. The Company
will be required to conduct substantial additional research, development and
clinical trials and to receive necessary regulatory clearances that, together
with future general and administrative expenses, are expected to result in
significant expenses for the foreseeable future. No assurance can be given as to
the ability of the Company to achieve significant and sustained revenues or
realize sustained profitable operating results. See "Management's Discussion and
Analysis of Financial Condition and Results of Operations."
 
     Dependence on GLIADEL and RPR.  The Company's prospects are highly
dependent on sales by RPR of the Company's first commercial product, GLIADEL,
which was commercially launched on February 25, 1997. Because of the very recent
commercial launch, there is effectively no information upon which to assess the
ability of the product to gain market acceptance or the extent of the marketing
efforts necessary to gain any such acceptance. The failure of GLIADEL to gain
market acceptance would have a material adverse effect on the Company's
business, financial condition and results of operations.
 
     To date, the Company has received clearance from the FDA to market GLIADEL
only for patients with recurrent glioblastoma multiforme for whom surgical
resection is indicated. The number of patients undergoing surgery for recurrent
glioblastoma multiforme is very limited. The Company believes that the total
number of patients in the United States who undergo surgery for recurrent
glioblastoma multiforme may be less than 10,000 per year. In order to expand the
indications for which GLIADEL may be used, the Company and RPR must successfully
complete additional lengthy clinical trials and thereafter receive clearance
from the FDA. No assurance can be given as to the ability of the Company or RPR
to successfully complete these clinical trials and to receive appropriate
regulatory clearance on a timely basis, or at all, and the inability to do so
would have a material adverse effect on the Company's business, financial
condition and results of operations. To date, the Company has received no
international regulatory approvals to market GLIADEL and there can be no
assurance that any such approvals will be obtained.
 
                                        7
<PAGE>   9
 
     The Company granted RPR exclusive worldwide (excluding Scandinavia)
marketing, sales and distribution rights for GLIADEL. The Company's agreements
with RPR do not impose any minimum purchase or sale requirements on RPR.
Therefore, the success of GLIADEL is entirely dependent upon the sales and
marketing efforts of RPR. The Company has no prior experience in dealing with
RPR for the sale of any products and RPR's oncology sales force has no prior
experience in marketing a product to neurosurgeons. There can be no assurance
that RPR will elect to aggressively market and promote GLIADEL and will
successfully do so, and the inability or unwillingness of RPR to do so would
have a material adverse effect on the Company's business, financial condition
and results of operations.
 
     The Company's agreements with RPR provide for additional payments to the
Company upon the timely achievement of designated milestones relating to further
clinical development and regulatory approvals. In many instances, achievement of
the milestone is dependent on the efforts of RPR. No assurance can be given that
any of these milestones will be satisfied in such a manner as will allow the
Company to become entitled to these payments. The potential milestone payments
under the RPR agreements are significant. Therefore, failure to meet the
milestones under the agreements could have a material adverse effect on the
Company's business, financial condition and results of operations. See
"Business -- Product and Development Programs -- Drug Delivery Business" and
"-- Sales, Marketing and Distribution."
 
     Reliance on Suppliers.  The Company currently is able to purchase certain
key components for GLIADEL and its product candidates only from single
suppliers. These suppliers are subject to many strict regulatory requirements.
There can be no assurance that these suppliers will comply, or have complied,
with applicable regulatory requirements or that they will otherwise continue to
supply the Company with the key components for its product candidates. In the
event that suppliers are unable or refuse to supply the Company, or will supply
the Company only at a prohibitive cost, there can be no assurance that the
Company could access additional sources at acceptable prices, on a timely basis,
or at all. The current formulation of GLIADEL utilizes BCNU (carmustine) as its
chemotherapeutic agent. BCNU is currently available only from a single source in
the United States and the Company is not aware of any supplier outside of the
United States. The Company currently obtains its BCNU from this United States
supplier on a purchase order basis and not pursuant to any long-term supply
agreement. While the Company is taking steps to obtain an additional supplier,
the process of qualifying a second supplier is lengthy, and there can be no
assurance that the Company's efforts will be successful. Failure to receive key
supplies necessary for the manufacture of GLIADEL on a timely basis at a
reasonable cost could result in delays of product shipments, which would have a
material adverse effect on the Company's business, financial condition and
results of operations. The manufacture of DOPASCAN requires a precursor to be
labeled with a radioactive isotope of iodine to form the final product. Only a
limited number of companies are capable of performing the necessary
radioiodination of the precursor and distribution of the final radioiodinated
product. While the Company currently has a development and supply arrangement
with one of these companies, there can be no assurance that the Company, if
necessary or desirable, will be able to enter into an agreement with another of
these companies for the radioiodination of the precursor on acceptable terms, or
at all, or that the Company's current supplier will meet the Company's need for
DOPASCAN. See "Business -- Manufacturing and Raw Materials."
 
     Limited Manufacturing Capabilities.  To commercialize GLIADEL, the Company
must be able to manufacture this product in commercial quantities in compliance
with regulatory requirements and at acceptable costs. The Company is
manufacturing GLIADEL at its manufacturing facility in Baltimore, Maryland,
which consists of production laboratories and a cleanroom occupying
approximately 12,500 square feet. The facility currently has the capacity to
manufacture approximately 8,000 GLIADEL treatments per year. The Company is
expanding the facility to increase capacity to approximately 30,000 treatments
per year in 1998. There can be no assurance that this expansion will be
successfully accomplished, or if so, whether such capacity will be sufficient to
meet demand. Although the Company believes the facility meets Good Manufacturing
Practices ("GMP") requirements and the facility has been inspected by the FDA,
the Company has manufactured only limited quantities of GLIADEL in the facility.
There can be no assurance that the Company will be able to continue to satisfy
applicable regulatory standards, including GMP requirements, and other
requirements relating to the manufacture of GLIADEL in the facility. The Company
also faces risks inherent in the operation of a single facility for manufacture
of GLIADEL, including risks of
 
                                        8
<PAGE>   10
 
unforeseen plant shutdowns due to personnel, equipment or other factors, and the
possible inability of the facility to produce GLIADEL in quantities sufficient
to meet demand. Any delay in the manufacturing of GLIADEL could result in delays
of product shipments, which would have a material adverse effect on the
Company's business, financial condition and results of operations.
 
     Currently, the Company has no manufacturing capabilities for its product
candidates, and in order to complete the commercialization process of its
product candidates, the Company must either acquire, build or expand its
manufacturing facilities or rely on third parties to manufacture product
candidates. There can be no assurance that the Company will be able to acquire,
build or expand facilities that will meet the Company's quality, quantity and
timing requirements on acceptable terms, or at all, or that the Company will be
able to enter into manufacturing contracts with others on acceptable terms, or
at all, and the inability of the Company to do so could have a material adverse
effect on the Company's business, financial condition and results of operations.
Third-party manufacturers must also comply with FDA, United States Drug
Enforcement Administration ("DEA") and other regulatory requirements for their
facilities, including GMP regulations. Moreover, there can be no assurance that
the manufacturing of product candidates on a limited basis for investigational
use will lead to a successful transition to commercial, large scale production.
Small changes in methods of manufacture may affect the safety, efficacy or
controlled release of the product. Changes in methods of manufacture, including
commercial scale-up, can, among other things, require the performance of new
clinical studies. Should the Company decide to manufacture its other product
candidates, substantial start-up expenses would be incurred, expansion of
facilities would be required and additional personnel would have to be hired.
See "Business -- Manufacturing and Raw Materials."
 
     Technological Uncertainties.  Except for GLIADEL, the Company does not
expect to generate revenues from product sales for at least the next several
years, if at all. Substantially all of the Company's resources have been, and
for the foreseeable future will continue to be, dedicated to the discovery,
development and commercialization of proprietary products for the diagnosis,
treatment and prevention of neurological diseases and conditions and for
targeted, controlled drug delivery using biodegradable polymers for the
treatment of cancer and other diseases. The Company's product candidates will
require additional development, extensive preclinical and clinical trials,
regulatory approval and additional investment prior to any commercialization. In
certain cases, the Company's compounds, such as GPI-5000, GPI-6000 and GPI-2138,
are "prototypes," which the Company is using to establish proof of principle of
the relevant mechanism of action, but which the Company does not intend to
develop into a product, because of pharmacokinetic characteristics of the
compound, the Company's proprietary position with respect to such compound or
for other reasons. There can be no assurance that the Company's product
development efforts will progress as expected, or at all. In addition, the
Company's product candidates are subject to the risks of failure inherent in the
development of products based on new technologies. These risks include the
possibilities that the Company's new approaches to the diagnosis, treatment and
prevention of neurological diseases and conditions and targeted, controlled drug
delivery will not result in any products that gain market acceptance; that any
or all of the Company's product candidates will be found to be unsafe,
ineffective, or otherwise fail to receive necessary regulatory clearances or, if
granted, such clearances will not be revoked; that any or all of the products,
if safe and effective, will be difficult to manufacture on a large scale or
uneconomical to market; that proprietary rights of third parties will preclude
the Company from marketing such products; or that third parties will market
superior or more cost-effective products. As a result, there can be no assurance
that the Company's activities will result in any commercially viable products.
See "Business -- Patents and Proprietary Technology" and "-- Competition."
 
     Need for Additional Partners.  The Company's strategy for the research,
development and commercialization of its product candidates has required, and
will continue to require, the Company to enter into various arrangements with
corporate and academic collaborators, licensors, licensees and others, and the
Company will, therefore, be dependent upon the success of these parties in
performing their responsibilities and obligations. The Company is actively
seeking partners to assist in the development of DOPASCAN as well as lead
compounds in the Company's neurotrophic drug program. There can be no assurance
that the Company will be able to enter into collaborative arrangements or
license agreements that the Company deems necessary or appropriate to develop
and commercialize its product candidates, or that any or all of the contemplated
 
                                        9
<PAGE>   11
 
benefits from such collaborative arrangements or license agreements will be
realized. Failure to obtain such arrangements or agreements could result in
delays in marketing the Company's product candidates or the inability to proceed
with the development, manufacture or sale of product candidates. Certain of the
collaborative arrangements that the Company currently has or may enter into in
the future may place responsibility on the collaborative partner for preclinical
testing, clinical trials and/or preparation and submission of applications for
regulatory approval of potential pharmaceutical or other products. Should a
collaborative partner fail to develop or commercialize successfully any product
candidate to which it has rights, the Company's business, financial condition
and results of operations could be materially and adversely affected. There can
be no assurance that collaborators will not pursue alternative technologies or
product candidates either on their own or in collaboration with others,
including the Company's competitors, as a means for developing treatments for
the diseases or disorders targeted by the Company's collaborative arrangements.
Collaborative arrangements may also require the Company to meet certain
regulatory, research or other development milestones and expend minimum levels
of funds, and there can be no assurance that the Company will be successful in
doing so. Failure of the Company to meet its obligations under its collaborative
arrangements could result in a termination of those arrangements and could have
a material adverse effect on the Company's business, financial condition and
results of operations. See "Business -- Sales, Marketing and Distribution" and
"-- Technology Licensing Agreements."
 
     Likely Volatility of Stock Price.  The market price of the Company's Common
Stock has been and is likely to continue to be highly volatile, and an
investment in these securities involves substantial risks. The market prices for
securities of biotechnology companies (including the Company) have been highly
volatile, and the stock market from time to time has experienced significant
price and volume fluctuations that may be unrelated to the operating performance
of a particular company. A number of factors could result in the Company's
failure to meet the expectations of securities analysts or investors and may
have a significant impact on the price of the Company's Common Stock. Such
factors include, but are not limited to, announcements by the Company or its
competitors of clinical results, technological innovations, product sales, new
products or product candidates, developments or disputes concerning patent or
proprietary rights, regulatory developments affecting the Company's products, as
well as market conditions for emerging growth companies and biopharmaceutical
companies, economic and other internal and external factors and period-to-period
fluctuations in results of operations. See "Price Range of Common Stock and
Dividend Policy."
 
     Uncertainty Regarding Patents and Proprietary Technology.  The Company's
success will depend in part on its ability to obtain, maintain and enforce
patent protection for its products and processes or license rights to patents,
maintain trade secret protection and operate without infringing upon the
proprietary rights of others. The degree of patent protection afforded to
pharmaceutical and biotechnological inventions is uncertain, and a number of
Guilford's product candidates are subject to this uncertainty. Guilford is aware
of a company which has asserted in a public filing that it has patent
applications claiming the use of certain of its immunosuppressive compounds and
certain multidrug resistance compounds for nerve growth applications, as well as
a patent and patent applications relating to compounds which it claims are
useful in nerve growth applications. While the Company does not believe that its
neurotrophic compounds infringe on such company's patent, no assurance can be
given as to the ability of Guilford's patents and patent applications to
adequately protect its neurotrophic product candidates, including GPI-1046, or
that Guilford's neurotrophic product candidates will not infringe or be
dominated by this company's patent or patent applications, if issued. There can
be no assurance that any patent applications filed by, or assigned or licensed
to, the Company will be granted, that the Company will develop additional
products or processes that are patentable, or that any patents issued to, or
licensed by, the Company will provide the Company with any competitive
advantages or adequate protection for its products. In addition, there can be no
assurance that any existing or future patents or intellectual property issued
to, or licensed by, the Company will not subsequently be challenged, invalidated
or circumvented by others.
 
     Guilford's policy is to control the disclosure and use of its know-how and
trade secrets under confidentiality agreements with employees, consultants and
other parties. There can be no assurance, however, that its confidentiality
agreements will be honored, that others will not independently develop
equivalent or competing technology, that disputes will not arise concerning the
ownership of intellectual property or the
 
                                       10
<PAGE>   12
 
applicability of confidentiality obligations or that disclosure of Guilford's
trade secrets will not occur. To the extent that consultants or other research
collaborators use intellectual property owned by others in their work with the
Company, disputes may also arise as to the rights to related or resulting
intellectual property.
 
     Guilford supports and collaborates in research conducted in universities
and in governmental research organizations. There can be no assurance that the
Company will have or be able to acquire exclusive rights to the inventions or
technical information derived from such collaborations or that disputes will not
arise as to rights in derivative or related research programs conducted by the
Company. In addition, in the event of a contractual breach by the Company,
certain of the Company's collaborative research contracts provide for the return
of technology rights (including any patents or patent applications) to the
contract sponsors.
 
     Questions of infringement of intellectual property rights, including patent
rights, may involve highly technical and subjective analyses. There can be no
assurance that any of the Company's existing or future products or technologies
do not or will not infringe the rights of other parties, that such other parties
may not in the future initiate legal action against the Company to enforce their
claims or that, if such actions are brought, the Company would be successful in
defending itself.
 
     If the Company is required to defend against charges of infringement of
patent or proprietary rights of third parties or to protect its own patent or
proprietary rights against third parties, including its neurotrophic product
candidates, the Company may incur substantial costs and could lose rights to
develop or market certain products or be required to pay monetary damages or
royalties to license proprietary rights from third parties. In response to
actual or threatened litigation, the Company may seek licenses from third
parties or attempt to redesign its products or processes to avoid infringement;
however, there can be no assurance that the Company will be able to obtain
licenses on acceptable terms, or at all, or redesign its products or processes.
In addition to being a party to patent infringement litigation, the Company
could be required to participate in patent interference proceedings declared by
the United States Patent and Trademark Office, which would be expensive and
time-consuming, even if the Company were to prevail in such a proceeding. The
Company may also be forced to initiate legal proceedings to protect its patent
position or other proprietary rights. These proceedings typically are costly,
protracted, and offer no assurance of success. See "Business -- Patents and
Proprietary Technology."
 
     Dependence on Licenses of Intellectual Property.  The Company has licensed
certain intellectual property from third parties, including certain intellectual
property underlying GLIADEL and DOPASCAN. Under the terms of its license
agreements, the Company is obligated to exercise diligence, achieve certain
milestones, and expend minimum amounts of resources in bringing potential
products to market and make certain royalty, milestone and patent cost
reimbursement payments. In addition, each of these agreements contains certain
record keeping and reporting obligations. Each agreement is terminable by either
party, upon notice, if the other party defaults in its obligations. There can be
no assurance that the Company will be able to meet its obligations under these
agreements on a timely basis, or at all. Should the Company default under any of
these agreements, the Company may lose its right to market and sell any products
based on the licensed technology. In such event, the Company's business,
financial condition and results of operations would be materially and adversely
affected. The agreements also require the Company to pay a royalty to these
parties on sales of GLIADEL, and, if successfully developed, DOPASCAN.
 
     Aspects of the technology licensed under the Company's license agreements
may be subject to certain rights held by the United States government (the
"Government Rights"). These rights include a non-exclusive, royalty-free,
worldwide license to practice or have practiced such inventions for any
governmental purpose. In addition, the United States government has the right to
grant licenses which may be exclusive under any of such inventions to a
third-party if it determines that: (i) adequate steps have not been taken to
commercialize such inventions; (ii) such action is necessary to meet public
health or safety needs; or (iii) such action is necessary to meet requirements
for public use under federal regulations. The government also has the right to
take title to a subject invention if there is failure to disclose the invention
and elect title within specified time limits. In addition, the government may
acquire title in any country in which a patent application is not filed within
specified time limits. Federal law requires any licensor of an invention that
was partially funded by the federal government to obtain a covenant from any
exclusive licensee to manufacture
 
                                       11
<PAGE>   13
 
products using the invention substantially in the United States. Further, the
Government Rights include the right to use and disclose without limitation
technical data relating to licensed technology that was developed in whole or in
part at government expense. Provisions recognizing these Government Rights are
contained in the Company's principal technology license agreements. See
"Business -- Technology Licensing Agreements."
 
   
     Uncertainty of Preclinical and Clinical Trial Results.  Before obtaining
regulatory approval for the commercial sale of any of its product candidates,
the Company must demonstrate through preclinical and clinical trials that the
product is safe and effective for use in the clinical indication for which
approval is sought. The Company and RPR intend to commence a Phase III clinical
trial for GLIADEL for initial surgery for malignant glioma, and the Company
recently completed enrollment in a multi-center Phase II clinical trial for
DOPASCAN. There can be no assurance that the results of these trials will be
successful, and adverse results from either of these trials would have a
material adverse effect on the Company's business, financial condition and
results of operations. There can be no assurance that the Company will be
permitted to undertake or continue clinical trials for any of its product
candidates, or, if permitted, that such products will be demonstrated to be safe
and effective. Moreover, the results from preclinical studies and early clinical
trials may not be predictive of results that will be obtained in later stage
clinical trials. There can be no assurance that the Company's present or future
clinical trials will demonstrate the safety and efficacy of any product
candidates or will result in any necessary regulatory approval to market
products.
    
 
     Government Regulation and Product Approvals.  The Company's research,
preclinical development and clinical trials and the manufacturing and marketing
of its product candidates are subject to extensive regulation by numerous
governmental authorities in the United States and other countries, including,
but not limited to, the FDA and the DEA. Except for GLIADEL, none of the
Company's product candidates has received marketing clearance from the FDA, and
none has received clearance from any other foreign regulatory authority for
commercial sale. As a condition to approval of the Company's product candidates
under development, the FDA could require additional preclinical, clinical or
other studies. Any such requirement for the Company to perform additional
preclinical, clinical or other studies or purchase data from other companies
could have a material adverse effect on the Company's business, financial
condition and results of operations.
 
     In order to obtain FDA clearance of a product for an indication, the
Company must demonstrate to the satisfaction of the FDA that the product is safe
and effective for its intended use and that the product is capable of being
manufactured in accordance with applicable regulatory standards. There can be no
assurance that the Company will be able to demonstrate the foregoing elements
with respect to any of its product candidates or with respect to an expansion of
the labeling of GLIADEL, that the FDA will clear any of its product candidates
or such labeling expansion or that, if such product candidates or such labeling
expansion is cleared, the FDA will clear the full scope of intended use and
labeling sought by the Company. Failure to obtain regulatory approvals or
clearances on a timely basis could have a material adverse effect on the
Company's business, financial condition and results of operations. Once FDA
clearance is obtained, the FDA may also require post-marketing testing and
surveillance to monitor the record of the approved product and continued
compliance with regulatory requirements. In addition, product approvals may be
withdrawn if compliance with regulatory requirements is not maintained or if
problems concerning safety or efficacy of the product occur following approval.
 
     The process of obtaining FDA and other required approvals or licenses and
of meeting other regulatory requirements to test and market drugs, including
controlled substances and radiolabeled drugs, is rigorous and lengthy and has
required, and will continue to require, the expenditure of substantial
resources. All of the Company's product candidates will need to be the subject
of further clinical and other studies. Unsatisfactory clinical trial results and
other delays in obtaining regulatory approvals or licenses would prevent the
marketing of products developed by the Company, and pending the receipt of such
approvals or licenses and the meeting of other regulatory requirements, the
Company will not receive product revenues or royalties.
 
     The Company hopes to capitalize on current FDA regulations, as applicable,
that permit accelerated or expedited approval or treatment use of, and cost
recovery for, certain experimental drugs. These regulations are limited to drug
products intended to treat seriously debilitating or life-threatening diseases
and that
 
                                       12
<PAGE>   14
 
provide meaningful therapeutic benefit to patients over existing treatments or
that are for diseases for which no satisfactory or alternative therapy exists,
among other requirements. There can be no assurance that the Company's product
candidates will qualify for expedited or accelerated approvals or for treatment
use and cost recovery.
 
     Controlled drug products and radiolabeled drugs are subject to special
regulations in addition to those applicable to other drugs. Certain of the
Company's products and product candidates (including DOPASCAN) are or may be
subject to regulation by the DEA as controlled substances and other federal
agencies as radiolabeled drugs. The Company has obtained registrations for its
facilities from the DEA and exceptions from the DEA with respect to various of
its activities involving DOPASCAN, including the shipment of certain quantities
of a precursor of this product candidate to an overseas collaborative partner.
However, there can be no assurance that such exceptions will be sufficient to
cover future activities of the Company, will not be revoked, or that other
requirements to test, manufacture and market controlled substances or
radiolabeled drugs can be satisfied, or that the Company will be able to obtain
additional necessary approvals or licenses to meet state, federal and
international regulatory requirements to manufacture and distribute its
products. See "Business -- Governmental Regulation and Product Testing."
 
     Novel Alternative Technologies and Therapeutic Approaches.  Many of the
Company's product development efforts represent novel alternative therapeutic
approaches and new technologies used, among other things, in the diagnosis and
monitoring of Parkinson's disease, the promotion of nerve growth and the
prevention of neuronal damage, and have not been widely studied. There is no
assurance that these approaches and technologies will be successful. Moreover,
the Company is applying these approaches and technologies to discover new
treatments for conditions that are also the subject of research and development
efforts by numerous other companies. The Company's competitors may succeed in
developing technologies or products that are more efficacious or cost-effective
than those of the Company. Rapid technological change or developments by others
may result in the Company's technology or product candidates becoming obsolete
or noncompetitive. See "Business -- Competition."
 
     Competition and Technological Change.  The Company is involved in evolving
technological fields in which developments are expected to continue at a rapid
pace. Guilford's future success depends upon its ability to compete in the
research, development and commercialization of products and technologies in its
areas of focus. Competition from pharmaceutical, chemical and biotechnology
companies, universities and research institutions is intense and expected to
increase. Many of these competitors have substantially greater research and
development capabilities and experience and manufacturing, marketing, financial
and managerial resources than the Company and represent significant competition
for the Company. Acquisitions of competing companies by large pharmaceutical
companies or other companies could enhance financial, marketing and other
resources available to these competitors. These competitors may develop products
which are superior to those under development by the Company. The Company is
aware of the development by other companies and research scientists of
alternative approaches to the treatment of malignant glioma, the diagnosis of
Parkinson's disease, the promotion of nerve growth and repair, the treatment and
prevention of neuronal damage, and the treatment of cocaine addiction. There can
be no assurance that developments by others will not render the Company's
products or technologies noncompetitive or obsolete, or that the Company will be
able to keep pace with technological developments.
 
     Any product candidate that the Company develops and for which it gains
regulatory approval, including GLIADEL, must then compete for market acceptance
and market share. For certain of the Company's product candidates, an important
factor will be the timing of market introduction of competitive products.
Accordingly, the relative speed with which the Company and competing companies
can develop products, complete the clinical testing and approval processes, and
supply commercial quantities of the products to the market is expected to be an
important determinant of market success. Other competitive factors include
capabilities of the Company's collaborators, product efficacy and safety, timing
and scope of regulatory approval, product availability, marketing and sales
capabilities, reimbursement coverage, the amount of clinical benefit of the
Company's product candidates relative to their cost, method of administration,
price and patent protection. There can be no assurance that the Company's
competitors will not develop more effective or more affordable products or
achieve earlier product development completion, patent protection, regulatory
 
                                       13
<PAGE>   15
 
approval or product commercialization than the Company. The achievement of any
of these goals by the Company's competitors could have a material adverse effect
on the Company's business, financial condition and results of operations. See
"Business -- Competition."
 
     Future Capital Needs; Uncertainty of Additional Funding.  The Company will
require substantial funds in order to continue its research and development
programs and preclinical and clinical testing and to manufacture and, where
applicable, market its products. The Company's capital requirements depend on
numerous factors, including the progress of its research and development
programs, the progress of preclinical and clinical testing, the time and costs
involved in obtaining regulatory approvals, the cost of filing, prosecuting,
defending and enforcing any patent claims and other intellectual property
rights, competing technological and market developments, changes in the
Company's existing research relationships, the ability of the Company to
establish collaborative arrangements, the development of collaborative and
licensing agreements and other arrangements and the progress of manufacturing
scale-up efforts.
 
     The Company believes that the net proceeds of the offering and the interest
earned thereon, together with its existing resources, will be sufficient to fund
the Company's activities for at least the next three years. There can be no
assurance, however, that changes in the Company's research and development and
commercialization plans or other factors affecting the Company's operating
expenses including potential acquisitions will not result in the expenditure of
these proceeds and the Company's other resources before that time.
 
     The Company anticipates that it will fund future capital requirements
through a combination of its existing working capital coupled with the net
proceeds from this offering, revenues generated under its agreements with RPR
relating to GLIADEL, public or private financings (as necessary), additional
collaborative or other research and development agreements, commercialization
and marketing arrangements with corporate partners or other potential sources.
The Company's ability to raise future capital on acceptable terms is dependent
on conditions in the public and private equity markets and the performance of
the Company, as well as the overall performance of other companies in the
biopharmaceutical and biotechnology sectors. There can be no assurance that
required future financing arrangements will be available on acceptable terms, or
at all. See "Management's Discussion and Analysis of Financial Condition and
Results of Operations."
 
     Limited Clinical and Regulatory Compliance Capabilities.  The Company has
limited resources in the areas of product testing and regulatory compliance, and
thus will have to expend capital to acquire and expand such capabilities, reach
collaborative arrangements with third parties to provide these capabilities or
contract with third parties to provide these capabilities in order to carry its
products through the necessary regulatory approvals and prepare its product
candidates for commercialization and marketing.
 
     Reimbursement Uncertainty.  Sales of the Company's product candidates will
depend in part on the availability of reimbursement from third-party health care
payors, such as government and private insurance plans. Given the recent
commercial launch of GLIADEL, reimbursement policies for GLIADEL are not
currently known. No assurance can be given that any reimbursement will be
available at all or will be available at price levels sufficient to realize an
appropriate return on the Company's investment in GLIADEL or other products in
development.
 
     Risk of Product Liability.  The Company may potentially become subject to
large liability claims and significant defense costs as a result of the design,
manufacture or marketing of, or the conduct of clinical trials involving, its
products. A product liability related claim or recall could have a material
adverse effect on the Company's business, financial condition and results of
operations. The Company currently maintains only $10 million of product
liability insurance covering clinical trials and product sales, and there can be
no assurance that such or any future insurance coverage obtained by the Company
will be adequate or that claims, if any, will be covered by the Company's
insurance. Product liability insurance varies in cost, can be difficult to
obtain and may not be available in the future on terms acceptable to the
Company, if at all. An inability to obtain or maintain sufficient insurance
coverage at an acceptable cost or otherwise protect against potential product
liability claims could prevent or inhibit the clinical development and/or
commercialization of any products developed by the Company.
 
                                       14
<PAGE>   16
 
     Dependence on Qualified Personnel and Consultants.  The Company is highly
dependent on the principal members of its management and scientific staff,
including the Company's Chief Executive Officer, Craig R. Smith, M.D., and
member of the Company's Board of Directors and Chairman of the Company's
Scientific Advisory Board, Solomon H. Snyder, M.D. The loss by the Company of
the services of either of these individuals or other members of its senior
management could have a material adverse effect on the Company's business,
financial condition and results of operations. Although the Company has entered
into a consulting agreement with Dr. Snyder and an employment agreement with Dr.
Smith that provide for the protection of the Company's proprietary rights,
either Dr. Snyder or Dr. Smith may terminate his relationship with the Company
at any time. Accordingly, there can be no assurance that either of these
individuals or other employees or consultants will remain with the Company or
that, in the future, these employees or consultants will not organize, or become
employed by or associated with companies competitive with the Company.
 
     The Company's planned activities will require individuals with expertise in
many areas including, without limitation, preclinical testing, clinical trial
management, regulatory affairs, manufacturing and business development. These
activities will require the addition of new personnel, including management
personnel and the development of additional expertise by existing management
personnel. Recruiting and retaining qualified personnel, collaborators, advisors
and consultants will be critical to the Company's activities, and there can be
no assurance that the Company will be able to attract and retain the personnel
necessary for the development of the Company's business. There is significant
competition for experienced scientists from numerous pharmaceutical,
biotechnology and health care companies and academic and other research
institutions. The inability to hire such personnel or to develop such expertise
could have a material adverse effect on the Company's business, financial
condition and results of operations. In addition, the Company is dependent on
collaborators at research institutions and its Scientific Advisory Board members
and consultants. See "Business -- Employees" and "-- Scientific Advisory Board."
 
     Lack of Sales and Marketing Experience.  The Company currently has not
established a sales force, and the Company has no experience in marketing or
selling a product in a commercial setting. In the event the Company decides to
establish an in-house sales force, there can be no assurance its efforts will be
successful. In addition, if the Company succeeds in bringing additional products
to market, it will compete with many other companies that currently have
extensive and well-funded marketing and sales operations. There can be no
assurance that the Company's marketing and sales efforts would compete
successfully against such other companies. See "Business -- Sales, Marketing and
Distribution."
 
     Hazardous and Radioactive Materials; Environmental Matters; Animal
Testing.  Research and development processes sponsored by the Company involve
the controlled use of hazardous and radioactive materials. The Company and its
collaborative partners are subject to international, federal, state and local
laws and regulations governing the use, manufacture, storage, handling and
disposal of hazardous and radioactive materials. The Company believes that the
safety procedures relating to its in-house research and development and
manufacturing efforts comply in all material respects with the standards
prescribed by such laws and regulations. However, the risk of accidental
contamination or injury from these materials cannot be completely eliminated.
Moreover, there can be no assurance that the Company's collaborative partners
are in compliance with such standards or that the Company and its collaborative
partners will be in compliance with such standards in the future. In such event,
the business, financial condition or results of operations of the Company may be
materially adversely affected, and the Company and/or its collaborative partners
could be held liable for damages, fines or other liability, and any such
liability could exceed the resources of the Company. Although the Company
believes that it is and will continue to be in compliance in all material
respects with applicable environmental laws and regulations and currently does
not expect to make material capital expenditures for environmental control
facilities in the near term, there can be no assurance that the Company will not
be required to incur significant costs to comply with environmental laws and
regulations in the future or that the business, financial condition or results
of operations the Company will not be materially adversely affected by current
or future environmental laws or regulations. In addition, much of the research
and development efforts sponsored by the Company involves use of laboratory
animals. The Company may be adversely affected by changes in laws, regulations
or accepted clinical procedures or by social pressures that
 
                                       15
<PAGE>   17
 
would restrict the use of animals in testing or by actions against the Company
or its collaborators by groups or individuals opposed to such testing.
 
     Shares Eligible for Future Sale; Registration and Exchange Rights.  As of
December 31, 1996, the Company had approximately 13,979,490 shares of Common
Stock outstanding. As of that date, there were options to purchase approximately
an aggregate of 2,494,756 shares of Common Stock and warrants to purchase
312,934 shares outstanding. A significant portion of the outstanding Common
Stock and shares issuable upon exercise of outstanding options are freely
tradeable. Except under certain limited circumstances, the Company and its
officers and directors and certain stockholders who own an aggregate of
approximately 4,993,031 shares of Common Stock and shares issuable upon the
exercise of outstanding options have agreed not to sell or otherwise dispose of
any of their shares for a period of 90 days after the effective date of the
offering without the consent of Oppenheimer & Co., Inc. At any time without
notice, Oppenheimer & Co., Inc. may, in its sole discretion, release all or any
portion of the securities subject to lock-up agreements. On March 5, 1997, Abell
exercised its put right for its 80% equity interest in Gell which converted into
750,000 shares of the Company's Common Stock. As a result of that exercise, and
to the extent that outstanding stock options and warrants are exercised, the
interests of the Company's stockholders have been and will be diluted. In
addition, Abell and other holders of the Company's Common Stock and warrants
(representing approximately an aggregate of 2,712,934 shares) have demand and/or
piggyback registration rights. These rights may be exercised at any time and
would permit the resale of some or all of such shares in the public market. If
the Company were required to include shares in a Company-initiated registration
pursuant to the exercise of registration rights, the sale of such shares could
have a material adverse effect on the Company's ability to raise additional
capital. No prediction can be made as to the effect, if any, that sales of
shares of Common Stock or the availability of such shares for sale will have on
the market prices of the Common Stock prevailing from time to time. The
possibility that substantial amounts of Common Stock may be sold in the public
market may adversely affect prevailing market prices for the Common Stock and
could impair the Company's ability to raise capital through the sale of its
equity securities. See "Underwriting."
 
     Discretion Over Use of Proceeds.  The primary purposes of this offering are
to increase the Company's funds available for working capital for further
clinical development of its product candidates, research and development of its
product programs, expansion of the Company's drug delivery business and general
corporate purposes. The Company may also use a portion of the net proceeds of
the offering to acquire or invest in complementary businesses or technologies.
The Company has not designated specific amounts of the net proceeds for
particular purposes. Accordingly, the Company will have broad discretion with
respect to the use of the proceeds derived from the offering. See "Use of
Proceeds."
 
     Anti-takeover Provisions; Preferred Stock.  The Company's Amended and
Restated Certificate of Incorporation, as amended, and the Delaware General
Corporation Law contain certain provisions, including the requirements of
Section 203 of the Delaware General Corporation Law, that may delay or prevent
an attempt by a third party to acquire control of the Company. The Company has
adopted a stockholder rights plan which may have the effect of deterring hostile
or coercive attempts to acquire the Company through the distribution of rights
to stockholders enabling those stockholders to acquire shares of the Company's
Common Stock, or that of an acquirer, at a substantial discount to the public
market price should any person or group acquire more than 20% of the Common
Stock without approval of the Board of Directors under certain circumstances.
The Company has reserved 300,000 shares of Series A Junior Participating
Preferred Stock for issuance in connection with the stockholder rights plan. The
Company is authorized to issue an additional 4,700,000 shares of Preferred Stock
in one or more series, having terms fixed by the Board of Directors without a
stockholder vote. While the Board of Directors has no current intentions or
plans to issue any Preferred Stock, issuance of these shares could also be used
as an anti-takeover device. See "Description of Capital Stock."
 
     Absence of Dividends.  The Company has never declared or paid any cash
dividends on its Common Stock and does not intend to do so for the foreseeable
future. In addition, the Company is prohibited from paying any cash dividends
under the terms of its loan agreements with Signet Bank and the Maryland
Industrial Development Financing Authority. See "Price Range of Common Stock and
Dividend Policy."
 
                                       16
<PAGE>   18
 
                                USE OF PROCEEDS
 
     The net proceeds to the Company from the sale of 3,250,000 shares of Common
Stock offered hereby are estimated to be $83.6 million ($96.2 million if the
Underwriters' over-allotment option is exercised in full), at an assumed public
offering price of $27.25 per share. The Company anticipates using the proceeds
for general corporate purposes, including: (i) further clinical development of
DOPASCAN through Phase III clinical trials and appropriate regulatory filings;
(ii) research, preclinical and clinical development of neurotrophic and
neuroprotective product candidates; and (iii) expansion of the Company's drug
delivery business, including the development of new polymer-based oncology
products. A portion of the net proceeds will be used for working capital. The
Company may also use a portion of the net proceeds to acquire or invest in
complementary businesses or technologies. Presently, the Company has no plans or
commitments and is not engaged in any negotiations with respect to such
transactions. Pending such uses, the Company intends to invest the net proceeds
in investment-grade, interest-bearing securities. See "Risk
Factors -- Discretion Over Use of Proceeds."
 
                                 CAPITALIZATION
 
     The following table sets forth the capitalization of the Company as of
December 31, 1996, and as adjusted to reflect the sale of the shares offered
hereby at an assumed offering price of $27.25 per share and the receipt of the
estimated net proceeds therefrom.
<TABLE>
<CAPTION>
                                                                             DECEMBER 31, 1996
                                                                          -----------------------
                                                                           ACTUAL     AS ADJUSTED
                                                                          --------    -----------
                                                                              (IN THOUSANDS)
<S>                                                                       <C>         <C>
Long-term debt.........................................................   $ 10,905     $  10,905
                                                                          --------     --------- 
Stockholders' equity:
     Preferred Stock, $.01 par value; 4,700,000 authorized; none issued
      or outstanding...................................................         --            --
     Series A Junior Participating Preferred Stock, $.01 par value;
      300,000 shares authorized; none issued or outstanding............         --            --
     Common Stock, $.01 par value; 20,000,000 shares authorized;
      13,979,490 shares issued and outstanding; 17,229,490 shares
      outstanding, as adjusted (1).....................................        140           172
     Additional paid-in capital........................................     90,880       174,461
     Notes receivable on common stock..................................       (129)         (129)
     Accumulated deficit...............................................    (14,874)      (14,874)
     Unrealized gain on available for sale securities..................         62            62
     Deferred compensation.............................................       (202)         (202)
                                                                          --------     --------- 
          Total stockholders' equity...................................     75,877       159,490
                                                                          --------     ---------
               Total capitalization....................................   $ 86,782     $ 170,395
                                                                          ========     =========
</TABLE>
 
- ---------------
   
(1) Excludes: (i) 750,000 shares of Common Stock issued pursuant to Abell's
    exercise on March 5, 1997 of its right to put its interest in Gell to
    Guilford; (ii) options to purchase 2,494,756 shares of Common Stock issuable
    upon exercise of options outstanding at December 31, 1996 at a weighted
    average exercise price of $12.43 per share; and (iii) 312,934 shares of
    Common Stock issuable upon exercise of outstanding warrants at a weighted
    average exercise price of $7.19 per share. On April 1, 1997, at a special
    meeting of stockholders of the Company, the Company's Amended and Restated
    Certificate of Incorporation was amended to increase the number of
    authorized shares of Common Stock from 20,000,000 shares to 40,000,000
    shares.
    
 
                                       17
<PAGE>   19
 
                PRICE RANGE OF COMMON STOCK AND DIVIDEND POLICY
 
     The Company's Common Stock is listed on the Nasdaq National Market under
the symbol "GLFD." The following table sets forth the range of high and low bid
prices for the Common Stock as reported on the Nasdaq National Market for the
periods indicated below.
 
   
<TABLE>
<CAPTION>
                                                                                HIGH      LOW
                                                                               ------    ------
<S>                                                                            <C>       <C>
1995
First Quarter...............................................................   $ 4.17    $ 2.83
Second Quarter..............................................................     4.08      3.17
Third Quarter...............................................................     9.17      4.08
Fourth Quarter..............................................................    10.67      7.33
1996
First Quarter...............................................................    16.17     10.17
Second Quarter..............................................................    23.33     13.33
Third Quarter...............................................................    19.67     11.33
Fourth Quarter..............................................................    22.25     16.00
1997
First Quarter...............................................................    29.00     20.75
Second Quarter (through April 4, 1997)......................................    23.00     20.25
</TABLE>
    
 
     As of February 28, 1997, there were approximately 144 holders of record of
the Common Stock. See "Risk Factors -- Likely Volatility of Stock Price."
 
     The Company has never declared or paid any cash dividends and does not
intend to do so for the foreseeable future. The Company currently intends to
retain all earnings, if any, to finance the development of its business. Under
the Company's loan agreements with Signet Bank, during the term of the loans,
the Company may not declare any cash dividends on its Common Stock without the
prior written consent of Signet Bank and the Maryland Industrial Development
Financing Authority.
 
                                       18
<PAGE>   20
 
                      SELECTED CONSOLIDATED FINANCIAL DATA
                      (IN THOUSANDS EXCEPT PER SHARE DATA)
 
     The following selected consolidated financial data with respect to the
Company for the period from inception on July 14, 1993 through December 31, 1993
and for each of the years in the three year period ended December 31, 1996 have
been derived from the Company's consolidated financial statements which have
been audited by KPMG Peat Marwick LLP, the Company's independent auditors. The
Company's consolidated financial statements as of December 31, 1995 and 1996,
and for each of the years in the three year period ended December 31, 1996,
including the Notes thereto, are included elsewhere in this Prospectus. The
information set forth below should be read in conjunction with the Company's
Consolidated Financial Statements and Notes thereto and "Management's Discussion
and Analysis of Financial Condition and Results of Operations" included
elsewhere herein.
<TABLE>
<CAPTION>
                                                       JULY 14, 1993
                                                    (DATE OF INCEPTION)     YEARS ENDED DECEMBER 31,
                                                      TO DECEMBER 31,     ----------------------------
                                                           1993            1994       1995      1996
                                                    -------------------   -------   --------   -------
<S>                                                 <C>                   <C>       <C>        <C>
STATEMENT OF OPERATIONS DATA:
Total revenues....................................        $    --         $    --   $    586   $28,020
Expenses:
     Research and development.....................          1,061           2,869      9,688    18,761
     General and administrative...................            367           2,369      4,367     6,736
     Compensation expense -- warrants.............             --             991         --        --
                                                       ----------         -------   --------   -------
          Total operating expenses................          1,428           6,229     14,055    25,497
                                                       ----------         -------   --------   -------
     Income (loss) from operations................         (1,428)         (6,229)   (13,469)    2,523
     Other income (expenses), net.................             15             332        832     2,550
                                                       ----------         -------   --------   -------
Net income (loss).................................        $(1,413)        $(5,897)  $(12,637)  $ 5,073
                                                    ==============        =======   ========   =======
Primary earnings (loss) per common share (1)......        $ (0.50)        $ (1.36)  $  (1.70)  $  0.35
                                                    ==============        =======   ========   =======
 
Weighted average common and common equivalent
  shares used to compute primary earnings (loss)
  per share (1)...................................          2,834           4,332      7,436    14,634
Fully diluted earnings (loss) per share (1).......        $ (0.50)        $ (1.36)  $  (1.70)  $  0.34
                                                    ==============        =======   ========   =======
Weighted average common and common equivalent
  shares used to compute fully diluted earnings
  (loss) per share (1)............................          2,834           4,332      7,436    15,140
 
<CAPTION>
                                                                       DECEMBER 31,
                                                    --------------------------------------------------
                                                           1993            1994       1995      1996
                                                    -------------------   -------   --------   -------
<S>                                                 <C>                   <C>       <C>        <C>
BALANCE SHEET DATA:
Cash, cash equivalents and investments (2)........         $2,562         $11,834    $19,454   $77,439
Total assets (2)..................................          3,258          14,562     26,048    93,659
Long-term debt....................................             --           1,431      4,696    10,905
Total stockholders' equity........................          2,887          11,421     17,773    75,877
</TABLE>
 
- ---------------
(1) For information concerning the calculation of earnings (loss) per share, see
    Note 2 of Notes to Consolidated Financial Statements.
 
(2) Includes restricted investments of $10.1 million at December 31, 1996. See
    Note 6 of Notes to Consolidated Financial Statements.
 
                                       19
<PAGE>   21
 
                    MANAGEMENT'S DISCUSSION AND ANALYSIS OF
                 FINANCIAL CONDITION AND RESULTS OF OPERATIONS
 
     The following discussion is qualified in its entirety by the more detailed
information and the Consolidated Financial Statements and Notes thereto
appearing elsewhere in this Prospectus. The following discussion contains
forward-looking statements, including, but not limited to, those concerning the
commencement and completion of clinical trials, the Company's strategic plans,
anticipated expenditures and the need for additional funds, which involve risks
and uncertainties. The Company's actual results may differ significantly from
the results discussed in the forward-looking statements. Factors that could
cause or contribute to such differences include, but are not limited to, those
discussed in "Risk Factors" as well as those discussed elsewhere in this
Prospectus.
 
GENERAL
 
     Guilford, founded in 1993, is a biopharmaceutical company engaged in the
development and commercialization of novel products in two principal areas: (i)
targeted and controlled drug delivery systems using proprietary biodegradable
polymers for the treatment of cancer and other diseases; and (ii) therapeutic
and diagnostic products for neurological diseases and conditions.
 
     In 1996, the Company reported net earnings of $5.1 million. However, prior
to the second quarter of 1996, the Company had incurred net operating losses
from its inception through the first quarter of 1996 and again in the fourth
quarter of 1996. Through December 31, 1996, the Company had an accumulated
deficit of $14.9 million. To date, substantially all of the Company's revenues
have been recognized as research and development or milestone payments under the
Company's collaborations. Except for GLIADEL, the Company's product candidates
are not expected to generate revenues for at least the next several years, if at
all, and the recognition of material revenues for GLIADEL sales is subject to
significant uncertainty. While the Company reported net income for the second
and third quarters of 1996, this was the result of significant and non-recurring
milestone payments from RPR with respect to GLIADEL. The Company does not
anticipate that 1997 will be profitable, and there can be no assurance that the
Company will ever achieve or sustain profitability in the future. Furthermore,
the Company expects to experience quarter-to-quarter and year-to-year
fluctuations in its operating results based upon the timing and amount of sales
of GLIADEL, the timing and realization of milestone and other payments under the
Company's agreements with RPR and other existing and potential collaborations as
well as expenses relating to the Company's research and development, clinical
and manufacturing activities. See "Risk Factors -- History of Losses;
Uncertainty of Future Profitability" and "-- Dependence on GLIADEL and RPR."
 
RESULTS OF OPERATIONS
 
  Years Ended December 31, 1996, 1995 and 1994
 
     In 1996, the Company recognized $28.0 million in revenues, primarily
consisting of a total of $27.5 million in non-recurring milestone payments made
by RPR in June and September 1996. In 1995, the Company recognized $0.6 million
in revenues, primarily consisting of a non-refundable license fee payment
pursuant to the Company's agreement with DRL related to DOPASCAN. The Company
recognized no revenues in 1994. The Company will be required to pay a royalty to
MIT on sales of GLIADEL pursuant to the license agreement under which the
Company acquired the underlying technology for this product. The Company
anticipates reporting these amounts upon commencement of GLIADEL sales as cost
of goods sold in future periods.
 
     Research and development expenses increased to $18.8 million in 1996 as
compared to $9.7 million in 1995 and $2.9 million in 1994. The increase in these
costs from 1995 to 1996 of $9.1 million was primarily attributable to expenses
related to increased personnel costs and contracted research, consulting and
laboratory supplies. During 1996, the Company accelerated its neuroimmunophilin,
neurotrophic and addictive therapeutics research and development programs,
initiated and completed enrollment of a multi-center Phase II clinical trial in
the United States for DOPASCAN, finalized preparation of its new drug
application for GLIADEL (submitted in February 1996) and prepared for the
commercial launch of
 
                                       20
<PAGE>   22
 
GLIADEL. In 1996, research and development expenses also included a non-cash
charge of $1.2 million as compensation expense relating to certain consulting
agreements intended to enhance the Company's ability to develop new polymer
technologies and products for the delivery of chemotherapeutics in indications
where local tumor recurrence is likely and controlled release may be more
effective than current therapies. The Company expects it will be required to
record varying amounts quarterly of up to an additional $2.2 million in the
aggregate of non-cash compensation charges in research and development expenses
through 2001 relating to such agreements. The increase in research and
development costs from 1994 to 1995 of $6.8 million was primarily attributable
to the filing of a Treatment IND for GLIADEL, preparation for the filing of an
NDA for GLIADEL, undertaking and completing certain Phase II clinical trials for
DOPASCAN and research costs primarily related to the Company's neurotrophic,
neuroprotective and cocaine addiction therapeutics programs as well as continued
scale-up of the Company's research and development programs. The Company
anticipates that its research and development expenses will continue to increase
significantly in future periods.
 
     General and administrative expenses increased to $6.7 million in 1996 as
compared to $4.4 million in 1995 and $2.4 million in 1994. The increases in
general and administrative expenses of $2.3 million from 1995 to 1996 and of
$2.0 million from 1994 to 1995 were attributable to higher personnel costs
related to an increase in the number of employees necessary to support the
Company's research and development and commercialization activities.
Additionally, indirect personnel costs, including recruiting and relocation
costs, have increased as the total number of employees has increased. Increases
in costs related to patenting and other activities related to establishment and
preservation of the Company's intellectual property and costs related to
operations as a public company also contributed to increased general and
administrative expenditures over the periods covered. The Company anticipates
that its general and administrative expenses will continue to increase in future
periods.
 
     Other income and expense relates primarily to interest income and interest
expense. Interest income increased to $3.1 million in 1996 compared to $0.8
million in 1995 and $0.3 million in 1994. The increases were primarily
attributable to an increase in the average invested capital resulting from the
Company's equity offerings and in 1996 from revenues from RPR. In 1996 and 1995,
the Company incurred interest expense of $0.5 million and $0.2 million,
respectively, relating to borrowings under its loan agreements with Signet Bank
providing for the construction of manufacturing, administrative and research and
development facilities and the purchase of related equipment. In 1994, interest
expense was negligible.
 
LIQUIDITY AND CAPITAL RESOURCES
 
     The Company's cash and investments were $77.4 million at December 31, 1996.
Included in this amount is $10.1 million of restricted cash held as collateral
with respect to certain of the Company's indebtedness. The Company had incurred
an accumulated deficit at December 31, 1996 of $14.9 million and expects to
continue to incur additional operating losses from time to time in the future.
 
     The Company incurred capital expenditures of $9.1 million in 1996 compared
to $3.7 million in 1995 and $2.3 million in 1994. These capital expenditures
were related to the construction of the Company's GLIADEL manufacturing facility
and related tenant improvements for research and development laboratories and
administrative offices. Additionally, other purchases included capital
equipment, including laboratory and manufacturing equipment, and computer
hardware and software to support the Company's activities.
 
     The Company had available approximately $1.8 million at December 31, 1996
under its existing loan agreements with Signet Bank to finance the remaining in
process tenant improvements related to the construction of research and
development laboratories and related areas. To finance capital equipment, the
Company in September 1996 finalized a $5.0 million operating lease arrangement
with General Electric Capital Corporation for the financing of certain
equipment. Such financing, along with other sources, is expected to provide for
the Company's equipment needs at least through the second quarter of 1997. At
December 31, 1996, $3.0 million was available under this arrangement to lease
additional equipment.
 
     During 1997 and 1998, the Company expects to make additional capital
expenditures of approximately $3.7 million to expand the Company's GLIADEL
manufacturing plant capacity from 8,000 to 30,000 treatments annually. The
Company expects to use the capital available under its loan agreement with RPR
to fund
 
                                       21
<PAGE>   23
 
the expansion. Under this loan agreement, the Company has the right to borrow up
to an aggregate of $7.5 million under certain conditions for such purposes. As
of January 2, 1997, $4.0 million was available under the agreement; the
remainder is available no earlier than 12 nor later than 18 months following
funding of the initial tranche. Any principal amounts borrowed under this loan
agreement are due five years from the date borrowed and will carry an interest
rate equal to the lowest rate paid by RPR from time to time on its most senior
indebtedness. Both principal and interest due under this arrangement may, at the
Company's election, be repaid by off-setting certain amounts due to the Company
under the agreements with RPR. No amounts were outstanding under this loan at
December 31, 1996.
 
     The Company will require substantial funds in order to continue its
research and development programs and preclinical and clinical testing and to
manufacture and, where applicable, market its products. The Company's capital
requirements depend on numerous factors, including the progress of its research
and development programs, the progress of preclinical and clinical testing, the
time and costs involved in obtaining regulatory approvals, the cost of filing,
prosecuting, defending and enforcing any patent claims and other intellectual
property rights, competing technological and market developments, changes in the
Company's existing research relationships, the ability of the Company to
establish collaborative arrangements, the development of collaborative and
licensing agreements and other arrangements and the progress of manufacturing
scale-up efforts.
 
     The Company believes that the net proceeds of the offering and the interest
earned thereon, together with its existing resources, will be sufficient to fund
the Company's activities for at least the next three years. There can be no
assurance, however, that changes in the Company's research and development and
commercialization plans or other factors affecting the Company's operating
expenses including potential acquisitions will not result in the expenditure of
these proceeds and the Company's other resources before that time.
 
     The Company anticipates that it will fund future capital requirements
through a combination of its existing working capital coupled with the net
proceeds from this offering, revenues generated under its agreements with RPR
relating to GLIADEL, public or private financings (as necessary), additional
collaborative or other research and development agreements, commercialization
and marketing arrangements with corporate partners or other potential sources.
The Company's ability to raise future capital on acceptable terms is dependent
on conditions in the public and private equity markets and the performance of
the Company, as well as the overall performance of other companies in the
biopharmaceutical and biotechnology sectors. There can be no assurance that
required future financing arrangements will be available on acceptable terms, or
at all.
 
                                       22
<PAGE>   24
 
                                    BUSINESS
 
OVERVIEW
 
     Guilford is a biopharmaceutical company engaged in the development and
commercialization of novel products in two principal areas: (i) targeted and
controlled drug delivery systems using proprietary biodegradable polymers for
the treatment of cancer and other diseases; and (ii) therapeutic and diagnostic
products for neurological diseases and conditions.
 
     The Company's first product in its drug delivery business is GLIADEL, a
novel treatment for glioblastoma multiforme, the most common and rapidly fatal
form of brain cancer. GLIADEL was cleared for marketing by the FDA in September
1996 for use as an adjunct to surgery to prolong survival in patients with
recurrent glioblastoma multiforme for whom surgical resection is indicated.
GLIADEL was commercially launched in the United States on February 25, 1997 by
the Company's marketing partner, RPR. RPR is submitting marketing applications
in other countries and the Company and RPR are planning further clinical trials
of GLIADEL to seek to expand its labeling. The Company also intends to broaden
its line of polymer-based oncology products through the use of other
chemotherapeutic agents, different polymer systems and various formulations, and
may also consider developing polymer drug delivery for other applications.
 
     The Company's lead neurological product candidate is DOPASCAN, a
radiolabeled tropane derivative that is being developed for the diagnosis and
monitoring of Parkinson's disease. The Company has completed enrollment in a
multi-center Phase II clinical trial of DOPASCAN in the United States and is
preparing to commence Phase III clinical trials later this year. The Company
also is developing other neurological product candidates, including: (i)
neurotrophic drugs to promote nerve growth and repair, which may have
applications for spinal cord injuries, peripheral neuropathies and
neurodegenerative diseases, such as Alzheimer's disease and Parkinson's disease;
(ii) neuroprotective drugs to reduce neuronal damage due to stroke or severe
head trauma; and (iii) drugs to treat addictive disorders.
 
                                       23
<PAGE>   25
 
PRODUCT AND DEVELOPMENT PROGRAMS
 
     The following table summarizes the current status of the Company's product,
product candidates and research programs:
 
<TABLE>
<CAPTION>
 PROGRAM/PRODUCT CANDIDATES      DISEASE INDICATIONS/CONDITIONS       STATUS (1)             CORPORATE PARTNER
- ----------------------------     -------------------------------     -------------     ------------------------------
<S>                              <C>                                 <C>               <C>
DRUG DELIVERY BUSINESS
GLIADEL                          Recurrent glioblastoma              Market            RPR,
  (3.85% BCNU)                   multiforme                                            Orion Farmos (Scandinavia)
                                 Initial treatment of malignant      Phase III(2)      RPR,
                                 glioma                                                Orion Farmos (Scandinavia)
GLIADEL                          Malignant glioma                    Phase I           RPR,
  (6.5% up to 20% BCNU)                                                                Orion Farmos (Scandinavia)(3)
Other polymer-based products     Various cancers                     Research          RPR (4)
NEUROLOGICAL PRODUCTS
DOPASCAN                         Imaging agent to diagnose and       Phase II          DRL (Asia) (5)
                                 monitor Parkinson's disease
NEUROTROPHIC DRUGS
Neuroimmunophilin ligands        Nerve growth and repair             Preclinical       --
                                 (Parkinson's disease,
                                 Alzheimer's disease, multiple
                                 sclerosis, stroke, spinal cord
                                 injury and peripheral
                                 neuropathies)
NEUROPROTECTIVE DRUGS
Pre-synaptic glutamate           Stroke, severe head trauma,         Research          --
  inhibitors                     ALS, epilepsy and Parkinson's
                                 disease
NOS inhibitor                    Stroke, severe head trauma          Research          --
PARS inhibitor                   Stroke, severe head trauma          Research          --
ADDICTION THERAPEUTICS
Dopamine transporter ligand      Cocaine addiction                   Research          --
</TABLE>
 
- ---------------
(1) "Research" includes initial research related to specific molecular targets,
    synthesis of new chemical entities and assay development for the
    identification of lead compounds. "Preclinical" includes testing of lead
    compounds in vitro and in animal models, pharmacology and toxicology
    testing, product formulation and process development prior to the
    commencement of clinical trials.
 
(2) A trial is expected to commence in mid-1997.
 
(3) Orion Farmos has certain rights of first refusal.
 
(4) RPR has certain rights of first offer.
 
(5) Japan, Korea and Taiwan.
 
     Development and commercialization of the Company's product and product
candidates is subject to numerous risks and uncertainties. See "Risk Factors."
 
DRUG DELIVERY BUSINESS
 
     The Company's drug delivery business currently involves the use of
biodegradable polymers for targeted and controlled drug delivery of
chemotherapeutic drugs to treat cancer. Delivering high drug concentrations
locally for a sustained period of time may increase the efficacy of chemotherapy
in controlling tumor growth and may decrease the side effects associated with
systemic drug administration. Guilford has developed expertise in the discovery,
clinical development and manufacturing of polymer-based drug delivery products.
 
                                       24
<PAGE>   26
 
  GLIADEL
 
     The Company's first product in its drug delivery business is GLIADEL, a
novel treatment for malignant glioma, the most common and rapidly fatal form of
primary brain cancer. GLIADEL is a white wafer about the size of a dime made of
a proprietary biodegradable polymer which contains the cancer chemotherapeutic
drug BCNU (carmustine). Up to eight GLIADEL wafers are implanted in the cavity
created when a neurosurgeon removes the brain tumor. The wafers gradually
degrade in the cavity and deliver BCNU directly to the tumor site in high
concentrations for an extended period of time without exposing the rest of the
body to the toxic side effects of BCNU. GLIADEL is used to complement standard
therapy with surgery, radiation therapy and systemic chemotherapy in patients
with recurrent glioblastoma multiforme. In a North American Phase III clinical
trial, GLIADEL was shown to increase the six-month survival rate by more than
50% in these patients. The availability of GLIADEL gives physicians a new
treatment option for this rapidly fatal disease.
 
     On September 23, 1996 the FDA cleared the Company's NDA for GLIADEL for use
as an adjunct to surgery to prolong survival in patients with recurrent
glioblastoma multiforme for whom surgery is indicated. RPR began commercial sale
of GLIADEL in the United States on February 25, 1997 through its existing
oncology sales force. Prior to launch, GLIADEL was available to neurosurgeons in
the United States through a Treatment IND cleared by the FDA. A Treatment IND
protocol is a clinical trial that allows the use of a product prior to FDA
marketing clearance. The Treatment IND protocol was approved in over 170
hospitals in the United States and more than 450 treatments were distributed.
 
     GLIADEL has been studied in trials involving over 650 patients, including
two Phase III multi-center, randomized, double-blind, placebo-controlled
clinical trials. The results of a trial conducted in the United States and
Canada involving 222 patients undergoing surgery for recurrent malignant glioma
were published in the April 22, 1995 issue of The Lancet. Patients received
either GLIADEL or a placebo wafer. This trial examined GLIADEL's additive effect
to survival, adjunctive to the best treatments currently available for brain
cancer, i.e., surgery, radiation therapy and in some cases, systemic
chemotherapy. The survival rate at six months, the primary endpoint, was 47% in
the placebo group and 60% in the GLIADEL group, with an improvement in median
survival of eight weeks (a 35% increase). In this trial, which formed the basis
for FDA marketing clearance of the NDA for GLIADEL, the survival rate for 145
patients with recurrent glioblastoma multiforme at six months was 36% in the
placebo group and 56% in the GLIADEL group (a greater than 50% increase) with an
improvement in median survival of eight weeks. These results were statistically
significant after adjustment for prognostic factors, and no clinically important
adverse effects attributable to the drug were reported in either trial.
 
     In June 1996, the Company entered into a strategic agreement with RPR
granting RPR the worldwide (excluding Scandinavia) rights to market, sell and
distribute GLIADEL. During 1996, RPR paid Guilford $27.5 million in milestone
payments, $7.5 million in an equity investment in Company Common Stock and
extended to the Company a $7.5 million line of credit, which the Company intends
to use to expand its annual manufacturing capacity from 8,000 to 30,000
treatments (each consisting of eight GLIADEL wafers). Under the agreements with
RPR, Guilford receives a combined transfer price and royalty of 35% to 40% of
the net sales of GLIADEL. GLIADEL could earn additional payments totaling up to
$40.0 million (including $7.5 million in the form of an equity investment),
subject to achievement of certain milestone events, including expanded labeling
in the United States to include use of GLIADEL at the time of initial surgery
and international marketing approvals. The Company will be required to pay a
royalty to MIT on sales of GLIADEL pursuant to the license agreement under which
the Company acquired the underlying technology for this product.
 
     Guilford and RPR have initiated a series of new clinical trials for the
purpose of seeking to expand the market for GLIADEL. A Phase III randomized,
double-blind, placebo-controlled trial in patients undergoing initial surgery
for malignant glioma is planned to commence in mid-1997. In addition, Guilford
has initiated a Phase I clinical trial to test the safety of escalating the
concentration of BCNU in GLIADEL from 3.85% to 20%, following preclinical
studies suggesting that higher concentrations of BCNU in GLIADEL may be even
more effective and appear to be safe.
 
                                       25
<PAGE>   27
 
     In October 1995, the Company entered into an agreement with Orion Farmos, a
major Scandinavian health care company, for the sales, marketing and
distribution of GLIADEL in Scandinavia. The agreement provides for payments to
Guilford based on GLIADEL sales made by Orion Farmos in Scandinavia. Orion
Farmos has commenced sales of GLIADEL in Scandinavia on a named hospital basis.
 
     For a discussion of certain risks related to GLIADEL, see "Risk
Factors -- Dependence on GLIADEL and RPR" and "-- Reliance on Suppliers."
 
     Other Polymer-Based Drug Delivery Products.  The Company intends to broaden
its line of polymer-based products to include drug delivery products for the
treatment of tumors outside the central nervous system. Other cancers that may
be suitable for this type of targeted therapeutic approach include tumors of the
prostate, ovaries, head and neck, breast, esophagus, liver, pancreas, lung and
colon. In addition, the Company is investigating other polymer systems and
additional configurations such as gels, beads and rods for stereotactic
implantation. As part of this effort, the Company has entered into two research
collaborations with a biomedical engineering laboratory at Johns Hopkins to
discover new polymers and to advise the Company on new product development. In
June 1996, the Company entered into a license agreement with MIT and Johns
Hopkins relating to a patent application claiming certain biodegradable polymers
for use in connection with the controlled local delivery of certain
chemotherapeutic agents (including paclitaxel (Taxol(R)) and camptothecin) for
treating solid tumors. In July 1996, the Company entered into a license
agreement with Johns Hopkins relating to two issued United States patents
relating to polyphosphoesters. In addition, the Company has established a
strategic partnership with RPR to commercialize GLIADEL and evaluate the
opportunity to incorporate RPR's proprietary chemotherapeutics in Guilford's
proprietary polymer systems.
 
NEUROLOGICAL PRODUCTS PROGRAM
 
     DOPASCAN.  The Company's lead neurological product candidate is DOPASCAN, a
radiolabeled tropane derivative that is being developed for the diagnosis and
monitoring of Parkinson's disease. DOPASCAN is administered intravenously in
very small quantities and allows physicians to obtain images of dopamine neurons
in the brain. Dopamine neurons are highly concentrated in a specialized area of
the brain that degenerates in Parkinson's disease. Parkinson's disease is a
common neurodegenerative disorder affecting more than 600,000 patients in the
United States. In its early stages, Parkinson's disease can be very difficult to
clinically distinguish from other diseases with similar symptoms but which do
not respond well or at all to specific therapy for Parkinson's disease. In order
to properly treat these patients, it is important to establish an accurate early
diagnosis. Unfortunately there are no diagnostic tests currently available that
can detect the neuronal degeneration in Parkinson's disease and the typical
delay between the onset of symptoms and clinical diagnosis is more than two
years. The only way to establish the diagnosis at present is through repeated
physician visits and the use of therapeutic trials of drugs such as L-Dopa,
which carry with them the risk of unnecessary, sometimes severe, side effects.
 
     DOPASCAN is administered by a single intravenous injection. The next day,
the patient returns to the hospital and lies under a SPECT camera for about 30
minutes to have images taken. The images obtained with the SPECT camera identify
loss of dopamine neurons in the brain. To date, over 1,000 patients have been
imaged in the United States and Europe using DOPASCAN. In initial United States
Phase II trials DOPASCAN accurately differentiated patients clinically diagnosed
with Parkinson's disease from those without the disease. The Company has
completed enrollment in a multi-center Phase II clinical trial of DOPASCAN in
the United States and expects the study report to be available in the second
quarter of 1997. The Company intends to commence Phase III clinical trials in
North America prior to the end of 1997. In addition, the Company expects to
undertake further clinical trials in Europe to support European regulatory
filings.
 
     The Company has entered into an agreement with DRL, a leading Japanese
radiopharmaceutical company, to develop and commercialize DOPASCAN in Japan,
Korea and Taiwan. DRL has informed the Company that it has completed Phase I
clinical trials, and intends to commence Phase II clinical trials in Japan later
this year. The Company intends to seek partners for distribution of this product
in other territories, including the United States and Europe.
 
                                       26
<PAGE>   28
 
  Neurotrophic Drugs
 
     Guilford is developing small molecule, orally bioavailable compounds to
promote nerve growth and repair (neurotrophic agents) for the treatment of
neurological disorders. The degeneration or damage of nerve cells in the brain
and peripheral neurons resulting from certain diseases and conditions causes a
loss of either central nervous system function (e.g., Alzheimer's disease,
Parkinson's disease, multiple sclerosis, spinal cord injury and stroke) or
peripheral nerve function (e.g., diabetic neuropathy and other peripheral
neuropathies). Under normal circumstances, damaged nerves have a very limited
ability to regrow, which poses a major obstacle for the treatment of these
conditions.
 
     In 1990, scientists at Johns Hopkins led by Dr. Solomon H. Snyder
discovered that a binding protein for commonly used immunosuppressive agents
such as tacrolimus (FK-506), was concentrated 10 to 50 fold higher in the brain
than in the immune system. The Johns Hopkins scientists went on to discover that
commonly used immunosuppressive drugs can promote nerve growth, and Guilford has
exclusively licensed from Johns Hopkins a United States patent application
claiming these discoveries. Guilford and Johns Hopkins scientists further
discovered that the mechanism of nerve growth promotion is independent of the
mechanism responsible for immunosuppression, and is mediated by binding to the
major neuroimmunophilin in the brain. This binding was discovered to initiate a
previously unknown neurotrophic cascade.
 
     Based on these discoveries, the Company has synthesized hundreds of
proprietary small molecule neuroimmunophilin ligands in several distinct
chemical series that promote nerve growth without being immunosuppressive. The
Company has filed numerous patent applications in the United States and
internationally relating to both novel compositions and methods of treating
neurological disorders utilizing these compounds. These compounds induce nerve
growth directly, as well as potentiate nerve growth in the presence of nerve
growth factors. Several of Guilford's lead compounds have exhibited neurotrophic
effects at picomolar and even sub-picomolar concentrations in in vitro nerve
cell cultures. In March 1997, the Company was issued a United States patent for
the compositions and uses of a series of neuroimmunophilin ligands as
neurotrophic agents for the treatment of neurodegenerative disorders. See "Risk
Factors -- Uncertainty Regarding Patents and Proprietary Technology."
 
   
     Experimental results of one of the Company's lead products, GPI-1046, were
reported in 1996 and published in the March 4, 1997 issue of the Proceedings of
the National Academy of Sciences. In two animal models of Parkinson's disease,
GPI-1046 demonstrated neuroprotective and neuroregenerative effects and recovery
of behavioral function. In one experiment where a neurotoxin and GPI-1046 were
administered simultaneously, the compound produced a 90% protection and/or
regeneration of the nigral-striatal dopamine neurons, the dopamine neurons which
are selectively lost in Parkinson's disease. In another experiment where
GPI-1046 was administered up to one month following the administration of the
neurotoxin, approximately 30% regeneration of functional striatal dopamine
neurons and near complete normalization of behavior in the affected animals was
observed. In addition to animal models of Parkinson's disease, GPI-1046 has been
shown to promote nerve regeneration in a rat model of peripheral nerve injury.
In this model, GPI-1046 increased the size and number of axons and also
increased the degree of myelination of nerve cells in a damaged sciatic nerve,
leading to partial functional improvement in the paralyzed leg. Further,
GPI-1046 and other compounds exhibited systemic activity, oral bioavailability,
and the ability to cross the blood-brain barrier, unlike many naturally
occurring nerve growth factors.
    
 
     GPI-1046 is currently undergoing the necessary preclinical toxicology,
pharmacokinetic and additional testing, including primate studies, to support
clinical trials. In addition, Company scientists have designed and synthesized
additional compounds from several distinct chemical series with improved potency
and efficacy compared to GPI-1046, and several of these compounds are in
preclinical development. One such example, GPI-1216, potently promotes neurite
outgrowth in chick sensory neurons in cell culture in sub-picomolar
concentrations, and is 50% more efficacious than GPI-1046 in an in vivo model of
Parkinson's disease. Additional lead compounds from other patent series, such as
GPI-1152 and GPI-1234, are also more than 50% more efficacious than GP-1046 in
vivo. The Company intends to commence preliminary clinical trials with one of
its lead compounds in late 1997 or early 1998. See "Risk
Factors -- Technological Uncertainties."
 
     The Company's neuroimmunophilin ligands have produced nerve regeneration
following multiple routes of administration, including oral administration.
Further, neuroimmunophilin ligands are able to cross the
 
                                       27
<PAGE>   29
 
blood-brain barrier, while many naturally-occurring nerve growth factors,
proteins and peptides are not orally bioavailable and do not cross the
blood-brain barrier. Guilford intends to investigate the utility of its
compounds in a range of neurological disorders (Parkinson's disease and
Alzheimer's disease), multiple sclerosis, spinal cord injury and various
peripheral neuropathies.
 
     The Company is currently in discussions with several multinational
pharmaceutical companies regarding a collaboration for this program, however
there can be no assurance that the Company will enter into any such
collaboration.
 
  Neuroprotective Drugs
 
     Guilford is developing novel compounds to protect brain cells against
damage from ischemia (the lack of oxygen delivery from reduced blood flow) and
other insults and disorders which cause damage due to massive release of
excitatory amino acid neurotransmitters such as glutamate. The Company's
approach is to identify and clinically test compounds that have the ability to
intervene at three distinct steps in a biochemical pathway leading to neuronal
damage: (i) pre-synaptic inhibition of glutamate; (ii) inhibition of NOS; and
(iii) inhibition of PARS.
 
     In normal brain function, the pre-synaptic release of the neurotransmitter
glutamate, resulting in stimulation of post-synaptic glutamate receptors
(including N-methyl-D-aspartate (NMDA)), plays a critical role in many central
neuronal functions. However, in conditions such as ischemia, epilepsy and
Huntington's disease, there is a massive increase in pre-synaptic glutamate
release, which results in excessive activation of post-synaptic glutamate
receptors. This, in turn, causes excess production of the neurotransmitter
nitric oxide, mediated by the enzyme NOS, which results in damage to cellular
DNA. The nerve cell then attempts to repair such damage, mediated by the enzyme
PARS, which leads to depletion of cell energy and cell death.
 
  Pre-Synaptic Glutamate Inhibitors
 
     To date, a number of biopharmaceutical companies have attempted to find
compounds which might block the effects of excess glutamate on post-synaptic
glutamate receptors. However, a number of post-synaptic glutamate antagonists
have been associated with toxicities.
 
     Guilford scientists have succeeded in inhibiting the pre-synaptic release
of glutamate, that is, preventing excessive levels of glutamate from being
produced and released in the first place. The Company has identified compounds
which exhibit nanomolar potency in vitro. The Company has filed both composition
of matter patent applications, relating to several series of novel compounds,
and method of use patent applications, relating to this novel mechanism to
inhibit excess glutamate during conditions of neurodegeneration. GPI-5000, the
Company's prototype pre-synaptic glutamate inhibitor, has demonstrated
significant neuroprotectant activity in several cell culture and animal models
of neurodegeneration. In both in vitro and in vivo models of focal ischemia,
GPI-5000 exhibited approximately 90% neuroprotection of cortical neurons. To the
Company's knowledge, such a magnitude of neuroprotection is significantly
greater than that reported by post-synaptic glutamate receptor antagonists,
calcium channel antagonists or pH modulators tested under similar conditions. In
addition, because GPI-5000, as well as Guilford's other series of proprietary
compounds, do not interact with post-synaptic glutamate receptors, they may not
be associated with the toxicities associated with post-synaptic glutamate
antagonists. "Prototype" as used here and elsewhere in this document designates
a compound which the Company uses to establish proof of principle of the
relevant mechanism of action, but which it does not intend to develop into a
product because of pharmacokinetic characteristics of the compound, the
Company's proprietary position with respect to such compound or for other
reasons. The Company is currently seeking to develop proprietary lead compounds
in this program through medicinal chemistry around GPI-5000 and other compounds.
See "Risk Factors -- Technological Uncertainties."
 
     The Company is currently testing compounds in animal models of stroke and
other disorders believed to be associated with glutamate toxicity, such as ALS,
epilepsy, severe head trauma, and Parkinson's disease. Certain of these
compounds have shown significant neuroprotective activity in preclinical models.
 
                                       28
<PAGE>   30
 
  NOS Inhibitors
 
     The Company is developing drugs to inhibit the formation of nitric oxide, a
neurotransmitter that mediates certain important actions of glutamate. When
excess glutamate is released (e.g., due to stroke or severe head trauma), a
variety of biochemical effects occur, including activation of NOS, an enzyme
that synthesizes nitric oxide from the amino acid arginine. In animal models of
vascular stroke, treatment with nitroarginine, a NOS inhibitor, blocked 70% of
neuronal damage. Further, there are three distinct known forms of NOS: neuronal
NOS (nNOS), inducible NOS (iNOS) and endothelial NOS (eNOS). In animal models of
stroke, there is a 50% reduction of neuronal damage in a "knock-out" mouse
lacking nNOS. In contrast, inhibition of eNOS will reduce blood flow to the
brain during stroke, thus aggravating nerve cell damage. Consequently, there is
considerable interest in identifying compounds which selectively inhibit nNOS.
The Company is currently investigating novel mechanisms to selectively inhibit
nNOS activity. The Company has an exclusive license to an issued United States
patent which relates to the use of NOS inhibitors to prevent or treat disease
conditions caused by glutamate neurotoxicity.
 
  PARS Inhibitors
 
     The Company is developing compounds which inhibit PARS, an intracellular
enzyme that is involved in the repair of damaged DNA. Nitric oxide has been
shown to damage DNA in nerve cells and to trigger the activation of PARS, which
in turn leads to depletion of energy in the cell, resulting in cell death.
Guilford and Johns Hopkins scientists have shown that inhibitors of PARS can
prevent neurotoxicity in cultures of cerebral cortical neurons, suggesting that
they may be effective in treating stroke and neurodegenerative diseases. Using a
prototype small molecule PARS inhibitor, GPI-6000, Guilford scientists have
demonstrated that administration of that compound significantly decreases nerve
cell loss in a rat model of focal ischemia. The Company is using GPI-6000 to
establish proof of principle of the relevant mechanism of action but does not
intend to further develop this compound into a product. The Company is currently
seeking to develop proprietary lead small molecule PARS inhibitors for the
treatment of neurological disorders through medicinal chemistry around GPI-6000
and other compounds. See "Risk Factors -- Technological Uncertainties." The
Company has an exclusive license to an issued United States patent which relates
to the use of PARS inhibitors to treat disease conditions caused by NMDA
neurotoxicity.
 
  Addiction Therapeutics
 
     In February 1995, Guilford formed Gell, a corporate joint venture with
Abell focusing on the development of therapeutics for cocaine addiction and
other addictive behaviors. On March 5, 1997, Abell exercised its right to put
its interest in Gell to Guilford for 750,000 shares of Guilford Common Stock.
Thereafter, Gell became a wholly-owned subsidiary of Guilford. See
"-- Technology Licensing Agreements." Gell seeks to identify and develop
selective cocaine antagonists and mixed agonist/antagonists which will have
clinical utility in the treatment of cocaine addiction and overdose and other
addictive behaviors. It is estimated that 2.1 million people (nearly 1% of the
United States population) use cocaine on a weekly basis and that several hundred
thousand use it daily. At present, cocaine treatment options are generally
limited to counseling, psychotherapy and participation in self-help groups.
 
     The Company's cocaine addiction therapeutics program focuses on the
development of drugs which prevent cocaine from binding to dopamine transporters
while minimally affecting normal dopamine transport function. Within the past
decade, the mechanism by which cocaine exerts its addictive behaviors has been
elucidated. Scientists have found that cocaine facilitates the action of
dopamine in the brain by inhibiting the function of the dopamine transporter.
Dopamine uptake and cocaine binding occur at distinct sites on the transporter.
Therefore it may be possible to design drugs that specifically inhibit cocaine
binding while permitting the transporter to maintain its normal function.
 
     Guilford scientists have identified and synthesized novel compounds with
specificity for the cocaine recognition site in the brain and the Company has
filed patent applications covering several classes of compounds. A prototype
compound, GPI-2138, is 17 times more potent in binding to the cocaine binding
site than in inhibiting dopamine uptake, compared to cocaine. In animal
experiments, GPI-2138 blocked certain
 
                                       29
<PAGE>   31
 
behavioral effects produced by cocaine, including hyperlocomotion and cocaine
self-administration. Company scientists have synthesized other compounds which
exhibit a binding-to-uptake ratio in vitro of as high as 38 times greater than
cocaine. The Company has also entered into a cooperative research and
development agreement with the National Institute of Drug Abuse to identify and
develop cocaine antagonists. In addition to cocaine addiction, other forms of
addiction, including alcohol and heroin addiction, may result from facilitation
of dopaminergic neurotransmission in certain areas of the brain. As a result,
Guilford scientists are currently investigating whether GPI-2138 and related
compounds may block the addictive properties of alcohol and heroin in laboratory
animals. The Company is using GPI-2138 to establish proof of principle of the
relevant mechanism of action but does not intend to further develop this
compound into a product. The Company is currently seeking to develop proprietary
lead compounds in this program through medicinal chemistry around GPI-2138 and
other compounds. See "Risk Factors -- Technological Uncertainties."
 
STRATEGY
 
     Guilford's strategy in its drug delivery business is to capitalize on the
FDA clearance and commercial launch of GLIADEL and the Company's relationship
with RPR, Johns Hopkins and MIT by seeking to broaden the treatment indications
of GLIADEL and introducing new polymer-based drug delivery products. The Company
believes that its expertise in the discovery, development and manufacturing of
polymer-based drug delivery products positions Guilford to develop or acquire
new drug delivery technologies that could be complementary to GLIADEL. In its
neurological products business, Guilford plans to continue to develop novel
diagnostic and therapeutic product candidates that offer unique advantages over
competing products and technologies. Guilford will actively seek corporate
partners for these programs in order to minimize the costs and risks associated
with clinical development, capitalize on the capabilities of its partners and
enhance commercialization opportunities for its product candidates. Guilford
will seek to retain co-promotion rights for certain of its products in the
United States. At present, the Company does not intend to manufacture its small
molecule compounds.
 
MANUFACTURING AND RAW MATERIALS
 
     The Company manufactures GLIADEL using a proprietary process at its 12,500
square foot manufacturing facility in Baltimore, Maryland. Approximately 5,500
square feet of packaging, quality control, laboratory, and warehouse space were
added in 1996 to support the commercial launch of GLIADEL. The facility has been
in operation since April 1995 and was inspected by the FDA in October 1995. The
Company's current facilities are designed to enable the Company to produce up to
8,000 GLIADEL treatments annually. During 1997 and 1998, the Company expects to
make additional capital expenditures of approximately $3.7 million to expand the
Company's GLIADEL manufacturing plant capacity from 8,000 to 30,000 treatments
annually. The Company expects to draw on the capital available under its $7.5
million loan agreement with RPR to fund the expansion. See "Risk
Factors -- Limited Manufacturing Capabilities."
 
     The Company believes that the various materials used in GLIADEL are readily
available and will continue to be available at reasonable prices. Nevertheless,
the active chemotherapeutic ingredient in GLIADEL, the generic drug BCNU, is
currently being supplied by a single vendor. While the Company believes that it
has an adequate supply of BCNU to meet current demand and has entered into an
agreement for process development of BCNU with a potential second source of
BCNU, any interruption in the ability of the current supplier to deliver this
ingredient could prevent the Company from delivering the product on a timely
basis. The Company depends upon the availability of certain single-source raw
materials in its formulations, but is seeking alternate suppliers for most of
these raw materials as well. There can be no assurance that such sources can be
secured successfully on terms acceptable to the Company, or at all. Failure of
any supplier to provide sufficient quantities of raw material in accordance with
GMP could cause delays in clinical trials and commercialization of products. See
"Risk Factors -- Reliance on Suppliers."
 
     In October 1995 and July 1996, the Company entered into development and
contract manufacturing agreements with Nordion International Inc., a leading
supplier of radiolabeled products based in Canada, and its European subsidiary,
Nordion Europe S.A. (collectively, "Nordion"). Pursuant to these agreements, the
Company synthesizes the precursor of DOPASCAN and supplies it to Nordion, which
then radiolabels
 
                                       30
<PAGE>   32
 
DOPASCAN with Iodine-123 for distribution to hospitals involved in the clinical
trials in North America and Europe, respectively. During the term of these
agreements, Nordion has agreed not to perform development, manufacture or supply
services for any competing Iodine-123 radiolabeled imaging diagnostic for
Parkinson's disease based on dopamine transporter binding. Nordion's obligations
under the October 1995 agreement terminated as of November 30, 1996 and the
obligations under the July 1996 agreement will terminate on July 31, 1997 or
earlier in certain specified circumstances. The Company is currently negotiating
a new agreement respecting the manufacture and supply of DOPASCAN to support the
Company's planned Phase III clinical trials. However, there can be no assurance
that any such agreement will be reached on terms acceptable to the Company.
 
GOVERNMENT REGULATION AND PRODUCT TESTING
 
     All domestic prescription pharmaceutical manufacturers are subject to
extensive regulation by the federal government, principally the FDA and, to a
lesser extent, by state and local and perhaps foreign governments if products
are marketed abroad. Biologics and controlled drug products, such as vaccines
and narcotics, and radiolabeled drugs, are regulated more stringently than are
other drugs. The Federal Food, Drug, and Cosmetic Act and other federal statutes
and regulations govern or influence the development, testing, manufacture,
labeling, storage, approval, advertising, promotion, sale and distribution of
prescription pharmaceutical products. Pharmaceutical manufacturers are also
subject to certain recordkeeping and reporting requirements. Noncompliance with
applicable requirements can result in warning letters, fines, recall or seizure
of products, total or partial suspension of production and/or distribution,
refusal of the government to enter into supply contracts or to approve marketing
applications and criminal prosecution.
 
     Upon FDA approval, a drug may only be marketed for the approved indications
in the approved dosage forms and at the approved dosages. The FDA also may
require post-marketing testing and surveillance to monitor the record of the
approved product. Manufacturers of approved drug products are subject to ongoing
compliance with FDA regulations. For example, the FDA mandates that drugs be
manufactured in conformity with GMP regulations. In complying with the GMP
regulations, manufacturers must continue to expend time, money and effort in
production, recordkeeping and quality control to ensure that the product meets
applicable specifications and other requirements. The FDA periodically inspects
drug manufacturing facilities to ensure compliance with applicable GMP
requirements. Failure to comply subjects the manufacturer to possible FDA
action, such as suspension of manufacturing, seizure of the product or voluntary
recall of a product. Adverse experiences with the product must be reported to
the FDA. The FDA also may require the submission of any lot of the product for
inspection and may restrict the release of any lot that does not comply with FDA
regulations, or may otherwise order the suspension of manufacture, recall or
seizure. Product approvals may be withdrawn if compliance with regulatory
requirements is not maintained or if problems concerning safety or efficacy of
the product occur following approval.
 
FULL CLINICAL TESTING REQUIREMENTS
 
     The steps required before a newly marketed drug may be commercially
distributed in the United States include: (i) conducting appropriate preclinical
laboratory and animal tests; (ii) submitting to the FDA an application for an
Investigational New Drug ("IND"), which must become effective before clinical
trials may commence; (iii) conducting well-controlled human clinical trials that
establish the safety and efficacy of the drug product; (iv) filing with the FDA
a NDA for non-biological drugs; and (v) obtaining FDA approval of the NDA prior
to any commercial sale or shipment of the non-biological drug. In addition to
obtaining FDA approval for each indication to be treated with each product, each
domestic drug manufacturing establishment must register with the FDA, list its
drug products with the FDA, comply with GMP requirements and be subject to
inspection by the FDA. Foreign manufacturing establishments distributing drugs
in the United States also must comply with GMP requirements, list their
products, and are subject to periodic inspection by FDA or by local authorities
under agreement with FDA.
 
     With respect to a drug product with an active ingredient not previously
approved by the FDA, the manufacturer must usually submit a full NDA, including
complete reports of preclinical, clinical and laboratory studies, to prove that
the product is safe and effective. A full NDA may also need to be submitted
 
                                       31
<PAGE>   33
 
for a drug product with a previously approved active ingredient if studies are
required to demonstrate safety and efficacy, such as when the drug will be used
to treat an indication for which the drug was not previously approved, or where
the method of drug delivery is changed. In addition, the manufacturer of an
approved drug may be required to submit for the FDA's review and approval a
supplemental NDA, including reports of appropriate clinical testing, prior to
marketing the drug with additional indications or making other significant
changes to the product or its manufacture. A manufacturer intending to conduct
clinical trials ordinarily will be required first to submit an IND to the FDA
containing information relating to previously conducted preclinical studies.
 
     Preclinical testing includes formulation development, laboratory evaluation
of product chemistry and animal studies to assess the potential safety and
efficacy of the product formulation. Preclinical tests usually must be conducted
in accordance with the FDA regulations concerning Good Laboratory Practices
("GLPs"). The results of the preclinical tests are submitted to the FDA as part
of the IND and are reviewed by the FDA prior to authorizing the sponsor to
conduct clinical trials in human subjects. Unless the FDA objects to an IND, the
IND will become effective 30 days following its receipt by the FDA. There is no
certainty that submission of an IND will result in FDA authorization to commence
clinical trials or that authorization of one phase of a clinical trial will
result in authorization of other phases or that the performance of any clinical
trials will result in FDA approval.
 
     Clinical trials for new drugs typically are conducted in three phases and
are subject to detailed protocols. Clinical trials involve the administration of
the investigational drug product to human subjects. Each protocol indicating how
the clinical trial will be conducted must be submitted for review to the FDA as
part of the IND. The FDA's review of a study protocol does not necessarily mean
that, if the study is successful, it will constitute proof of efficacy or
safety. Further, each clinical study must be conducted under the auspices of an
independent institutional review board ("IRB") established pursuant to FDA
regulations. The IRB considers, among other factors, ethical concerns and
informed consent requirements. The FDA or the IRB may require changes in a
protocol both prior to and after the commencement of a trial. There is no
assurance that the IRB or the FDA will permit a study to go forward or, once
started, to be completed. Clinical trials may be placed on hold at any time for
a variety of reasons, particularly if safety concerns arise, or regulatory
requirements are not met.
 
     The three phases of clinical trials are generally conducted sequentially,
but they may overlap. In Phase I, the initial introduction of the drug into
humans, the drug is tested for safety, side effects, dosage tolerance,
metabolism and clinical pharmacology. Phase II involves controlled tests in a
larger but still limited patient population to determine the efficacy of the
drug for specific indications, to determine optimal dosage and to identify
possible side effects and safety risks. Phase II testing for an indication
typically takes at least from one and one-half to two and one-half years to
complete. If preliminary evidence suggesting effectiveness has been obtained
during Phase II evaluations, expanded Phase III trials are undertaken to gather
additional information about effectiveness and safety that is needed to evaluate
the overall benefit-risk relationship of the drug and to provide an adequate
basis for physician labeling. Phase III studies for a specific indication
generally take at least from two and one-half to five years to complete. There
can be no assurance that Phase I, Phase II or Phase III testing will be
completed successfully within any specified time period, if at all, with respect
to any of the Company's product candidates.
 
     Reports of results of the preclinical studies and clinical trials for
non-biological drugs are submitted to the FDA in the form of an NDA for approval
of marketing and commercial shipment. User fee legislation enacted in 1992 now
requires the submission of $240,000 to cover the costs of FDA review of an NDA.
The NDA typically includes information pertaining to the preparation of drug
substances, analytical methods, drug product formulation, details on the
manufacture of finished product as well as proposed product packaging and
labeling. Submission of an NDA does not assure FDA approval for marketing. The
application review process generally takes two to three years to complete,
although reviews of treatments for cancer and other serious or life-threatening
diseases may be accelerated. The approval process may take substantially longer
if, among other things, the FDA has questions or concerns about the safety
and/or efficacy of a product. In general, the FDA requires at least two properly
conducted, adequate and well-controlled clinical studies demonstrating efficacy
with sufficient levels of statistical assurance. The FDA also may request
long-term toxicity studies or
 
                                       32
<PAGE>   34
 
other studies relating to product safety or efficacy. For example, the FDA may
require additional clinical tests following NDA approval to confirm product
safety and efficacy (Phase IV clinical tests). Notwithstanding the submission of
such data, the FDA ultimately may decide that the application does not satisfy
its regulatory criteria for approval.
 
     Phase III or other clinical studies may be conducted after, rather than
before, FDA approval under certain circumstances. For example, the FDA may
determine under its expedited or accelerated approval regulations that earlier
studies may establish an adequate basis for drug product approval, provided that
the sponsor agrees to conduct additional studies after approval to verify safety
and effectiveness. Treatment with an experimental drug of patients not in
clinical trials may also be allowed under a Treatment IND before general
marketing begins and pending FDA approval. Charging for an investigational drug
also may be allowed under a Treatment IND to recover certain costs of
development if various requirements are met. These cost-recovery, treatment and
expedited or accelerated approval regulations are limited, for example, to drug
products intended to treat AIDS or other serious or life-threatening diseases
and that provide meaningful therapeutic benefit to patients over existing
treatments or that are for diseases for which no satisfactory alternative
therapy exists. No assurances exist that the Company's product candidates will
qualify for cost-recovery, expedited or accelerated approvals or for treatment
use.
 
     The full NDA process for newly marketed non-biological drugs takes a number
of years and involves the expenditure of substantial resources. There can be no
assurance that any approval will be granted on a timely basis, or at all or that
the Company will have sufficient resources to carry such potential products
through the regulatory approval process.
 
ABBREVIATED TESTING REQUIREMENTS
 
     The Drug Price Competition and Patent Term Restoration Act of 1984
("DPC-PTR Act") established abbreviated procedures for obtaining FDA approval
for many non-biological drugs which are off-patent and whose marketing
exclusivity has expired. Applicability of the DPC-PTR Act means that a full NDA
is not required for approval of a competitive product. Abbreviated requirements
are applicable to drugs which are, for example, either bioequivalent to brand
name drugs, or otherwise similar to brand name drugs, such that all the safety
and efficacy studies previously done on the innovator product need not be
repeated for approval. Changes in approved drug products, such as in the
delivery system, dosage form, or strength, can be the subject of abbreviated
application requirements. There can be no assurance that abbreviated
applications will be available or suitable for the Company's non-biological drug
products or that FDA approval of such applications can be obtained.
 
     A five year period of market exclusivity is provided for newly marketed
active ingredients of drug products not previously approved and a three-year
period for certain changes in approved drug products that require for approval
the submission of safety and efficacy information (other than bioequivalence
studies). A period of five years is available for new chemical entities not
previously approved by FDA. A period of three years is available for changes in
approved products, such as in delivery systems of previously approved products.
Both periods of marketing exclusivity mean that abbreviated applications, which
generally rely to some degree on approvals or on some data submitted by previous
applicants for comparable innovator drug products, cannot be approved during the
period of exclusivity. The market exclusivity provisions of the DPC-PTR Act bar
only the marketing of competitive products that are the subject of abbreviated
applications, not products that are the subject of full NDAs. The DPC-PTR Act
also may provide a maximum time of five years to be restored to the life of any
one patent for the period it takes to obtain FDA approval of a drug product,
including biological drugs. No assurances exist that the exclusivity or patent
restoration benefits of the DPC-PTR Act will apply to any product candidates of
the Company.
 
OTHER REGULATION
 
     Products marketed outside the United States which are manufactured in the
United States are subject to certain FDA regulations, as well as regulation by
the country in which the products are to be sold. The Company also would be
subject to foreign regulatory requirements governing clinical trials and
pharmaceuti-
 
                                       33
<PAGE>   35
 
cal sales, if products are marketed abroad. Whether or not FDA approval has been
obtained, approval of a product by the comparable regulatory authorities of
foreign countries must usually be obtained prior to the commencement of
marketing of the product in those countries. The approval process varies from
country to country and the time required may be longer or shorter than that
required for FDA approval.
 
     The Company also is governed by other federal, state and local laws of
general applicability. These laws include, but are not limited to, those
regulating working conditions enforced by the Occupational Safety and Health
Administration and regulating environmental hazards under such statutes as the
Toxic Substances Control Act, the Resource Conservation and Recovery Act and
other environmental laws enforced by the United States Environmental Protection
Agency ("USEPA"). The DEA regulates controlled substances, such as narcotics.
Establishments handling controlled substances must, for example, be licensed and
inspected by the DEA, and may be subject to export, import, security and
production quota requirements. Radiolabeled products, including drugs, are also
subject to regulation by the Department of Transportation and to state and
federal licensing requirements. Various states often have comparable health and
environmental laws, such as those governing the use and disposal of controlled
and radiolabeled products.
 
     While the Company is not actively involved in product areas involving
biotechnology and has no current plans to develop products utilizing modern
biotechnology, if the Company were to move in that direction, it would
potentially be subject to extensive regulation. The USEPA, the FDA and other
federal and state regulatory bodies have developed or are in the process of
developing specific requirements concerning products of biotechnology that may
affect research and development programs and product lines. The Company is
unable to predict whether any governmental agency will adopt requirements,
including regulations, which would have a material and adverse effect on any
future product applications involving biotechnology.
 
PATENTS AND PROPRIETARY TECHNOLOGY
 
     Guilford believes that patent and trade secret protection is crucial to its
business and that its future will depend in part on its ability to obtain
patents, maintain trade secret protection and operate without infringing the
proprietary rights of others. As of December 31, 1996, the Company owned or had
licensed rights to 49 United States and 106 foreign patents and 32 United States
and 100 foreign patent applications with claims relating to its biodegradable
polymer, imaging, neurotrophic, neuroprotective and cocaine addiction
therapeutics programs. In March 1997, the Company was issued a United States
patent for the compositions and uses of a series of neuroimmunophilin ligands as
neurotrophic agents for the treatment of neurodegenerative disorders.
 
   
     The role, validity and value of patents, licenses and proprietary
technology in the business of the Company are subject to various uncertainties
and contingencies. The Company's success will depend in part on its ability to
obtain, maintain and enforce patent protection for its products and processes or
license rights to patents, maintain trade secret protection and operate without
infringing upon the proprietary rights of others. The degree of patent
protection afforded to pharmaceutical and biotechnological inventions is
uncertain, and a number of Guilford's product candidates are subject to this
uncertainty. The Company is aware of a company which has asserted in a public
filing that it has patent applications claiming the use of certain of its
immunosuppressive compounds and multidrug resistance compounds for nerve growth
applications, as well as a patent and patent applications relating to compounds
which it claims are useful in nerve growth applications. While the Company does
not believe that its neurotrophic compounds infringe on such company's patent,
no assurance can be given as to the ability of the Company's patents and patent
applications to adequately protect the Company's neurotrophic product
candidates, including GPI-1046, or that the Company's neurotrophic product
candidates will not infringe or be dominated by this company's patent or patent
applications, if issued. There can be no assurance that any patent application
filed by, or assigned or licensed to, the Company will be granted, that the
Company will develop additional products or processes that are patentable, or
that any patents issued to, or licensed by, the Company will provide the Company
with any competitive advantages or adequate protection for its products. In
addition, there can be no assurance that any existing or future patents or
intellectual property issued to, or licensed by, the Company will not
subsequently be challenged, invalidated or circumvented by others.
    
 
     It is Guilford's policy to control the disclosure and use of Guilford's
know-how and trade secrets under confidentiality agreements with employees,
consultants and other parties. There can be no assurance, however,
 
                                       34
<PAGE>   36
 
that its confidentiality agreements will be honored, that others will not
independently develop equivalent or competing technology, that disputes will not
arise concerning the ownership of intellectual property or the applicability of
confidentiality obligations, or that disclosure of Guilford's trade secrets will
not occur. To the extent that consultants or other research collaborators use
intellectual property owned by others in their work with the Company, disputes
may also arise as to the rights to related or resulting intellectual property.
 
     Guilford supports and collaborates in research conducted in universities
and in governmental research organizations. There can be no assurance that the
Company will have or be able to acquire exclusive rights to the inventions or
technical information derived from such collaborations or that disputes will not
arise as to rights in derivative or related research programs conducted by the
Company. In addition, in the event of a contractual breach by the Company,
certain of the Company's collaborative research contracts provide for transfer
of technology (including any patents or patent applications) to the contract
sponsors.
 
     If the Company is required to defend against charges of infringement of
patent or proprietary rights of third parties or to protect its own patent or
proprietary rights against third parties, the Company may incur substantial
costs and could lose rights to develop or market certain products or be required
to pay monetary damages or royalties to license proprietary rights from third
parties. In response to actual or threatened litigation, the Company may seek
licenses from third parties or attempt to redesign its products or processes to
avoid infringement; however, there can be no assurance that the Company will be
able to obtain licenses on acceptable terms or at all or redesign its products
or processes. In addition to being a party to patent infringement litigation,
the Company could be required to participate in patent interference proceedings
declared by the United States Patent and Trademark Office, which would be
expensive and time-consuming, even if the Company were to prevail in such a
proceeding. The Company may also be forced to initiate legal proceedings to
protect its patent position or other proprietary rights. These proceedings
typically are costly, protracted, and offer no assurance of success.
 
TECHNOLOGY LICENSING AGREEMENTS
 
     In March 1994, the Company entered into an agreement with Scios Inc.
("Scios") (the "GLIADEL Agreement") pursuant to which the Company licensed from
Scios exclusive worldwide rights to 35 United States patents and patent
applications as well as 100 corresponding international patents and patent
applications for polyanhydride biodegradable polymer technology for use in the
field of tumors of the central nervous system and cerebral edema. GLIADEL is
covered by a United States patent which expires in 2010 and certain related
international patents and patent applications. In April 1994, Scios assigned all
of its rights and obligations under the GLIADEL Agreement to MIT. Under the
terms of the GLIADEL Agreement, Guilford is obligated to pay a royalty on all
net sales of products incorporating such technology as well as a percentage of
all royalties received by Guilford from sublicensees and certain advance and
minimum annual royalty payments. In 1996, Guilford paid $1.1 million in royalty
payments to MIT related to payments made to the Company from RPR and Orion
Farmos related to GLIADEL. Guilford has exclusive worldwide rights to the
technology for brain cancer therapeutics, subject to certain conditions,
including a requirement to perform appropriate preclinical tests and file an IND
with the FDA within 24 months of the identification of a drug-polymer product
having greater efficacy than GLIADEL. In addition, Guilford is obligated to
spend a minimum dollar amount in developing products resulting from the
technology through 1997 and to meet certain development milestones. Although the
Company believes that it can comply with such obligations, failure of the
Company to perform these obligations could result in the Company losing its
right to the new polymer-based product.
 
     In June 1996, the Company entered into a license agreement with MIT and
Johns Hopkins respecting a patent application covering certain biodegradable
polymers for use in connection with the controlled local delivery of certain
chemotherapeutic agents (including paclitaxel (Taxol(R)) and camptothecin) for
treating solid tumors. Under this agreement, the Company is obligated to make
certain annual and milestone payments to MIT and to pay royalties based on any
sales of products incorporating the technology licensed to Guilford.
Furthermore, under the terms of the agreement, the Company has committed to
spend minimum amounts to develop the technology and to meet certain development
milestones. Although the Company believes that it
 
                                       35
<PAGE>   37
 
can comply with such obligations, failure of the Company to perform these
obligations could result in the Company losing its rights to such technology.
 
     In July 1996, the Company entered into a license agreement with Johns
Hopkins for two United States patents respecting certain polyphosphoesters
("PPE") polymers developed at Johns Hopkins. This agreement, among other things,
requires Guilford to pay certain processing, maintenance and/or up-front fees,
milestone payments and royalties, a portion of proceeds from sublicenses, and
fees and costs related to patent prosecution and maintenance and to spend
minimum amounts for and meet deadlines regarding development of this technology.
In the event of termination of these licenses, the Company could lose its rights
to use of the licensed technology. The Company has also entered into a sponsored
research agreement with Johns Hopkins with respect to this PPE technology and
has a right of first negotiation regarding inventions that result from this
work.
 
     The Company obtained exclusive worldwide rights to DOPASCAN pursuant to a
March 1994 license agreement (the "RTI Agreement") with Research Triangle
Institute ("RTI"), which grants Guilford rights to various United States and
international patents and patent applications relating to binding ligands for
certain receptors in the brain which are or may be useful as dopamine neuron
imaging agents. DOPASCAN and certain related precursors and analogues are
covered by United States patents which start expiring in 2009, as well as
certain related international patents and patent applications. Under the RTI
Agreement, the Company reimbursed RTI for certain past patent-related expenses
and agreed to make annual payments to RTI to support mutually agreed upon
research to be conducted at RTI through March 1999. In addition, the Company is
obligated to pay RTI a royalty on gross revenues to Guilford from products
derived from the licensed technology and from sublicensee proceeds and to make
certain minimum royalty payments following the first commercial sale of such
products. In January 1997, the Company paid RTI $32,000 as a result of a payment
received from DRL, the Company's DOPASCAN partner in Japan. Guilford must use
commercially reasonable efforts to develop products related to the licensed
technology and to meet certain performance milestones. Failure of the Company to
perform its obligations under the RTI Agreement in the future could result in
termination of the license.
 
     Guilford and Johns Hopkins are parties to two exclusive license agreements
covering the following technologies: (i) neurotrophic use of neuroimmunophilin
ligands, which was jointly discovered by scientists at, and is jointly owned by,
Johns Hopkins and Guilford; and (ii) inhibition of NOS and PARS for
neuroprotective uses. These agreements, among other things, require Guilford to
pay certain processing, maintenance, and/or up-front fees, milestone payments
and royalties, a portion of proceeds from sublicenses, and fees and costs
related to patent prosecution and maintenance and to spend minimum amounts for
and meet deadlines regarding development of the technologies. In the event of
termination of these licenses, the Company could lose its rights to use of the
licensed technology (or in the case of joint inventions, exclusive use of such
technology).
 
     Gell, through which the Company conducts its cocaine addiction therapeutics
program, was initially formed in February 1995 as a joint venture owned 80% by
Abell and 20% by Guilford. The $2.5 million in capital invested by Abell in Gell
has funded the cocaine addiction therapeutics program since inception. On March
5, 1997, Abell exercised its right to put its interest in Gell to Guilford for
750,000 shares of Guilford Common Stock. Thereafter Gell became a wholly-owned
subsidiary of the Company.
 
  United States Government Rights
 
     Aspects of the technology licensed under the Company's license agreements
may be subject to certain Government Rights. These rights include a
non-exclusive, royalty-free worldwide license to practice or have practiced such
inventions for any governmental purpose. In addition, the United States
government has the right to grant licenses which may be exclusive under any of
such inventions to a third-party if it determines that: (i) adequate steps have
not been taken to commercialize such inventions; (ii) such action is necessary
to meet public health or safety needs; or (iii) such action is necessary to meet
requirements for public use under federal regulations. The government also has
the right to take title to a subject invention if there is failure to disclose
the invention and elect title within specified time limits. In addition, the
government may acquire title in any country in which a patent application is not
filed within specified time limits. Federal law requires any
 
                                       36
<PAGE>   38
 
licensor of an invention that was partially funded by the federal government to
obtain a covenant from any exclusive licensee to manufacture products using the
invention substantially in the United States. Further, the Government Rights
include the right to use and disclose without limitation technical data relating
to licensed technology that was developed in whole or in part at government
expense. Provisions recognizing these Government Rights are contained in the
Company's principal technology license agreements.
 
SALES, MARKETING AND DISTRIBUTION
 
     In general, the Company's strategy is to seek to establish strategic
alliances with larger pharmaceutical companies to develop and promote products
that require extensive development, sales and marketing resources. Within the
United States, the Company may seek to retain co-promotion rights with respect
to some or all compounds or indications in any such strategic alliances, or the
Company may elect to market and distribute its products directly where the
commercial prospects so warrant.
 
     In June 1996, the Company entered into a marketing, sales and distribution
rights agreement and other related agreements with RPR granting RPR worldwide
(excluding Scandinavia) marketing, sales, promotion and distribution rights for
GLIADEL. Upon execution of these agreements, the Company received $7.5 million
for 281,531 shares of Common Stock. Furthermore, in addition to an aggregate of
$27.5 million in rights payments made by RPR upon execution of the agreements in
June 1996 and FDA clearance of the GLIADEL NDA in September 1996, the agreements
with RPR provide for up to an additional $40 million in payments in the event
that certain regulatory and other milestones are achieved, although there can be
no assurance that any or all of such milestones will be attained and certain of
these payments are contingent on international regulatory filings and
clearances, the timing and extent of which are largely within the control of
RPR. Moreover, RPR may, under certain circumstances, fund up to approximately
$17 million for the development of higher dose forms of GLIADEL being developed
by the Company and for certain additional clinical studies related to GLIADEL.
Finally, under these agreements, the Company has the right under certain
circumstances to borrow up to an aggregate of $7.5 million to expand the
Company's GLIADEL manufacturing and related facilities. In addition to the
payments outlined above, the Company will act as the exclusive manufacturer of
GLIADEL and will receive transfer price payments and royalties based on any "net
sales" (as defined in the agreements with RPR) of GLIADEL. RPR's exclusive
rights terminate in a particular country upon the later of the expiration of the
last to expire of certain patents applicable in that country or the last
commercial sale of GLIADEL in that country. Under the Company's agreements with
RPR, RPR has an exclusive six-month period following development of new polymer
technology by the Company to make an offer to license such technology for
oncology applications.
 
     In October 1995, the Company entered into an agreement appointing Orion
Farmos distributor for GLIADEL in Scandinavia, and in December 1995 the Company
entered into an agreement with DRL for the marketing, sale and distribution of
DOPASCAN in Japan, Korea and Taiwan. See "Risk Factors -- Dependence on GLIADEL
and RPR" and "-- Lack of Sales and Marketing Experience."
 
COMPETITION
 
     The Company is involved in evolving technological fields in which
developments are expected to continue at a rapid pace. Guilford's success
depends upon its ability to effectively compete in the research, development and
commercialization of products and technologies in its areas of focus.
Competition from pharmaceutical, chemical and biotechnology companies,
universities and research institutes is intense and expected to increase. Many
of these competitors have substantially greater research and development
capabilities, experience and manufacturing, marketing, financial and managerial
resources and represent significant competition for the Company. Acquisitions of
competing companies by large pharmaceutical or other companies could enhance the
financial, marketing and other resources available to these competitors. These
competitors may develop products which are superior to those under development
by the Company.
 
     The Company is aware of several competing approaches under development for
the treatment of malignant glioma including using radioactive seeds for
interstitial radiotherapy, increasing the permeability of the blood-brain
barrier to chemotherapeutic agents, sensitizing cancer cells to chemotherapeutic
agents using gene therapy and developing chemotherapeutics directed to specific
receptors in brain tumors. To the
 
                                       37
<PAGE>   39
 
Company's knowledge, none of these approaches has resulted in compounds studied
in randomized, controlled trials which have shown them to be superior to
conventional therapy.
 
     The Company believes that two other companies are clinically evaluating
imaging agents for dopamine neurons. In addition, a variety of radiolabeled
compounds for use with Positron Emission Tomography ("PET") scanners have been
used to image dopamine neurons successfully in patients with Parkinson's
disease. PET scanning is currently only available in a limited number of
hospitals in the United States and Europe.
 
     A number of companies have shown interest in trying to develop neurotrophic
agents to promote nerve growth and repair in neurodegenerative disorders and
traumatic central nervous system injuries. However much of this activity has
focused on naturally occurring growth factors. Such large molecules generally
cannot cross the blood-brain barrier and thus present problems in administration
and delivery. One company has announced that certain of its neuroimmunophilin
ligands showed positive results in stimulating nerve growth in an animal model
of nerve crush, and has disclosed that it has made patent filings covering
compounds and uses in connection with nerve growth promotion. In addition,
another company announced that IGF-1 showed positive results in clinical trials
of a peripheral neurodegenerative disorder.
 
     There is intense competition to develop an effective and safe
neuroprotective drug or biological agent. Calcium channel antagonists, calpain
inhibitors, adenosine receptor antagonists, free radical scavengers, superoxide
dismutase inducers, proteoloytic enzyme inhibitors, phospholipase inhibitors and
a variety of other agents are under active development by others. Glutamate or
NMDA receptor antagonists are under development by several other companies.
 
     In the field of cocaine addiction, most of the investigated compounds to
date have been studied by academic and government groups. Further, much of this
work has been with known agents, such as carbamazepine, that are commercially
available for other indications. Guilford is aware of another company that is
investigating the use of butylcholinesterase as a treatment for acute cocaine
overdose. The Company is aware of one company that is investigating an
immunological approach in an attempt to develop a cocaine vaccine. The Company
is not aware of other commercial research programs targeting specific cocaine
antagonists, which do not interfere with normal dopamine neuron function.
 
     Any product candidate that the Company develops and for which it gains
regulatory approval, including GLIADEL, must then compete for market acceptance
and market share. For certain of the Company's product candidates, an important
factor will be the timing of market introduction of competitive products.
Accordingly, the relative speed with which the Company and competing companies
can develop products, complete the clinical testing and approval processes, and
supply commercial quantities of the products to the market is expected to be an
important determinant of market success. Other competitive factors include
capabilities of the Company's collaborators, product efficacy and safety, timing
and scope of regulatory approval, product availability, marketing and sales
capabilities, reimbursement coverage, the amount of clinical benefit of the
Company's product candidates relative to their cost, method of administration,
price and patent protection. There can be no assurance that the Company's
competitors will not develop more effective or more affordable products or
achieve earlier product development completion, patent protection, regulatory
approval or product commercialization than the Company. The achievement of any
of these goals by the Company's competitors could have a material adverse effect
on the Company's business, financial condition and results of operations.
 
FACILITIES
 
     In August 1994, the Company entered into a master lease for an
approximately 83,000 square foot building in Baltimore, Maryland. The Company
currently occupies 23,000 square feet for office space, 12,500 square feet for
manufacturing space, and 35,000 square feet of research and development
laboratories. The remaining 12,500 square feet is available for additional
laboratories or manufacturing facilities. The master lease expires in July 2005.
Two five-year renewal options are available to the Company or the Company may
exercise a purchase option any time after the ninth year for the then current
fair market value.
 
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<PAGE>   40
 
PRODUCT LIABILITY AND INSURANCE
 
     Product liability risk is inherent in the testing, manufacture, marketing
and sale of the Company's product candidates, and there can be no assurance that
the Company will be able to avoid significant product liability exposure. While
the Company currently maintains $10,000,000 of product liability insurance
covering clinical trials and produced sales, there can be no assurance that such
or any future insurance coverage obtained by the Company will be adequate or
that claims will be covered by the Company's insurance. The Company's insurance
policies provide coverage on a claims-made basis and are subject to annual
renewal. Product liability insurance varies in cost, can be difficult to obtain
and may not be available to the Company in the future on acceptable terms, or at
all. See "Risk Factors -- Risk of Product Liability."
 
EMPLOYEES
 
     At December 31, 1996, the Company employed 138 individuals. By February 28,
1997 that number was 156. Of these 156 employees, 130 were employed in the areas
of research and product development and in manufacturing and quality control of
GLIADEL. The remaining 26 employees performed general and administrative
functions, including executive, finance and administration, legal and business
development. To date, the Company has experienced no work stoppages related to
labor issues and believes its relations with its employees are good.
 
     All employees are required to enter into a confidentiality agreement with
the Company. Hiring and retaining qualified personnel are important factors for
the Company's future success. The Company is likely to continue to add personnel
particularly in the areas of research, clinical research and operations,
including manufacturing. Intense competition exists for these qualified
personnel from other biotechnology and biopharmaceutical companies, academic,
research and governmental organizations. There can be no assurance that the
Company will be able to continue to hire qualified personnel and, if hired, that
the Company will be able to retain these individuals. See "Risk
Factors -- Dependence on Qualified Personnel and Consultants."
 
SCIENTIFIC ADVISORY BOARD
 
     Guilford's Scientific Advisory Board consists of individuals with
recognized expertise in fields related to Guilford's research and development
programs. The Scientific Advisory Board meets with the Company at least twice a
year to discuss research priorities and new developments in neuroscience and
consults with and meets informally with the Company on an as-needed basis.
 
     The following persons are members of Guilford's Scientific Advisory Board:
 
     SOLOMON H. SNYDER, M.D. has been a Director of the Company and Chairman of
the Scientific Advisory Board since the Company's inception in July 1993. Dr.
Snyder received his M.D. in 1962 from Georgetown Medical School, trained as a
Research Associate with Julius Axelrod at the National Institute of Mental
Health and completed his Psychiatry Residency at Johns Hopkins Hospital. He is
presently Director of the Department of Neuroscience at Johns Hopkins Medical
School and Distinguished Service Professor of Neuroscience, Pharmacology and
Molecular Sciences, and Psychiatry. Dr. Snyder has received a number of awards
including the Albert Lasker Award in Basic Biomedical Research, the Wolf Prize
and the Bower Award. He is a member of the United States National Academy of
Sciences, the Institute of Medicine and the American Academy of Arts and
Sciences. Dr. Snyder is a director of Scios.
 
     Dr. Snyder has provided consulting services to the Company under consulting
agreements since August 1993. In September 1995, the Company and Dr. Snyder
entered into a new consulting agreement pursuant to which Dr. Snyder will
provide consulting services to the Company through August 1998, unless the
agreement is further extended or earlier terminated. Under the agreement, Dr.
Snyder performs consulting and advisory services as requested by the Company for
a minimum of 24 days and a maximum of 38 days per year, subject to adjustment
under certain circumstances. With certain limited exceptions, Dr. Snyder has
agreed not to engage in any business activity with or provide any consulting or
related services to any organization which directly competes with the Company
during the term of the agreement and for a period of one year thereafter.
 
     JOSEPH COYLE, M.D. is Chairman of the consolidated Department of Psychiatry
and Ebens Draper Professor of Psychiatry and Neuroscience at the Harvard Medical
School. He obtained his M.D. from Johns
 
                                       39
<PAGE>   41
 
Hopkins in 1969 and completed his Psychiatry Residency at Johns Hopkins. His
research involves clinical as well as basic studies of neurotransmitter systems
and drug actions in the brain. He has received numerous honors, including the
McAlpin Award of the National Mental Health Association, the Gold Medal Award of
the Society for Biological Psychiatry and election to the Institute of Medicine
of the National Academy of Sciences.
 
     SAMUEL H. BARONDES, M.D. is the Jeanne and Sanford Robertson Professor of
Neurobiology and Psychiatry and Director of the Center for Neurobiology and
Psychiatry at the University of California, San Francisco. He received his M.D.
from Columbia University in 1958, trained in internal medicine at the Peter Bent
Brigham Hospital, in molecular biology at the National Institutes of Health and
in psychiatry at the McLean and Massachusetts General Hospitals. Dr. Barondes
has received a number of awards including the Royer Award and the Stillmark
Medal, is a member of the Institute of Medicine, and also serves as President of
the McKnight Endowment Fund for Neuroscience.
 
     ROBERT LANGER, PH.D. is presently Germeshausen Professor in the Department
of Chemical Engineering at MIT. Dr. Langer obtained his Ph.D. from MIT in 1974
and since then has been a member of the MIT faculty. Dr. Langer is a leading
authority on polymer drug delivery systems. He has received numerous awards
including election to the United States National Academy of Sciences, the
National Academy of Engineering and the Institute of Medicine.
 
     IRA SHOULSON, M.D. obtained his M.D. from the University of Rochester in
1971 where he completed internal medicine and neurology residencies. He is
presently Louis C. Lasagna Professor of Experimental Therapeutics and Professor
of Neurology, Pharmacology and Medicine at the University of Rochester. He is
the recipient of numerous honors including the Modern Medicine Award for
Distinguished Achievement. Dr. Shoulson is a national leader in the design and
execution of major clinical trials evaluating drug actions in Parkinson's
disease, Huntington's disease and other movement disorders. Dr. Shoulson has
served two terms as a member of the Peripheral and Central Nervous System
Advisory Committee of the FDA.
 
     ANNE YOUNG, M.D., PH.D. obtained her M.D. and Ph.D. degrees from Johns
Hopkins Medical School in 1973 and 1974, respectively, and completed her
Neurology Residency at the University of California in San Francisco. She served
on the faculty of the Neurology Department at the University of Michigan and
since 1991 has been Julieanne Dorn Professor of Neurology at the Harvard Medical
School and Chief of the Neurology Service at the Massachusetts General Hospital.
She has received numerous honors including election to the American Academy of
Arts and Sciences. Her laboratory research focuses on the actions of excitatory
amino acids in the brain, while her clinical research deals with movement
disorders.
 
                                       40
<PAGE>   42
 
                                   MANAGEMENT
 
DIRECTORS AND EXECUTIVE OFFICERS
 
     The directors and executive officers of the Company are as follows:
 
   
<TABLE>
<CAPTION>
                 NAME                     AGE                        POSITION
- --------------------------------------    ---     ----------------------------------------------
<S>                                       <C>     <C>
Craig R. Smith, M.D. .................    51      Chairman of the Board of Directors, President
                                                  and Chief Executive Officer
John P. Brennan.......................    54      Senior Vice President, Operations
Andrew R. Jordan......................    49      Senior Vice President, Chief Financial Officer
                                                  and Treasurer
David R. Savello, Ph.D. ..............    51      Senior Vice President, Drug Development
Earl Webb Henry, M.D. ................    49      Vice President, Clinical Research
Ross S. Laderman......................    50      Vice President, Regulatory Affairs
Nicholas Landekic.....................    38      Vice President, Business Development
Thomas C. Seoh........................    39      Vice President, General Counsel and Secretary
Peter D. Suzdak, Ph.D. ...............    38      Vice President, Research
George L. Bunting, Jr.(1).............    56      Director
Richard L. Casey(1)...................    50      Director
Elizabeth M. Greetham(2)..............    47      Director
Solomon H. Snyder, M.D.(2)............    58      Chairman of Scientific Advisory Board and
                                                  Director
W. Leigh Thompson, M.D., Ph.D.(2).....    58      Director
</TABLE>
    
 
     --------------------
     (1) Member of the Audit Committee.
     (2) Member of the Compensation Committee.
 
     CRAIG R. SMITH, M.D. has been a Director of the Company since its inception
in July 1993. Dr. Smith was elected President and Chief Executive Officer in
August 1993 and was elected Chairman of the Board in January 1994. Prior to
joining the Company, Dr. Smith was Senior Vice President for Business and Market
Development at Centocor, Inc., a biotechnology company. Dr. Smith joined
Centocor in 1988 as Vice President of Clinical Research after serving on the
Faculty of the Department of Medicine at Johns Hopkins Medical School for 13
years. Dr. Smith received his M.D. from the State University of New York at
Buffalo in 1972 and received training in Internal Medicine at The Johns Hopkins
Hospital from 1972 to 1975.
 
   
     JOHN P. BRENNAN joined the Company as Vice President, Operations in January
1994 and became Senior Vice President, Operations in January 1997. From 1980 to
1993, he was Vice President, Technical Operations and Manufacturing for G.D.
Searle and Co., a pharmaceutical company, and was responsible for the operation
of manufacturing plants in North America, Latin America and Europe and worldwide
pharmaceutical and process technology from 1980 to 1993. From 1977 to 1980, Mr.
Brennan was General Manager of the E.R. Squibb & Sons, Inc. manufacturing
facility in Humacao, Puerto Rico. Mr. Brennan held various technical positions
at Smith Kline Corporation from 1960 to 1977. Mr. Brennan has 36 years of
experience in the pharmaceutical industry. Mr. Brennan received his B.S. in
Chemistry from the Philadelphia College of Pharmacy and Science in 1968 and
attended the Wharton Graduate Management Program in 1976.
    
 
   
     ANDREW R. JORDAN joined the Company as Vice President, Secretary, Treasurer
and Chief Financial Officer in September 1993 and became Senior Vice President,
Treasurer and Chief Financial Officer in January 1997. Prior to joining the
Company, Mr. Jordan held various positions with KPMG Peat Marwick LLP, a public
accounting firm, beginning in 1973, including partner since 1983. Mr. Jordan's
experience at KPMG Peat Marwick LLP included advising early stage and emerging
technology companies and initial and secondary public equity and debt offerings.
He received his B.A. from Rutgers College in 1969 and his MBA from Rutgers
Graduate School of Business in 1973 and is a Certified Public Accountant.
    
 
                                       41
<PAGE>   43
 
   
     DAVID R. SAVELLO, PH.D. joined the Company as Senior Vice President, Drug
Development in April 1997. Prior to joining the Company, Dr. Savello was
employed by Glaxo Wellcome, Inc. ("Glaxo") since 1985, most recently as Vice
President, North American Regulatory Affairs from 1995 to 1997. Prior to 1995,
Dr. Savello served as Vice President, Drug Development and later as Vice
President, Regulatory Affairs and Compliance, at the affiliated entity Glaxo
Research Institute. Dr. Savello's duties at Glaxo have included leading United
States and Canadian regulatory operations and International Research and
Development, Quality Assurance, and Good Manufacturing Practices for all bulk
drug substance and clinical supplies manufacturing and packaging. Dr. Savello
received his Ph.D. and M.S. in pharmaceuticals from the University of Maryland
in 1972 and 1971, respectively, and his B.S. in pharmacy in 1968 from the
Massachusetts College of Pharmacy.
    
 
     EARL WEBB HENRY, M.D. joined the Company in January 1995 as Vice President,
Clinical Research. Prior to joining the Company, Dr. Henry was the global head
of clinical research for central nervous system products at Sandoz Research
Institute. He began at Sandoz as the Executive Director of Clinical Research in
1992. From 1987 to 1992, he was an Associate Director then a Senior Associate
Director of Clinical Research at Pfizer Central Research. From 1979 to 1986 he
was an attending physician at the Children's Hospital in Boston. Dr. Henry
received his B.S. in Chemistry at the University of Illinois and his M.D. at the
University of Chicago.
 
     ROSS S. LADERMAN, M.P.H. joined the Company as Vice President, Regulatory
Affairs in February 1994. Prior to joining Guilford, Mr. Laderman was Deputy
Director, Division of Scientific Investigations in the Office of Compliance of
the Center for Drug Evaluation and Research of the FDA. Mr. Laderman's career at
the FDA spanned 25 years during which time he worked in investigations,
compliance, public affairs and executive management. He received the
Commissioner's Special Citation and the Award of Merit from the FDA. Mr.
Laderman received his B.A. in Biology from MacMurray College and an M.P.H. from
Johns Hopkins University.
 
     NICHOLAS LANDEKIC joined the Company in March 1995 as Vice President,
Business Development. From January 1992 to February 1995, Mr. Landekic was
Senior Director of Business Development at Cephalon, Inc. and was responsible
for licensing and other corporate collaborations. From 1989 to 1992, he was a
Senior Manager of Product Planning at Bristol-Myers Squibb Company and was
responsible for worldwide commercial development and strategic planning for
currently marketed and new central nervous system products. From 1985 to 1989,
Mr. Landekic worked for Johnson & Johnson Corporation in a variety of positions
in business development and finance. Mr. Landekic received his M.B.A. in
Finance/Marketing from the State University of New York at Albany, M.A. in
Biology from Indiana University and a B.S. in Biology from Marist College.
 
     THOMAS C. SEOH joined the Company in April 1995 as Vice President, General
Counsel and Secretary. From 1992 to 1995, Mr. Seoh was affiliated with the ICN
Pharmaceuticals, Inc. ("ICN") group, as Vice President and Associate General
Counsel of ICN from 1994 to 1995, Vice President, General Counsel and Secretary
of Viratek, Inc. from 1993 to 1994 and Deputy General Counsel of SPI
Pharmaceuticals, Inc. from 1992 to 1994, providing legal function support for
pharmaceutical operations, research and development and corporate development.
From 1990 to 1992, Mr. Seoh was General Counsel and Secretary of Consolidated
Press U.S., Inc., the North American holding company of the Sydney,
Australia-based Consolidated Press group. Prior thereto, Mr. Seoh was associated
with the New York and London law offices of Lord, Day & Lord, Barrett Smith. Mr.
Seoh received his J.D. and A.B. from Harvard University.
 
     PETER D. SUZDAK, PH.D. joined the Company in March 1995 as Vice President,
Research. Prior thereto, Dr. Suzdak was Director of Neurobiology at Novo Nordisk
A/S and was responsible for all neurobiology research from 1993 to 1995, and
Department Head for Receptor Neurochemistry from 1988 to 1992 as well as a
member of the drug discovery management group from 1989 to 1995. Prior thereto,
Dr. Suzdak was a Pharmacology Research Associate in the Clinical Neuroscience
Branch of the National Institute of Mental Health in Bethesda, Maryland from
1985 to 1988. Dr. Suzdak received his Ph.D. in Neuroscience from the University
of Connecticut and a B.S. in Pharmacy from St. Johns University.
 
                                       42
<PAGE>   44
 
     GEORGE L. BUNTING, JR. has been a Director of the Company since May 1996.
Mr. Bunting is President and Chief Executive Officer of Bunting Management
Group, a position he has held since July 1991. He formerly served as Chairman of
the Board and Chief Executive Officer of the Noxell Corporation (a Procter &
Gamble Company as of November 1989). Mr. Bunting joined Noxell Corporation in
1966 as a Product Manager. In 1968, he was elected to the Board of Directors of
Noxell Corporation. In March 1970, he was elected to the position of Executive
Vice President and served as President and Chief Executive Officer from November
1973 until April 1986 when he became Chairman and Chief Executive Officer. Mr.
Bunting is a director of Crown Central Petroleum Corporation, Mercantile
Bankshares Corporation, PHH Corporation, and USF&G Corporation. He is currently
Chairman of Johns Hopkins Medicine, Health Systems, and Hospital, as well as a
Trustee of Johns Hopkins.
 
     RICHARD L. CASEY has been a Director of the Company since its inception in
July 1993 and served as its Chairman of the Board from inception through
December 1993. Mr. Casey is Chairman of the Board, President and Chief Executive
Officer of Scios. He joined Scios in December 1987 as President and Chief
Executive Officer and has served as a Director since that time. Mr. Casey was
elected Chairman of the Board of Scios in November 1992. Mr. Casey has over 20
years experience in the pharmaceutical industry and has served in various
positions with ALZA Corporation, Syntex Medical Diagnostics and Eli Lilly and
Company. Mr. Casey serves on the boards of directors of Karo Bio AB, a Swedish
biotechnology company affiliated with Scios, and VIVUS Inc., a medical devices
company located in Menlo Park, California.
 
     ELIZABETH M. GREETHAM has been a Director of the Company since November
1995. Since 1992, Ms. Greetham has been portfolio manager of WPG Life Sciences
Fund, L.P. and WPG Institutional Life Sciences Fund, L.P., and since 1990 she
has been involved in healthcare investments for institutional, growth and high
individual net worth accounts at Weiss, Peck & Greer, L.L.C. She is President of
Libracorn Financial Consultants and a member of the boards of directors of Medco
Research, Inc., Chemex Pharmaceuticals, Inc., Progenics Pharmaceuticals, Inc.,
Access Pharmaceuticals Inc., Pathogenesis Corp., Sangstat Medical Corp., Chirex
Inc. and Repligen Corporation.
 
     SOLOMON H. SNYDER, M.D. has been a Director of the Company and Chairman of
the Scientific Advisory Board since the Company's inception in July 1993. Dr.
Snyder received his M.D. in 1962 from Georgetown Medical School, trained as a
Research Associate with Julius Axelrod at the National Institute of Mental
Health and completed his Psychiatry Residency at Johns Hopkins Hospital. He is
presently Director of the Department of Neuroscience at Johns Hopkins Medical
School and Distinguished Service Professor of Neuroscience, Pharmacology and
Molecular Sciences, and Psychiatry. Dr. Snyder has received a number of awards
including the Albert Lasker Award in Basic Biomedical Research, the Wolf Prize
and the Bower Award. He is a member of the United States National Academy of
Sciences, the Institute of Medicine and the American Academy of Arts and
Sciences. Dr. Snyder is a director of Scios.
 
     W. LEIGH THOMPSON, M.D. PH.D. has been a Director of the Company since
April 1995. Dr. Thompson joined Eli Lilly and Company in 1982 and was appointed
Executive Vice President for Research in 1991 and Chief Scientific Officer in
1993. Dr. Thompson retired from Eli Lilly and Company in December 1994 and is
currently President and Chief Executive Officer of Profound Quality Resources,
Ltd., an independent consulting firm advising clients in the pharmaceutical
industry and is a director of Chrysalis International Corporation, Corvas
International, Inc., Ergo Science Corp., La Jolla Pharmaceutical Co.,
GeneMedicine, Inc., and Orphan Medical, Inc.
 
   
     The Board of Directors has a Compensation Committee and an Audit Committee.
The Compensation Committee of the Company's Board of Directors oversees the
compensation practices of the Company, including determining policies and
practices, changes in compensation and benefits for management, determination of
employee benefits and all other matters relating to employee compensation. The
Compensation Committee also administers the 1993 Employee Share Option and
Restricted Share Plan. The Audit Committee reviews the internal accounting
procedures of the Company, consults with the Company's independent accountants
and reviews the services provided by and fees charged by such accountants.
    
 
     All directors hold office until the annual meeting of stockholders and
until a successor is duly elected and qualified. Officers are elected to serve
until their successors are appointed or until their removal either by a
 
                                       43
<PAGE>   45
 
majority of the Board of Directors or the Chairman of the Board. The Company's
Amended and Restated By-laws, as amended, authorize the Board of Directors from
time to time to determine the number of its members. The Board currently has six
members, with no vacancies. Vacancies in unexpired terms and any additional
positions created by board action may be filled by the stockholders or by a
majority of the directors then in office, although fewer than a quorum, or by a
sole remaining director. Under an agreement with Abell, in the event of an
exchange of Abell's interest in Gell for 750,000 shares of Common Stock, so long
as the total number of shares of Common Stock owned by Abell exceeds 5% of the
outstanding Common Stock, the Company has agreed to nominate and recommend a
person designated by Abell as a candidate for election to the Company's Board of
Directors at the Company's next annual meeting of stockholders. By mutual
agreement prior to the Company's 1996 Annual Meeting of Stockholders, the
Company discharged its obligation to nominate such candidate designated by Abell
by nominating Mr. Bunting to the Board. On March 5, 1997, Abell exercised its
right to put its interest in Gell to Guilford for 750,000 shares of Common Stock
and, after the offering, will own 5.2% of the Common Stock.
 
                                       44
<PAGE>   46
 
                             PRINCIPAL STOCKHOLDERS
 
   
     The following table sets forth certain information regarding the principal
stockholders of Common Stock as of April 7, 1997, including each person known by
the Company to be the beneficial owner of more than five percent of the
outstanding Common Stock, the Company's Chief Executive Officer and the four
other most highly compensated executive officers of the Company for the fiscal
year ended December 31, 1996, each of the directors of the Company, certain
other holders and all officers and directors of the Company as a group.
    
 
   
<TABLE>
<CAPTION>
                                                                                 PERCENTAGE OF OWNERSHIP
               NAME AND ADDRESS                  SHARES BENEFICIALLY    -----------------------------------------
          OF PRINCIPAL STOCKHOLDERS                   OWNED (1)         BEFORE THE OFFERING    AFTER THE OFFERING
- ----------------------------------------------   -------------------    -------------------    ------------------
<S>                                              <C>                    <C>                    <C>
Scios.........................................        1,450,000                 9.8%                   8.0%
     2450 Bayshore Parkway
     Mountain View, CA 94043
The Abell Foundation, Inc. ...................          937,500                 6.3%                   5.2%
     111 South Calvert Street
     Baltimore, MD 21202
FMR Corp. ....................................          738,250(2)              5.0%                   4.1%
     82 Devonshire Street
     Boston, Massachusetts 02109
Arnold H. Snider
     Deerfield Capital, L.P. .................          703,575(3)              4.8%                   3.9%
     Deerfield Management Company.............           46,425(3)              0.3%                   0.3%
     450 Lexington Avenue, Suite 1930
     New York, NY 10017
T. Rowe Price Associates, Inc. ...............          813,450(4)              5.5%                   4.5%
     100 East Pratt Street
     Baltimore, Maryland 21202
Rhone-Poulenc Rorer Pharmaceuticals, Inc. ....          281,531                 1.9%                   1.6%
     500 Arcola Road
     Collegeville, Pennsylvania 19426
Craig R. Smith, M.D. .........................          460,897(5)              3.1%                   2.5%
Andrew R. Jordan..............................          187,259(6)              1.3%                   1.0%
John P. Brennan...............................          120,234(7)               *                      *
Nicholas Landekic.............................           33,603(8)               *                      *
Earl W. Henry.................................           45,170(9)               *                      *
Solomon H. Snyder, M.D. ......................          605,217(10)             4.1%                   3.3%
Richard L. Casey..............................        1,519,900(11)            10.2%                   8.4%
     c/o Scios
     2450 Bayshore Parkway
     Mountain View, CA 94043
George L. Bunting, Jr. .......................           15,000(12)              *                      *
Elizabeth M. Greetham.........................          225,950(13)             1.5%                   1.3%
W. Leigh Thompson, M.D., Ph.D. ...............           33,750(14)              *                      *
 
All directors and officers as a group (14
  persons)....................................        3,382,628                22.3%                  18.4%
</TABLE>
    
 
- ---------------
   * Less than one percent.
 
   
 (1) Beneficial ownership is determined in accordance with the rules of the
     Commission and generally includes voting or investment power with respect
     to securities. Shares of the Company's Common Stock subject to options or
     warrants currently exercisable within 60 days of April 7, 1997 are deemed
     outstanding for purposes of computing the percentage ownership of the
     person holding such option or warrant but are not deemed outstanding for
     purposes of computing the percentage ownership of any other person. Except
     where indicated otherwise, and subject to community property laws where
    
 
                                       45
<PAGE>   47
 
     applicable, the persons named in the table above have sole voting and
     investment power with respect to all shares of the Company's Common Stock
     shown as beneficially owned by them.
 
 (2) Based on a Schedule 13G filed by this holder on February 14, 1997, which
     disclosed that various persons have the right to receive or the power to
     direct the receipt of dividends from, or the proceeds from the sale of, the
     Company's Common Stock.
 
 (3) Based on a Schedule 13D dated July 16, 1996, Mr. Snider has reported
     beneficial ownership of 750,000 shares of Common Stock, 703,575 of which
     are held by Deerfield Capital, L.P. ("DCLP"), and 46,425 of which are held
     by Deerfield Management Company ("DMC"). According to the Schedule 13D, Mr.
     Snider is the President, Director and sole shareholder of Snider Capital
     Corp., which is the general partner of DCLP, and the President, Director
     and sole shareholder of Snider Management Corporation, which is the general
     partner of DMC.
 
 (4) Based on a Schedule 13G filed on February 14, 1997, disclosing that these
     securities are owned by various individual and institutional investors
     including the T. Rowe Price New Horizons Fund, Inc. (which owns 700,500
     shares of Common Stock representing 5.0% of the shares outstanding as of
     February 14, 1997), for which T. Rowe Price Associates, Inc. ("Price
     Associates") serves as investment advisor with the power to direct
     investments and/or sole power to vote securities. For purposes of the
     reporting requirements of the Exchange Act, Price Associates is deemed to
     be a beneficial owner of such securities, however, Price Associates
     expressly disclaims that it is in fact, the beneficial owner of such
     securities.
 
   
 (5) Includes options to acquire 40,034 shares of Common Stock exercisable
     within 60 days of April 7, 1997, and 1,578 shares of Common Stock and
     options to acquire 3,583 shares of Common Stock exercisable within 60 days
     of April 7, 1997 held by Dr. Smith's spouse, an employee of the Company.
     Dr. Smith disclaims beneficial ownership of the securities held by his
     spouse.
    
 
   
 (6) Includes 150 shares owned by a child sharing Mr. Jordan's household, of
     which Mr. Jordan disclaims beneficial ownership, and options to acquire
     35,095 shares of Common Stock exercisable within 60 days of April 7, 1997.
     Does not include 750 shares owned by another child of Mr. Jordan who does
     not share Mr. Jordan's household, as to which shares Mr. Jordan disclaims
     beneficial ownership.
    
 
   
 (7) Includes options to acquire 39,783 shares of Common Stock exercisable
     within 60 days of April 7, 1997.
    
 
   
 (8) Includes options to acquire 24,688 shares of Common Stock exercisable
     within 60 days of April 7, 1997.
    
 
   
 (9) Includes options to acquire 3,750 shares of Common Stock exercisable within
     60 days of April 7, 1997, and 9,375 shares of Common Stock and options to
     acquire 719 shares of Common Stock exercisable within 60 days of April 7,
     1997 held by Dr. Henry's wife, an employee of the Company. Dr. Henry
     disclaims beneficial ownership of the securities held by his spouse.
    
 
   
(10) Includes options to acquire 30,000 shares of Common Stock exercisable
     within 60 days of April 7, 1997. Does not include 1,450,000 shares owned by
     Scios. Dr. Snyder is a member of the Board of Directors of Scios and may be
     deemed to have shared voting and investment power over these shares. Dr.
     Snyder disclaims beneficial ownership of the shares owned by Scios.
    
 
   
(11) Mr. Casey is an executive officer and Chairman of the Board of Directors of
     Scios. He may be deemed to have voting and investment power over the shares
     held by Scios. Mr. Casey disclaims beneficial ownership of these shares.
     Mr. Casey has direct ownership over an additional 9,900 shares and options
     to acquire 60,000 shares exercisable within 60 days of April 7, 1997.
    
 
   
(12) Includes options to acquire 15,000 shares of Common Stock exercisable
     within 60 days of April 7, 1997.
    
 
   
(13) Represents shares held by WPG-Life Sciences Fund, L.P. (the "Fund") and
     WPG-Institutional Life Sciences Fund, L.P. (the "Institutional Fund"). Ms.
     Greetham serves as Portfolio Manager of both the Fund and the Institutional
     Fund. Ms. Greetham is a controlling person of Libracorn Financial
     Consultants ("Libracorn"), a limited partner of the Fund which, through its
     interest in the Fund, has a 1.55% interest in the shares held by the Fund.
     Ms. Greetham disclaims beneficial ownership of the shares held by the Fund
     and the Institutional Fund except to the extent of her beneficial interest
     through Libracorn. Includes options to acquire 15,000 shares of Common
     Stock exercisable within 60 days of April 7, 1997.
    
 
   
(14) Includes options to acquire 33,750 shares of Common Stock exercisable
     within 60 days of April 7, 1997.
    
 
                                       46
<PAGE>   48
 
                          DESCRIPTION OF CAPITAL STOCK
 
   
     The Company's authorized capital stock consists of 40,000,000 shares of the
Common Stock, par value $0.01 per share, and 4,700,000 shares of undesignated
preferred stock, par value $0.01 per share and 300,000 shares of Series A Junior
Participating Preferred Stock, par value $0.01 per share. As of December 31,
1996, there were 13,979,490 shares of Common Stock (reflecting the 3-for-2 stock
split effective as of November 12, 1996) and no shares of preferred stock
outstanding. As of December 31, 1996, there were outstanding options to purchase
approximately an additional 2,494,756 shares of the Company's Common Stock and
warrants to purchase 312,934 additional shares of Common Stock.
    
 
COMMON STOCK
 
   
     Holders of shares of Common Stock are entitled to one vote for each share
held of record on matters to be voted on by the stockholders of the Company.
Stockholders do not have cumulative voting rights in the election of directors.
Holders of shares of Common Stock will be entitled to receive dividends, subject
to the superior rights of preferred stockholders, if any, when, as and if
declared by the Board of Directors. The Company currently intends to retain all
future earnings for use in the operation of its business and, therefore, does
not anticipate paying any case dividends on its Common Stock in the foreseeable
future. Upon the dissolution, liquidation or sale of substantially all of the
assets of the Company, after payment in full of all amounts required to be paid
to creditors and subject to the rights, if any, of the holders of any preferred
stock, the holders of the Common Stock are entitled to share ratably in the
assets of the Company legally available for distribution to its stockholders.
Holders of Common Stock have no preemptive, subscription, redemption or
conversion rights. The Company has the right to repurchase certain shares of
Common Stock issued to certain officers and other employees of the Company in
the event of termination of employment. All of the issued and outstanding shares
of Common Stock are, and all shares of Common Stock to be sold in this offering
will be, duly authorized, validly issued, fully paid and non-assessable.
    
 
PREFERRED STOCK
 
     The Company's Board of Directors may without further action by the
Company's stockholders, from time to time, direct the issuance of shares of
preferred stock in series and may, at the time of issuance, determine the
rights, preferences and limitation of each series. The holders of preferred
stock would normally be entitled to receive a preference payment in the event of
any liquidation, dissolution or winding-up of the Company before any payment is
made to the holders of Common Stock.
 
     The ability of the Company's Board of Directors to issue preferred stock
may delay or prevent a takeover or change in control of the Company. To the
extent that this ability has this effect, removal of the Company's incumbent
Board of Directors and management may be rendered more difficult. Further, this
may have an adverse impact on the ability of stockholders of the Company to
participate in a tender or exchange offer for the Common Stock and in so doing
diminish the market value of the Common Stock.
 
RIGHTS PLAN
 
     On September 26, 1995, the Board of Directors of the Company approved a
stockholder rights plan (the "Rights Plan") designed to protect stockholders in
the event of an unsolicited attempt to acquire the Company, including a gradual
accumulation of shares in the open market, a partial or two-tier tender offer
that does not treat all stockholders equally, and other takeover tactics which
the Board of Directors believes may be abusive and not in the best interests of
stockholders. The implementation of the Rights Plan increases the Board of
Director's power in the event of an unsolicited proposal by giving the Board of
Directors more time and the opportunity to evaluate an offer and exercise its
good faith business judgment to take appropriate steps to protect and advance
stockholders' interests by negotiating with the bidder, auctioning the Company,
implementing a recapitalization or restructuring designed as an alternative to
the offer, or taking other action.
 
                                       47
<PAGE>   49
 
In connection with the Rights Plan, the Company designated 300,000 shares of
Series A Junior Participating Preferred Stock, par value $0.01 per share.
 
     Under the Rights Plan, each holder of the Company's Common Stock is
entitled to purchase 1/1,000th of a share of Series A Junior Participating
Preferred Stock. Currently, the Rights are neither exercisable nor traded
separately from the Common Stock. The Rights will be exercisable only if a
person or group in the future becomes the beneficial owner of 20% or more of the
Common Stock or announces a tender or exchange offer which would result in its
ownership of 20% or more of the Common Stock. Ten days after a public
announcement that a person has become the beneficial owner of 20% or more of the
Common Stock, each holder of a Right, other than the acquiring person, would be
entitled to purchase one share of Common Stock of the Company for each Right at
one-half of the then-current price. If the Company is acquired in a merger, or
50% or more of the Company's assets are sold in one or more related
transactions, each Right would entitle the holder thereof to purchase common
stock of the acquiring company at half of the then-current market price of such
common stock. At any time after a person or group of persons becomes the
beneficial owner of 20% or more of the Common Stock, the Board of Directors may
exchange one share of Common Stock for each Right, other than Rights held by the
acquiring person.
 
     The Board of Directors generally may redeem the Rights at any time until
ten days following the public announcement that person or group of persons has
acquired beneficial ownership of 20% or more of the outstanding Common Stock.
The redemption price is $0.01 per Right.
 
LIMITATION OF LIABILITY AND INDEMNIFICATION OF DIRECTORS AND OFFICERS
 
   
     The Company's Amended and Restated Certificate of Incorporation, as amended
(the "Certificate"), provides that a director shall not be personally liable to
the Company or its stockholders for monetary damages for breach of fiduciary
duty as a director, except: (i) for any breach of the director's duty of loyalty
to the Company or its stockholders; (ii) for acts or omissions not in good faith
or which involve intentional misconduct or knowing violations of law; (iii) for
liability under Section 174 of the Delaware General Corporation Law (relating to
certain unlawful dividends, stock repurchases or stock redemptions); or (iv) for
any transaction from which the director derived an improper personal benefit.
    
 
     The Company's Certificate also provides that directors and officers are to
be indemnified to the fullest extent permitted under Delaware law. The Company
has entered into indemnification agreements with each of its current directors
and officers and will enter into such agreements with future directors and
officers, which agreements provide for indemnification of, and advancement of
expenses to such persons to the greatest extent permitted by Delaware law,
including by reason of action or inaction occurring in the past and
circumstances in which indemnification and the advancement of expenses are
discretionary under Delaware law. The Company believes that the limitation of
liability provision in its Certificate, its Amended and Restated By-laws and the
indemnification agreements will facilitate the Company's ability to continue to
attract and retain qualified individuals to serve as directors of the Company.
 
     The Certificate authorizes the Company to purchase and maintain insurance
for the purposes of indemnification. The Company maintains a standard form of
directors' and officers' liability insurance policy, which provides coverage to
the Company's officers and directors for certain liabilities. At present, there
is no pending litigation or proceeding involving any director, officer, employee
or agent for which indemnification will be required or permitted under the
Certificate, Amended and Restated By-laws or indemnification agreements. The
Company is not aware of any threatened litigation or proceeding which may result
in a claim for such indemnification.
 
SECTION 203 OF THE DELAWARE CORPORATION LAW
 
     The Company is subject to the provisions of Section 203 of the Delaware
General Corporation Law ("Section 203"). Under Section 203, certain "business
combinations" between a Delaware corporation whose stock generally is publicly
traded or held of record by more than 2,000 stockholders and an "interested
stockholder" are prohibited for a three-year period following the date that such
stockholder became an interested stockholder, unless: (i) the corporation has
elected in its original certificate of incorporation not to
 
                                       48
<PAGE>   50
 
be governed by Section 203 (the Company did not make such an election); (ii) the
business combination was approved by the Board of Directors of the corporation
before the other party to the business combination became an interested
stockholder; (iii) upon consummation of the transaction that made it an
interested stockholder, the interested stockholder owned at least 85% of the
voting stock of the corporation outstanding at the commencement of the
transaction (excluding voting stock owned by directors who are also officers or
held in employee benefit plans in which the employees do not have a confidential
right to tender or vote stock held by the plan); or (iv) the business
combination was approved by the Board of Directors of the corporation and
ratified by two-thirds of the voting stock which the interested stockholder did
not own. The three-year prohibition also does not apply to certain business
combinations proposed by an interested stockholder following the announcement or
notification of certain extraordinary transactions involving the corporation and
a person who had not been an interested stockholder during the previous three
years or who became an interested stockholder with the approval of the majority
of the corporation's directors. The term "business combination" is defined
generally to include mergers or consolidations between a Delaware corporation
and an "interested stockholder," transactions with an "interested stockholder"
involving the assets or stock of the corporation or its majority-owned
subsidiaries and transactions which increase an interested stockholder's
percentage ownership of stock. The term "interested stockholder" is defined
generally as a stockholder who, together with affiliates and associates, owns
(or, within three years prior, did own) 15% or more of a Delaware corporation's
voting stock. Section 203 could prohibit or delay a merger, takeover or other
change in control of the Company and therefore could discourage attempts to
acquire the Company.
 
STOCKHOLDER MEETINGS AND OTHER PROVISIONS
 
     Under the Amended and Restated By-laws, special meetings of the
stockholders of the Company may be called only by a majority of the members of
the Board of Directors, the Chairman or holders of 30% of the voting stock of
the Company. Stockholders are required to comply with certain advance notice
provisions with respect to any nominations of candidates for election to the
Company's Board of Directors or other proposals submitted for stockholder vote.
The Company's Certificate provides that the authorized number of directors may
be changed only by resolution of the Board of Directors. These provisions may
have the effect of deterring hostile takeovers or delaying changes in control or
management of the Company.
 
TRANSFER AGENT AND REGISTRAR
 
     The Transfer Agent and Registrar for the Common Stock is American Stock
Transfer & Trust Company.
 
                                       49
<PAGE>   51
 
                                  UNDERWRITING
 
     Subject to the terms and conditions of the Underwriting Agreement, the
Company has agreed to sell to each of the Underwriters named below, and each of
the Underwriters, for whom Oppenheimer & Co., Inc., Alex. Brown & Sons
Incorporated and Hambrecht & Quist LLC are acting as Representatives, has
severally agreed to purchase from the Company, the respective number of shares
of Common Stock set forth opposite the name of each Underwriter below.
 
<TABLE>
<CAPTION>
                                    NAME                                    NUMBER OF SHARES
    ---------------------------------------------------------------------   ----------------
    <S>                                                                     <C>
    Oppenheimer & Co., Inc. .............................................
    Alex. Brown & Sons Incorporated......................................
    Hambrecht & Quist LLC................................................
 
                                                                            -------------
         Total...........................................................       3,250,000
                                                                            =============
</TABLE>
 
     The Underwriters propose to offer the shares of Common Stock directly to
the public initially at the public offering price set forth on the cover page of
this Prospectus and in part to certain securities dealers at such price less a
concession of $     per share. The Underwriters may allow, and such dealers may
reallow, a concession not in excess of $     per share to certain other brokers
and dealers. After the shares of Common Stock are released for sale to the
public, the offering price and other selling terms may from time to time be
varied by the Representatives. The Underwriters are obligated to take and pay
for all of the shares of Common Stock offered hereby (other than those covered
by the over-allotment option described below) if any are taken.
 
     The Company has granted to the Underwriters an option, exercisable for up
to 30 days after the date of this Prospectus, to purchase up to an aggregate of
487,500 additional shares of Common Stock to cover over-allotments, if any. If
the Underwriters exercise such option, the Underwriters have severally agreed,
subject to certain conditions, to purchase approximately the same percentage
thereof that the number of shares to be purchased by each of them bears to the
3,250,000 shares of Common Stock offered hereby. The Underwriters may exercise
such option only to cover over-allotments made in connection with the sale of
the shares of Common Stock offered hereby. The Representatives have advised the
Company that the Underwriters do not intend to confirm sales in excess of 5% of
the shares offered hereby to any account over which they exercise discretionary
authority.
 
     The Company has agreed to indemnify the Representatives of the Underwriters
and the several Underwriters against certain liabilities, including, without
limitation, liabilities under the Securities Act of 1993, as amended (the
"Securities Act").
 
     In connection with this offering, the Underwriters and other selling group
members and their respective affiliates may engage in transactions that
stabilize, maintain or otherwise affect the market price of the Common Stock.
Such transactions may include stabilization transactions effected in accordance
with Rule 103 of Regulation M, pursuant to which such persons may bid for or
purchase Common Stock for the purpose of stabilizing its market price. The
Underwriters also may create a short position for the account of the
Underwriters by selling more Common Stock in connection with the offering than
they are committed to purchase from the Company, and in such case may purchase
Common Stock in the open market following completion of the offering to cover
all or a portion of such short position. The Underwriters may also cover all or
a portion of such short position, up to 487,500 shares of common stock, by
exercising the Underwriters' over-allotment option referred to above. In
addition, Oppenheimer & Co., Inc., on behalf of the Underwriters, may impose
"penalty bids" under contractual arrangements with the Underwriters whereby it
may reclaim
 
                                       50
<PAGE>   52
 
from an Underwriter (or dealer participating in the offering) for the account of
the other Underwriters, the selling concession with respect to Common Stock that
is distributed in the offering but subsequently purchased for the account of the
Underwriters in the open market. Any of the transactions described in this
paragraph may result in the maintenance of the price of the Common Stock at a
level above that which might otherwise prevail in the open market. None of the
transactions described in this paragraph is required, and, if they are
undertaken, they may be discontinued at any time.
 
     The Company's officers and directors and certain stockholders who own an
aggregate of approximately 4,993,031 shares of Common Stock and shares issuable
upon the exercise of outstanding options have agreed that they will not directly
or indirectly, sell, offer, contract to sell, make a short sale, pledge or
otherwise dispose of any shares of Common Stock (or any securities convertible
into or exchangeable or exercisable for any other rights to purchase or acquire
Common Stock other than shares of Common Stock issuable upon exercise of
outstanding options) owned by them, for a period of 90 days after the date of
this Prospectus, without the prior written consent of Oppenheimer & Co., Inc.,
subject to certain limited exceptions. The Company has also agreed not to issue,
sell or register with the Commission for its own account or otherwise dispose
of, directly or indirectly, any equity securities of the Company (or any
securities convertible into or exercisable or exchangeable for equity securities
of the Company) for a period of 90 days after the date of this Prospectus,
without the prior written consent of Oppenheimer & Co., Inc., subject to certain
limited exceptions. Oppenheimer & Co., Inc. may in its sole discretion and at
any time without notice, release all or any portion of the securities subject to
lock-up agreements.
 
                                 LEGAL MATTERS
 
     Certain legal matters with respect to the shares of Common Stock offered
hereby will be passed upon for the Company by Hogan & Hartson L.L.P., Baltimore,
Maryland. Certain legal matters will be passed upon for the Underwriters by
Cooley Godward LLP, San Francisco, California.
 
                                    EXPERTS
 
     The consolidated financial statements of Guilford Pharmaceuticals Inc. and
subsidiaries as of December 31, 1995 and December 31, 1996, and for each of the
years in the three year period ended December 31, 1996 have been included herein
and in the Registration Statement on Form S-3 (together with all amendments and
Exhibits thereto, the "Registration Statement") in reliance upon the report of
KPMG Peat Marwick LLP, independent certified public accountants, appearing
elsewhere herein, and upon the authority of said firm as experts in accounting
and auditing.
 
     The information relating to the patents and proprietary rights of the
Company has been reviewed by Nath & Associates, attorneys at law, Washington,
D.C. Such information is included in reliance upon information provided by Nath
& Associates upon the authority of such firm as an expert in patents and
proprietary information.
 
                             AVAILABLE INFORMATION
 
     The Company is subject to the informational requirements of the Exchange
Act, and in accordance therewith files reports, proxy statements and other
information with the Commission. Such reports, proxy statements and other
information can be inspected and copied at the public reference facilities
maintained by the Commission at Room 1024, Judiciary Plaza, 450 Fifth Street,
N.W., Washington, D.C. 20549, and at the Commission's Regional Offices in New
York (Seven World Trade Center, Suite 1300, New York, New York 10048) and
Chicago (Suite 1400, Northwestern Atrium Center, 500 West Madison Street,
Chicago, Illinois 60661). Copies of such material can also be obtained at
prescribed rates from the Public Reference Section of the Commission at Room
1024, Judiciary Plaza, 450 Fifth Street, N.W., Washington, D.C. 20549. The
Commission also maintains a World Wide Web site that contains reports, proxy
statements and other information regarding registrants, including the Company,
that file such information electronically with the Commission. The address of
the Commission's Web site is http:www.sec.gov.
 
                                       51
<PAGE>   53
 
     The Company has filed with the Commission the Registration Statement under
the Securities Act with respect to the Common Stock offered hereby. This
Prospectus does not contain all the information set forth in the Registration
Statement, certain parts of which are omitted in accordance with the rules and
regulations of the Commission. For further information, reference is made to the
Registration Statement, copies of which may be obtained upon payment of a fee
prescribed by the Commission, or may be examined free of charge, at the Public
Reference Section of the Commission.
 
                                       52
<PAGE>   54
 
   
                         GUILFORD PHARMACEUTICALS INC.
    
 
                   INDEX TO CONSOLIDATED FINANCIAL STATEMENTS
 
<TABLE>
<CAPTION>
                                                                                         PAGE
                                                                                         ----
<S>                                                                                      <C>
Independent Auditors' Report..........................................................   F-2
Consolidated Balance Sheets...........................................................   F-3
Consolidated Statements of Operations.................................................   F-4
Consolidated Statements of Stockholders' Equity.......................................   F-5
Consolidated Statements of Cash Flows.................................................   F-6
Notes to Consolidated Financial Statements............................................   F-7
</TABLE>
 
                                       F-1
<PAGE>   55
 
                          INDEPENDENT AUDITORS' REPORT
 
The Board of Directors and Stockholders of
Guilford Pharmaceuticals Inc.:
 
     We have audited the accompanying consolidated balance sheets of Guilford
Pharmaceuticals Inc. and subsidiaries as of December 31, 1995 and 1996, and the
related consolidated statements of operations, stockholders' equity and cash
flows for each of the years in the three-year period ended December 31, 1996.
These consolidated financial statements are the responsibility of the Company's
management. Our responsibility is to express an opinion on these consolidated
financial statements based on our audits.
 
     We conducted our audits in accordance with generally accepted auditing
standards. Those standards require that we plan and perform the audit to obtain
reasonable assurance about whether the financial statements are free of material
misstatement. An audit includes examining, on a test basis, evidence supporting
the amounts and disclosures in the financial statements. An audit also includes
assessing the accounting principles used and significant estimates made by
management, as well as evaluating the overall financial statement presentation.
We believe that our audits provide a reasonable basis for our opinion.
 
     In our opinion, the consolidated financial statements referred to above
present fairly, in all material respects, the financial position of Guilford
Pharmaceuticals Inc. and subsidiaries as of December 31, 1995 and 1996, and the
results of their operations and their cash flows for each of the years in the
three-year period ended December 31, 1996, in conformity with generally accepted
accounting principles.
 
                                                KPMG Peat Marwick LLP
 
Baltimore, Maryland
February 28, 1997
 
                                       F-2
<PAGE>   56
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
                          CONSOLIDATED BALANCE SHEETS
                       (IN THOUSANDS, EXCEPT SHARE DATA)
                                     ASSETS
 
<TABLE>
<CAPTION>
                                                                             DECEMBER 31,
                                                                        ----------------------
                                                                          1995          1996
                                                                        --------      --------
<S>                                                                     <C>           <C>
Current assets:
  Cash and cash equivalents..........................................   $  4,260      $ 16,560
  Short-term investments.............................................     11,552        20,097
  Short-term investments -- restricted...............................        250         1,608
  Collaborative research receivable..................................        556           376
  Inventory..........................................................         --         1,533
  Other current assets...............................................        291           435
                                                                        ---------     ---------
          Total current assets.......................................     16,909        40,609
Investments..........................................................         --        30,653
Investments -- restricted............................................      3,392         8,521
Property and equipment, net..........................................      5,456        13,455
Other assets.........................................................        291           421
                                                                        ---------     ---------
          Total assets...............................................   $ 26,048      $ 93,659
                                                                        =========     =========
 
LIABILITIES AND STOCKHOLDERS' EQUITY
Current liabilities:
  Accounts payable...................................................   $  1,640      $  2,038
  Bond payable -- current portion....................................        293           941
  Term loan payable -- current portion...............................         --           540
  Accrued expenses and other current liabilities.....................      1,646         3,358
                                                                        ---------     ---------
          Total current liabilities..................................      3,579         6,877
Long-term liabilities:
  Bond payable, less current portion.................................      4,696         6,588
  Term loan payable, less current portion............................         --         4,317
                                                                        ---------     ---------
          Total liabilities..........................................      8,275        17,782
Stockholders' equity:
  Preferred stock, par value $.01 per share. Authorized 4,700,000
     shares, none issued.............................................         --            --
  Series A junior participating preferred stock, par value $.01 per
     share. Authorized 300,000 shares, none issued...................         --            --
  Common stock, par value $.01 per share. Authorized 20,000,000
     shares; 10,189,598 (6,793,065 pre-split) and 13,979,490 issued
     and outstanding at December 31, 1995 and 1996, respectively.....         68           140
  Additional paid-in capital.........................................     38,121        90,880
  Notes receivable on common stock...................................       (139)         (129)
  Accumulated deficit................................................    (19,947)      (14,874)
  Unrealized gain on available-for-sale securities...................         --            62
  Deferred compensation..............................................       (330)         (202)
                                                                        ---------     ---------
          Total stockholders' equity.................................     17,773        75,877
                                                                        ---------     ---------
          Total liabilities and stockholders' equity.................   $ 26,048      $ 93,659
                                                                        =========     =========
</TABLE>
 
          See accompanying notes to consolidated financial statements.
 
                                       F-3
<PAGE>   57
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
                     CONSOLIDATED STATEMENTS OF OPERATIONS
                     (IN THOUSANDS, EXCEPT PER SHARE DATA)
 
<TABLE>
<CAPTION>
                                                                   YEAR ENDED DECEMBER 31,
                                                           ---------------------------------------
                                                              1994          1995          1996
                                                           ----------    ----------    -----------
<S>                                                        <C>           <C>           <C>
Revenues:
  Contract and license revenue..........................   $       --    $      556    $    27,600
  Revenues under collaborative agreements...............           --            30            420
                                                           ----------    ----------    ----------- 
          Total revenues................................           --           586         28,020 
Operating expenses:                                                                                
  Research and development..............................        2,869         9,155         17,850 
  Research and development -- Gell Pharmaceuticals                                                 
     Inc................................................           --           533            911 
  General and administrative............................        2,369         4,367          6,736 
  Compensation expense -- warrants......................          991            --             -- 
                                                           ----------    ----------    ----------- 
          Total operating expenses......................        6,229        14,055         25,497 
                                                           ----------    ----------    ----------- 
Income (loss) from operations...........................       (6,229)      (13,469)         2,523 
Other income (expense):                                                                            
  Interest income.......................................          336           823          3,070 
  Other income..........................................           --           199              8
  Interest expense......................................           (4)         (190)          (528)
                                                           ----------    ----------    -----------
          Net income (loss).............................   $   (5,897)   $  (12,637)   $     5,073
                                                           ==========    ==========    ===========
Primary earnings (loss) per common share:...............   $    (1.36)   $    (1.70)   $      0.35
                                                           ==========    ==========    ===========
 
Weighted average common and common equivalent shares
  outstanding -- primary................................        4,332         7,436         14,634
 
Fully diluted earnings (loss) per common share:.........   $    (1.36)   $    (1.70)   $      0.34
                                                           ==========    ==========    ===========
Weighted average common and common equivalent shares
  outstanding -- fully diluted..........................        4,332         7,436         15,140
</TABLE>
 
          See accompanying notes to consolidated financial statements.
 
                                       F-4
<PAGE>   58
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
                CONSOLIDATED STATEMENTS OF STOCKHOLDERS' EQUITY
                  YEARS ENDED DECEMBER 31, 1994, 1995 AND 1996
                       (IN THOUSANDS, EXCEPT SHARE DATA)
<TABLE>
<CAPTION>
                                         PREFERRED STOCK       COMMON STOCK                   NOTES                   UNREALIZED
                                       -------------------  ------------------  ADDITIONAL  RECEIVABLE                  GAIN ON
                                         NUMBER               NUMBER             PAID-IN    ON COMMON  ACCUMULATED   AVAILABLE FOR
                                       OF SHARES   AMOUNT   OF SHARES   AMOUNT   CAPITAL      STOCK      DEFICIT    SALE SECURITIES
                                       ----------  -------  ----------  ------  ----------  ---------  -----------  ---------------
<S>                                    <C>         <C>      <C>         <C>     <C>         <C>        <C>          <C>
Balance, December 31, 1993............  2,423,333   $  24      582,608   $  6    $  4,378     $(108)    $  (1,413)       $  --
Issuance of common stock in initial
  public offering at $8.00* per share,
  net of offering costs...............                       1,875,000     19      12,848
Issuance of warrants..................                                                 10
Issuance of common stock..............                          39,129      1          89       (90)
Issuance of Series A Convertible
  Preferred Stock.....................     50,000       1                             249
Compensation related to issuance of
  common stock and grant of common
  stock options.......................                                                273
Amortization of deferred
  compensation........................
Conversion of Series A Preferred
  Stock............................... (2,473,333)    (25)   1,075,361     10          15
Exercise of warrants..................                          85,217      1         195
Reduction in notes receivable on
  common stock........................                                                           49
Compensation expense -- warrants......                                                991                  
Net loss for the year.................                                                                     (5,897)
                                       ------------  -----   ----------- -----   --------     ------    ---------        ----- 
Balance, December 31, 1994............     --       $  --    3,657,315   $ 37    $ 19,048     $(149)    $  (7,310)       $  --
Issuance of common stock in secondary
  public offering at $6.50* per share,
  net of offering costs...............                       3,000,000     30      17,901
Other issuances of common stock.......                          63,286      1         280
Exercise of warrants by Scios Nova....                          72,464                166
Equity proceeds from Gell
  Pharmaceuticals relating to the put
  option..............................                                                726
Amortization of deferred
  compensation........................
Reduction in notes receivable on
  common stock........................                                                           10
Net loss for the year.................                                                                    (12,637)
                                       ------------  -----   ----------- -----   --------     ------    ---------        ----- 
Balance, December 31, 1995............     --        $ --    6,793,065   $ 68    $ 38,121     $(139)    $ (19,947)       $  --
Issuance of common stock in secondary
  public offering at $20.00* per
  share, net of offering costs........                       2,300,000     23      42,880
Other issuances of common stock.......                         226,595      2       7,679
Three-for-two stock split.............                       4,659,830     47         (47)
Equity proceeds from Gell
  Pharmaceuticals relating to the put
  option..............................                                              1,076
Amortization of stock option
  compensation........................                                              1,171
Amortization of deferred
  compensation........................
Reduction in notes receivable on
  common stock........................                                                           10
Unrealized gain on available for sale
  securities..........................                                                                                      62
Net income for the year...............                                                                      5,073
                                       ------------  -----   ----------- -----   --------     ------    ---------        ----- 
Balance, December 31, 1996............     --        $ --   13,979,490   $140    $ 90,880     $(129)    $ (14,874)       $  62
                                       ============  =====  =========== =====    ========     ======    =========        =====
 
<CAPTION>
 
                                                          TOTAL
                                          DEFERRED    STOCKHOLDERS'
                                        COMPENSATION     EQUITY
                                        ------------  -------------
<S>                                    <C>            <C>
Balance, December 31, 1993............     $   --       $   2,887
Issuance of common stock in initial
  public offering at $8.00* per share,
  net of offering costs...............                     12,867
Issuance of warrants..................                         10
Issuance of common stock..............                         --
Issuance of Series A Convertible
  Preferred Stock.....................                        250
Compensation related to issuance of
  common stock and grant of common
  stock options.......................       (273)             --
Amortization of deferred
  compensation........................         68              68
Conversion of Series A Preferred
  Stock...............................                         --
Exercise of warrants..................                        196
Reduction in notes receivable on
  common stock........................                         49
Compensation expense -- warrants......                        991
Net loss for the year.................                     (5,897)
                                           ------        --------
Balance, December 31, 1994............     $ (205)      $  11,421
Issuance of common stock in secondary
  public offering at $6.50* per share,
  net of offering costs...............                     17,931
Other issuances of common stock.......       (237)             44
Exercise of warrants by Scios Nova....                        166
Equity proceeds from Gell
  Pharmaceuticals relating to the put
  option..............................                        726
Amortization of deferred
  compensation........................        112             112
Reduction in notes receivable on
  common stock........................                         10
Net loss for the year.................                    (12,637)
                                           ------        --------
Balance, December 31, 1995............     $ (330)      $  17,773
Issuance of common stock in secondary
  public offering at $20.00* per
  share, net of offering costs........                     42,903
Other issuances of common stock.......                      7,681
Three-for-two stock split.............                         --
Equity proceeds from Gell
  Pharmaceuticals relating to the put
  option..............................                      1,076
Amortization of stock option
  compensation........................                      1,171
Amortization of deferred
  compensation........................        128             128
Reduction in notes receivable on
  common stock........................                         10
Unrealized gain on available for sale
  securities..........................                         62
Net income for the year...............                      5,073
                                           ------        --------
Balance, December 31, 1996............     $ (202)      $  75,877
                                           ======        ========
</TABLE>
 
- ---------------
 
* Per share prices are pre-stock split
 
          See accompanying notes to consolidated financial statements.
 
                                       F-5
<PAGE>   59
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
                     CONSOLIDATED STATEMENTS OF CASH FLOWS
                                 (IN THOUSANDS)
 
<TABLE>
<CAPTION>
                                                                     YEAR ENDED DECEMBER 31,
                                                                 --------------------------------
                                                                   1994        1995        1996
                                                                 --------    --------    --------
<S>                                                              <C>         <C>         <C>
Cash Flows From Operating Activities:
  Net income (loss)...........................................   $ (5,897)   $(12,637)   $  5,073
  Adjustments to reconcile net income (loss) to net cash
     provided by (used in) operating activities:
     Depreciation and amortization............................         44         567       1,102
     Noncash compensation expense.............................      1,059         122       1,309
     Provision for loss related to advance to underwriter.....        175          --          --
  Changes in assets and liabilities:
     Collaborative research receivable........................         --        (556)        180
     Inventory................................................         --          --      (1,533)
     Other current assets.....................................       (288)       (177)       (144)
     Other assets.............................................       (120)          4        (130)
     Accounts payable.........................................        964         428         398
     Accrued expenses and other liabilities...................        375       1,177       1,712
                                                                 ---------   ---------   ---------
  Net cash provided by (used in) operating activities.........     (3,688)    (11,072)      7,967
                                                                 ---------   ---------   ---------
Cash Flows From Investing Activities:
  Investment in purchases of property and equipment...........     (2,343)     (3,706)     (9,101)
  Maturities of held-to-maturity investments..................         --      40,071      48,368
  Purchases of held-to-maturity investments...................     (7,544)    (47,470)    (56,557)
  Purchases of available-for-sale investments.................         --          --     (36,076)
  Restricted investments......................................       (250)         --      (1,358)
                                                                 ---------   ---------   ---------
  Net cash used in investing activities.......................    (10,137)    (11,105)    (54,724)
                                                                 ---------   ---------   ---------
Cash Flows From Financing Activities:
  Net proceeds from issuances of common stock.................     13,372      18,113      50,584
  Proceeds from bond and term loan issuances..................      1,431       3,558       7,867
  Equity proceeds from Gell Pharmaceuticals Inc. relating to
     the put option...........................................         --         726       1,076
  Principal payments on bond payable..........................         --          --        (470)
  Proceeds received on subscriptions receivable...............        500          --          --
                                                                 ---------   ---------   ---------
  Net cash provided by financing activities...................     15,303      22,397      59,057
                                                                 ---------   ---------   ---------
Net increase in cash and cash equivalents.....................      1,478         220      12,300
Cash and cash equivalents at the beginning of year............      2,562       4,040       4,260
                                                                 ---------   ---------   ---------
Cash and cash equivalents at the end of year..................   $  4,040    $  4,260    $ 16,560
                                                                 =========   =========   =========
Supplemental disclosures of cash flow information:
  Net interest paid...........................................   $     --    $    165    $    470
  Unrealized gain on available-for-sale securities............         --          --          62
  Issued shares of common stock in lieu of cash bonus.........         --          28          --
  Issuances of common stock to executive officers.............        273         237          --
  Collateral transferred from unrestricted to restricted
     investments, net.........................................   $    902    $  2,490    $  5,129
                                                                 =========   =========   =========
</TABLE>
 
          See accompanying notes to consolidated financial statements.
 
                                       F-6
<PAGE>   60
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
                   NOTES TO CONSOLIDATED FINANCIAL STATEMENTS
 
                        DECEMBER 31, 1994, 1995 AND 1996
 
(1)  ORGANIZATION AND BUSINESS ACTIVITIES
 
     Guilford Pharmaceuticals Inc. along with its subsidiaries, ("Guilford" or
the "Company") is a biopharmaceutical company engaged in the development and
commercialization of novel products in two principal areas: (i) targeted and
controlled drug delivery systems using proprietary biodegradable polymers for
the treatment of cancer and other diseases; and (ii) therapeutic and diagnostic
products for neurological diseases and conditions.
 
(2)  SUMMARY OF SIGNIFICANT ACCOUNTING POLICIES
 
  Principles of consolidation
 
     The consolidated financial statements include the accounts of Guilford
Pharmaceuticals Inc. and subsidiaries, all of which are wholly-owned. All
significant intercompany balances and transactions are eliminated in
consolidation.
 
  Development stage company
 
     During 1996, the Company received regulatory clearance from the U.S. Food
and Drug Administration ("FDA") to commence sales of GLIADEL(R). In addition,
the Company entered into a major strategic alliance with a corporate partner to
market and sell the product on a worldwide basis (excluding Scandinavia) and
recognized revenue from various corporate partnering activities. The Company
expects to recognize additional revenue from similar sources in the future and
from future sales of GLIADEL commencing in 1997. Accordingly, the Company
believes it is no longer in the development stage and has removed the references
and reporting requirements of SFAS No. 7, "Accounting and Reporting by
Development Stage Companies".
 
  Investment in Gell Pharmaceuticals Inc.
 
     The Company has a 20% equity interest in Gell Pharmaceuticals Inc. ("Gell")
and exercises significant influence over both operations and financial matters
of Gell (see Notes 14 and 15). In addition, the 80% stockholder has a currently
exercisable put option to exchange such equity interest for 750,000 shares of
common stock of the Company. The equity contributed to Gell by the 80%
stockholder approximated the fair value of the 750,000 shares of common stock of
the Company at the inception of Gell as determined by an independent investment
banker. Accordingly, the Company records substantially all of the contributions
of Gell by such stockholder as equity relating to the put option, which is
deemed by the Company and its investment banker to be an equity instrument of
the Company. In addition, the Company charges to operations approximately 100%
of the costs incurred from Gell's activities. The Company includes the dilutive
effect of the Company's common shares that would be issued under this currently
exercisable put option (using the treasury stock method) in its calculation of
primary and fully diluted earnings (loss) per share.
 
  Use of estimates
 
     The preparation of financial statements in conformity with generally
accepted accounting principles requires management to make estimates and
assumptions that affect the reported amounts of assets and liabilities and
disclosure of contingent assets and liabilities at the date of the financial
statements and the reported amounts of revenues and expenses during the
reporting period. Actual results could differ from those estimates.
 
                                       F-7
<PAGE>   61
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(2)  SUMMARY OF SIGNIFICANT ACCOUNTING POLICIES -- (CONTINUED)

  Cash and cash equivalents
 
     The Company considers all highly liquid investments with an original
maturity of three months or less when purchased to be cash equivalents.
 
  Investments
 
     Investments consist primarily of debt securities backed by the U.S.
government and commercial paper of U.S. companies. Investments may include
financial instruments which the Company believes will be held-to-maturity or may
be held available-for-sale. Classification of investments is made at the time
these investments are purchased. Held-to-maturity securities are those
securities in which the Company has the ability and intent to hold until
maturity. All other securities are classified as available-for-sale.
 
     Available-for-sale securities are recorded at fair value. Unrealized gains
and losses on available-for-sale securities are excluded from the results of
operations and are reported as a separate component of stockholders' equity
until realized. Realized gains and losses from the sale of available-for-sale
securities are determined on a specific identification basis. Held-to-maturity
securities are recorded at amortized cost, adjusted for the amortization or
accretion of premiums or discounts.
 
     A decline in the market value of any available-for-sale or held-to-maturity
security below cost that is deemed to be other than temporary would result in a
reduction in the carrying amount of such security to fair value. Such impairment
would be charged to operations in the period in which the decline in value is
deemed to be other than temporary. The Company has not recorded any such
permanent impairments since its inception.
 
  Concentration of credit risk
 
     The Company invests its excess cash in accordance with a policy objective
that seeks to preserve both liquidity and safety of principal. The policy limits
investments to certain instruments issued by institutions with strong investment
grade credit ratings and places restrictions on their terms and concentrations
by type and issuer. The Company has not realized any significant losses on its
investments.
 
  Fair value of financial instruments
 
     The fair value of financial instruments is determined by reference to
various market data and other valuation techniques, as appropriate. The fair
values of financial instruments approximate their recorded value.
 
  Property and equipment
 
     Property and equipment are recorded at cost, including interest on funds
borrowed to finance the construction of tenant improvements. Depreciation and
amortization are provided using the straight-line method over the estimated
useful lives of the assets, generally three to seven years for furniture and
equipment, and over the shorter of the estimated useful life of improvements or
lease term for such leasehold improvements. Expenditures for repairs and
maintenance are expensed as incurred.
 
  Revenue Recognition -- collaborative research, contract and license agreements
 
     Collaborative research revenue from cost-reimbursement agreements is
recorded as the related expenses are incurred, up to the contractual limits and
when the Company meets its performance obligations under the respective
agreements. Contract and licensing revenue is recognized when milestones are met
and the Company's significant performance obligations have been satisfied in
accordance with the terms of the
 
                                       F-8
<PAGE>   62
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(2)  SUMMARY OF SIGNIFICANT ACCOUNTING POLICIES -- (CONTINUED)

respective agreements. Cash received that is related to future performance under
such contracts is deferred and recognized as revenue when earned.
 
  Research and development, patent and royalty costs
 
     Research and development, patent, and royalty costs are expensed as
incurred.
 
  Inventories
 
     Inventories are stated at the lower of cost or market, using the first-in,
first-out (FIFO) method.
 
  Accounting for income taxes
 
     Deferred tax assets and liabilities are determined based on differences
between the financial reporting and tax basis of assets and liabilities and are
measured using the enacted tax rates and laws that will be in effect when the
differences are expected to reverse. The measurement of deferred tax assets is
reduced, if necessary, by a valuation allowance for any tax benefits which are
not expected to be realized. The effect on deferred tax assets and liabilities
of a change in tax rates is recognized in the period that such tax rate changes
are enacted.
 
  Stock-based compensation
 
     The Company accounts for share option issuances in accordance with the
provisions of APB No. 25, "Accounting for Stock Issued to Employees", and
related interpretations. As such, deferred compensation is recorded to the
extent that the current market price of the underlying stock exceeds the
exercise price on the date of grant. Such deferred compensation is amortized
over the respective vesting periods of such option grants. On January 1, 1996,
the Company adopted the disclosure requirements of SFAS No. 123, "Accounting for
Stock-Based Compensation" which allows entities to continue to apply the
provisions of APB No. 25 for financial statement reporting purposes and provide
pro forma net income (loss) and pro forma earnings (loss) per share footnote
disclosures for employee stock option grants made in 1995 and 1996 as if the
fair-value based method defined in SFAS No. 123 had been applied. The Company
has elected to continue to apply the financial statement reporting provisions of
APB No. 25 and to provide the pro forma disclosure provisions of SFAS No. 123.
Transactions with non-employees, in which goods or services are the
consideration received for the issuance of equity instruments, are accounted for
under the fair-value based method defined in SFAS No. 123 (see Note 9).
 
  Stock split
 
     On October 15, 1996, the Company's Board of Directors declared a
three-for-two stock split of the Company's common stock. Earnings (loss) per
share data has been adjusted to reflect the stock split for all periods
presented.
 
  Earnings (loss) per share
 
     The computation of earnings (loss) per share for 1996 and 1995 was based on
the weighted average common shares outstanding during the year, and includes,
when their effect is dilutive, common stock equivalents consisting of warrants,
stock options and put rights.
 
     The computation of loss per share in 1994 was based on the weighted average
common shares outstanding and includes common and common equivalent shares
issued during the 12 month period prior to the Company's June 1994 initial
public offering.
 
                                       F-9
<PAGE>   63
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(2)  SUMMARY OF SIGNIFICANT ACCOUNTING POLICIES -- (CONTINUED)
  Reclassifications
 
     Certain reclassifications have been made to the 1994 and 1995 consolidated
financial statements to conform with the 1996 financial statement presentation.
 
(3)  INVESTMENTS
 
     Investments available-for-sale and held-to-maturity securities by major
security type and class of security at December 31, 1995 and 1996, are as
follows:
 
<TABLE>
<CAPTION>
                                                                  GROSS         GROSS
                                                                UNREALIZED    UNREALIZED
                                                                 HOLDING       HOLDING       FAIR
                         1995                         COSTS       GAINS         LOSSES       VALUE
    ----------------------------------------------   -------    ----------    ----------    -------
    <S>                                              <C>        <C>           <C>           <C>
                                                                     (IN THOUSANDS)
    Held-to-maturity:
      U.S. Treasury Securities....................   $ 9,681       $  1         $   --      $ 9,682
      Corporate Debt Securities...................     5,513         --             (2)       5,511
      Other Debt Securities.......................        --         --             --           --
                                                     -------    -------       --------      -------
                                                     $15,194       $  1         $   (2)     $15,193
                                                     =======    =======       ========      =======
    1996
    Available-for-sale:
      U.S. Treasury Securities....................   $33,459       $167         $ (106)     $33,520
      Corporate Debt Securities...................     1,190          4             (1)       1,193
      Other Debt Securities.......................     1,427         13            (15)       1,425
                                                     -------    -------       --------      -------
                                                     $36,076       $184         $ (122)     $36,138
                                                     -------    -------  -    --------      -------
    Held-to-maturity:
      U.S. Treasury Securities....................   $23,051       $ 83         $  (88)     $23,046
      Corporate Debt Securities...................     1,690         18             (2)       1,706
      Other Debt Securities.......................        --         --             --           --
                                                     -------    -------       --------      -------
                                                     $24,741       $101         $  (90)     $24,752
                                                     -------    -------       --------      -------
                                                     $60,817       $285         $ (212)     $60,890
                                                     =======    =======       ========      =======
</TABLE>
 
     Maturities of debt securities classified as available-for-sale and
held-to-maturity were as follows at December 31, 1996 (maturities of
mortgage-backed securities and collateralized mortgage obligations have been
presented based upon estimated cash flows, assuming no change in the current
interest rate environment):
<TABLE>
<CAPTION>
                                                        HELD-TO-MATURITY       AVAILABLE-FOR-SALE
                                                      --------------------    --------------------
                                                       DECEMBER 31, 1996       DECEMBER 31, 1996
                                                      --------------------    --------------------
                                                      AMORTIZED     FAIR      AMORTIZED     FAIR
                                                        COST        VALUE       COST        VALUE
                                                      ---------    -------    ---------    -------
    <S>                                               <C>          <C>        <C>          <C>
                                                         (IN THOUSANDS)          (IN THOUSANDS)
 
<CAPTION>
    <S>                                               <C>          <C>        <C>          <C>
    Due in 1 year or less (1)......................    $20,935     $20,975     $ 9,177     $ 9,291
    Due in 1-2 years...............................      3,806       3,777      14,945      14,885
    Due in 2-5 years...............................         --          --      11,954      11,962
                                                      --------     ------- 
                                                       $24,741     $24,752     $36,076     $36,138
                                                      ========     ======= 
</TABLE>
 
- ---------------
(1) Includes $8,521 of restricted securities (see Note 6) included in
    "Investments -- restricted."
 
                                      F-10
<PAGE>   64
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(4)  COMPOSITION OF CERTAIN FINANCIAL STATEMENT CAPTIONS

<TABLE>
<CAPTION>
                                                                          DECEMBER 31,
                                                                      --------------------
                                                                       1995         1996
                                                                      -------      -------
    <S>                                                               <C>          <C>
                                                                         (IN THOUSANDS)
 
<CAPTION>
    <S>                                                               <C>          <C>
    Inventory:
      Raw materials................................................   $    --      $   600
      Work in process..............................................        --          432
      Finished goods...............................................        --          501
                                                                      --------     -------
                                                                      $    --      $ 1,533
                                                                      ========     =======
    Property and Equipment:
      Laboratory equipment.........................................   $   978      $ 1,322
      Manufacturing equipment......................................       528        1,677
      Computer and office equipment................................     1,258        2,126
      Leasehold improvements.......................................     2,253        9,767
      Construction in process......................................     1,050          276
                                                                      --------     -------
                                                                      $ 6,067      $15,168
      Less accumulated depreciation and amortization...............      (611)      (1,713)
                                                                      --------     -------
                                                                      $ 5,456      $13,455
                                                                      ========     =======
    Accrued Expenses and Other Current Liabilities:
      Consulting and contracted research...........................   $   401      $   935
      Payroll and related costs....................................       681        1,238
      Other current liabilities....................................       564        1,185
                                                                      --------     -------
                                                                      $ 1,646      $ 3,358
                                                                      ========     =======
</TABLE>
 
(5)  SIGNIFICANT CONTRACTS AND LICENSING AGREEMENTS
 
  Agreements with Rhone-Poulenc Rorer Pharmaceuticals Inc.
 
     In June 1996, the Company entered into a Marketing, Sales and Distribution
Rights Agreement (together with related agreements, the "RPR Agreements") with
Rhone-Poulenc Rorer Pharmaceuticals Inc. and its parent corporation
(collectively "RPR") granting RPR worldwide marketing rights (excluding
Scandinavia) for GLIADEL. The Company received $15 million upon the signing of
these agreements ($7.5 million as an equity investment and $7.5 million as a
non-refundable rights payment). On September 23, 1996, the Company obtained
clearance from the FDA for GLIADEL for recurrent glioblastoma multiforme where
surgical tumor removal is indicated and, accordingly, received a $20 million
non-refundable milestone payment from RPR. RPR is obligated to make up to $40
million in additional milestone payments, including $7.5 million in the form of
an equity investment, only if the Company achieves certain regulatory approvals.
In addition, RPR may also fund up to $17 million for the development of a
higher-dose GLIADEL product and to fund certain additional clinical studies
related to GLIADEL. The Company will manufacture and supply GLIADEL to RPR and
receive a transfer price and royalties based on sales.
 
     Under the RPR Agreements, the Company has the right to borrow up to an
aggregate of $7.5 million under certain conditions, $4.0 million is available no
earlier than January 2, 1997, and the remainder no earlier than 12 nor later
than 18 months following funding of the initial tranche. The loan proceeds would
be used to provide additional polymer product manufacturing capacity expansion.
Any principal amounts borrowed under this loan agreement are due five years from
the date borrowed and will carry an interest rate equal to the
 
                                      F-11
<PAGE>   65
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(5)  SIGNIFICANT CONTRACTS AND LICENSING AGREEMENTS -- (CONTINUED)

lowest rate paid by of RPR on its most senior indebtedness. Both the principal
and interest due under this agreement may, at the Company's election, be repaid
by offsetting certain amounts due to the Company under the RPR Agreements.
 
  Other contracts and agreements
 
     In October 1995, the Company entered into a license and distribution
agreement with Orion Corporation Farmos ("Orion Farmos") which provides that
Orion Farmos pay to the Company a licensing fee of $100,000, which amount was
received in 1996, and $100,000 upon Orion Farmos' first submission to a
governmental regulatory authority in Finland, Denmark, Norway or Sweden.
Additionally, the Company will receive both a transfer price on materials
shipped to Orion Farmos and royalties on future product sales, if any.
 
     In December 1995, the Company entered into an agreement with Daiichi
Radioisotope Laboratories, Ltd. ("DRL") which provides that DRL pay to the
Company a non-refundable license fee of $555,500, which amount was earned in
1995, and a milestone payment of $555,500 upon the filing of the first
application for the regulatory approval in certain foreign countries.
Additionally the Company receives both a transfer price on materials shipped to
DRL and royalties on future product sales, if any.
 
     The Company has entered into licensing, technology transfer and development
agreements with The Johns Hopkins University under which it is required to make
certain payments for patent maintenance costs, processing fees, license payments
and development payments aggregating approximately $995,000 through 1999. The
Company has agreed to spend $500,000 per year through 2003 with respect to their
internal research and development activities on advancing such technologies and
may be required to make certain payments, as defined, to The Johns Hopkins
University should agreed-upon milestones be attained. In addition, the Company
is required to pay a royalty on the net sales of all licensed products, if any,
as well as a percentage of all royalties received by the Company from
sublicensees, if any.
 
     The Company has also entered into various other licensing, research and
development agreements whereby they are committed to fund certain mutually
agreed-upon research and development projects, either on a best efforts basis or
upon attainment of certain performance milestones, as defined, or both, for
various periods unless canceled by the respective parties. Such future amounts
to be paid are approximately $1.4 million through 1998. In addition, the Company
is required to pay a royalty on the net sales of all licensed products, if any,
as well as a percentage of all royalties received by the Company from
sublicensees, if any.
 
     Royalty expenses relating to certain sublicensing agreements aggregated
approximately $32,000 in 1995 and $1.1 million in 1996.
 
(6)  FINANCING AGREEMENTS
 
  Bond agreements
 
     In December 1994, the Company entered into a bond financing arrangement
with Signet Bank under which the Company could borrow up to $8,000,000 for
capital improvements and for the purchase of certain equipment and furniture.
The bond was issued by the Maryland Economic Development Corporation with a 30%
guaranty of the outstanding borrowings by the Maryland Industrial Development
Financing Authority ("MIDFA"). The bond is to be repaid monthly, together with
interest at the London Interbank Overseas Rate ("LIBOR") plus 75 basis points
adjusted monthly (6.7% at December 31, 1996) over 102 months commencing July
1996. The Company is required to meet certain financial covenants, the most
restrictive of which requires the Company to maintain cash collateral equal to
50% of its outstanding indebtedness under the bond less $100,000. The amount of
the Company's cash collateral under the bond will be reduced
 
                                      F-12
<PAGE>   66
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(6)  FINANCING AGREEMENTS -- (CONTINUED)
quarterly beginning in October 1996 by an amount equivalent to 50% of the
principal repaid during the prior quarter. The Company may not declare any cash
dividends on its capital stock without the prior written consent of Signet Bank
and MIDFA. During 1996, the Company borrowed the remaining available principal
amount under the Signet Bank bond financing of $8 million. The outstanding
principal balance was $5.0 million and $7.5 million at December 31, 1995 and
1996, respectively.
 
  Term loan agreements
 
     The Company has entered into a $6.7 million term loan agreement with Signet
Bank for other tenant improvements. Under the terms of the loan agreement,
interest is charged monthly on the outstanding balance using LIBOR plus
five-eighths percent (0.625%) per annum. Principal payments are to be repaid
based on seventy-two (72) monthly installments commencing May, 1997. The Company
is required to maintain cash collateral equal to the outstanding principal
balance over the life of the loan. The Company had outstanding $4.9 million
under this loan at December 31, 1996.
 
     Under the bond and term loan agreements, the Company has set aside $3.4
million and $8.5 million at December 31, 1995 and 1996, respectively, as
collateral (together with the Bank's security interest in tenant improvements
and equipment) which is included in the accompanying consolidated balance sheets
as noncurrent assets under "Investments -- restricted".
 
  Revolving line of credit
 
     The Company has available a $250,000 revolving line of credit agreement
with a bank which requires interest at the bank's internal cost of funds plus 1%
and is payable on demand. The line of credit is fully secured by a U.S. Treasury
Note which is recorded under "Short-term investments -- restricted". There were
no amounts outstanding under the line of credit at December 31, 1995 and 1996.
 
  Master lease agreement
 
     In September 1996, the Company entered into a $5.0 million Master Lease
Agreement ("Master Agreement") with General Electric Capital Corporation
("GECC"). Each equipment lease the Company executes under the Master Agreement
is for a term of 49 months and requires an irrevocable letter of credit issued
from a banking institution equal to 70% of the equipment cost covered by each
such lease, which percentage decreases upon the annual anniversary of each lease
under the Master Agreement. The Company has leased $2.0 million in equipment
under operating leases as of December 31, 1996 collateralized by U.S. Treasury
notes aggregating approximately $1.4 million which are recorded under
"Short-term investments -- restricted".
 
(7)  CAPITAL TRANSACTIONS
 
     On October 15, 1996, the Board of Directors declared a three-for-two stock
split. All of the following transactions have been adjusted to reflect the stock
split. In June 1996, the Company entered into a stock purchase agreement with
RPR (see Note 5) whereby, RPR purchased 281,531 shares of the Company's common
stock for $7.5 million. In March 1996, the Company completed a public equity
offering of 3,450,000 shares of its common stock, $.01 par value providing net
proceeds of approximately $42.9 million to the Company. In August 1995, the
Company completed an additional public offering of 4,500,000 shares of common
stock, $.01 par value per share, providing net proceeds of approximately $17.9
million to the Company. In June 1994, the Company completed its initial public
offering of 2,812,500 shares of common stock providing approximately $12.9
million in net proceeds. In connection with the offering, the Company
 
                                      F-13
<PAGE>   67
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(7)  CAPITAL TRANSACTIONS -- (CONTINUED)

granted warrants to purchase 312,934 shares, as adjusted, of common stock to the
underwriter exercisable at $7.19 per share through June 24, 1999.
 
     The Company has awarded or sold 67,500, 58,694 and 39,129 shares of its
common stock to certain officers during 1995, 1994 and 1993, respectively. Such
shares are subject to the terms of the 1993 Employee Share Option and Restricted
Share Plan (see Note 9). As a result, the Company recorded deferred compensation
of approximately $510,000, which amount is being charged ratably to operations
over the various vesting periods.
 
(8)  STOCKHOLDER RIGHTS PLAN
 
     In September 1995, the Board of Directors adopted a Stockholder Rights Plan
("Rights Plan") in which preferred stock purchase rights ("Rights") were granted
at the rate of one Right for each share of common stock. All rights expire on
October 10, 2005. At December 31, 1996, the Rights were neither exercisable nor
traded separately from the Company's common stock, and become exercisable only
if a person or group becomes the beneficial owner of 20% or more of the
Company's common stock or announces a tender or exchange offer which would
result in its ownership of 20% or more of the Company's common stock. Each
holder of a Right, other than the acquiring person, would be entitled to
purchase $120 worth of common stock of the Company for each Right at the
exercise price of $60 per Right, which would effectively enable such Rights
holders to purchase common stock at one-half of the then current price.
 
     If the Company is acquired in a merger, or 50% or more of the Company's
assets are sold in one or more related transactions, each Right would entitle
the holder thereof to purchase $120 worth of common stock of the acquiring
company at the exercise price of $60 per Right. At any time after a person or
group of persons becomes the beneficial owner of 20% or more of the common
stock, the Board of Directors, on behalf of all stockholders, may exchange one
share of common stock for each Right, other than Rights held by the acquiring
person.
 
(9)  SHARE OPTION AND RESTRICTED SHARE PLANS
 
  The 1993 Employee Share Option and Restricted Share Plan
 
     The 1993 Employee Share Option and Restricted Share Plan, (the "1993
Plan"), was established to provide eligible individuals with an opportunity to
acquire or increase an equity interest in the Company and to encourage such
individuals to continue in the employment of the Company. Share options are
granted at the fair market value of the stock on the day immediately preceding
the date of grant or date of initial employment, if later. Share options are
exercisable for a period not to exceed ten years from the date of grant. In
general, share options vest over four years.
 
     Shares awarded under the restricted share provisions of the 1993 Plan are
valued at the fair market value of the stock on the day immediately preceding
the date of award and require a vesting period determined by the Board of
Directors. Should an individual leave the employment of the Company for any
reason, the award recipient would forfeit their ownership rights for all shares
not otherwise fully vested.
 
     At December 31, 1996, the maximum shares issuable under the 1993 Plan is
2,700,000, of which up to 300,000 may be issuable under the restricted share
provisions.
 
                                      F-14
<PAGE>   68
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(9)  SHARE OPTION PLANS -- (CONTINUED)

  The Directors' Plan
 
     The Director's Stock Option Plan (the "Directors' Plan") was established to
provide non-employee directors an opportunity to acquire or increase an equity
interest in the Company. Under the Directors' Plan, 300,000 shares of common
stock are reserved for issuance at an exercise price not less than fair value of
the Company's common stock on the day immediately preceding the date of grant.
Such options vest 50% at the end of year one and 100% at the end of year two.
Under the Directors' Plan 60,000 and 37,500 options were granted during 1995 and
1996, of which 30,000 are exercisable as of December 31, 1996. In 1996, the
Company granted 120,000 options outside of the Directors' Plan to two directors
with an exercise price of $13.54 (market value at date of grant). Approximately
90,000 options vested in 1996 and the remaining 30,000 options vest in equal
amounts in 1997 and 1998.
 
  Consultants
 
     In 1996, the Company granted options to each of two consultants to purchase
up to 225,000 (post-split) shares of the Company's common stock, valid for 10
years from issuance, with varying exercise prices. Vesting periods are based on
either the passage of time or based upon the achievement of certain milestones,
which, if ever achieved, would result in accelerated vesting of up to 150,000
(post-split) of the aforementioned options for each consultant. In 1996, the
Company recognized $1.2 million in non-cash compensation expense in accordance
with SFAS 123 relating to the value of such stock options (as established using
the Black Scholes pricing model) and it expects to charge varying amounts (up to
an additional $2.2 million in the aggregate) of non-cash compensation expense to
operations through 2001 relating to such agreements.
 
     Additional information with respect to the Company's option activity is
summarized as follows:
 
<TABLE>
<CAPTION>
                                                                                   WEIGHTED-
                                                                      SHARE         AVERAGE
                                                                     OPTIONS     EXERCISE PRICE
                                                                    ---------    --------------
    <S>                                                             <C>          <C>
    Balance, December 31, 1993...................................      42,392        $ 0.77
      Granted....................................................     219,452          3.01
      Exercised..................................................          --            --
      Canceled...................................................     (40,217)         5.69
                                                                    ---------        ------
    Balance, December 31, 1994...................................     221,627          2.09
      Granted....................................................     586,725          5.28
      Exercised..................................................     (19,565)         0.77
      Canceled...................................................      (6,750)         3.75
                                                                    ---------        ------
    Balance, December 31, 1995...................................     782,037          4.50
      Granted....................................................   1,777,740         15.61
      Exercised..................................................     (58,363)         3.02
      Canceled...................................................      (6,658)        10.82
                                                                    ---------        ------
    Balance, December 31, 1996...................................   2,494,756        $12.43
                                                                    =========        ======
</TABLE>
 
                                      F-15
<PAGE>   69
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(9)  SHARE OPTION PLANS -- (CONTINUED)

     Options outstanding and exercisable by price range as of December 31, 1996
are as follows:
 
<TABLE>
<CAPTION>
                           OPTIONS OUTSTANDING                                      OPTIONS EXERCISABLE
- -------------------------------------------------------------------------     -------------------------------
                    OUTSTANDING     WEIGHTED-AVERAGE                          EXERCISABLE
    RANGE OF           AS OF           REMAINING         WEIGHTED-AVERAGE       AS OF        WEIGHTED-AVERAGE
EXERCISE PRICES     12/31/1996      CONTRACTUAL LIFE      EXERCISE PRICE      12/31/1996      EXERCISE PRICE
- ----------------    -----------     ----------------     ----------------     ----------     ----------------
<S>                 <C>             <C>                  <C>                  <C>            <C>
 $  0.0 - $10.00       721,349             8.8                $ 4.62            141,651           $ 4.58
 $10.01 - $20.00     1,712,656             9.5                $15.41            135,000           $13.58
 $20.01 - $30.00        60,751             9.3                $21.34                  0           $    0
                                            --
                    -----------      -------------         -----------       -----------         -------- 
                     2,494,756             9.3                $12.43            276,651           $ 8.97
                    ===========      =============         ===========       ===========         ======== 
</TABLE>
 
     At December 31, 1996, there were 743,433 additional shares available for
grant under the 1993 Plan and 202,500 shares available for grant under the
Directors' Plan.
 
  Pro forma option information
 
     The per share weighted-average fair value of all stock options granted
during 1995 and 1996 was $2.35 and $7.16 on the date of grant using the Black
Scholes option-pricing model with the following weighted-average assumptions:
1996 -- expected dividend yield 0%, risk-free interest rate of 6.1%, volatility
of 50% and an expected life of 4 years; 1995 -- expected dividend yield 0%,
risk-free interest rate of 5.3%, volatility of 50% and an expected life of 4
years. The per share weighted-average fair value of stock options granted during
1996 to consultants was $6.12 using similar assumptions.
 
     The Company applies APB No. 25 in accounting for share options granted to
employees and, accordingly, no compensation expense has been recognized related
to such options to the extent that such options were granted at an exercise
price that equaled the fair market value at the grant date. Had the Company
determined compensation cost based on the fair value at the grant date for its
stock options under SFAS No. 123, (using the Black-Scholes option-pricing
model), the Company's net income (loss) would have been reduced (increased) to
the pro forma amounts indicated below:
<TABLE>
<CAPTION>
                                                                            1995        1996
                                                                          --------     ------
                                                                            (IN THOUSANDS)
                                                                          (EXCEPT SHARE DATA)
 
    <S>                                                   <C>             <C>          <C>
    Net income (loss)..................................   As reported     $(12,637)    $5,073
                                                          Pro forma        (12,740)     4,383
    Primary earnings (loss) per share..................   As reported        (1.70)      0.35
                                                          Pro forma          (1.71)      0.30
    Fully diluted earnings (loss) per share............   As reported        (1.70)      0.34
                                                          Pro forma          (1.71)      0.29
</TABLE>
 
     Pro forma net income (loss) reflects only options granted in 1995 and 1996.
Therefore, the full impact of calculating compensation cost for stock options
under SFAS No. 123 is not reflected in the pro forma net income (loss) amounts
presented above because compensation cost is reflected over the vesting period
and compensation cost for options granted prior to January 1, 1995 is not
considered.
 
(10)  INCOME TAXES
 
     As of December 31, 1996, the Company had net operating loss ("NOL")
carryforwards available for Federal income tax purposes of approximately $10.3
million which expire at various dates between 2008 to 2010. NOL carryforwards
are subject to ownership change limitations and may also be subject to various
other
 
                                      F-16
<PAGE>   70
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(10)  INCOME TAXES -- (CONTINUED)

limitations on the amounts to be utilized. As of December 31, 1996, the Company
had foreign tax credit carryforwards of approximately $61,000 expiring in 2000
and 2001, and general business tax credit carryforwards of $450,000 expiring
between 2008 and 2011.
 
     Current income taxes aggregating $179,000 were offset by a deferred benefit
of $179,000, resulting in no provision for income taxes in 1996 (none in 1995
and 1994).
 
     Actual income tax expense differs from the expected income tax expense
computed at the effective federal rate as follows:
<TABLE>
<CAPTION>
                                                                 1994       1995       1996
                                                                -------    -------    -------
                                                                       (IN THOUSANDS)
    <S>                                                         <C>        <C>        <C>
    Computed "expected" tax expense at statutory rate........   $(2,004)   $(4,296)   $ 1,725
    State income tax, net of federal benefit.................      (265)      (567)       230
    Research collaboration revenue...........................        --         --        557
    Compensatory stock grants................................       397         --         --
    Change in valuation allowance increase (decrease)........     1,871      4,849     (2,552)
    Other....................................................         1         14         40
                                                                -------    -------    -------
                                                                $    --    $    --    $    --
                                                                =======    =======    =======
</TABLE>
 
     Realization of net deferred tax assets related to the Company's NOL
carryforwards and other items is dependent on future earnings, which are
uncertain. Accordingly, a valuation allowance has been established equal to net
deferred tax assets which are not likely to be realized in the future, resulting
in net deferred tax assets of approximately $179,000 at December 31, 1996. The
change in the valuation allowance was an increase of approximately $4.8 million
in 1995 and a decrease of approximately $2.6 million in 1996.
 
     Significant components of the Company's deferred tax assets and liabilities
as of December 31, 1995 and 1996 are shown below.
<TABLE>
<CAPTION>
                                                                            DECEMBER 31,
                                                                         ------------------
                                                                          1995       1996
                                                                         -------    -------
                                                                           (IN THOUSANDS)
    <S>                                                                  <C>        <C>
    Deferred tax assets:
         Net operating loss carryforwards.............................   $ 7,261    $ 3,971
         Research and experimentation credits.........................       447        450
         Compensatory stock grants....................................       197        861
         Alternative minimum tax credit carryforward..................        --        179
         Accrued expenses.............................................        67        257
         Contribution carryover and capitalized start-up costs........        48         38
                                                                         -------    -------
                                                                           8,020      5,756
    Deferred tax liabilities:
         Prepaid expenses and depreciation............................        44        153
                                                                         -------    -------
    Net deferred tax assets...........................................     7,976      5,603
         Valuation allowance..........................................    (7,976)    (5,424)
                                                                         -------    -------
    Net deferred tax assets reported..................................   $    --    $   179
                                                                         =======    =======
</TABLE>
 
                                      F-17
<PAGE>   71
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(11)  RELATED PARTY TRANSACTIONS
 
     In September 1995, the Company entered into a three year consulting
agreement with the Chairman of its Scientific Advisory Board (the "Consultant")
who is also a nonemployee director whereby the Consultant is to provide
consulting and advisory services as requested by the Company. The Company is
obligated to pay an annual consulting fee of $150,000 (1st year), $160,000 (2nd
year), and $170,000 (3rd year) and has granted the Consultant 90,000 stock
options at fair market value. These options will vest one-third upon each
anniversary of the grant date so long as the individual remains a consultant
under the agreement.
 
     Notes receivable on common stock aggregating $139,500 and $129,750 at
December 31, 1995 and 1996, respectively, represent amounts due from officers of
the Company and are reflected as a reduction from stockholders' equity.
 
     Scios, Inc., a significant stockholder, has billed the Company for certain
services and equipment purchases related to the Company's research and
development activities aggregating $173,000, $233,000 and $295,000 in 1994, 1995
and 1996, respectively.
 
(12)  LEASE AGREEMENTS
 
     The Company has a master lease arrangement related to the land and building
which it presently occupies which expires in July 2005 with options to renew for
two five-year periods. The Company has the option to purchase the building after
the ninth year for its then current fair market value. The annual rental
aggregates approximately $306,000 and the Company pays for substantially all
occupancy related costs.
 
     The Company's future minimum lease payments under operating leases for
years subsequent to December 31, 1996 are as follows:
 
<TABLE>
<CAPTION>
                            YEAR ENDING DECEMBER 31                           (IN THOUSANDS)
    -----------------------------------------------------------------------   --------------
    <S>                                                                       <C>
           1997............................................................       $  870
           1998............................................................          797
           1999............................................................          798
           2000............................................................          764
           2001............................................................          331
           2002 and thereafter.............................................        1,123
                                                                                 -------
                                                                                  $4,683
                                                                                 ======= 
</TABLE>
 
     Facility and equipment rent expense aggregated approximately $37,000,
$452,000, and $680,000 in 1994, 1995 and 1996, respectively.
 
(13)  401(K) PROFIT SHARING PLAN
 
     The Company has a 401(k) Profit Sharing Plan (the "401(k) Plan") available
to all employees meeting certain eligibility criteria which permits participants
to contribute up to 15% of their compensation not to exceed the limits
established by the Internal Revenue Code. The Company may make "matching
contributions" equal to a percentage of a participant's contribution or may
contribute a discretionary amount to the Plan. The Company's contributions to
the 401(k) Plan were approximately $6,000, $9,000 and $11,000 for 1994, 1995,
and 1996 respectively.
 
     Effective January 1, 1997, the Company has elected to make "matching
contributions" in the Company's common stock equal to 50% of the first 6% of an
employee's salary contributed to such employees 401(k) Plan account. Such
amounts vest 25% per year based on a participant's years of service with the
Company.
 
                                      F-18
<PAGE>   72
 
                         GUILFORD PHARMACEUTICALS INC.
                                AND SUBSIDIARIES
 
           NOTES TO CONSOLIDATED FINANCIAL STATEMENTS -- (CONTINUED)
 
(14)  GELL PHARMACEUTICALS INC.
 
     In February 1995, the Company and The Abell Foundation, Inc., a
Baltimore-based not-for-profit corporation ("Abell"), established Gell. Gell was
formed primarily to track Abell's $2.5 million equity investment that, in
substance, was intended to purchase 750,000 shares of the Company's common stock
at the transaction date, which shares had an approximate fair market value of
$2.4 million. Abell received an 80% equity interest in Gell for $2,500,000 while
Guilford received a 20% equity interest for nominal cash consideration and
technology "know-how," which had a net carrying value of zero at the transaction
date.
 
     Under a master services agreement with Gell (the "Gell Agreement"), the
Company provides all of the personnel, resources and related administration and
research services for appropriate reimbursement of such costs incurred by the
Company on behalf of Gell.
 
     Accordingly, as the Company receives the $2.5 million from Gell, it
recognizes as paid-in-capital the cash received attributable to the fair value
of Abell's "put option" (which fair value has been established as approximately
$2.4 million by independent investment bankers). The excess cash of
approximately $100,000 is recorded as a reimbursement of certain costs incurred
by the Company on behalf of Gell. The Company has recorded approximately 100% of
the costs incurred from Gell's operations.
 
     Abell has a put right, immediately effective upon closing of the Gell
Agreement in 1995, which requires the Company to issue 750,000 shares of the
Company's common stock (which amount was fixed at closing) in exchange for
Abell's shares in Gell (see Note 15).
 
     The Company has received $1.9 million from Gell through December 31, 1996
and has recorded the derived fair value of the equity instrument (put option) as
paid in capital ($726,000 and $1.8 million at December 31, 1995 and 1996,
respectively). Certain costs incurred by the Company on behalf of Gell ($30,000
in 1995 and $45,000 in 1996) have been reimbursed by Gell and such reimbursement
has been recorded in the accompanying consolidated statement of operations.
Actual cash expenditures (including $422,000 of capitalized equipment) incurred
by the Company on behalf of Gell aggregated $1.9 million through December 31,
1996.
 
(15)  SUBSEQUENT EVENT (UNAUDITED)
 
     On March 5, 1997, Abell exercised its put option to receive the 750,000
shares of the Company's common stock to which it was entitled. This number of
shares was fixed and agreed to at the inception of the Gell transaction.
 
                                      F-19
<PAGE>   73
 
                     [This page intentionally left blank.]
<PAGE>   74
 
                     [This page intentionally left blank.]
<PAGE>   75
 
                     [This page intentionally left blank.]
<PAGE>   76
 
- ------------------------------------------------------------
- ------------------------------------------------------------
 
     NO DEALER, SALESPERSON OR ANY OTHER PERSON HAS BEEN AUTHORIZED TO GIVE ANY
INFORMATION OR TO MAKE ANY REPRESENTATIONS IN CONNECTION WITH THIS OFFERING
OTHER THAN THOSE CONTAINED IN THIS PROSPECTUS, AND, IF GIVEN OR MADE, SUCH
INFORMATION OR REPRESENTATIONS MUST NOT BE RELIED UPON AS HAVING BEEN AUTHORIZED
BY THE COMPANY OR ANY UNDERWRITER. THIS PROSPECTUS DOES NOT CONSTITUTE AN OFFER
TO SELL OR A SOLICITATION OF ANY OFFER TO BUY BY ANYONE IN ANY JURISDICTION IN
WHICH SUCH OFFER TO SELL OR SOLICITATION IS NOT AUTHORIZED, OR IN WHICH THE
PERSON MAKING SUCH OFFER OR SOLICITATION IS NOT QUALIFIED TO DO SO, OR TO ANY
PERSON TO WHOM IT IS UNLAWFUL TO MAKE SUCH OFFER OR SOLICITATION. NEITHER THE
DELIVERY OF THIS PROSPECTUS NOR ANY SALE MADE HEREUNDER SHALL, UNDER ANY
CIRCUMSTANCES, CREATE ANY IMPLICATION THAT THERE HAS BEEN NO CHANGE IN THE
AFFAIRS OF THE COMPANY SINCE THE DATE AS OF WHICH INFORMATION IS FURNISHED.
 
                            ------------------------
 
                               TABLE OF CONTENTS
 
<TABLE>
<CAPTION>
                                                        PAGE
                                                        ----
<S>                                                     <C>
Incorporation of Certain Documents by Reference........   2
Prospectus Summary.....................................   3
Risk Factors...........................................   7
Use of Proceeds........................................  17
Capitalization.........................................  17
Price Range of Common Stock and Dividend Policy........  18
Selected Consolidated Financial Data...................  19
Management's Discussion and Analysis of Financial
  Condition and Results of Operations..................  20
Business...............................................  23
Management.............................................  41
Principal Stockholders.................................  45
Description of Capital Stock...........................  47
Underwriting...........................................  50
Legal Matters..........................................  51
Experts................................................  51
Available Information..................................  51
Financial Statements................................... F-1
</TABLE>
- ------------------------------------------------------------
- ------------------------------------------------------------

- ------------------------------------------------------------
- ------------------------------------------------------------
 
                                3,250,000 SHARES
 
                       (GUILFORD PHARMACEUTICALS LOGO)
 
                                  COMMON STOCK
 
                          ---------------------------
                              P R O S P E C T U S
                          ---------------------------
                            OPPENHEIMER & CO., INC.
 
                               ALEX. BROWN & SONS
                                  INCORPORATED
 
                               HAMBRECHT & QUIST
                                          , 1997
 
- ------------------------------------------------------------
- ------------------------------------------------------------
<PAGE>   77
 
                                    PART II
                     INFORMATION NOT REQUIRED IN PROSPECTUS
 
ITEM 14. OTHER EXPENSES OF ISSUANCE AND DISTRIBUTION.
 
     The following table sets forth the fees and expenses in connection with the
issuance and distribution of the securities being registered hereunder. Except
for the SEC registration fee and NASD filing fee, all amounts are estimates.
 
<TABLE>
    <S>                                                                          <C>
    SEC registration fee......................................................   $ 31,078
    NASD filing fee...........................................................     10,776
    Nasdaq National Market Additional Listing Fee.............................     17,500
    Accounting fees and expenses..............................................     55,000
    Legal fees and expenses...................................................     75,000
    Blue Sky fees and expenses (including counsel fees).......................      5,000
    Printing and engraving expenses...........................................     50,000
    Transfer Agent and Registrar fees and expenses............................      5,000
    Miscellaneous expenses....................................................     50,646
                                                                                 --------
         Total................................................................   $300,000
                                                                                 ========
</TABLE>
 
ITEM 15. INDEMNIFICATION OF DIRECTORS AND OFFICERS.
 
     Section 145 of the Delaware General Corporation Law ("DGCL") authorizes a
court to award, or a corporation's board of directors to grant, indemnity to
directors and officers under certain circumstances for liabilities incurred in
connection with their activities in such capacities (including reimbursement for
expenses incurred). Article NINTH of the Company's Amended and Restated
Certificate of Incorporation, as amended, provides that the Company will
indemnify its directors and officers to the full extent permitted by law and
that no director shall be liable for monetary damages to the Registrant or its
stockholders for any breach of fiduciary duty, except to the extent provided by
applicable law (i) for any breach of the director's duty of loyalty to the
Registrant or its stockholders, (ii) for acts or omissions not in good faith or
which involve intentional misconduct or a knowing violation of law, (iii)
pursuant to Section 174 of the Delaware General Corporate Law or (iv) for any
transaction from which such director derived an improper personal benefit. In
addition, under indemnification agreements entered into with its directors and
officers, the Registrant is obligated, to the fullest extent permissible by the
DGCL, as it currently exists or may be amended, to indemnify and hold harmless
its directors, from and against all expense, liability and loss reasonably
incurred or suffered by such directors.
 
ITEM 16. EXHIBITS AND FINANCIAL STATEMENT SCHEDULES.
 
     (a) Exhibits:
 
   
<TABLE>
<CAPTION>
     NUMBER                                       DESCRIPTION
    ---------    -----------------------------------------------------------------------------
    <C>          <S>
     1.01        Form of Underwriting Agreement
     4.01*       Specimen Stock Certificate
     4.02**      Rights Agreement dated September 26, 1995
     5.01        Opinion of Hogan & Hartson L.L.P. as to the legality of the Common Stock
                 being registered
    23.01        Consent of Hogan & Hartson L.L.P. (contained in Exhibit 5.01)
    23.02        Consent of KPMG Peat Marwick LLP
    23.03****    Consent of Nath & Associates
    24.01***     Power of Attorney (contained on signature page)
</TABLE>
    
 
- ---------------
   * Incorporated by reference from the Registrant's Registration Statement on
     Form S-1 (No. 33-76938) declared effective June 16, 1994.
  ** Incorporated by reference from the Registrant's Form 8-K filed October 10,
     1995.
   
 *** Filed as an Exhibit to the Registrant's Registration Statement on Form S-3
     (No. 333-23001) filed on March 7, 1997.
    
   
**** Filed as an Exhibit to the Registrant's Amendment No. 2 to the Registration
     Statement on Form S-3 (No. 333-23001) filed on March 27, 1997.
    
 
                                      II-1
<PAGE>   78
 
     (b) Financial Statement Schedules.
 
     Not Applicable
 
ITEM 17. UNDERTAKINGS.
 
     Insofar as indemnification by the Registrant for liabilities arising under
the Securities Act of 1933 (the "Act") may be permitted to directors, officers
and controlling persons of the Registrant pursuant to the foregoing provisions,
or otherwise, the Registrant has been advised that in the opinion of the
Securities and Exchange Commission such indemnification is against public policy
as expressed in the Act and is, therefore, unenforceable. In the event that a
claim for indemnification against such liabilities (other than the payment by
the Registrant of expenses incurred or paid by a director, officer, or
controlling person of the Registrant in the successful defense of any action,
suit or proceeding) is asserted by such director, officer, or controlling person
in connection with the securities being registered, the Registrant will, unless
in the opinion of its counsel the matter has been settled by controlling
precedent, submit to a court of appropriate jurisdiction the question whether
such indemnification by it is against public policy as expressed in the Act and
will be governed by the final adjudication of such issue.
 
     The Registrant hereby undertakes that:
 
          (1) For purposes of determining any liability under the Securities Act
     of 1933, the information omitted from the form of prospectus filed as part
     of this Registration Statement in reliance upon Rule 430A and contained in
     a form of prospectus filed by the Registrant pursuant to Rule 424(b)(1) or
     (4) or 497(h) under the Securities Act shall be deemed to be part of this
     Registration Statement as of the time it was declared effective.
 
          (2) For the purpose of determining any liability under the Securities
     Act of 1933, each post-effective amendment that contains a form of
     prospectus shall be deemed to be a new registration statement relating to
     the securities offered therein, and the offering of such securities at that
     time shall be deemed to be the initial bona fide offering thereof.
 
          The undersigned registrant hereby undertakes that for the purposes of
     determining any liability under the Securities Act of 1933, each filing of
     the Registrant's Annual Report pursuant to Section 13(a) or Section 15(d)
     of the Securities Exchange Act of 1934 (and, where applicable, each filing
     of an employee benefit plan's annual report pursuant to Section 15(d) of
     the Securities Exchange Act of 1934) that is incorporated by reference in
     the Registration Statement shall be deemed to be a new Registration
     Statement relating to the Securities offered therein, and the offering of
     such Securities at that time shall be deemed to be the initial bona fide
     offering thereof.
 
                                      II-2
<PAGE>   79
 
                        SIGNATURES AND POWER OF ATTORNEY
 
   
     Pursuant to the requirements of the Securities Act of 1933, the Registrant
certifies that it has reasonable grounds to believe that it meets all of the
requirements for filing on Form S-3 and has duly caused this Registration
Statement to be signed on its behalf by the undersigned, thereunto duly
authorized, in the City of Baltimore, State of Maryland, on April 7, 1997.
    
 
                                          GUILFORD PHARMACEUTICALS INC.
 
                                          By:    /s/ CRAIG R. SMITH, M.D.
                                            ------------------------------------
                                                    CRAIG R. SMITH, M.D.
                                               PRESIDENT AND CHIEF EXECUTIVE
                                                           OFFICER
 
     Pursuant to the requirements of the Securities Act of 1933, this
Registration Statement has been signed by the following persons in the
capacities and on the date indicated.
 
   
<TABLE>
<CAPTION>
                  SIGNATURE                                  TITLE                     DATE
- ---------------------------------------------   --------------------------------   -------------
<C>                                             <S>                                <C>
          /s/ CRAIG R. SMITH, M.D.              Chief Executive Officer,           April 7, 1997
- ---------------------------------------------   President and Director
            CRAIG R. SMITH, M.D.                (Principal Executive Officer)
 
            /s/ ANDREW R. JORDAN                Vice President, Chief Financial    April 7, 1997
- ---------------------------------------------   Officer, and Treasurer
              ANDREW R. JORDAN                  (Principal Financial Officer and
                                                Principal Accounting Officer)
 
                      *                         Director                           April 7, 1997
- ---------------------------------------------
           SOLOMON H. SNYDER, M.D.
 
                      *                         Director                           April 7, 1997
- ---------------------------------------------
              RICHARD L. CASEY
 
                      *                         Director                           April 7, 1997
- ---------------------------------------------
           GEORGE L. BUNTING, JR.
 
                      *                         Director                           April 7, 1997
- ---------------------------------------------
       W. LEIGH THOMPSON, M.D., PH.D.
 
                      *                         Director                           April 7, 1997
- ---------------------------------------------
            ELIZABETH M. GREETHAM
 
        *By /s/ CRAIG R. SMITH, M.D.
- ---------------------------------------------
            CRAIG R. SMITH, M.D.
              ATTORNEY-IN-FACT
</TABLE>
    
 
                                      II-3
<PAGE>   80
 
                                 EXHIBIT INDEX
 
   
<TABLE>
<CAPTION>
 NUMBER                                         DESCRIPTION
- ---------    ---------------------------------------------------------------------------------
<S>          <C>
 1.01        Form of Underwriting Agreement
 4.01*       Specimen Stock Certificate
 4.02**      Rights Agreement dated September 26, 1995
 5.01        Opinion of Hogan & Hartson L.L.P. as to the legality of the Common Stock being
             registered
23.01        Consent of Hogan & Hartson L.L.P. (contained in Exhibit 5.01)
23.02        Consent of KPMG Peat Marwick LLP
23.03****    Consent of Nath & Associates
24.01***     Power of Attorney (contained on signature page)
</TABLE>
    
 
- ---------------
  * Incorporated by reference from the Registrant's Registration Statement on
    Form S-1 (No. 33-76938) declared effective June 16, 1994.
 
 ** Incorporated by reference from the Registrant's Form 8-K filed October 10,
    1995.
 
   
 *** Filed as an Exhibit to the Registrant's Registration Statement on Form S-3
     (No. 333-23001) filed on March 7, 1997.
    
 
   
**** Filed as an Exhibit to the Registrant's Amendment No. 2 to the Registration
     Statement on Form S-3 (No. 333-23001) filed on March 27, 1997.
    

<PAGE>   1
                                                                    EXHIBIT 1.01




                         GUILFORD PHARMACEUTICALS INC.

                                  COMMON STOCK

                             UNDERWRITING AGREEMENT


                                                                          , 1997
                                                          ----------------

Oppenheimer & Co., Inc.
Alex. Brown & Sons Incorporated
Hambrecht & Quist LLC
c/o Oppenheimer & Co., Inc.
Oppenheimer Tower
World Financial Center
New York, New York 10281

On behalf of the Several
Underwriters named on
Schedule I attached hereto.

Ladies and Gentlemen:

         GUILFORD PHARMACEUTICALS INC., a Delaware corporation (the "Company"),
proposes, subject to the terms and conditions contained herein, to sell to you
and the other underwriters named on Schedule I to this Agreement (the
"Underwriters"), for whom you are acting as Representatives (the
"Representatives"), an aggregate of 3,250,000 shares (the "Firm Shares") of the
Company's Common Stock, $.01 par value per share (the "Common Stock").  The
respective amounts of the Firm Shares to be so purchased by the several
Underwriters are set forth opposite their names in Schedule I hereto.  The
Company also proposes to grant to the Underwriters an option to purchase up to
an additional 487,500 shares of Common Stock (the "Option Shares") from them
for the purpose of covering over-allotments in connection with the sale of the
Firm Shares.  The Firm Shares and the Option Shares are together called the
"Shares."

         1.      SALE AND PURCHASE OF THE SHARES.  On the basis of the
representations, warranties and covenants contained in, and subject to the
terms and conditions of, this Agreement:

                 (a)      The Company agrees to sell to the Underwriters, and
each Underwriter agrees, severally and not jointly, to purchase from the
Company, at a price of $__________ per share (the "Initial Price"), the number
of Firm Shares set forth opposite the name of such Underwriter in Schedule I to
this Agreement, subject to adjustment in accordance with Section 10 hereof.


<PAGE>   2

                 (b)      The Company grants to the several Underwriters an
option to purchase all or any part of the Option Shares at the Initial Price.
The number of Option Shares to be purchased by each Underwriter shall be the
same percentage (adjusted by the Representatives to eliminate fractions) of the
total number of Option Shares to be purchased by the Underwriters as such
Underwriter is purchasing of the Firm Shares.  Such option may be exercised
only to cover over-allotments in the sales of the Firm Shares by the
Underwriters and may be exercised in whole or in part at any time on or before
12:00 noon, New York City time, on the business day two days before the Firm
Shares Closing Date (as defined below), and only once thereafter within 30 days
after the date of this Agreement, upon written or telegraphic notice, or verbal
or telephonic notice confirmed by written or telegraphic notice, by the
Representatives to the Company no later than 12:00 noon, New York City time, on
the business day two days before the Firm Shares Closing Date or at least two
business days before the Option Shares Closing Date (as defined below), as the
case may be, setting forth the number of Option Shares to be purchased and the
time and date (if other than the Firm Shares Closing Date) of such purchase.

         2.      DELIVERY AND PAYMENT.  Delivery by the Company of the Firm
Shares to the Representatives for the respective accounts of the Underwriters,
and payment of the purchase price by wire transfer, certified or official bank
check or checks payable in same-day funds drawn to the order of the Company,
against delivery of certificates therefor to the Representatives for the
several accounts of the Underwriters, shall take place at the offices of
Oppenheimer & Co., Inc., at Oppenheimer Tower, World Financial Center, New
York, New York 10281, at 10:00 a.m., New York City time, (a) on the third full
business day following the first day that the Shares are traded, (b) if this
Agreement is executed and delivered after 4:30 p.m. New York City Time, on the
fourth business day following the date of this Agreement, or (c) at such other
time or date, but not later than the fourth full business day following the
Effective Date (as hereinafter defined), as shall be agreed upon by the Company
and the Representatives (such time and date of delivery and payment are called
the "Firm Shares Closing Date").

         In the event the option with respect to the Option Shares is
exercised, delivery by the Company of the Option Shares to the Representatives
for the respective accounts of the Underwriters and payment of the purchase
price by wire transfer, certified or official bank check or checks payable in
New York Clearing House (next day) funds to the order of the Company shall take
place at the offices of Oppenheimer & Co., Inc. specified above at the time and
on the date (which may be the same date as, but in no event shall be earlier
than, the Firm Shares Closing Date) specified in the notice referred to in
Section 1(b) (such time and date of delivery and payment are called the "Option
Shares Closing Date").  The Firm Shares Closing Date and the Option Shares
Closing Date are called, individually, a "Closing Date" and, together, the
"Closing Dates."

         Certificates evidencing the Shares shall be registered in such names
and shall be in such denominations as the Representatives shall request at
least two full business days before the Firm Shares Closing Date or, in the
case of Option Shares, on the day of notice of exercise of the option as
described in Section l(c) and shall be made available to the Representatives
for




                                     2.
<PAGE>   3

checking and packaging, at such place as is designated by the Representatives,
on the Firm Shares Closing Date (or the Option Shares Closing Date in the case
of the Option Shares).

         3.      REGISTRATION STATEMENT AND PROSPECTUS; PUBLIC OFFERING.  The
Company has prepared in conformity with the requirements of the Securities Act
of 1933, as amended (the "Securities Act"), and the published rules and
regulations thereunder (the "Rules") adopted by the Securities and Exchange
Commission (the "Commission") a registration statement on Form S-3 (No.
333-23001), including a preliminary prospectus relating to the Shares, and has
filed with the Commission the Registration Statement (as hereinafter defined)
and such amendments thereof as may have been required to the date of this
Agreement.  The number of executed copies requested by you of such Registration
Statement (including all amendments thereof) and of the related preliminary
prospectus have heretofore been delivered by the Company to you.  The term
"preliminary prospectus" means any preliminary prospectus (as described in Rule
430 of the Rules), including the documents incorporated by reference therein,
included at any time as a part of the Registration Statement.  The Registration
Statement, as amended at the time and on the date it became effective (the
"Effective Date"), including all documents incorporated by reference therein
and all exhibits and information, if any, deemed to be part of the Registration
Statement pursuant to Rule 424(b), Rule 430A, Rule 434 and Rule 462(b) of the
Rules, is called the "Registration Statement." The term "Prospectus" means the
prospectus, including the documents incorporated by reference therein, in the
form first used to confirm sales of the Shares (whether such prospectus was
included in the Registration Statement at the time of effectiveness or was
subsequently filed with the Commission pursuant to Rule 424(b) of the Rules).

         The Company understands that the Underwriters propose to make a public
offering of the Shares in the United States, as set forth in and pursuant to
the Prospectus and an offer of the Shares on a private placement basis in
Canada in the provinces of British Columbia, Ontario and Quebec, as soon after
the Effective Date and the date of this Agreement as the Representatives deem
advisable.  The Canadian private placement shall be pursuant to an offering
memorandum (the "Offering Memorandum") comprised of the Prospectus and a
Canadian wrapper.  The Company hereby confirms that the Underwriters and
dealers have been authorized to distribute or cause to be distributed each
preliminary prospectus and Offering Memorandum and are authorized to distribute
the Prospectus (as from time to time amended or supplemented if the Company
furnishes amendments or supplements thereto to the Underwriters).

         4.      REPRESENTATIONS AND WARRANTIES OF THE COMPANY.  The Company
hereby represents and warrants to each Underwriter as follows:

                 (a)      On the Effective Date, the Registration Statement
complied, and on the date of the Prospectus and the Offering Memorandum, on the
date any post-effective amendment to the Registration Statement shall become
effective, on the date any supplement or amendment to the Prospectus or
Offering Memorandum is filed with the Commission and on each Closing Date, the
Registration Statement, the Prospectus and the Offering Memorandum (and any
amendment thereof or supplement thereto) will comply in all material respects
with the applicable provisions of the Securities Act and the Rules; the
Registration Statement did not, as






                                       3.
<PAGE>   4

of the Effective Date, contain any untrue statement of a material fact or omit
to state any material fact required to be stated therein or necessary in order
to make the statements therein not misleading; and on the other dates referred
to above neither the Registration Statement, the Prospectus, nor the Offering
Memorandum, nor any amendment thereof or supplement thereto, will contain any
untrue statement of a material fact or will omit to state any material fact
required to be stated therein or necessary in order to make the statements
therein not misleading.  When any related preliminary prospectus was first
filed with the Commission (whether filed as part of the Registration Statement
or any amendment thereto or pursuant to Rule 424(a) of the Rules) and when any
amendment thereof or supplement thereto was first filed with the Commission,
such preliminary prospectus as amended or supplemented complied in all material
respects with the applicable provisions of the Securities Act and the Rules did
not contain any untrue statement of a material fact or omit to state any
material fact required to be stated therein or necessary in order to make the
statements therein, in the light of the circumstances under which they were
made, not misleading; provided, however, that none of the representations and
warranties in this paragraph 4(a) shall apply to statements in, or omissions
from, the Registration Statement, the Prospectus or the Offering Memorandum
made in reliance upon, and in conformity with, information herein or otherwise
furnished in writing to the Company by or on behalf of the Underwriters for use
in the Registration Statement, the Prospectus or the Offering Memorandum.  With
respect to the preceding sentence, the only information furnished in writing by
the Representatives on behalf of the several Underwriters specifically for
inclusion in the Registration Statement, any preliminary prospectus, the
Prospectus or the Offering Memorandum is the last paragraph on the cover page,
the paragraphs with respect to stabilization and passive market making on the
inside front cover page of the Prospectus, the names of the Underwriters and
paragraphs 2, 4 and 5 contained under the caption "Underwriting" in the
Prospectus.  Notwithstanding the foregoing, if any revised prospectus shall be
provided to the Underwriters by the Company for use in connection with the
offering of the Shares that differs from the prospectus referred to in the
immediately preceding sentence (whether or not such revised prospectus is
required to be filed with the Commission pursuant to Rule 424(b) of the Rules),
the term "Prospectus" shall refer to such revised prospectus from and after the
time it is first provided to the Underwriters for such use.

                 (b)      The financial statements of the Company (including
all notes and schedules thereto) included in the Registration Statement and
Prospectus present fairly the financial position, the results of operations,
the statements of cash flows and the statements of stockholders' equity and the
other information purported to be shown therein of the Company at the
respective dates and for the respective periods to which they apply and such
financial statements have been prepared in conformity with generally accepted
accounting principles, consistently applied throughout the periods involved.
The summary and selected financial data included in the Prospectus present
fairly the information shown therein as at the respective dates and for the
respective periods specified, and the summary and selected financial data have
been presented on a basis consistent with the financial statements so set forth
in the Prospectus and other financial information.

                 (c)      To the knowledge of the Company, KPMG Peat Marwick
LLP, whose report is filed with the Commission as a part of the Registration
Statement, are and, during the





                                       4.
<PAGE>   5

periods covered by their report, were independent public accountants as
required by the Securities Act and the Rules.

                 (d)      The Company and each of its Subsidiaries is a
corporation duly organized, validly existing and in good standing under the
laws of the State of Delaware.  The Company has no subsidiary or subsidiaries
and does not control, directly or indirectly, any corporation, partnership or
joint venture except for Gell Pharmaceuticals Inc., GPI Holdings Inc., GPI NIL
Holdings Inc. and Holabird Holdings N.V. ("Holabird").  Holabird is a
corporation duly organized under the laws of the Netherlands.  Holabird is
currently inactive and has no assets or liabilities.  The Company and each such
subsidiary or other entity (collectively, "Subsidiaries") is duly qualified as
a foreign corporation in each jurisdiction in which the character or location
of its assets or properties (owned, leased or licensed) or the nature of its
business makes such qualification necessary except for such jurisdictions where
the failure to so qualify would not have a material adverse effect on the
assets or properties, business, results of operations, prospects or condition
(financial or otherwise) of the Company (a "Material Adverse Effect").  The
qualification of the Company in Maryland is the only such qualification
required.  The Company has all requisite corporate power and authority, and all
necessary authorizations, approvals, consents, orders, licenses, certificates
and permits of and from all governmental or regulatory bodies or any other
person or entity, to own, lease and license its assets and properties and
conduct its businesses as now being conducted and as described in the
Registration Statement and the Prospectus except for such authorizations,
approvals, consents, orders, material licenses, certificates and permits the
failure of which to obtain would not have a Material Adverse Effect.

                 (e)      Each of the Company and its Subsidiaries owns, or
possesses adequate and enforceable rights to use, each of the patents listed in
the Registration Statement and each preliminary prospectus under the caption
"Business -- Patents and Proprietary Technology" (the "Patents") and, except as
disclosed in the Registration Statement and the Prospectus, owns or possesses
adequate and enforceable rights to use all trademarks, trademark applications,
trade names, service marks, copyrights, copyright applications, licenses,
know-how and other similar rights and proprietary knowledge (collectively with
the Patents, "Intangibles") necessary for the conduct of its business as
described and as contemplated in the Registration Statement and the Prospectus.
Neither the Company nor any of its Subsidiaries has received any notice of any
infringement of or conflict with, nor, to the Company's knowledge, has
infringed, nor is infringing on asserted rights of others with respect to any
Intangibles which, singly or in the aggregate, if the subject of an unfavorable
decision, ruling or finding, would have a Material Adverse Effect.

                 (f)      Except as disclosed in the Prospectus and for the
security interest held by General Electric Capital Corporation ("GECC") on any
equipment leased by the Company pursuant to the Master Lease Agreement with
GECC, the Company and its Subsidiaries has good and marketable title to each of
the items of personal property which are reflected in the financial statements
referred to in Section 4(b) or are referred to in the Registration Statement
and the Prospectus as being owned by it and valid and enforceable leasehold
interests in each of the items of real and personal property which are referred
to in the Registration Statement and the





                                       5.
<PAGE>   6

Prospectus as being leased by it, in each case free and clear of all liens,
encumbrances, claims, security interests and defects, other than those
described in the Registration Statement and the Prospectus and those which do
not and will not have a Material Adverse Effect.

                 (g)      Except as disclosed in the Registration Statement and
the Prospectus, there is no action, suit or proceeding before or by any court
or governmental agency or body, domestic or foreign, pending or, to the
Company's best knowledge, threatened (and the Company does not know of any
basis therefor) against, or involving the assets, properties or business of,
the Company or its Subsidiaries (i) which is required to be disclosed in the
Prospectus or (ii) which is reasonably likely to have a Material Adverse
Effect.

                 (h)      Subsequent to the respective dates as of which
information is given in the Registration Statement and the Prospectus, except
as described therein, (i) there has not been any material adverse change in the
assets or properties, business, results of operations, prospects or condition
(financial or otherwise), of the Company or its Subsidiaries, whether or not
arising from transactions in the ordinary course of business; (ii) none of the
Company or its Subsidiaries has sustained any material loss or interference
with its assets, businesses or properties (whether owned or leased) from fire,
explosion, earthquake, flood or other calamity, whether or not covered by
insurance, or from any labor dispute or any court or legislative or other
governmental action, order or decree which would have a Material Adverse
Effect; and (iii) since the date of the latest balance sheet included in the
Registration Statement and the Prospectus, except as reflected therein, none of
the Company or its Subsidiaries has (1) issued any securities other than the
issuance of securities pursuant to the exercise of options granted under stock
option plans or agreements existing prior to the date of the latest balance
sheet included in the Registration Statement and Prospectus or incurred any
liability or obligation, direct or contingent, for borrowed money, except such
liabilities or obligations incurred in the ordinary course of business, (2)
entered into any material transaction not in the ordinary course of business or
(3) declared or paid any dividend or made any distribution on any shares of its
capital stock or redeemed, purchased or otherwise acquired or agreed to redeem,
purchase or otherwise acquire any shares of its capital stock.

                 (i)      There is no document or contract of a character
required to be described in or to be filed as an exhibit to the Registration
Statement which is not described or filed as required.  Each agreement
described in the Registration Statement and the Prospectus or listed in the
Exhibits to the Registration Statement or any document incorporated by
reference therein is in full force and effect and is valid and enforceable by
the Company in accordance with its terms, assuming the due authorization,
execution and delivery thereof by each of the other parties thereto.  Neither
the Company nor, to the Company's knowledge, any other party is in default in
the observance or performance of any term or obligation to be performed by it
under any such agreement, and no event has occurred which with notice or lapse
of time or both would constitute such a default, in any such case which default
or event would have a Material Adverse Effect.  No default exists, and no event
has occurred which with notice or lapse of time or both would constitute a
default, in the due performance and observance of any term, covenant or
condition, by the Company of any other agreement or instrument to which the
Company is a





                                       6.
<PAGE>   7
party or by which it or its properties or business may be bound or affected
which default or event would have a Material Adverse Effect.

                 (j)      None of the Company or its Subsidiaries is in
violation of any franchise, license, permit, judgment, decree, order, statute,
rule or regulation, where the consequences of such violation would have a
Material Adverse Effect or of any term or provision of its Certificate of
Incorporation or Bylaws.

                 (k)      Neither the execution, delivery and performance of
this Agreement by the Company nor the consummation of any of the transactions
contemplated hereby (including, without limitation, the issuance and sale by
the Company of the Shares) will give rise to a right to terminate or accelerate
the due date of any payment due under, or conflict with or result in the breach
of any term or provision of, or constitute a default (or an event which with
notice or lapse of time or both would constitute a default) under, or require
any consent or waiver under, or result in the execution or imposition of any
lien, charge or encumbrance upon any properties or assets of the Company
pursuant to the terms of, any indenture, mortgage, deed of trust or other
agreement or instrument to which the Company or its Subsidiaries is a party or
by which it or its Subsidiaries or any of their properties or businesses is
bound or any franchise, license, permit, judgment, decree, order, statute, rule
or regulation applicable to the Company or its Subsidiaries or violate any
provision of the Certificate of Incorporation or Bylaws of the Company or its
Subsidiaries, except for such consents or waivers which have already been
obtained and are in full force and effect.

                 (l)      The Company has authorized, and, at December 31, 1996
had outstanding,  capital stock as set forth in the Registration Statement and
Prospectus under the heading "Capitalization" in the Prospectus; there have
been no changes in the outstanding capital stock of the Company since that date
except to the extent that certain outstanding options and warrants set forth in
the footnotes thereto may have been exercised.  The certificates evidencing the
Shares are in due and proper legal form and have been duly authorized for
issuance by the Company.  All of the issued and outstanding shares of Common
Stock have been duly authorized and validly issued and are fully paid and
nonassessable and none of them was issued in violation of any preemptive or
other similar right.  The Shares, when issued and sold pursuant to this
Agreement, will be duly authorized and validly issued and fully paid and
nonassessable. Except as disclosed in the Registration Statement and the
Prospectus, there are no preemptive rights or any restriction upon the voting
or transfer of any securities of the Company pursuant to its Certificate of
Incorporation, Bylaws or other governing documents or any agreement or other
instrument to which the Company is a party or by which it may be bound. The
issued shares of capital stock of each of the Company's Subsidiaries have been
duly authorized and validly issued, are fully paid and nonassessable and are
owned by the Company free and clear of any perfected security interest or, any
other security interests, liens, encumbrances, equities or claims.  Except as
disclosed in the Registration Statement and the Prospectus, there is no
outstanding option, warrant or other right calling for the issuance of, and
there is no commitment, plan or arrangement to issue, any securities or
obligations convertible into any shares of capital stock of the Company or its
Subsidiaries or any such options, rights, convertible securities or
obligations.





                                       7.
<PAGE>   8
                 (m)      There are no holders of securities of the Company
who, by reason of the filing of the Registration Statement under the Securities
Act or the execution by the Company of this Agreement, have the right, not
previously satisfied or waived, to request or demand that the Company register
under the Securities Act such securities held by them.  Certain shareholders
and each director and executive officer of the Company, holding in the
aggregate 3,742,889 shares of Common Stock and options to purchase 1,250,142
shares of Common Stock have delivered to the Representatives its, his or her
enforceable written agreement (collectively, the "Lock-Up Agreements") that it,
he or she will not, directly or indirectly, from the date thereof and until a
period of 90 days, after the date of this Agreement, sell, offer, contract to
sell, make a short sale, pledge, otherwise dispose of, or reduce its, his or
her risk through the use of any option, put, call or other derivative security
relative to, (collectively, "sell") any shares of Common Stock (or any
securities convertible into or exchangeable or exercisable for any other rights
to purchase or acquire Common Stock) owned by it, him or her, without the prior
written consent of Oppenheimer & Co., Inc.  To the knowledge of the Company,
from March 7, 1997 through the date hereof, no such shareholder, officer or
director has sold any of its Common Stock (or any securities convertible into
or exchangeable or exercisable for other rights to purchase or acquire Common
Stock) or reduce its, his or her risk through the use of any option, put, call
or other derivative security relative to its Common Stock.

                 (n)      All necessary corporate action has been duly and
validly taken by the Company to authorize the execution, delivery and
performance of this Agreement and the issuance and sale of the Shares by the
Company.  This Agreement has been duly and validly authorized, executed and
delivered by the Company and constitutes a legal, valid and binding obligation
of the Company enforceable against the Company in accordance with its terms,
except (i) as the enforceability hereof may be limited by bankruptcy,
insolvency, reorganization, moratorium or other similar laws affecting the
enforcement of creditors' rights generally and by general equitable principles
and (ii) to the extent that rights to indemnity or contribution under this
Agreement may be limited by Federal and state securities laws or the public
policy underlying such laws.

                 (o)      No labor dispute with the employees of the Company
exists or, to the knowledge of the Company, is threatened; and the Company is
not aware of any existing or imminent labor disturbance by the employees of any
of its principal suppliers or contractors which would have a Material Adverse
Effect.  The Company is not aware of any threatened or pending litigation
between the Company or its Subsidiaries and any of its executive officers
which, if adversely determined, could have a Material Adverse Effect and has no
reason to believe that any such officers will not remain in the employment of
the Company.  No collective bargaining agreement exists with any of the
Company's or its Subsidiaries' employees and, to the knowledge of the Company,
no such agreement is imminent.

                 (p)      No transaction has occurred between or among the
Company and any of its affiliates, its  officers or directors or any affiliate
or affiliates of any such officer or director that is required to be described
in and is not described in the Registration Statement and the Prospectus or any
document incorporated by reference therein.





                                       8.
<PAGE>   9
                 (q)      The Company has not taken, nor will it take, directly
or indirectly, any action designed to or which might reasonably be expected to
cause or result in, or which has constituted or which might reasonably be
expected to constitute, the stabilization or manipulation of the price of the
Common Stock of the Company.

                 (r)      Each of the Company and its Subsidiaries has filed
all Federal, state, local and foreign tax returns which were required to be
filed to the date hereof, or has received extensions thereof, and such returns
are each true, correct and complete in all material respects, and has paid all
taxes shown on such returns and all assessments received by it to the extent
that the same are material and have become due, and there are no tax audits or
investigations pending, which if adversely determined would have a Material
Adverse Effect.

                 (s)      The books, records and accounts of the Company
accurately and fairly reflect, in reasonable detail, the transactions in, and
dispositions of, the assets of, and the results of operations of, the Company.
The Company maintains a system of internal accounting controls sufficient to
provide reasonable assurances that (i) transactions are executed in accordance
with management's general or specific authorizations, (ii) transactions are
recorded as necessary to permit preparation of financial statements in
accordance with generally accepted accounting principles and to maintain asset
accountability, (iii) access to assets is permitted only in accordance with
management's general or specific authorization and (iv) the recorded
accountability for assets is compared with the existing assets at reasonable
intervals and appropriate action is taken with respect to any differences.

                 (t)      Neither the Company, its Subsidiaries, nor to the
Company's knowledge, any director, officer, employee, agent or other person
acting on behalf of the Company or its Subsidiaries, has, in the course of his
actions for, or on behalf of, the Company violated or is in violation of any
provision of the Foreign Corrupt Practices Act of 1977 or made any bribe,
rebate, payoff, influence payment, kickback or other unlawful payment.

                 (u)      Each approval, consent, order, authorization,
designation, declaration or filing of, by or with any regulatory,
administrative or other governmental body necessary in connection with the
execution and delivery by the Company of this Agreement and the consummation of
the transactions herein contemplated required to be obtained or performed by
the Company (except such additional steps as may be required by the National
Association of Securities Dealers, Inc. (the "NASD") or may be necessary to
qualify the Shares for public offering by the Underwriters under the Securities
Act or state securities or Blue Sky laws has been obtained or made and is in
full force and effect).

                 (v)      The Shares have been authorized for listing on The
Nasdaq National Market.

                 (w)      There are no affiliations with the NASD among the
Company's officers, directors or, to the best of the knowledge of the Company,
any five percent or greater shareholder of the Company, except as set forth in
the Registration Statement or otherwise disclosed in writing to the
Representatives of the Underwriters.





                                       9.
<PAGE>   10
                 (x)      (i) Each of the Company and its Subsidiaries is in
compliance in all material respects with all rules, laws and regulation
relating to the use, treatment, storage and disposal of toxic substances and
protection of health or the environment ("Environmental Laws") which are
applicable to its business, (ii) none of the Company or its Subsidiaries has
received any notice from any governmental authority or third party of an
asserted claim under Environmental Laws, (iii) to the Company's knowledge, no
facts currently exist that will require the Company or its Subsidiaries to make
future material capital expenditures to comply with Environmental Laws, and
(iv) no property which is or has been owned, leased or occupied by the Company
or its Subsidiaries has been designated as a Superfund site pursuant to the
Comprehensive Environmental Response, Compensation and Liability Act of 1980,
as amended (42 U.S.C. Section 9601, et seq.), or otherwise designated as a
contaminated site under applicable state or local law.

                 (y)      The Company is not an "investment company" within the
meaning of the Investment Company Act of 1940, as amended (the "Investment
Company Act").

         5.      CONDITIONS OF THE UNDERWRITERS' OBLIGATIONS.  The obligations
of the Underwriters under this Agreement are several and not joint.  The
respective obligations of the Underwriters to purchase the Shares are subject
to each of the following terms and conditions:

                 (a)      Notification that the Registration Statement has
become effective shall have been received by the Representatives, and the
Prospectus shall have been timely filed with the Commission in accordance with
Section 6(a)(i) of this Agreement.

                 (b)      No order preventing or suspending the use of any
preliminary prospectus or the Prospectus shall have been or shall be in effect
and no order suspending the effectiveness of the Registration Statement shall
be in effect and no proceedings for such purpose shall be pending before or
threatened by the Commission, and any requests for additional information on
the part of the Commission (to be included in the Registration Statement or the
Prospectus or otherwise) shall have been complied with to the satisfaction of
the Representatives.

                 (c)      The representations and warranties of the Company
contained in this Agreement and in the certificate delivered pursuant to
Section 5(d) hereof shall be true and correct in all material respects when
made and on and as of each Closing Date as if made on such date, and the
Company shall have performed all covenants and agreements and satisfied all the
conditions in all material respects contained in this Agreement required to be
performed or satisfied by it at or before such Closing Date.

                 (d)      The Representatives shall have received on each
Closing Date a certificate, addressed to the Representatives and dated such
Closing Date, of the chief executive officer and the chief financial officer of
the Company to the effect that (i) the signers of such certificate have
examined the Registration Statement, the Prospectus and this Agreement and that
the representations and warranties of the Company in this Agreement are true
and correct in all respects on and as of such Closing Date with the same effect
as if made on such Closing Date and the Company has performed all covenants and
agreements and satisfied all conditions





                                      10.
<PAGE>   11
contained in this Agreement in all material respects required to be performed
or satisfied by it at or prior to such Closing Date, and (ii) no stop order
suspending the effectiveness of the Registration Statement has been issued and
to the best of their knowledge, no proceedings for that purpose have been
instituted or are pending under the Act.

                 (e)      The Representatives shall have received from KPMG
Peat Marwick LLP, on the date this Agreement is executed and on each Closing
Date, a letter dated such date, in form and substance satisfactory to the
Representatives and their counsel, to the effect that they are independent
public accountants with respect to the Company within the meaning of the
Securities Act and the Rules and that:

                          (i)     in their opinion the audited financial
statements and the related financial statement schedules, if any, included in
the Registration Statement and the Prospectus and covered by their reports
therein comply as to form in all material respects with the applicable
accounting requirements of the Securities Act and the Rules;

                          (ii)    on the basis of a reading of the amounts
included in the Registration Statement and the Prospectus under the headings
"Summary Financial Data" and "Selected Financial Data," carrying out certain
procedures (but not an audit in accordance with generally accepted auditing
standards) which would not necessarily reveal matters of significance with
respect to the comments set forth in such letter, a reading of the minutes of
the meetings of the stockholders and directors of the Company, and inquiries of
certain officials of the Company who have responsibility for financial and
accounting matters of the Company as to transactions and events subsequent to
the date of the latest audited financial statements, except as disclosed in the
Registration Statement and the Prospectus, nothing came to their attention
which caused them to believe that:

                                  (A)      the amounts in "Summary Financial
Data" and "Selected Financial Data" included in the Registration Statement and
the Prospectus do not agree with the corresponding amounts in the audited and
unaudited financial statements from which such amounts were derived; or

                                  (B)      with respect to the Company there
were, at a specified date not more than five business days prior to the date of
the letter, any change in the capital stock of the Company, increase in
long-term debt of the Company or decreases in net current assets of the Company
or decreases in the stockholders' equity of the Company, as compared with the
amounts shown on the Company's audited December 31, 1996 balance sheet included
in the Registration Statement.

                          (iii)   they have performed certain other procedures
as may be permitted under Generally Acceptable Auditing Standards as a result
of which they determined that certain information of an accounting, financial
or statistical nature (which is limited to accounting, financial or statistical
information derived from the general accounting records of the Company) set
forth in the Registration Statement and the Prospectus and reasonably specified
by the Representatives agrees with the accounting records of the Company; and





                                      11.
<PAGE>   12
                          (iv)    based upon the procedures set forth in
clauses (ii) and (iii) above and a reading of the amounts included in the
Registration Statement under the headings "Summary Financial Data" and
"Selected Financial Data" included in the Registration Statement and Prospectus
and a reading of the financial statements, from which certain of such data were
derived, nothing has come to their attention that give them reason to believe
that the "Summary Financial Data" and "Selected Financial Data" included in the
Registration Statement and Prospectus do not comply as to the form in all
material respects with the applicable accounting requirements of the Securities
Act and the Rules or that the information set forth therein is not fairly
stated in relation to the financial statements from which it was derived, or
that the financial statements included in the Registration Statement or
Prospectus from which certain of such data were derived are not in conformity
with generally accepted accounting principles applied on a basis substantially
consistent with that of the audited financial statements included in the
Registration Statement and Prospectus.

         References to the Registration Statement and the Prospectus in this
paragraph (e) are to such documents as amended and supplemented as of the date
of the letter.

                 (f)      The Representatives shall have received on each
Closing Date from Hogan & Hartson, L.L.P., counsel for the Company, an opinion,
addressed to the Representatives and dated such Closing Date, stating in effect
that:

                          (i)     Each of the Company and its Subsidiaries (as
used in this Section 5(f) only, the term "Subsidiaries" shall not be deemed to
include Holabird) was incorporated and is validly existing and in good standing
under the laws of the State of Delaware.  The Company is duly qualified and in
good standing as a foreign corporation in Maryland.

                          (ii)    Each of the Company and its Subsidiaries has
the corporate power and corporate authority under its Certificate of
Incorporation and the Delaware General Corporation Law, as amended (the
"DGCL"), to own, lease, license and operate its assets and properties and
conduct their business as it may be described in the Prospectus and with
respect to the Company to enter into, deliver and perform this Agreement as of
the date of such opinion and to issue and sell the Shares.

                          (iii)   Except as disclosed elsewhere in this
Agreement, the Company has authorized and outstanding capital stock as of the
date of the Capitalization table in the Prospectus as set forth in the
Prospectus under the heading "Capitalization"; there have been no changes in
the outstanding capital stock of the Company since that date except to the
extent that certain outstanding options and warrants set forth in the footnotes
thereto may have been exercised and for the issuance of 750,000 shares of
Common Stock to The Abell Foundation on March 5, 1997 upon exercise of its put
right with respect to its ownership interest in Gell Pharmaceuticals Inc.; the
form of certificate evidencing the Shares complies with the requirements of
Section 158 of the DGCL; all of the outstanding shares of Common Stock of the
Company have been duly authorized and validly issued and, assuming receipt of
the consideration therefor as provided in resolutions of the Company's Board of
Directors authorizing issuance thereof, are fully paid and nonassessable under
the DGCL.  There are no





                                      12.
<PAGE>   13
statutory preemptive rights to subscribe for or to purchase or acquire any
shares of Common Stock of the Company or its Subsidiaries pursuant to the
Company's Certificate of Incorporation or Bylaws or any agreement filed as an
exhibit to the Registration Statement.  The Shares, when issued and sold
pursuant to this Agreement, will be validly issued, fully paid and
nonassessable under the DGCL.  To such counsel's knowledge, except as disclosed
in the Registration Statement and the Prospectus, there is no outstanding
option, warrant or other right calling for the issuance of securities of the
Company or any of its Subsidiaries.  The issued shares of capital stock of each
of the Company's Subsidiaries have been duly authorized and validly issued, are
fully paid and nonassessable and are owned by the Company free and clear of any
perfected security interest or, to the knowledge of such counsel, any other
security interests, liens, encumbrances, equities or claims.

                          (iv)    To such counsel's knowledge, no holders of
securities of the Company have rights, which have not been waived or complied
with, to the registration of shares of Common Stock or other securities,
because of the filing of the Registration Statement by the Company or the
offering contemplated hereby.

                          (v)       This Agreement has been duly authorized,
executed and delivered by the Company.

                          (vi)    The execution, delivery and performance as of
the date hereof of this Agreement by the Company do not (i) violate the DGCL or
the Certificate of Incorporation or the Bylaws of the Company or (ii) to such
counsel's knowledge, breach or constitute a default under any contract or
agreement filed as an exhibit to the Registration Statement, the Company's
Report on Form 10-K for the year ended December 31, 1996 (the "Form 10-K") or
referenced in paragraph (xiii) hereof.

                          (vii)   No consent, approval, authorization or order
of any governmental or regulatory body is required for the performance of this
Agreement by the Company as of the date of such opinion, except such as have
been obtained under the Securities Act and such as may be required by the NASD
pursuant to its Corporate Finance Rules or under state securities or Blue Sky
laws in connection with the purchase and distribution of the Shares by the
several Underwriters or such as may be required under the Investment Company
Act (as to which no opinion need be expressed).

                          (viii)  The Registration Statement, all preliminary
prospectuses and the Prospectus and each amendment or supplement thereto
(except for the financial statements and supporting schedules and other
financial and statistical data derived therefrom included therein or omitted
therefrom, as to which such counsel need express no opinion) comply as to form
in all material respects with the requirements of the Securities Act and the
Rules.  In passing upon compliance as to form only, such counsel may assume
that all statements made in the Registration Statement and the Prospectus are
correct and complete.

                          (ix)    The Registration Statement has become
effective under the Securities Act; and, to such counsel's knowledge, no stop
order suspending the effectiveness of





                                      13.
<PAGE>   14
the Registration Statement or suspending or preventing the use of the
Prospectus has been issued and no proceedings for that purpose have been
instituted or are threatened under the Securities Act; any required filing of
the Prospectus and any supplement thereto pursuant to Rule 424(b) of the Rules
has been made in the manner and within the time period required by such Rule
424(b).

                          (x)     The Shares have been authorized for listing
on The Nasdaq National Market System.

                          (xi)    The statements under the captions "Risk
Factors--Government Regulation and Product Approvals" and "Business-Government
Regulation and Product Testing," insofar as such statements purport to
summarize applicable provisions of the Federal Food, Drug, and Cosmetic Act, as
amended, and the regulations promulgated thereunder, are accurate summaries in
all material respects of the provisions purported to be summarized under such
captions in the Prospectus.

                          (xii)   The authorized Common Stock of the Company
conforms in all material respects to the description thereof contained in the
Prospectus under the caption "Description of Capital Stock."

                          (xiii)  The descriptions under the caption
"Business-Technology Licensing Agreements" of certain provisions of the
agreement dated March 15, 1994 between Scios Inc. and the Company, the
agreement dated March 18, 1994 between the Company and the Research Triangle
Institute, the agreement dated June 25, 1996 between the Company, MIT and Johns
Hopkins, the agreement dated July 17, 1996 between the Company and Johns
Hopkins, the and the agreements dated January 2, 1996 and February 5, 1996
between the Company and Johns Hopkins are accurate in all material respects.

                 To the extent deemed advisable by such counsel, they may rely
as to matters of fact on certificates of responsible officers of the Company
and public officials and on the opinions of the counsel satisfactory to the
Representatives as to matters which are governed by laws other than the DGCL or
the Federal laws of the United States; provided that such counsel shall state
that in their opinion the Underwriters and they are justified in relying on
such other opinions.  Copies of such certificates and other opinions shall be
furnished to the Representatives and counsel for the Underwriters.

         Based solely upon an officers' certificate and such counsel's review
of its litigation docket and an inquiry of attorneys who provide services to
the Company, such counsel also shall confirm that, to such counsel's knowledge,
there are no legal or governmental proceedings pending or threatened against
the Company or its Subsidiaries except as set forth on Schedule II attached
hereto.

         In addition, such counsel shall state that during the course of the
preparation of the Registration Statement, such counsel participated in
conferences with officers and other representatives of the Company, with
representatives of the independent public accountants of





                                      14.
<PAGE>   15
the Company and with you and your representatives.  While such counsel has not
undertaken to determine independently, and does not assume any responsibility
for, the accuracy, completeness, or fairness of the statements in the
Registration Statement or Prospectus (except as specified in opinions (xi),
(xii) and (xiii), such counsel may state on the basis of these conferences and
its activities as counsel to the Company in connection with the Registration
Statement that no facts have come to such counsel's attention which cause such
counsel to believe that (i) the Registration Statement, at the time it became
effective, contained an untrue statement of a material fact or omitted to state
a material fact required to be stated therein or necessary to make the
statements therein not misleading, or that the Prospectus, as of its date and
as of any Closing Date, contained or contains an untrue statement of a material
fact or omitted or omits to state a material fact necessary in order to make
the statements therein, in the light of the circumstances under which they were
made, not misleading, (ii) there are any contracts or documents of a character
required to be described in the Registration Statement or the Prospectus or to
be filed as exhibits to the Registration Statement that are not described or
referred to therein or so filed or (iii) there are no contracts or documents of
a character required to be filed as an exhibit to the Company's Report on Form
10-K pursuant to Item 601(b)(10) of Regulation S-K under the Securities Act;
provided that in making the foregoing statements (which shall not constitute an
opinion), such counsel shall not be required to express any view as to patent
or trademark matters or the financial statements and supporting schedules and
other financial and statistical information, and data derived therefrom
included in or omitted from the Registration Statement or the Prospectus.

                 (g)      The Representatives shall have received on each
Closing Date from Nath & Associates, patent counsel for the Company, an opinion
addressed to the Representatives and dated such Closing Date, and stating in
effect that:

                          (i)     The statements in the Prospectus and
Registration Statement under the captions "Risk Factors - Uncertainty Regarding
Patents and Proprietary Technology," "Business - Patents, and Proprietary
Technology," and "Business-Technology License Agreements" have been reviewed by
such patent counsel and are accurate in all material respects and fairly
present the information disclosed therein.

                          (ii)    To the best of such patent counsel's
knowledge, after due inquiries, such patent counsel believes the Registration
Statement and the Prospectus do not contain any untrue statement of material
fact, or do not omit to state any material fact which would be required to be
stated in the Registration Statement and the Prospectus or are necessary to
make the statements therein not misleading.

                          (iii)   Except as disclosed in the Prospectus, the
Company has obtained all material intellectual property licenses required for
the conduct of its business and, to the best of such patent counsel's
knowledge, after due inquiry, such licenses are in full force and effect and
the Company is complying therewith in all material respects.

                          (iv)    Except as, and to the extent set forth, in
the Prospectus, to the best of such patent counsel's knowledge, after due
inquiry, the Company is not under any obligation





                                      15.
<PAGE>   16
to pay to any third party royalties or fees of any kind whatsoever with respect
to such technology or any related intellectual properties developed, employed,
or used in the present conduct of the Company's affairs.

                          (v)     To the best of such patent counsel's
knowledge, there is no claim or action by any person pertaining to, or
proceeding, pending or threatened, which challenges the rights of the Company
with respect to the Company's patents, trademarks and intellectual property
licenses.

                 (h)      All proceedings taken in connection with the sale of
the Firm Shares and the Option Shares as herein contemplated shall be
reasonably satisfactory in form and substance to the Representatives and their
counsel, and the Underwriters shall have received from Cooley Godward LLP,
counsel for the Underwriters, an opinion, addressed to the Representatives and
dated such Closing Date, with respect to the Shares, the Registration Statement
and the Prospectus, and such other related matters, as the Representatives may
reasonably request, and the Company shall have furnished to Cooley Godward LLP
such documents as they may reasonably request for the purpose of enabling them
to pass upon such matters.

                 (i)      The Representatives shall have received copies of the
Lock-up Agreements executed by each entity or person described in Section 4(m).

         6.      COVENANTS OF THE COMPANY.

                 (a)      The Company covenants and agrees with the several
Underwriters as follows:

                          (i)     The Company shall prepare the Prospectus in a
form approved by the Representatives and file such Prospectus pursuant to Rule
424(b) under the Securities Act not later than the Commission's close of
business on the second business day following the execution and delivery of
this Agreement, or, if applicable, such earlier time as may be required by Rule
430A(a)(3) under the Securities Act, and shall promptly advise the
Representatives (i) when any amendment to the Registration Statement shall have
become effective, (ii) of any request by the Commission for any amendment of
the Registration Statement or the Prospectus or for any additional information,
(iii) of the prevention or suspension of the use of any preliminary prospectus
or the Prospectus or of the issuance by the Commission of any stop order
suspending the effectiveness of the Registration Statement or the institution
or threatening of any proceeding for that purpose and (iv) of the receipt by
the Company of any notification with respect to the suspension of the
qualification of the Shares for sale in any jurisdiction or the initiation or
threatening of any proceeding for such purpose.  The Company shall not file any
amendment of the Registration Statement or supplement to the Prospectus unless
the Company has furnished the Representatives a copy for their review prior to
filing and shall not file any such proposed amendment or supplement to which
the Representatives reasonably object.  The Company shall use its best efforts
to prevent the issuance of any such stop order and, if issued, to obtain as
soon as possible the withdrawal thereof.





                                      16.
<PAGE>   17
                          (ii)    If, at any time when a prospectus relating to
the Shares is required to be delivered under the Securities Act and the Rules,
any event occurs as a result of which the Prospectus as then amended or
supplemented would include any untrue statement of a material fact or omit to
state any material fact necessary to make the statements therein in the light
of the circumstances under which they were made not misleading, or if it shall
be necessary to amend or supplement the Prospectus to comply with the
Securities Act or the Rules, the Company promptly shall prepare and file with
the Commission, subject to the second sentence of paragraph (i) of this Section
6(a), an amendment or supplement which shall correct such statement or omission
or an amendment which shall effect such compliance.

                          (iii)   The Company shall make generally available to
its security holders and to the Representatives as soon as practicable, but not
later than 45 days after the end of the 12-month period beginning at the end of
the fiscal quarter of the Company during which the Effective Date occurs (or 90
days if such 12-month period coincides with the Company's fiscal year), an
income statement (which need not be audited) of the Company, covering such
12-month period, which shall satisfy the provisions of Section 11(a) of the
Securities Act or Rule 158 of the Rules.

                          (iv)    The Company shall furnish to the
Representatives and counsel for the Underwriters, without charge, signed copies
of the Registration Statement (including all exhibits thereto and amendments
thereof) and to each other Underwriter a copy of the Registration Statement
(without exhibits thereto) and all amendments thereof and, so long as delivery
of a prospectus by an Underwriter or dealer may be required by the Securities
Act or the Rules, as many copies of any preliminary prospectus and the
Prospectus and any amendments thereof and supplements thereto as the
Representatives may reasonably request.

                          (v)     The Company shall cooperate with the
Representatives and their counsel in endeavoring to qualify the Shares for
offer and sale in connection with this offering under the state Blue Sky laws
of such jurisdictions (including in Canada the provinces of British Columbia,
Ontario and Quebec) as the Representatives may designate and shall maintain
such qualifications in effect so long as required for the distribution of the
Shares; provided, however, that the Company shall not be required in connection
therewith, as a condition thereof, to qualify as a foreign corporation or to
execute a general consent to service of process in any jurisdiction or subject
itself to taxation as doing business in any jurisdiction.

                          (vi)    For a period of five years after the date of
this Agreement, the Company shall supply to the Representatives, and to each
other Underwriter who may so request in writing, copies of such financial
statements and other periodic and special reports as the





                                      17.
<PAGE>   18
Company may from time to time distribute generally to the holders of any class
of its capital stock and furnish to the Representatives a copy of each annual
and other report it shall be required to file with the Commission.

                          (vii)   Without the prior written consent of the
Representatives, for a period of 90 days after the date of this Agreement, the
Company shall not issue, sell or register with the Commission, or otherwise
dispose of, directly or indirectly, any equity securities of the Company (or
any securities convertible into or exercisable or exchangeable for equity
securities of the Company), except for the issuance of the Shares pursuant to
the Registration Statement, the issuance of shares pursuant to the Company's
existing stock option plans (as amended or supplemented from time to time),
existing employee share purchase plan or existing separate stock option
agreements exchange rights or warrants, in each case if disclosed in the
Prospectus, or the issuance of Common Stock in connection with a corporate
partnering transaction if such shares may not be sold or transferred by such
corporate partner prior to the expiration of the 90-day period set forth
herein.  In the event that, during this period, any shares are issued to any of
the Company's officers or directors pursuant to the Company's existing stock
option plan or employee share purchase plan, the Company shall obtain the
written agreement of such grantee or purchaser or holder of such registered
securities that, for a period of 90 days after the date of this Agreement, such
person will not, directly or indirectly, without the prior written consent of
Oppenheimer & Co., Inc., sell, offer, contract to sell, make a short sale,
pledge, otherwise dispose of, or reduce its, his or her risk through the use of
any option, put, call or other derivative security relative to, any shares of
Common Stock (or any securities convertible into or exchangeable or exercisable
for any other rights to purchase or acquire Common Stock other than shares of
Common Stock issuable upon exercise of outstanding options) owned by such
person.

                          (viii)  On or before completion of this offering, the
Company shall make all filings required under applicable securities laws and by
Nasdaq.

                 (b)      The Company agrees to pay, or reimburse if paid by
the Representatives, whether or not the transactions contemplated hereby are
consummated or this Agreement is terminated, all costs and expenses of the
Company incident to the public offering of the Shares in the United States and
the private placement of the Shares in Canada and the performance of the
obligations of the Company under this Agreement including those relating to:
(i) the preparation, printing, filing and distribution of the Registration
Statement, including all exhibits thereto, each preliminary prospectus, the
Prospectus, all amendments and supplements to the Registration Statement and
the Prospectus, and the filing and distribution of this Agreement; (ii) the
preparation and delivery of certificates for the Shares to the Representatives;
(iii) the registration or qualification of the Shares for offer and sale under
the securities or Blue Sky laws of the various jurisdictions referred to in
Section 6(a)(v), including the reasonable fees and disbursements of counsel for
the Underwriters in connection with such registration and qualification and the
preparation, printing, distribution and shipment of preliminary and
supplementary Blue Sky memoranda; (iv) the furnishing (including costs of
shipping and mailing) to the Representatives and to the Underwriters of copies
of each preliminary prospectus, the Prospectus and all amendments or
supplements to the Prospectus, and of the several documents





                                      18.
<PAGE>   19
required by this Section to be so furnished, as may be reasonably requested for
use in connection with the offering and sale of the Shares by the Underwriters
or by dealers to whom Shares may be sold; (v) the filing fees of the NASD in
connection with its review of the terms of the public offering and reasonable
fees and disbursements of counsel for the Underwriters in connection with such
review; (vi) the furnishing (including costs of shipping and mailing) to the
Representatives and to the Underwriters of copies of all reports and
information required by Section 6(a)(vi); (vii) the inclusion of the Shares for
quotation on the Nasdaq National Market; and (viii) all transfer taxes, if any,
with respect to the sale and delivery of the Shares by the Company to the
Underwriters.  Subject to the provisions of Section 9, the Underwriters agree
to pay, whether or not the transactions contemplated hereby are consummated or
this Agreement is terminated, all costs and expenses incident to the
performance of the obligations of the Underwriters under this Agreement not
payable by the Company pursuant to the preceding sentence, including, without
limitation, the fees and disbursements of counsel for the Underwriters.

         7.      INDEMNIFICATION.

                 (a)      The Company agrees to indemnify and hold harmless
each Underwriter and each person, if any, who controls any Underwriter within
the meaning of Section 15 of the Securities Act or Section 20 of the Exchange
Act or under Canadian securities law in the provinces of British Columbia,
Ontario and Quebec against any and all losses, claims, damages and liabilities,
joint or several (including any reasonable investigation, legal and other
expenses incurred in connection with, and any amount paid in settlement of, any
action, suit or proceeding or any claim asserted), to which they, or any of
them, may become subject under the Securities Act, the Exchange Act or other
Federal or state or provincial law or regulation, at common law or otherwise,
insofar as such losses, claims, damages or liabilities arise out of or are
based upon (i) any untrue statement or alleged untrue statement of a material
fact contained in any preliminary prospectus, the Registration Statement, the
Prospectus, the Offering Memorandum or any amendment thereof or supplement
thereto, or arise out of or are based upon any omission or alleged omission to
state therein a material fact required to be stated therein or necessary to
make the statements therein not misleading or (ii) any breach of the
representations and warranties set forth in Section 4 hereof; provided,
however, that such indemnity shall not inure to the benefit of any Underwriter
(or any person controlling such Underwriter) on account of any losses, claims,
damages or liabilities arising from the sale of the Shares to any person by
such Underwriter if such untrue statement or omission or alleged untrue
statement or omission was made in such preliminary prospectus, the Registration
Statement, the Prospectus or the Offering Memorandum, or such amendment or
supplement, in reliance upon and in conformity with information furnished in
writing to the Company by the Representatives on behalf of any Underwriter
specifically for use therein and; provided, further, that the foregoing
indemnity agreement with respect to any preliminary prospectus shall not inure
to the benefit of any Underwriter or any person controlling such Underwriter,
from whom the person asserting any such losses, claims, damages or liabilities
purchased Shares, if a copy of the Prospectus (as then amended or supplemented,
if the Company shall have furnished any amendments or supplements thereto) was
not sent or given by or on behalf of such Underwriter to such person, if
required by law so to have been delivered, at or prior to the written
confirmation of the sale of the Shares





                                      19.
<PAGE>   20
to such person, and if the Prospectus (as so amended or supplemented) would
have cured the defect giving rise to such loss, claim, damage or liability.

                 (b)      Each Underwriter agrees, severally and not jointly,
to indemnify and hold harmless the Company, each person, if any, who controls
the Company within the meaning of Section 15 of the Securities Act or Section
20 of the Exchange Act, each director of the Company, each officer of the
Company who signs the Registration Statement to the same extent as the
foregoing indemnity from the Company to each Underwriter, but only insofar as
such losses, claims, damages or liabilities arise out of or are based upon any
untrue statement or omission or alleged untrue statement or omission which was
made in any preliminary prospectus, the Registration Statement or the
Prospectus, or any amendment thereof or supplement thereto, contained in the
last paragraph of the cover page, in the paragraphs relating to stabilization
and passive market making on the inside front cover page of the Prospectus, the
list of Underwriters and the statements contained in paragraphs 2, 4 and 5
under the caption "Underwriting" in the Prospectus; provided, however, that the
obligation of each Underwriter to indemnify the Company (including any
controlling person, director or officer thereof) shall be limited to the net
proceeds received by the Company from such Underwriter.

                 (c)      Any party that proposes to assert the right to be
indemnified under this Section will, promptly after receipt of notice of
commencement of any action, suit or proceeding against such party in respect of
which a claim is to be made against an indemnifying party or parties under this
Section, notify each such indemnifying party of the commencement of such
action, suit or proceeding, enclosing a copy of all papers served.  No
indemnification provided for in Section 7(a) or 7(b) shall be available to any
party who shall fail to give notice as provided in this Section 7(c) if the
party to whom notice was not given was unaware of the proceeding to which such
notice would have related and was prejudiced by the failure to give such notice
but the omission so to notify such indemnifying party of any such action, suit
or proceeding shall not relieve it from any liability that it may have to any
indemnified party for contribution or otherwise other than under this Section.
In case any such action, suit or proceeding shall be brought against any
indemnified party and it shall notify the indemnifying party of the
commencement thereof, the indemnifying party shall be entitled to participate
in, and, to the extent that it shall wish, jointly with any other indemnifying
party similarly notified, to assume the defense thereof, with counsel
reasonably satisfactory to such indemnified party, and after notice from the
indemnifying party to such indemnified party of its election so to assume the
defense thereof and the approval by the indemnified party of such counsel, the
indemnifying party shall not be liable to such indemnified party for any legal
or other expenses, except as provided below and except for the reasonable costs
of investigation subsequently incurred by such indemnified party in connection
with the defense thereof.  The indemnified party shall have the right to employ
its counsel in any such action, but the fees and expenses of such counsel shall
be at the expense of such indemnified party unless (i) the employment of
counsel by such indemnified party has been authorized in writing by the
indemnifying parties, (ii) the indemnified party shall have reasonably
concluded that there may be a conflict of interest between the indemnifying
parties and the indemnified party in the conduct of the defense of such action
(in which case the indemnifying parties shall not have the right to direct the
defense of such action on behalf of the indemnified party) or (iii) the
indemnifying parties shall not have





                                      20.
<PAGE>   21
employed counsel to assume the defense of such action within a reasonable time
after notice of the commencement thereof, in each of which cases the fees and
expenses of one counsel shall for all similarly situated indemnified parties be
at the expense of the indemnifying parties.  An indemnifying party shall not be
liable for any settlement of any action, suit, proceeding or claim effected
without its written consent, which consent shall not unreasonably be withheld.

         8.      CONTRIBUTION.  In order to provide for just and equitable
contribution in circumstances in which the indemnification provided for in
Section 7(a) or 7(b) is due in accordance with its terms but for any reason is
held to be unavailable from the Company, the Company and the Underwriters shall
contribute to the aggregate losses, claims, damages and liabilities (including
any investigation, legal and other expenses reasonably incurred in connection
with, and any amount paid in settlement of, any action, suit or proceeding or
any claims asserted, but after deducting any contribution received by the
Company from persons other than the Underwriters, such as persons who control
the Company within the meaning of the Securities Act, officers of the Company
who signed the Registration Statement and directors of the Company, who may
also be liable for contribution) to which the Company and one or more of the
Underwriters may be subject in such proportion as is appropriate to reflect the
relative benefits received by the Company on the one hand and the Underwriters
on the other from the offering of the Shares or, if such allocation is not
permitted by applicable law or indemnification is not available as a result of
the indemnifying party not having received notice as provided in Section 7
hereof, in such proportion as is appropriate to reflect not only the relative
benefits referred to above but also the relative fault of the Company on the
one hand and the Underwriters on the other in connection with the statements or
omissions which resulted in such losses, claims, damages, liabilities or
expenses, as well as any other relevant equitable considerations.  The relative
benefits received by the Company and the Underwriters shall be deemed to be in
the same proportion as (x) the total proceeds from the offering (net of
underwriting commissions but before deducting expenses) received by the
Company, as set forth in the table on the cover page of the Prospectus, bear to
(y) the underwriting commissions received by the Underwriters, as set forth in
the table on the cover page of the Prospectus.  The relative fault of the
Company or the Underwriters shall be determined by reference to, among other
things, whether the untrue or alleged untrue statement of a material fact
related to information supplied by the Company or the Underwriters and the
parties' relative intent, knowledge, access to information and opportunity to
correct or prevent such statement or omission.  The Company and the
Underwriters agree that it would not be just and equitable if contribution
pursuant to this Section 8 were determined by pro rata allocation (even if the
Underwriters were treated as one entity for such purpose) or by any other
method of allocation which does not take account of the equitable
considerations referred to above.  Notwithstanding the provisions of this
Section 8, (i) in no case shall any Underwriter (except as may be provided in
the Agreement Among Underwriters) be liable or responsible for any amount in
excess of the underwriting discount applicable to the Shares purchased by such
Underwriter hereunder, and (ii) the Company shall be liable and responsible for
any amount in excess of such underwriting discount; provided, however, that no
person guilty of fraudulent misrepresentation (within the meaning of Section
11(f) of the Securities Act) shall be entitled to contribution from any person
who was not guilty of such fraudulent misrepresentation.  For purposes of this
Section 8, each person, if any, who controls an Underwriter within the meaning
of Section 15 of the Securities





                                      21.
<PAGE>   22
Act or Section 20(a) of the Exchange Act shall have the same rights to
contribution as such Underwriter, and each person, if any, who controls the
Company within the meaning of the Section 15 of the Securities Act or Section
20(a) of the Exchange Act, each officer of the Company who shall have signed
the Registration Statement and each director of the Company shall have the same
rights to contribution as the Company, subject in each case to clauses (i) and
(ii) in the immediately preceding sentence of this Section 8.  Any party
entitled to contribution will, promptly after receipt of notice of commencement
of any action, suit or proceeding against such party in respect of which a
claim for contribution may be made against another party or parties under this
Section, notify such party or parties from whom contribution may be sought, but
the omission so to notify such party or parties from whom contribution may be
sought shall not relieve the party or parties from whom contribution may be
sought from any obligation it or they may have hereunder or otherwise (except
as specifically provided in Section 7(c)).  No party shall be liable for
contribution with respect to any action, suit, proceeding or claim settled
without its written consent; provided, however, that such consent shall not be
unreasonably withheld.  The Underwriters' obligations to contribute pursuant to
this Section 8 are several in proportion to their respective underwriting
commitments and not joint.

         9.      TERMINATION.  This Agreement may be terminated with respect to
the Shares to be purchased on a Closing Date by the Representatives by
notifying the Company at any time:

                 (a)      in the absolute discretion of the Representatives at
or before any Closing Date: (i) if on or prior to such date, any domestic or
international event or act or occurrence has materially disrupted, or in the
opinion of the Representatives will materially disrupt, the securities markets;
(ii) if there has occurred any new outbreak or material escalation of
hostilities or other calamity or crisis the effect of which on the financial
markets of the United States is such as to make it, in the reasonable judgment
of the Representatives, inadvisable to proceed with the offering; (iii) if
there shall be such a material adverse change in general financial, political
or economic conditions or the effect of intentional conditions on the financial
markets in the United States is such as to make it, in the reasonable judgment
of the Representatives, inadvisable or impracticable to market the Shares; (iv)
if trading in the Shares has been suspended by the Commission or trading
generally on the New York Stock Exchange, Inc.  or Nasdaq has been suspended or
limited, or minimum or maximum ranges for prices for securities shall have been
imposed, by said exchanges or by order of the Commission, the NASD or any other
governmental or regulatory authority; or (v) if a banking moratorium has been
declared by any state or Federal authority, or

                 (b)      at or before any Closing Date, that any of the
conditions specified in Section 5 shall not have been fulfilled when and as
required by this Agreement.

                 If this Agreement is terminated pursuant to any of its
provisions, the Company shall not be under any liability to any Underwriter,
and no Underwriter shall be under any liability to the Company, except that (y)
if this Agreement is terminated by the Representatives or the Underwriters
because of any failure, refusal or inability on the part of the Company to
comply with the terms or to fulfill any of the conditions of this Agreement,
the Company will reimburse the Underwriters for all out-of-pocket expenses
(including the reasonable fees and





                                      22.
<PAGE>   23
disbursements of their counsel) incurred by them in connection with the
proposed purchase and sale of the Shares or in contemplation of performing
their obligations hereunder and (z) no Underwriter who shall have failed or
refused to purchase the Shares agreed to be purchased by it under this
Agreement, without some reason sufficient hereunder to justify cancellation or
termination of its obligations under this Agreement, shall be relieved of
liability to the Company or to the other Underwriters for damages occasioned by
its failure or refusal.

         10.     SUBSTITUTION OF UNDERWRITERS.  If one or more of the
Underwriters shall fail (other than for a reason sufficient to justify the
cancellation or termination of this Agreement under Section 9) to purchase on
any Closing Date the Shares agreed to be purchased on such Closing Date by such
Underwriter or Underwriters, the Representatives may find one or more
substitute underwriters to purchase such Shares or make such other arrangements
as the Representatives may deem advisable or one or more of the remaining
Underwriters may agree to purchase such Shares in such proportions as may be
approved by the Representatives, in each case upon the terms set forth in this
Agreement.  If no such arrangements have been made by the close of business on
the business day following such Closing Date,

                 (a)      if the number of Shares to be purchased by the
defaulting Underwriters on such Closing Date shall not exceed 10% of the Shares
that all the Underwriters are obligated to purchase on such Closing Date, then
each of the nondefaulting Underwriters shall be obligated to purchase such
Shares on the terms herein set forth in proportion to their respective
obligations hereunder; provided, that in no event shall the maximum number of
Shares that any Underwriter has agreed to purchase pursuant to Section 1 be
increased pursuant to this Section 10 by more than one-ninth of such number of
Shares without the written consent of such Underwriter, or

                 (b)      if the number of Shares to be purchased by the
defaulting Underwriters on such Closing Date shall exceed 10% of the Shares
that all the Underwriters are obligated to purchase on such Closing Date, then
the Company shall be entitled to an additional business day within which it
may, but is not obligated to, find one or more substitute underwriters
reasonably satisfactory to the Representatives to purchase such Shares upon the
terms set forth in this Agreement.

         In any such case, either the Representatives or the Company shall have
the right to postpone the applicable Closing Date for a period of not more than
five business days in order that necessary changes and arrangements (including
any necessary amendments or supplements to the Registration Statement or
Prospectus) may be effected by the Representatives and the Company.  If the
number of Shares to be purchased on such Closing Date by such defaulting
Underwriter or Underwriters shall exceed 10% of the Shares that all the
Underwriters are obligated to purchase on such Closing Date, and none of the
nondefaulting Underwriters or the Company shall make arrangements pursuant to
this Section within the period stated for the purchase of the Shares that the
defaulting Underwriters agreed to purchase, this Agreement shall terminate with
respect to the Shares to be purchased on such Closing Date without liability on
the part of any nondefaulting Underwriter to the Company and without liability
on the part of the Company, except in both cases as provided in Sections 6(b),
7, 8 and 9.  The provisions of this Section shall not in any way affect the
liability of any defaulting Underwriter to the





                                      23.
<PAGE>   24
Company or the nondefaulting Underwriters arising out of such default.  A
substitute underwriter hereunder shall become an Underwriter for all purposes
of this Agreement.

         11.     MISCELLANEOUS.  The respective agreements, representations,
warranties, indemnities and other statements of the Company and of the
Underwriters set forth in or made pursuant to this Agreement shall remain in
full force and effect, regardless of any investigation made by or on behalf of
any Underwriter or the Company or any of the officers, directors or controlling
persons referred to in Sections 7 and 8 hereof, and shall survive delivery of
and payment for the Shares.  The provisions of Sections 6(b), 7, 8 and 9 shall
survive the termination or cancellation of this Agreement.

         This Agreement has been and is made for the benefit of the
Underwriters and the Company and their respective successors and assigns, and,
to the extent expressed herein, for the benefit of persons controlling any of
the Underwriters, or the Company, and directors and officers of the Company,
and their respective successors and assigns, and no other person shall acquire
or have any right under or by virtue of this Agreement.  The term "successors
and assigns" shall not include any purchaser of Shares from any Underwriter
merely because of such purchase.

         All notices and communications hereunder shall be in writing and
mailed or delivered or by telephone or telegraph if subsequently confirmed in
writing, (a) if to the Representatives, c/o Oppenheimer & Co., Inc.,
Oppenheimer Tower, World Financial Center, New York, New York 10281 Attention:
Peter J. Crowley, with a copy to Gregory C. Smith, Cooley Godward LLP, One
Maritime Plaza, 20th Floor, San Francisco, California 94111, facsimile (415)
951-3699 and (b) if to the Company, to its agent for service as such agent's
address appears on the cover page of the Registration Statement, with a copy to
Michael J. Silver, Hogan & Hartson, L.L.P., 111 South Calvert, Suite 1600,
Baltimore, Maryland 21202, facsimile (410) 539-6981.

         This Agreement shall be governed by and construed in accordance with
the laws of the State of New York without regard to principles of conflict of
laws.





                                      24.
<PAGE>   25
         This Agreement may be signed in any number of counterparts, each of
which shall be an original, with the same effect as if the signatures thereto
and hereto were upon the same instrument.

         Please confirm that the foregoing correctly sets forth the agreement
among us.

                                               Very truly yours,


                                               GUILFORD PHARMACEUTICALS INC.



                                               By:                          
                                                  ------------------------------

                                               Title:                         
                                                     ---------------------------


The foregoing Underwriting Agreement
is hereby confirmed and accepted
as of the date first above written.


OPPENHEIMER & CO., INC.
ALEX. BROWN & SONS INCORPORATED
HAMBRECHT & QUIST LLC


As Representatives of the several
Underwriters named in Schedule I.

By:  OPPENHEIMER & CO., INC.



By:                                                
   -------------------------------------

Title:                                             
      ----------------------------------






                                      25.
<PAGE>   26
                                   SCHEDULE I



<TABLE>
<CAPTION>
                                                                                   NUMBER OF FIRM
 NAME OF UNDERWRITER                                                           SHARES TO BE PURCHASED
 <S>                                                                                  <C>
 Oppenheimer & Co., Inc.
 Alex. Brown & Sons Incorporated
 Hambrecht & Quist LLC





 Total . . . . . . . . . . . . . . . . . . . . . . . . . . . . . . .                             
                                                                                    =============

                                                                                      3,250,000
</TABLE>

<PAGE>   1

                                                                     EXHIBIT 5.1



                             HOGAN & HARTSON L.L.P.
                            111 SOUTH CALVERT STREET
                           BALTIMORE, MARYLAND  21202





                                 April 7, 1997



Board of Directors
Guilford Pharmaceuticals Inc.
6611 Tributary Street
Baltimore, Maryland  21224



Ladies and Gentlemen:

                 We are acting as counsel to Guilford Pharmaceuticals Inc., a
Delaware corporation (the "COMPANY"), in connection with its registration
statement on Form S-3, as amended (the "REGISTRATION STATEMENT") filed with the
Securities and Exchange Commission relating to the proposed public offering of
up to 3,737,500 shares of the Company's common stock, par value $.01 per share,
all of which shares (the "SHARES") are to be sold by the Company.  This opinion
letter is furnished to you at your request to enable you to fulfill the
requirements of Item 601(b)(5) of Regulation S-K, 17 C.F.R. Section
229.601(b)(5), in connection with the Registration Statement.

                 For purposes of this opinion letter, we have examined copies
of the following documents:

                 1.       An executed copy of the Registration Statement.

                 2.       The Amended and Restated Certificate of Incorporation
                          of the Company, as amended (the "Charter"), as
                          certified by the Secretary of the State of the State
                          of Delaware on April 7, 1997 and by the Secretary of
                          the Company on the date hereof as then being
                          complete, accurate and in effect.

                 3.       The Bylaws of the Company, as certified by the
                          Secretary of the Company on the date hereof as then
                          being complete, accurate and in effect.
<PAGE>   2
                 4.       The proposed form of Underwriting Agreement among the
                          Company and the several Underwriters to be named
                          therein, for whom Oppenheimer & Co., Inc., Alex.
                          Brown & Sons Incorporated and Hambrecht & Quist LLC
                          will act as representatives, filed as Exhibit 1.01 to
                          the Registration Statement (the "UNDERWRITING
                          AGREEMENT").

                 5.       Resolutions of the Board of Directors of the Company
                          adopted on February 18, 1997, as certified by the
                          Secretary of the Company on the date hereof as then
                          being complete, accurate and in effect, relating to
                          the issuance and sale of the Shares and arrangements
                          in connection therewith.

                 6.       A certificate of certain officers of the Company,
                          dated the date hereof, as to certain facts relating
                          to the Company.

                 In our examination of the aforesaid documents, we have assumed
the genuineness of all signatures, the legal capacity of natural persons, the
authenticity, accuracy and completeness of all documents submitted to us, and
the conformity with the original documents of all documents submitted to us as
certified, telecopied, photostatic, or reproduced copies.  This opinion letter
is given, and all statements herein are made, in the context of the foregoing.

                 This opinion letter is based as to matters of law solely on
the General Corporation Law of the State of Delaware.  We express no opinion
herein as to any other laws, statutes, regulations, or ordinances.

                 Based upon, subject to and limited by the foregoing, we are of
the opinion that following (i) final action of the Pricing Committee of the
Board of Directors of the Company approving the price of the Shares, (ii)
execution and delivery by the Company of the Underwriting Agreement, (iii)
effectiveness of the Registration Statement, (iv) issuance of the Shares
pursuant to the terms of the Underwriting Agreement and (v) receipt by the
Company of the consideration for the Shares specified in the resolutions of the
Board of Directors and the Pricing Committee referred to above, the Shares will
be validly issued, fully paid and nonassessable under the General Corporation
Law of the State of Delaware.

                 We assume no obligation to advise you of any changes in the
foregoing subsequent to the delivery of this opinion letter.  This opinion
letter has been prepared solely for your use in connection with the filing of
the Registration Statement on the date of this opinion letter and should not be
quoted in whole or in part or otherwise be referred to, nor filed with or
furnished to any governmental agency or other person or entity, without the
prior written consent of this firm.

                 We hereby consent to the filing of this opinion letter as
Exhibit 5.01 to the Registration Statement and to the reference to this firm
under the caption
<PAGE>   3
"Legal Matters" in the prospectus constituting a part of the Registration
Statement.  In giving this consent, we do not thereby admit that we are an
"expert" within the meaning of the Securities Act of 1933, as amended.


                                                Very truly yours,



                                                HOGAN & HARTSON L.L.P.


<PAGE>   1
                                                                  EXHIBIT 23.02


                         INDEPENDENT AUDITORS' CONSENT




The Board of Directors of
  Guilford Pharmaceuticals, Inc.:


        We consent to the use of our report included herein and to the
reference to our firm under the headings "Selected Consolidated Financial Data"
and "Experts" in the prospectus.
                                                    

                                                    /s/ KPMG Peat Marwick LLP
Baltimore, Maryland                                 KPMG Peat Marwick LLP
April 7, 1997


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