LA JOLLA, Calif. and NUTLEY, N.J. Sept. 26 /PRNewswire/ -- Agouron
Pharmaceuticals, Inc., (Nasdaq-NNM: AGPH) and Hoffmann-La Roche Inc. (Roche)
today announced they have initiated human clinical trials of an anti-cancer
MMP inhibitor designated AG3340.  In phase I clinical studies to be conducted
at Inveresk Research in Edinburgh, Scotland, the safety and pharmacokinetic
parameters of single and multiple oral doses of AG3340 will be evaluated in
healthy volunteers in order to determine an optimal dose and schedule for
administration of the drug in subsequent efficacy studies.
    AG3340 is a small, synthetic molecule designed to selectively inactivate
certain members of a family of enzymes known as matrix metalloproteases
(MMPs).  Some MMPs, such as gelatinases, stromelysins and collagenase-3, are
believed to play key roles in the invasion, metastasis and growth of many
malignant tumors.  Other MMPs, such as matrilysin and interstitial
collagenase, are believed to be involved in normal adult biological processes,
including collagen turnover and endometrial cycling.  Unlike MMP inhibitors
currently being developed by some other groups, AG3340 selectively inhibits
those MMPs believed to be required for tumor progression, but is relatively
inactive against other MMPs involved in normal biological processes.  A
primary goal of clinical studies of AG3340 is to determine whether its
distinctive selectivity results in a uniquely favorable profile of safety and
efficacy.
    In preclinical studies, AG3340 demonstrated significant anti-tumor and
anti-metastatic activity against several murine and human tumors growing in
laboratory animals.  In these studies, AG3340 proved active when administered
either orally or intraperitoneally.  A full panel of preclinical toxicology
studies showed AG3340 to be well tolerated and acceptable for human clinical
testing.
    AG3340 was originally designed by Agouron in collaboration with scientists
from Syntex (U.S.A.) Inc., now a member of the Roche Group.  AG3340 is
currently being developed by Agouron in collaboration with Roche.  Under terms
of the collaboration, Roche will bear 80% of development costs of AG3340 and
will lead commercialization of the drug outside of North America subject to
payment of royalties to Agouron.  Roche and Agouron will co-promote AG3340 in
North America and will share equally in profits derived from North American
sales of the drug.
    Headquartered in Nutley, N.J., Hoffmann-La Roche Inc. is an affiliate of
the multinational group of companies headed by Roche Holding Ltd. of Basel,
Switzerland.  One of the world's leading research-intensive health care
companies, Roche has discovered, developed and introduced numerous important
prescription pharmaceuticals.
    Agouron Pharmaceuticals, Inc. is a pioneer and leader in the development
and application of technologies that enable the atom by atom design of novel
synthetic drugs based upon the molecular structures of target proteins which
play key roles in human disease.  Agouron is currently applying these
technologies to the design and development of novel drugs for treatment of
cancer, AIDS and other serious diseases.

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