LA JOLLA, Calif., Feb. 1 /PRNewswire/ -- Agouron Pharmaceuticals, Inc.
(Nasdaq: AGPH) today reported potent in vitro antiviral activity against both
wild-type and resistant HIV strains for two investigational compounds being
developed by the company. Results will be presented by scientists this week
at the 6th Conference on Retroviruses and Opportunistic Infections in Chicago,
Illinois.
AG1549, A Novel Non-nucleoside Reverse Transcriptase Inhibitor (NNRTI)
Development of HIV-1 strains resistant to inhibitors of reverse
transcriptase makes the development of new agents in this class of compounds
imperative. AG1549 (formerly S-1153), a non-nucleoside reverse transcriptase
inhibitor (NNRTI), exhibits potent in vitro antiviral activity against
clinical isolates and HIV strains resistant to available RT inhibitors, with
EC(50) values ranging from 2.2 to 10.3 nM in cell-based assays. The in vitro
resistance profile was evaluated against a panel of recombinant HIV-1 strains
known to contain mutations conferring resistance to other NNRTIs, and
recombinant virus strains generated from clinical isolates. In contrast to
other commercially available NNRTIs, AG1549 exhibited significant potency
against NNRTI-resistant variants, including those that contain single and
multiple NNRTI mutations. These data indicate that AG1549 holds promise for
potential use against both wild-type and NNRTI-resistant HIV-1 strains.
Phase I/II trials are in progress. Agouron obtained exclusive rights in
July 1998 to the development and commercialization of AG1549 in North America,
Europe and many other countries. Shionogi & Co., Ltd. maintains rights to
commercialization in Japan, Korea, and Taiwan.
AG1776, A Novel HIV Protease Inhibitor
The emergence of HIV strains cross-resistant to protease inhibitors has
been associated with poor response to antiretroviral salvage regimens. AG1776
(formerly JE-2147), a potent inhibitor of HIV-1 protease, has demonstrated a
mean EC(50) of 47.6 nM against HIV-1 and HIV-2 laboratory strains and clinical
isolates in cell-based assays. The in vitro resistance profile was evaluated
against clinical isolates or recombinant viruses generated from plasma HIV-1
RNA samples from patients who had failed regimens containing indinavir,
ritonavir, saquinavir, and/or nelfinavir. Recombinant viruses containing key
protease mutations exhibited significant phenotypic resistance to all HIV
protease inhibitors tested, but remained fully susceptible to AG1776. These
data indicate that AG1776 holds promise for potential use as part of a
therapeutic regimen in antiretroviral therapy naive as well as protease
inhibitor-experienced patients.
Agouron obtained exclusive rights in July 1998 to the development and
commercialization of AG1776 in North America, Europe and many other countries.
Japan Energy Corporation will supply compound for development and maintains
rights to commercialization in Japan, Korea, and Taiwan.
Agouron Pharmaceuticals, Inc. is an integrated pharmaceutical company
committed to discovery, development, manufacturing, and marketing of
small-molecule drugs engineered to inactivate proteins that play key roles in
cancer, AIDS, and other serious diseases.
For further information about Agouron Pharmaceuticals, Inc., please see
Agouron's website at http://www.agouron.com.
SOURCE Agouron Pharmaceuticals, Inc.
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CONTACT:
Investors: Donna Nichols, Vice President,
Head of Corporate Communications, 619-622-3009, or Media: Joy
Schmitt, Associate Director, Product Public Relations,
619-622-3220, both of Agouron Pharmaceuticals, Inc.
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