Agouron Pharmaceuticals Inc. of LaJolla joins the list of companies that are developing a new class of orally bioavailable anti-HIV compounds known as protease inhibitors. In a presentation to the Interscience Conference on Antimicrobial Agents and Chemotherapy, Agouron revealed the chemical structure of a novel class of HIV protease inhibitors with unique binding interactions with the protease enzyme. The lead clinical candidate, a compound designated AG-1284, inactivated the protease enzyme with a potency equivalent to that of the most potent inhibitors of HIV protease previously reported in the scientific literature. Pharmacokinetic studies have demonstrated good oral bioavailability, and, more importantly, the doses of Agouron's compounds necessary to kill normal cells are 75 to 2,350 times higher than the doses necessary to inhibit HIV replication. Studies of AG-1284's ability to penetrate tissues are now underway, and animal toxicology studies are also planned.
Agouron is aggressively focusing on process development and scale-up activities in order to produce AG-1284 in a quick and cost-effective way. The company is optimistic that AG-1284 may begin human clinical trials in the last quarter of this year.
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