Agouron Pharmaceuticals Inc. announced Tuesday that it hasidentified a novel class of orally bioavailable HIV proteaseinhibitors whose preclinical performance "appears to equal orto exceed" that of "any HIV protease inhibitor yet reported byothers working in this field."
Agouron (NASDAQ:AGPH) scientist Krzysztof Appelt describedthe chemical structure of the compounds at the InterscienceConference on Antimicrobial Agents and Chemotherapy(ICAAC) in New Orleans. One of the compounds, designatedAG1284, inactivated the protease enzyme in vitro "with apotency equivalent to that of the most potent inhibitors of HIVprotease previously reported," the company said.
Agouron of La Jolla, Calif., added that in preclinical in vivoexperiments, oral administration of AG1284 resulted in plasmalevels of the compound several-fold higher than the minimumconcentration required for in vitro anti-HIV activity of thecompound.
An Agouron representative said one or two of the proteasecompounds may enter clinicals next year. Of other companiesdeveloping protease inhibitors, Hoffmann-La Roche is thefurthest along, with a compound in clinicals. -- BrendaSandburg
(c) 1997 American Health Consultants. All rights reserved.