Protease developers skirmish over possible pitfalls. Clearinghouse, P.O. Box 6003, Rockville, MD 20849-6003. 800-458-5231 ext. 5023.

Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.

Protease developers skirmish over possible pitfalls. Clearinghouse, P.O. Box 6003, Rockville, MD 20849-6003. 800-458-5231 ext. 5023.

J Int Assoc Physicians AIDS Care. 1995 Mar;1(2):13-6. Unique Identifier : AIDSLINE AIDS/95700333
Mascolini M

Abstract: Protease inhibitors were the dominating topic at the Second National Conference on Human Retroviruses and Related Infections, held January 29 through February 2, 1995. Currently, seventeen protease inhibitors are in development, most falling into three categories: C2 symmetrics, transition state analogs, and cyclic ureas. Dr. Martin Markowitz, of the Aaron Diamond AIDS Research Center, believes that combination therapies may be possible with protease inhibitors now in clinical trials. Unfortunately, there is some concern, based on Searle's SC-52151 inability to penetrate cellular targets, that alpha1 A-glycoprotein binding problems could haunt the development of protease compounds. Another potential problem overshadowing efforts in protease inhibitor development is resistance. While long-term resistance is of some concern, Markowitz suggests that stringing a steady combination of protease inhibitors could keep the virus permanently subdued. No consensus exists on which of two HIV therapies (high dose monotherapy or drug combinations) is best to pursue. It is believed resistance would be less likely with a combination of antivirals, but, as Dr. Noel Roberts of Hoffman-La Roche contends, resistance is inevitable and agents should be taken as long as they are effective. So far, saquinavir leads the pack in successfully advancing through the phase studies. Abbott's ABT-538 and Merck's L-524 are also showing beneficial effects on viral load. Both companies are pursuing aggressive trial strategies.

Keywords: Acquired Immunodeficiency Syndrome/BLOOD/*DRUG THERAPY/VIROLOGY CD4 Lymphocyte Count Drug Design Drug Industry Drug Resistance Human HIV Protease Inhibitors/CHEMICAL SYNTHESIS/*THERAPEUTIC USE Multicenter Studies Protein Binding Viremia NEWSLETTER ARTICLE

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M95B0922

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