Protease inhibitor update. Clearinghouse, P.O. Box 6003, Rockville, MD 20849-6003. 800-458-5231 ext. 5023. NLM AIDSLINE Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.

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Protease inhibitor update. Clearinghouse, P.O. Box 6003, Rockville, MD 20849-6003. 800-458-5231 ext. 5023.

Common Factor. 1995 Apr;(no 10):15. Unique Identifier : AIDSLINE AIDS/95700368
Colvin R; Haas G

Abstract: New clinical trial developments surrounding anti-HIV compounds, known as protease inhibitors, are discussed for the following drugs: Merck (MK-639), Searle (SC512151), Abbott (ABT-538), Hoffman LaRoche (Saquinavir), Agouron (AG-1343), and Vertex (VX-478). Merck's MK-639 shows marked reductions of HIV in blood, but resistance appears after six months. Side effects have been minimal, the most severe of which is the brief appearance of hyperbilirubinemia. Searle is stopping clinical development of SC512151 because of the drug's lack of anti-viral effect. Preliminary clinical data on Abbott's ABT-538 are promising, based on trials showing rises in CD4 counts, and evidence of very good bioavailability compared with other protease inhibitors. Saquinavir, the longest tested protease inhibitor, shows an ability to cause a two-fold reduction in HIV RNA plasma levels. Supplies of saquinavir are low. Roche intends to apply for accelerated approval of saquinavir in 1995. AG-1343 and VX-478 are just starting clinical trials, however, preclinical trials of AG-1343 show excellent bioavailability and pharmacokinetics.
Keywords: Clinical Trials CD4 Lymphocyte Count Drug Resistance, Microbial Human HIV/DRUG EFFECTS HIV Infections/DRUG THERAPY HIV Protease Inhibitors/PHARMACOLOGY/*THERAPEUTIC USE NEWSLETTER ARTICLE

KWDclinicaltrialscd4lymphocytecountdrugresistance,microbialhumanhiv/drugeffectshivinfections/drugtherapyhivproteaseinhibitors/pharmacology/KWDtherapeuticusenewsletterarticle
951130
M95B0898

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