Abstract:
Protease inhibitors block HIV by binding with its protease enzyme and it is hoped that they will be more potent and less toxic than nucleoside analogs. The companies Hoffmann-La Roche, Merck, Abbott, Searle, Agouron, Kyoto and Upjohn all have tested protease inhibitors in human trials. The drugs include L-524, ABT-538, AG- 1343, saquinavir, SC-52151, and SC-55389a. The protease inhibitors from Merck, Roche, and Abbott have shown higher anti-viral activity than any previous anti-HIV drug. Vertex, Burroughs Wellcome, and Kissei have conducted animal studies of VX-478, which shows promise in inhibiting the virus, with no toxicity. Other companies developing protease inhibitors include DuPont-Merck, Ciba-Geigy, Hoechst-Bayer, Nippon Mining, Parke-Davis, and Smith-Kline Beecham. Companies increasingly are combining protease inhibitors with nucleoside analogs, mainly AZT, in their large-scale efficacy studies in an effort to produce a strong and sustained anti-HIV effect. Potential cross-resistance to many of these compounds remains a major research issue. It is likely that at least one of the three leading companies in the field -- Merck, Abbott, or Roche -- will file for Food and Drug Administration approval in 1995. The National Drug Development Task Force is expected to announce the creation of a new task force on protease inhibitors.
Keywords: Animal Blood Proteins/METABOLISM Clinical Trials CD4 Lymphocyte Count/DRUG EFFECTS Drug Industry Drug Resistance Drug Therapy, Combination Human HIV Infections/BLOOD/*DRUG THERAPY/ENZYMOLOGY HIV Protease Inhibitors/METABOLISM/PHARMACOLOGY/*THERAPEUTIC USE Isoquinolines/ADMINISTRATION & DOSAGE/*THERAPEUTIC USE Oligopeptides/PHARMACOLOGY/THERAPEUTIC USE Protein Binding Pyrones/CHEMISTRY/PHARMACOLOGY/THERAPEUTIC USE Quinolines/ADMINISTRATION & DOSAGE/*THERAPEUTIC USE Rats Technology, Pharmaceutical Urea/ANALOGS & DERIVATIVES/METABOLISM/PHARMACOLOGY Warfarin/PHARMACOLOGY Zidovudine/ADMINISTRATION & DOSAGE/THERAPEUTIC USE NEWSLETTER ARTICLE 950530
M9551026
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Important note: Information in this article was accurate in 1995. The state of the art may have changed since the publication date.
