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  • Title: The next wave of protease inhibitors.
    Author: Smart T.
    Journal: GMHC Treat Issues; 1995 Jun; 9(6):4. PubMed ID: 11362690.
    Abstract:
    Three new protease inhibitors stand out in light of cross-resistance, either because they achieve levels in the blood that may overwhelm low-level resistance, or because data suggest that they will not be cross-resistant with compounds in current clinical trials. Agouron has released information from its first patient (Patient 001) to a complete phase I study of its protease inhibitor, AG1343. After two weeks on the drug, the patient's HIV level dropped by 99 to 99.7 percent, and his CD4 count went up by 120. At 28 days, the patient's viral load was undetectable and his oral leukoplakia had resolved. Agouron will not comment on data from other patients, but has said that some responses were more modest than what was seen in patient 001, and they have yet to see resistance in people or any rebounds in viral loads. Searle's S338 first generation drug failed. The manufacturer will not discuss the status of its compound at this stage. Upjohn's protease inhibitors are small molecules and are easier to manufacture than most of the other protease inhibitors. Two of their compounds have failed in preliminary clinical studies, and the most recent compound was toxic to the liver. Upjohn hopes that a third, and more potent compound, will be in human studies soon.
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