Abstract
This article provides an up-to-date review of the development of various peptidomimetic and non-peptidic inhibitors of HIV-1 protease. The antiviral and pharmacokinetic properties of these potential therapeutic compounds are presented along with their status in clinical evaluation. For selected inhibitors, clinical efficacy and the emergence of drug resistant mutants both in vitro and in vivo are also described. The emergence of drug-resistance may be reduced by using multiple drugs in combination. Accordingly, this report also includes information on in vitro drug synergy and combination trials between the protease inhibitors and various HIV-1 reverse transcriptase inhibitors.
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