Indinavir is an HIV-1 protease inhibitor (Ki = 0.358 nM). It is selective for HIV-1 protease over HIV-2 protease (Ki = 3.316 nM), as well as human cathepsin D, porcine pepsin, bovine chymosin, human plasma renin, Factor Xa, and elastase at 10 μM. It is also selective for wild-type HIV-1 protease over the protease inhibitor-resistant mutants A-44, K-60, and V-18 (Kis = 0.24, 15, 50, and 40 nM, respectively). Indinavir is active against multiple HIV-1 variants in cell-based assays (IC95s = 12-100 nM). Formulations containing indinavir have been used in combination with antiretroviral agents in the treatment of HIV infection.
