An HIV-1 protease inhibitor
Indinavir is an HIV-1 protease inhibitor (Ki = 0.358 nM).1 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).2 Indinavir is active against multiple HIV-1 variants in cell-based assays (IC95s = 12-100 nM).1 Formulations containing indinavir have been used in combination with antiretroviral agents in the treatment of HIV infection.
1.Vacca, J.P., Dorsey, B.D., Schleif, W.A., et al.L-735,524: An orally bioavailable human immunodeficiency virus type 1 protease inhibitorProc. Natl. Acad. Sci. USA91(9)4096-4100(1994) 2.Dorsey, B.D., McDonough, C., McDaniel, S.L., et al.Identification of MK-944a: A second clinical candidate from the hydroxylaminepentanamide isostere series of HIV protease inhibitorsJ. Med. Chem.43(18)3386-3399(2000)
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