Description
Indinavir is an HIV-1 protease inhibitor (K
i = 0.358 nM). It is selective for HIV-1 protease over HIV-2 protease (K
i = 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 (K
is = 0.24, 15, 50, and 40 nM, respectively). Indinavir is active against multiple HIV-1 variants in cell-based assays (IC
95s = 12-100 nM). Formulations containing indinavir have been used in combination with antiretroviral agents in the treatment of HIV infection.
References
[1] J P VACCA. L-735,524: an orally bioavailable human immunodeficiency virus type 1 protease inhibitor.[J]. Proceedings of the National Academy of Sciences of the United States of America, 1994, 91 9: 4096-4100. DOI:
10.1073/pnas.91.9.4096[2] BRUCE D. DORSEY. Identification of MK-944a: A Second Clinical Candidate from the Hydroxylaminepentanamide Isostere Series of HIV Protease Inhibitors[J]. Journal of Medicinal Chemistry, 2000, 43 18: 3386-3399. DOI:
10.1021/jm9903848
