Mozenavir

Mozenavir (DMP-450) is an orally active cyclic urea HIV-1 protease inhibitor with an IC₅₀ of 76 nM. Mozenavir inhibits replication by targeting viral protease, blocks viral polyprotein processing, and induces the production of core-uncondensed, immature, non-infectious viral particles in chronically infected cells. Mozenavir is applicable to research related to HIV infection^[1]. In Vitro:Mozenavir (DMP-450) potently and selectively inhibits purified HIV-1 protease, with a K_i of 0.28 nM against peptide substrates and an IC₅₀ of 76 nM against Gag polyprotein substrates^[1].
Mozenavir potently inhibits the replication of wild-type and mutant HIV strains in MT-2, Molt-4, PBMC and U937 cells, with a mean IC₉₀ of 144 nM. It also induces the production of immature viral particles, and exhibits low cytotoxicity in MT-2 cells (TC₅₀ > 80 μM)^[1].
Mozenavir shows reduced potency against single-mutant HIV strains (with a 2.8- to 7-fold increase in IC₉₀), and significantly reduced potency against double-mutant and in vitro-selected multi-mutant HIV strains (with a maximum 100-fold increase in IC₉₀)^[1]. In Vivo:Mozenavir (DMP-450) (10 μg-100 mg/kg; i.m., p.o.; single dose per quadriceps muscle, twice daily; 2 days) completely protects against HIV protease-mediated loss of luciferase signal in mouse skeletal muscle^[1].