Dapivirine

Dapivirine (TMC120) is a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM, inhibits a broad panel of HIV-1 isolates from different classes, inclucing a wide range of NNRTI-resistant isolates. Phase 3. (In Vitro) :Dapivirine (4-64 μM, 24, 48, 72, 96 and 120 hours) inhibits proliferation of glioma cells and induces apoptosis (16 μM, 12-48 h) .Dapivirine (8 and 16 μM, 12 h) enhances invasion of glioma cells.Dapivirine (16 μM, 12 h, 24 h and 48 h) promotes autophagy in U87 cells.Dapivirine (TMC120-R147681) apparently blocks infection in the primary cultures at a 10 nM concentration, but secondary cultures revealed that a 100 nM concentration was needed to completely prevent proviral integration. (In Vivo) :Dapivirine (16 mg/kg, once every 3 days for 12 days) exhibits potent antitumor activity in human glioblastoma models in mice.Dapivirine has been shown to have a half-life in the range of 65 to 90 h.