TMC310911 is a potent and orally active HIV type-1 (HIV-1) protease inhibitor with EC 50 values ranged from 2.2 nM to 14.2 nM for wild-type HIV-1 . TMC310911 has potent activity against a wide spectrum of recombinant HIV-1 isolates. TMC310911 has strong antiviral activity
In Vitro
For a panel of 2,011 recombinant isolates with decreased susceptibility to at least one of the currently approved protease inhibitors (PIs), the FC in TMC310911 EC 50 is ≤4 for 82% of isolates and ≤10 for 96% of isolates. The fold change (FC) in TMC310911 EC 50 is ≤4 and ≤10 for 72% and 94% of isolates with decreased susceptibility to Darunavir, respectively. In vitro resistance selection (IVRS) performed with r13025, a multiple-PI-resistant recombinant isolate, and TMC310911 selected for mutations L10F, I47V, and L90M (FC in TMC310911 EC 50 = 16). The TMC310911 EC 50 values against HIV-1/LAI and HIV-2/ROD in MT4 cells with EC 50 values of 14.2 nM and 2 nM, respectively, and HIV-1/LAI and HIV-1/SF2 in PBMCs with EC 50 values of 2.2 nM and 2.3 nM, respectively, and HIV-1/BaL in M/M cells with an EC 50 value of 13.9 nM. And the corresponding EC 90 values ranged from 5.0 to 94.7 nM. The TMC310911 CC 50 for MT4 cells is 9.9 μM. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
