tcsc0435 Etravirine

Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.

In Vitro: TMC125 is highly active against wild-type HIV-1 (50% effective concentration [EC₅₀]=1.4 to 4.8 nM) and shows some activity against HIV-2 (EC₅₀=3.5 μM). TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus. TMC125 has activity for 19 viruses with EC₅₀ of < 5 nM^[1].

In Vivo: Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group^[2].