依曲韦林

依曲韦林是一种非核苷逆转录酶抑制剂 (NNRTI)，是一种用于治疗HIV的药物。 Etravirine (TMC125)是一种非核苷类逆转录酶抑制剂(NNRTI)，用于治疗HIV。 Etravirine (TMC125), is highly active against wild-type HIV-1 with EC50 of 1.4 nM to 4.8 nM and shows some activity against HIV-2 with EC50 of 3.5 μM. TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus. 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. Etravirine (TMC125, R-165335) 是一种非核苷类逆转录酶抑制剂(NNRTI)，用于治疗HIV。

Target	Value
Reverse transcriptase

Etravirine (TMC125)，对野生型HIV-1高度有效，EC50为1.4 nM到4.8 nM，对HIV-2也表现出一定的活性，EC50 为3.5 μM。TMC125也会抑制一系列HIV-1 M型亚基和循环重组形式以及O型病毒。

Etravirine对抗性发展具有高的基因屏障。在IIb期试验，多次治疗的患者中，包括感染耐NNRTIs和耐蛋白酶抑制剂(PIs)病毒的患者，TMC125对现有NNRTIs耐药的HIV具有活性，与对照组具有相似的耐受性。