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 |
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Reverse transcriptase
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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。