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Etravirine

CAS No. : 269055-15-4

MCE 國際站：Etravirine

產(chǎn)品活性：Etravirine 是一種非核苷逆轉(zhuǎn)錄酶抑制劑 (NNRTI)，具有抗 HIV 的作用。

研究領(lǐng)域：Anti-infection

作用靶點(diǎn)：Reverse Transcriptase  |  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.

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.

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