Etravirine (TMC125) (Synonyms: R165335, TMC125) |
| Catalog No.GC15996 |
Etravirine(TMC125)은 HIV 치료에 사용되는 비뉴클레오시드 역전사효소 억제제(NNRTI)입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 269055-15-4
Sample solution is provided at 25 µL, 10mM.
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Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
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].
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].
References:
[1]. Andries, K., et al. TMC125, a novel next-generation nonnucleoside reverse transcriptase inhibitor active against nonnucleoside reverse transcriptase inhibitor-resistant human immunodeficiency virus type 1. Antimicrob Agents Chemother, 2004. 48(12): p. 468
[2]. Lazzarin, A., et al. Efficacy and safety of TMC125 (etravirine) in treatment-experienced HIV-1-infected patients in DUET-2: 24-week results from a randomised, double-blind, placebo-controlled trial. Lancet, 2007. 370(9581): p. 39-48.
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