Etravirine (TMC125)

Modify Date: 2024-01-03 08:11:25

Use of Etravirine (TMC125)

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

Name	etravirine
Synonym	More Synonyms

Description	Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used for the treatment of HIV.
Related Catalog	Signaling Pathways >> Anti-infection >> HIV Signaling Pathways >> Anti-infection >> Reverse Transcriptase Research Areas >> Infection
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].
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.

Hazard Codes	Xi

Benzonitrile, 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-

etravirine

4-({6-Amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl}oxy)-3,5-dimethylbenzonitrile

tmc 125

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Price: $166/10mM*1mLinDMSO

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