Etravirine-d6 is intended for use as an internal standard for the quantification of etravirine by GC- or LC-MS. Etravirine is a non-nucleoside reverse transcriptase inhibitor (NNRTI).1 It is active against the wild-type HIV-1 strains LAI, SF2, and Ba-L (EC50s = 1.4-4.8 nM) but not the HIV-2 strain ROD (EC50 = 3,479 nM). Etravirine is also active against 18 HIV-1 strains carrrying NNRTI resistance-associated mutations (EC50s = <5 nM). Etravirine (5 μM) increases intracellular processing of the viral polyproteins Gag and Gag-Pol and decreases viral particle production in HEK293T cells transfected with a plasmid encoding the NL4.3 infectious molecular clone of HIV-1.2 Formulations containing etravirine have been used in the treatment of HIV-1 infection.
|1. Andries, K., Azijn, H., Thielemans, T., 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. 48(12), 4680-4686 (2004).|2. Figueiredo, A., Moore, K.L., Mak, J., et al. Potent nonnucleoside reverse transcriptase inhibitors target HIV-1 Gag-Pol. PLoS Pathog. 2(11), e119 (2006).