(±)-Efavirenz-d5 is intended for use as an internal standard for the quantification of efavirenz by GC- or LC-MS. Efavirenz is a non-nucleoside reverse transcriptase inhibitor (NNRTI) that binds to wild-type and mutant HIV-1 RTs (Kis = 2.93 and 3.85-56.5 nM, respectively).1 It inhibits wild-type and mutant HIV-1 viral replication in MT-4 human T lymphoid cells (IC95s = 1.5-1,500 nM). Efavirenz also prevents RNA plus-strand initiation with an IC50 value of 17 nM.2 In vivo, efavirenz reduces HIV-1 cDNA in spleen of HIV-1-challenged HIV-susceptible transgenic rats.3 Formulations containing efavirenz have been used in combination therapy for the treatment of HIV-1.4,5
1.Young, S.D., Britcher, S.F., Tran, L.O., et al.L-743,726 (DMP-266): A novel, highly potent nonnucleoside inhibitor of the human immunodeficiency virus type 1 reverse transcriptaseAntimicrob. Agents Chemother.39(12)2602-2605(1995) 2.Grobler, J.A., Dornadula, G., Rice, M.R., et al.HIV-1 reverse transcriptase plus-strand initiation exhibits preferential sensitivity to non-nucleoside reverse transcriptase inhibitors in vitroJ. Biol. Chem.282(11)8005-8010(2007) 3.Goffinet, C., Allespach, I., and Keppler, O.T.HIV-susceptible transgenic rats allow rapid preclinical testing of antiviral compounds targeting virus entry or reverse transcriptionProc. Natl. Acad. Sci. U.S.A.104(3)1015-1020(2007) 4.Sheran, M.The nonnucleoside reverse transcriptase inhibitors efavirenz and nevirapine in the treatment of HIVHIV Clin.Trials6(3)158-168(2005) 5.Rakhmanina, N.Y., and van den Anker, J.N.Efavirenz in the therapy of HIV infectionExpert Opin. Drug Metab. Toxicol.6(1)95-103(2010)