Emivirine (MKC-442) is a non-nucleoside reverse transcriptase inhibitors (NNRTIs) with Ki values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively. Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity[1][2].
Emivirine (EMV) is also specific for HIV-1 RT and was without effect on HIV-2[2].Emivirine (EMV) has no obvious toxicity for human healthy cells[2].
Tthe approximate lethal oral dose of Emivirine (EMV) for rats was ≥3 g/kg for males and 2.5 g/kg for females[2].
[1]. Panita Decha, et al. Theoretical studies on the molecular basis of HIV-1RT/NNRTIs interactions. J Enzyme Inhib Med Chem. 2011 Feb;26(1):29-36.
[2]. G M Szczech, et al. Safety assessment, in vitro and in vivo, and pharmacokinetics of emivirine, a potent and selective nonnucleoside reverse transcriptase inhibitor of human immunodeficiency virus type 1. Antimicrob Agents Chemother. 2000 Jan;44(1):123-30.