Emivirine (MKC-442) is a potent and selective nonnucleoside reverse transcriptase inhibitor for human immunodeficiency virus type 1.

RNA polymerase activity (dGTP-dependent):0.01μM(ki), DNA polymerase activity (dTTP-dependent):0.20μM(ki)

Emivirine is a novel nonnucleoside reverse transcriptase inhibitor that displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity in vivo. IC50 against laboratory-adapted strains of HIV-1 ranged from 1.6 to 19 nM. Against clinical isolates, the IC50 for EMV ranged from 2 to 40 nM. The Ki values of 0.20 and 0.01 μM for dTTP- and dGTP-dependent DNA or RNA polymerase activity, respectively[1].

Emivirine displays potent and selective anti-human immunodeficiency virus type 1 (HIV-1) activity in vivo. Pharmacokinetics were linear for both rats and monkeys, and oral absorption was 68% in rats. Rats were given an oral dose of Emivirine at 10 mg/kg of body weight showed widespread distribution in tissue after 30 min. In rats given an oral dose of 250 mg/kg, there were equal levels of Emivirine in the plasma and the brain[2].