Lersivirine

Lersivirine (UK-453061) is potent and selective non-nucleoside reverse transcription inhibitor (NNRTI; IC₅₀=119 nM) with excellent efficacy against NNRTI-resistant viruses. Lersivirine exhibits potent antiretroviral activity against wild-type HIV virus and clinically relevant NNRTI-resistant strains^[1]. IC50 & Target: IC50: 119 nM (NNRT)^[1] In Vitro: Lersivirine demonstrates excellent activity against large panels of wild type and drug-resistant HIV consistent with the encouraging profile demonstrated against the isolated RT enzymes^[1]. In Vivo: Lersivirine (oral gavage; 0, 150, 350, and 500 mg/kg; once daily; gestation days 6 to 17, followed by cesarean section on gestation day 18. ) allows induction of hepatic metabolizing enzymes at the first 2 days at 250 mg/kg, after which the dose is increased to 500 mg/kg/day in Mated Crl:CD1(ICR) mice. Lersivirine leads to skeletal variations which related to delayed development and decreased fetal ossifications^[1].