Lersivirine

Lersivirine is a non-nucleoside, next generation reverse transcriptase inhibitor (IC50 = 118 nM for the wild-type HIV-1 enzyme). It inhibits a panel of 14 single-point mutant HIV-1 reverse transcriptases with mean IC50 values within 10-fold of the wild-type enzyme. Lersivirine inhibits HIV-1 virus replication in MT-2 cells with EC50 values of 5.04, 13.1, and 34.9 nM at multiplicities of infection (MOIs) of 0.005, 0.05, and 0.5, respectively, and displays synergistic or additive effects when used in combination with a variety of antiretroviral agents.