Doravirine

Doravirine (CAS No.: 1338225-97-0) is a non-nucleoside reverse transcriptase inhibitor (NNRTI) used to treat human immunodeficiency virus type 1 (HIV-1) infection. Its primary target is HIV-1 reverse transcriptase; by inhibiting the activity of this enzyme, it blocks the reverse transcription of viral RNA into DNA, thereby inhibiting viral replication. In vitro studies show that Doravirine has an IC50 of approximately 12 nM against wild-type HIV-1 strains, and IC50 values of 21, 31, and 33 nM against strains carrying the K103N, Y181C, and K103N/Y181C mutations, respectively, indicating that it retains strong antiviral activity against multiple drug-resistant mutant strains. In cell models, Doravirine exhibits similar antiviral activity against multiple HIV-1 subtypes and shows no cytotoxicity at concentrations up to 100 μM. In animal model studies, pharmacokinetic parameters in rats and dogs indicate good bioavailability and a moderate half-life, supporting its development as an oral anti-HIV drug. In drug screening studies, Doravirine is often used to evaluate the efficacy and resistance of novel anti-HIV drugs, and the doses or concentrations used in experiments typically depend on the experimental design and research objectives.