vicriviroc

Vicriviroc is an investigational small molecule, orally administered CCR5 receptor antagonist developed for the treatment of HIV-1 infection. It acts as a noncompetitive allosteric antagonist by binding to a hydrophobic pocket between the transmembrane helices near the extracellular surface of the C-C chemokine receptor type 5 (CCR5) receptor, inducing a conformational change that prevents HIV gp120 from binding and thus blocks viral entry into CD4+ cells. Vicriviroc is effective at nanomolar concentrations and was designed to be dosed once daily. It demonstrated potent activity against genetically diverse and drug-resistant R5-tropic HIV isolates in preclinical and clinical studies, with favorable pharmacokinetics and minimal drug interactions. The drug was developed by Schering-Plough but its development for HIV has been discontinued after Phase III trials[1][3][4][5][7].

Other names

vicriviroc [INN]306296-47-9