Vicriviroc (CAS: 599179-03-0 (maleate)) is a potent, orally active and selective CCR5 entry inhibitor of HIV-1. Vicriviroc is effective at nanomolar concentrations, it can be administered once daily. Vicriviroc binds to a small hydrophobic pocket between the transmembrane helices near the extracellular surface of the CCR5 receptor. Binding to this pocket induces a conformational change of the extracellular segment of CCR5 and prevents binding of gp120 to the target cell, consequently preventing the virus from entering the target cell at all.
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