Maraviroc: A Coreceptor CCR5 Antagonist for Management of HIV Infection

Raymond Yost; Timothy R. Pasquale; Eric G. Sahloff

Disclosures

Am J Health Syst Pharm. 2009;66(8):715-726. 

In This Article

Chemistry

Maraviroc is a small-molecule CCR5-ligand and an analogue of UK-107,453, a potent imidazopyridine ligand-efficient lead compound.[3] In in vitro studies, maraviroc inhibited CCR5 signaling and chemokine-dependent stimulation, had no effect on intracellular calcium concentrations, and did not lead to CCR5 internalization. Based on these findings, maraviroc was determined to have no agonistic activity and is an antagonist, either functional or inverse, of the CCR5 receptor.[3]

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