Maraviroc (MVC, UK-427,857) is the first member of a new class, the CCR5 antagonists. By an original mechanism of action, maraviroc binds to the CCR5 receptor in order to prevent HIV from binding and entering human cells. Maraviroc (Celsentri) is an orally administered drug available as 150 and 300 mg film-coated tablets. The current approved daily dosage of maraviroc is 300 mg bid in combination with other antiretroviral medications. Maraviroc plasma exposure is not dose proportional. After a rapid (but moderate) intestinal absorption, several inactive oxidized metabolites are produced via cytochrome P450 3A4 pathway. According to this liver metabolism, dosage adjustments are required when maraviroc is administered in combination with cytochrome P450 inhibitors or inducers. The potential for drug-drug interactions and the well-defined relationship between plasma concentrations and virological response suggest the usefulness of Therapeutic Drug Monitoring of maraviroc in HIV-infected patients.
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