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Updated: Jun 26, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
[Pharmacokinetics, interactions and mechanism of action of maraviroc]
1Departamento de Enfermedades infecciosas, Hospital Carlos III, Madrid, España. vsoriano@dragonet.es
Abstract:
Maraviroc (MVC, Celsentri) is an allosteric and reversible inhibitor of the CCR5 chemokine coreceptor. MVC is the first marketed CCR5 antagonist and the only oral entry inhibitor approved so far for the treatment of HIV infection. It has been approved for adults with previous antiretroviral exposure. MVC exclusively inhibits the replication of R5- tropic HIV-1 variants after binding to the transmembrane CCR5 receptor cavity. MVC is rapidly absorbed following oral administration, and plasma T(max) is achieved within 0.5- 4 hours after a 300 mg dose. Renal clearance is approximately 10-12 L/h. MVC is a substrate of the cytochrome P450 isoenzyme 3A4; therefore dose adjustments are required when co-administrated with other drugs that induce or inhibit CYP3A4. In addition, MVC dose adjustments are advised in patients with renal failure (CLcr <80 ml/min) only if they receive CYP3A4 inhibitors.
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