Maraviroc (DB04835): A Comprehensive Monograph on a First-in-Class CCR5 Antagonist from HIV-1 Therapy to Broad-Spectrum Immunomodulation

1.0 Executive Summary

Maraviroc (DrugBank ID: DB04835) represents a significant milestone in the history of antiretroviral therapy (ART). As the first orally bioavailable small molecule antagonist of the C-C chemokine receptor type 5 (CCR5), its approval marked the introduction of a new class of HIV medications in over a decade.[1] Developed by Pfizer and marketed under the brand names Selzentry and Celsentri, Maraviroc introduced a novel mechanism of action that fundamentally differs from preceding antiretroviral agents. Instead of inhibiting viral enzymes once HIV has already infected a host cell, Maraviroc functions as an entry inhibitor, blocking the virus at the cell surface before infection can occur.[3]

The drug's primary clinical indication is for the treatment of human immunodeficiency virus type 1 (HIV-1) infection, but its use is highly specific. It is effective only against viral strains that utilize the CCR5 co-receptor for cellular entry, known as CCR5-tropic (or R5) virus.[1] This mechanistic specificity necessitates pre-treatment viral tropism testing, positioning Maraviroc as an early example of personalized medicine in infectious disease management.[6] Its clinical utility is most established in treatment-experienced patients with multidrug-resistant HIV, for whom it provides a new therapeutic option with no cross-resistance to other drug classes.[2]