Potent and selective CCR5 antagonist with potent anti-HIV activity. It prevents HIV-1 gp120 binding to CCR5 preventing cell-cell fusion. Maraviroc inhibited MIP-1a (IC50 = 3.3 nM), MIP-1b (IC50 = 7.2 nM), and RANTES (IC50 = 5.2 nM) binding to CCR5-expressing HEK-293.1 Clinically useful antiretroviral drug. Many cancer cells express CCR5: Maraviroc blocked metastasis of basal breast2 and pancreatic cancer3 cells, induced cytotoxic and apoptotic effects in colorectal cancer cells4, reduced metastatic tumor growth in lungs5, and suppresses growth in acute ALL cells6. CCR5 inhibition with maraviroc induced macrophage repolarization with anti-tumoral effects.7
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