Cenicriviroc is a potent inhibitor of C-C chemokine receptors CCR5 and CCR2. It is an orally bioavailable derivative of TAK-779 with potent anti-HIV-1 activity. It blocks the binding of MIP-1α and MIP-1β to CCR5 with an IC₅₀ of 2.3 nM. It inhibits the binding of MCP-1 to CCR2b with an IC₅₀ of 5.9 nM. It inhibits the replication of R5X4HIV-1 in U87.CD4.CCR5 cells at a concentration of 100 nM. It shows potent anti-inflammatory and antifibrotic activity in animal models of fibrosis.