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  • An orally bioavailable, dual inhibitor of human C-C chemokine receptor types 2 (CCR2; CD192) and 5 (CCR5; CD195), with potential immunomodulating, anti-inflammatory and antiviral activities. Upon oral administration, cenicriviroc specifically binds to and prevents the activation of both CCR2 and CCR5. This inhibits the activation of CCR2/CCR5-mediated signal transduction pathways and may inhibit inflammatory processes. The G-protein coupled chemokine receptors CCR2 and CCR5 are expressed on the surface of monocytes and macrophages and stimulate their migration and infiltration; they play key roles in inflammation and autoimmune diseases. In addition, cenicriviroc inhibits human immunodeficiency virus (HIV)-1 entry via CCR5 coreceptor interaction.
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