NCIt definition : 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.;