Cenicriviroc

Cenicriviroc (TAK-652) is an orally active, dual CCR2/CCR5 antagonist, also inhibits both HIV-1 and HIV-2, and displays potent anti-inflammatory and antiinfective activity^[1]. In Vitro: Cenicriviroc prevents human immunodeficiency virus type 1 (HIV-1) from cellular entry^[2]. Regarding the 4 R5 HIV-2 clinical isolates tested, effective concentration 50% EC₅₀?for cenicriviroc are 0.03, 0.33, 0.45 and 0.98 nM. The dual-tropic and the X4-tropic HIV-2 strains are resistant to cenicriviroc with EC₅₀ at >1000 nM, and MPI at 33% and 4%, respectively^[3]. In Vivo: Cenicriviroc (≥20 mg/kg/day) significantly reduces monocyte/macrophage recruitment in vivo. At these doses, cenicriviroc shows antifibrotic effects, with significant reductions in collagen deposition, and collagen type 1 protein and mRNA expression across the three animal models of fibrosis. In the NASH model, cenicriviroc significantly reduces the non-alcoholic fatty liver disease activity score. Cenicriviroc treatment has no notable effect on body or liver/kidney weight^[1].