CCX832

CCX832 is an orally administered small-molecule antagonist of the chemerin receptor 1 (also known as ChemR23 or CMKLR1), developed by ChemoCentryx in alliance with GlaxoSmithKline as a potential anti-inflammatory and anti-psoriatic therapy. It selectively and potently blocks ChemR23, preventing binding of the adipokine chemerin and subsequent downstream PI3K/Akt, MAPK/ERK, p38 and related signalling cascades, thereby inhibiting chemerin-driven recruitment and activation of inflammatory cells, angiogenesis, vascular smooth muscle cell proliferation, and endothelial dysfunction.[1][2][3][5][7][8][9] CCX832 entered a phase 1 clinical trial in healthy volunteers but development was halted after review of phase 1 data, and it is now mainly used as a pharmacological tool compound to interrogate chemerin/ChemR23 biology in preclinical models of obesity, diabetes-associated vascular dysfunction, and cardiovascular disease.[2][3][8][9][12]