Darapladib

Darapladib is a novel inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme that may link lipid metabolism with inflammation, leading to the increased stability of atherosclerotic plaques present in the major arteries. During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM. Darapladib is being studied as a possible add-on treatment for atherosclerosis.