Darapladib

Importance of the field: Atherosclerosis is an inflammatory-immune mediated disease process. Plaque rupture is responsible for the clinical events of ischemic death, myocardial infarction, acute coronary syndromes and ischemic strokes. Lipoprotein-associated phospholipase A2 (Lp-PLA2) seems to play a major role in the development of such high-risk lesions, in both the coronary and carotid arteries. Darapladib is a selective inhibitor of Lp-PLA2.Areas covered in this review: An overview of darapladib by reviewing the studies (1990 – 2009) that have provided the rationale for the development of darapladib; and a discussion of its potential merit as a new therapeutic drug to target high-risk atherosclerosis.What the reader will gain: The reader should gain an understanding of the importance of inflammation during atherogenesis as well as of the biology of Lp-PLA2 and its proatherogenic role. Additional insights will be gained into the role of selective inhibitors of Lp-PLA2 as new therapeutic agents.Take home message: Darapladib is a selective inhibitor of Lp-PLA2 and represents a new class of therapeutic agents that target inflammation to treat high-risk atherosclerosis.