Darapladib

作者：Bui Quang T; Wilensky Robert L^*

来源：Expert Opinion on Investigational Drugs, 2010, 19(1): 161-168.

DOI：10.1517/13543780903501513

• acute coronary syndromes
• inflammation
• Lp-PLA(2)
• macrophages
• myocardial infarction

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 A(2) (Lp-PLA(2)) 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-PLA(2).
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-PLA(2) and its proatherogenie role. Additional insights will be gained into the role of selective inhibitors of Lp-PLA(2) as new therapeutic agents.
Take home message. Darapladib is a selective inhibitor of Lp-PLA(2) and represents a new class of therapeutic agents that target inflammation to treat high-risk atherosclerosis.

• 出版日期2010-1