Drug intelligence / Profile preview

darapladib

Development stage
Phase 3
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Darapladib is a selective, orally active small-molecule inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme implicated in the inflammatory processes underlying atherosclerosis and coronary heart disease. By inhibiting Lp-PLA2, darapladib was designed to reduce the formation of pro-inflammatory and pro-apoptotic products from oxidized low-density lipoprotein (LDL), thereby stabilizing atherosclerotic plaques and reducing their risk of rupture. The drug was developed primarily for the prevention and treatment of coronary heart disease, particularly in patients at high risk due to atherosclerosis. Despite promising preclinical results, large phase III clinical trials failed to demonstrate significant benefit over placebo in reducing major adverse cardiovascular events[1][5][6][7][8][9].

Brand names
darapladib
Other names
darapladib
02

Targets

PLA2G7 (Platelet-activating factor acetylhydrolase)

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