Drug intelligence / Profile preview

darapladib + rosuvastatin

Development stage
Discontinued
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

**darapladib + rosuvastatin** is an investigational combination therapy consisting of darapladib, a selective small-molecule inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), and rosuvastatin, an HMG-CoA reductase inhibitor (statin) widely used to lower cholesterol. This combination is designed to provide complementary cardiovascular protection by inhibiting vascular inflammation and atherothrombosis (darapladib) while effectively reducing LDL cholesterol (rosuvastatin). Darapladib was developed by GSK mainly for atherosclerotic cardiovascular disease, but its further clinical development as a monotherapy was discontinued after Phase 3 trials. Rosuvastatin is an approved statin used for the treatment of hypercholesterolemia and prevention of cardiovascular disease.

02

Targets

PLA2G7 (Platelet-activating factor acetylhydrolase)HMGCR (3-hydroxy-3-methylglutaryl-coenzyme A reductase)

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