Drug intelligence / Profile preview

rilapladib

Development stage
Phase 2
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Rilapladib is a potent and selective small molecule inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), also known as plasma platelet-activating factor acetyl hydrolase. Lp-PLA2 is an enzyme associated with the formation of atherosclerotic plaques and is found in the highly atherogenic subfraction of small dense LDL. Rilapladib was developed to reduce inflammation by inhibiting Lp-PLA2 activity, which may help stabilize atherosclerotic plaque and has been evaluated for use in both atherosclerosis and Alzheimer's disease. The drug was originally developed by GlaxoSmithKline (GSK) as part of its collaboration with Human Genome Sciences. Clinical trials included studies in patients with stable atherosclerosis and mild to moderate Alzheimer's disease; however, development for these indications has been discontinued[2][3][5][7].

Other names
SB659032SB-659032SB 659032
02

Targets

PLA2G7 (Platelet-activating factor acetylhydrolase)

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