Rilapladib is the third genomics-derived small molecule drug arising from the Human Genome Sciences-GlaxoSmithKline collaboration to enter clinical development. It is a lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor. Lp-PLA2 is an... Lp-PLA2 is an enzyme associated with the formation of atherosclerotic plaques.
- Mechanism
- Curator reviewed
Rilapladib is a Lp-PLA2 inhibitor. Lp-PLA2 has been found to be enriched in the highly atherogenic lipoprotein subfraction of small dense LDL, which is susceptible to oxidative modification. Moreover, enzyme levels are increased in patients with hyperlipidaemia, stroke, Type 1 and Type 2 diabetes mellitus, as well as in post-menopausal women. As such, plasma Lp-PLA2 levels tend to be elevated in those individuals who are considered to be at risk of developing accelerated atherosclerosis and clinical cardiovascular events. Thus, inhibition of the Lp-PLA2 enzyme would be expected to stop the build up of this fatty streak (by inhibition of the formation of lysophosphatidylcholine), and so be useful in the treatment of atherosclerosis.
- Primary indication
- Investigated for use/treatment in atherosclerosis and cardiovascular disorders.Curator reviewed
- Formula / weight
- C40H38F5N3O3S · 735.81 g/mol (avg)
- Code names
- GSK 659032 · SB-659032
Resolves to
NNBGCSGCRSCFEA-UHFFFAOYSA-NSMILESCOCCN1CCC(CC1)N(CC1=CC=C(C=C1)C1=CC=C(C=C1)C(F)(F)F)C(=O)CN1C(SCC2=C(F)C(F)=CC=C2)=CC(=O)C2=C1C=CC=C2What you can answer from here — as of June 15, 2026
Which drugs share a target with Rilapladib, and which of those have an active Phase 3 trial?
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