Darapladib

DB06311InvestigationalSmall molecule

Investigated for use/treatment in atherosclerosis.

Mechanism: Darapladib is a selective lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor. Lp-PLA2 is an enzymatic upstream mediator of inflammatory processes. Evidence from experimental settings show that the breakdown products from oxidized low density lipoprotein C (LDL-C)such as lysophosphatidylcholine species and oxidized nonesterified fatty acids are pro-inflammatory and pro-apoptotic. These products are suspected to cause athlerosclerosis progression and plaque vulnerability, which leads to increased risk of cardiovascular problems.
Curator reviewed
Primary indication: Investigated for use/treatment in atherosclerosis.Curator reviewed
Formula / weight: C₃₆H₃₈F₄N₄O₂S · 666.78 g/mol (avg)
Code names: 480848 · SB-480848

Resolves to

Compound

Clinical / RWD

Structure

InChIKeyWDPFJWLDPVQCAJ-UHFFFAOYSA-NSMILESCCN(CC)CCN(CC1=CC=C(C=C1)C1=CC=C(C=C1)C(F)(F)F)C(=O)CN1C2=C(CCC2)C(=O)N=C1SCC1=CC=C(F)C=C1

Targets

What you can answer from here — as of June 15, 2026

3Protein targetsEach mapped to UniProt, with action and pharmacological action

Listed above

8Clinical trialsPhase, status and sponsor resolved per trial

5+ReferencesStructured and connected to the statements they support

Which drugs share a target with Darapladib, and which of those have an active Phase 3 trial?

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