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Clopidogrel and proton pump inhibitors

National Taiwan University Hospital · FDA-approved active Small molecule

Clopidogrel is a P2Y12 inhibitor that reduces platelet aggregation, but proton pump inhibitors impair its activation, reducing its antiplatelet efficacy.

Clopidogrel is a P2Y12 inhibitor that reduces platelet aggregation, but proton pump inhibitors impair its activation, reducing its antiplatelet efficacy. Used for Acute coronary syndrome, Percutaneous coronary intervention with stent placement, Stroke prevention in patients with recent myocardial infarction or stroke.

At a glance

Generic nameClopidogrel and proton pump inhibitors
Also known asclopidogrel, rabeprazole, pantoprazole, esomeprazole
SponsorNational Taiwan University Hospital
Drug classAntiplatelet agent (thienopyridine) with drug-drug interaction study
TargetP2Y12 receptor (clopidogrel); CYP2C19 enzyme (PPI interaction)
ModalitySmall molecule
Therapeutic areaCardiovascular
PhaseFDA-approved

Mechanism of action

Clopidogrel is a prodrug that requires hepatic metabolism via CYP3A4 and CYP2C19 to become active. Proton pump inhibitors (PPIs) are potent CYP2C19 inhibitors that significantly reduce clopidogrel's conversion to its active metabolite, thereby diminishing its antiplatelet effect. This drug-drug interaction is a recognized clinical concern that may increase thrombotic risk in patients requiring dual antiplatelet therapy.

Approved indications

Common side effects

Key clinical trials

Primary sources

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SourceUsed for
ClinicalTrials.govTrial enrolment, design, endpoints, results

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