Ticagrelor

Antiplatelet agent, P2Y12 receptor inhibitor (reversible), Cyclopentyltriazolopyrimidine

Ticagrelor

Brilinta

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Summary

Classes

Antiplatelet agent, P2Y12 receptor inhibitor (reversible), Cyclopentyltriazolopyrimidine

Common uses

Acute coronary syndrome (with aspirin)▲0▼, Post-PCI dual antiplatelet therapy▲0▼, Secondary prevention >12 months post-MI (60 mg BID, PEGASUS-derived)▲0▼

Pharmacy

Starting dose

ACS/PCI: 180 mg PO loading dose, then 90 mg PO BID for 12 months; long-term post-MI: 60 mg BID

Preparations

60, 90 mg tablets

US FDA Max

90 mg BID (acute year); 60 mg BID (chronic post-MI)

Pharmacology

Routes

Oral

Onset

Antiplatelet effect within 30 minutes of loading dose (faster than clopidogrel)

Duration

12 hours

Half-life

~7 hours (parent); ~9 hours (active AR-C124910XX metabolite, accounts for ~30-40% of activity)

Bioavailability

~36% (oral)

Pregnancy

Limited data; weigh against alternatives.^{[citation needed]}

Legal status

Rx-only in US. Carries a Boxed Warning for bleeding risk and against aspirin maintenance doses above 100 mg/d (reduces ticagrelor efficacy, per PLATO subgroup analysis)

Purported mechanism

Ticagrelor is a reversible direct-acting P2Y12 receptor antagonist; unlike clopidogrel and prasugrel it does not require CYP-mediated bioactivation, so antiplatelet effect onset is faster, more predictable, and less CYP2C19-genotype-dependent.▲0▼ PLATO (2009) established mortality benefit over clopidogrel in ACS, but the requirement for BID dosing, increased dyspnea (~14%), and bradyarrhythmia signal complicate adherence. CYP3A4 substrate AND moderate inhibitor — strong CYP3A4 inhibitors raise exposure substantially.