Ticagrelor: a P2Y₁₂ antagonist for use in acute coronary syndromes

Abstract

Agents that inhibit platelet function are used routinely in the treatment and prevention of acute coronary syndromes. The main antiplatelet treatments used combine aspirin with one of the thienopyridine P2Y₁₂ antagonists, either clopidogrel or prasugrel. By blocking the synthesis of thromboxane A₂ in platelets and by blocking the effects of ADP, respectively, these agents reduce platelet activity, platelet aggregation and thrombus formation. Ticagrelor (marketed by AstraZeneca as Brilinta™ in the USA, and as Brilique^® or Possia^® in Europe) is a cyclopentyl-triazolo-pyrimidine, a new chemical class of P2Y₁₂ antagonist that is now approved for use in the wide spectrum of acute coronary syndromes. In this article we provide an overview of ticagrelor. We discuss the differences in mode of action compared with other P2Y₁₂ antagonists, examine its pharmacodynamic, pharmacokinetic and safety profile, and summarize the various clinical trials that have provided information on its efficacy in combination with aspirin. Ticagrelor appears to overcome some of the difficulties that have been encountered with other antiplatelet treatments, clopidogrel in particular.

Keywords::

• acute coronary syndrome
• antiplatelet therapy
• clopidogrel
• cyclopentyl-triazolo-pyrimidine
• P2Y₁₂ antagonists
• prasugrel
• thienopyridine
• thrombosis
• ticagrelor

Financial & competing interests disclosure

S Heptinstall, on behalf of the University of Nottingham, has received research grants for laboratory investigations on clopidogrel, prasugrel, ticagrelor and cangrelor; he is also a shareholder and director of Platelet Solutions Ltd, a spinout company of the University of Nottingham that engages in platelet function testing. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.