, Volume 71, Issue 7, pp 909-933

Ticagrelor

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Abstract

Ticagrelor (Brilique™; Brilinta™), a cyclopentyl-triazolo-pyrimidine antiplatelet agent, is the first oral antagonist of the P2Y12 receptor to offer reversible receptor binding. It is indicated in the EU for the prevention of atherothrombotic events in adults with acute coronary syndromes (ACS) [unstable angina pectoris, ST-segment elevation myocardial infarction [STEMI] or non-STEMI), including those managed medically or with percutaneous coronary intervention or coronary artery bypass grafting (CABG). Ticagrelor provides selective and reversible inhibition of adenosine diphosphate-induced platelet aggregation, with a faster onset and offset of action than that of clopidogrel, and is effective in the treatment of patients with ACS, with or without ST-segment elevation. In the large, randomized, double-blind, multicentre PLATO trial conducted in this patient population, ticagrelor was more effective than clopidogrel in terms of preventing ischaemic events over 12 months, providing a significantly lower risk of the primary composite endpoint of myocardial infarction, stroke or death from vascular causes, and was associated with an overall mortality benefit. The risk of major bleeding with ticagrelor, including bleeds related to CABG, did not differ from that seen with clopidogrel in this study, although ticagrelor was associated with more non-CABG-related major bleeds and fatal intracranial bleeding, albeit the latter bleeding events were rare. Further long-term and comparative efficacy and tolerability data are required to definitively position ticagrelor with respect to other antiplatelet agents, including prasugrel. However, the clinical data currently available indicate that ticagrelor is a promising option for the treatment of patients with ACS and may be of particular use in those at high risk of ischaemic events or unresponsive to clopidogrel.

Various sections of the manuscript reviewed by: F. Fernandez-Aviles, Department of Cardiology, Hospital General Universitario Gregorio Marañon, Complutense University School of Medicine, Madrid, Spain; N. Maugeri, Thrombosis Research Unit and Autoimmunity and Vascular Inflammation Unit, San Raffaele Scientific Institute, Milan, Italy; G. Melandri, Thoracic and Cardiovascular Department, Institute of Cardiology, Bologna University, Bologna, Italy; A. Palazzuoli, Department of Internal Medicine, Cardiology Section, University of Siena, Siena, Italy; D.S. Roffman, Department of Pharmacy Practice and Science, University of Maryland School of Pharmacy, Baltimore, MD, USA.