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Ticagrelor – toward more efficient platelet inhibition and beyond

Authors Kubisa MJ, Jezewski MP, Gasecka A, Siller-Matula JM, Postuła M

Received 27 September 2017

Accepted for publication 16 November 2017

Published 17 January 2018 Volume 2018:14 Pages 129—140

DOI https://doi.org/10.2147/TCRM.S152369

Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Hoa Le

Peer reviewer comments 3

Editor who approved publication: Professor Garry Walsh


Michał J Kubisa,1 Mateusz P Jezewski,1 Aleksandra Gasecka,2,3 Jolanta M Siller-Matula,4 Marek Postuła1

1Department of Experimental and Clinical Pharmacology, Centre for Preclinical Research and Technology (CEPT), 21st Chair and Department of Cardiology, Medical University of Warsaw, Warsaw, Poland; 3Vesicle Observation Centre, Laboratory of Experimental Clinical Chemistry, Academic Medical Centre, University of Amsterdam, the Netherlands; 4Department of Cardiology, Medical University of Vienna, Vienna, Austria

Abstract: Novel antiplatelet drugs, including ticagrelor, are being successively introduced into the therapy of atherothrombotic conditions due to their superiority over a standard combination of clopidogrel with acetylsalicylic acid in patients with acute coronary syndromes (ACS). A P2Y12 receptor antagonist, ticagrelor, is unique among antiplatelet drugs, because ticagrelor inhibits the platelet P2Y12 receptor in a reversible manner, and because it demonstrates a wide palette of advantageous pleiotropic effects associated with the increased concentration of adenosine. The pleiotropic effects of ticagrelor comprise cardioprotection, restoration of the myocardium after an ischemic event, promotion of the release of anticoagulative factors and, eventually, anti-inflammatory effects. Beyond the advantageous effects, the increased concentration of adenosine is responsible for some of ticagrelor’s adverse effects, including dyspnea and bradycardia. Large-scale clinical trials demonstrated that both standard 12-month therapy and long-term use of ticagrelor reduce the risk of cardiovascular events in patients with ACS, but at the expense of a higher risk of major bleeding. Further trials focused on the use of ticagrelor in conditions other than ACS, including ischemic stroke, peripheral artery disease and status after coronary artery bypass grafting. The results of these trials suggest comparable efficacy and safety of ticagrelor and clopidogrel in extra-coronary indications, but firm conclusions are anticipated from currently ongoing studies. Here, we summarize current evidence on the superiority of ticagrelor over other P2Y12 antagonists in ACS, discuss the mechanism underlying the drug–drug interactions and pleiotropic effects of ticagrelor, and present future perspectives of non-coronary indications for ticagrelor.

Keywords: ticagrelor, P2Y12, antiplatelet drugs, myocardial infarction, acute coronary syndromes, pleiotropism

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