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European Heart Journal Advance Access originally published online on July 24, 2009
European Heart Journal 2009 30(16):1964-1977; doi:10.1093/eurheartj/ehp296
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Published on behalf of the European Society of Cardiology. All rights reserved. © The Author 2009. For permissions please email: journals.permissions@oxfordjournals.org

P2Y12 inhibitors: differences in properties and mechanisms of action and potential consequences for clinical use

Lars Wallentin*

Uppsala Clinical Research Centre, University Hospital, SE 75185 Uppsala, Sweden

Received 14 March 2009; revised 28 May 2009; accepted 6 July 2009; online publish-ahead-of-print 24 July 2009.

* Corresponding author. Tel: +46 18 611 9507, Fax: +46 18 50 6638, Email: lars.wallentin{at}ucr.uu.se

Currently, clopidogrel is recommended for treatment of patients with acute coronary syndrome and/or percutaneous coronary intervention. However, the delayed onset of the effect and the occurrence of poor platelet inhibition responders with clopidogrel as well as non-compliance to dual antiplatelet treatment are associated with a raised risk of stent thrombosis. The molecular target of the active metabolite of clopidogrel and several emerging antiplatelet treatments is the P2Y12 receptor, which is the main platelet receptor responsible for ADP-induced platelet aggregation. Active metabolites of the thienopyridine prodrugs (ticlopidine, clopidogrel, and prasugrel) covalently bind to the P2Y12 receptor and are irreversible, indirect platelet inhibitors. The newer, direct-acting P2Y12 inhibitors (cangrelor and ticagrelor) change the conformation of the P2Y12 receptor, resulting in reversible, concentration dependent inhibition of the receptor. An understanding of the similarities and differences in the properties and mechanisms of action of these new inhibitors compared with clopidogrel is needed in order to optimize the development and use of these agents in clinical practice. The objectives of this systematic review are to summarize the pharmacokinetics, pharmacodynamics, and pharmacogenetics of the different P2Y12 inhibitors and to discuss the clinical implications for treatment of patients.

Key Words: Thienopyridine • Purinoceptor P2Y12 • Clopidogrel • Prasugrel • Cangrelor • Ticagrelor


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