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P2Y(12) inhibitors: differences in properties and mechanisms of action and potential consequences for clinical use
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Medical Sciences. Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Medicinska och farmaceutiska vetenskapsområdet, centrumbildningar mm, UCR-Uppsala Clinical Research Center. (UCR)
2009 (English)In: European Heart Journal, ISSN 0195-668X, E-ISSN 1522-9645, Vol. 30, no 16, 1964-1977 p.Article, review/survey (Refereed) Published
Abstract [en]

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 P2Y(12) 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 P2Y(12) receptor and are irreversible, indirect platelet inhibitors. The newer, direct-acting P2Y(12) inhibitors (cangrelor and ticagrelor) change the conformation of the P2Y(12) 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 P2Y(12) inhibitors and to discuss the clinical implications for treatment of patients.

Place, publisher, year, edition, pages
2009. Vol. 30, no 16, 1964-1977 p.
National Category
Medical and Health Sciences
URN: urn:nbn:se:uu:diva-124191DOI: 10.1093/eurheartj/ehp296ISI: 000269001300011PubMedID: 19633016OAI: oai:DiVA.org:uu-124191DiVA: diva2:317214
Available from: 2010-05-03 Created: 2010-05-03 Last updated: 2012-07-13Bibliographically approved

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