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Characteristics of new P2Y12 inhibitors
Journal of Cardiovascular Medicine, 2013The options for antithrombotic therapy have recently been expanded, facilitating optimal tailored treatment. Dual antiplatelet therapy with aspirin and an approved adenosine diphosphate P2Y12 receptor antagonist is recommended for the management of patients with acute coronary syndromes (ACS).
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Role of P2Y12 Receptor in Thrombosis
2015P2Y12 receptor is a 342 amino acid Gi-coupled receptor predominantly expressed on platelets. P2Y12 receptor is physiologically activated by ADP and inhibits adenyl cyclase (AC) to decrease cyclic AMP (cAMP) level, resulting in platelet aggregation. It also activates PI3 kinase (PI3K) pathway leading to fibrinogen receptor activation, and may protect ...
Yaqi, Zhang, Si, Zhang, Zhongren, Ding
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State of the art of new P2Y12 antagonists
Internal and Emergency Medicine, 2010The interaction of ADP with its platelet receptor P2Y12 plays a crucial role in platelet activation and thrombogenesis. This article reviews the pharmacology and clinical trials of specific antagonists of P2Y12. Clopidogrel is a thienopyridine with proven antithrombotic efficacy, but it has some important drawbacks: (a) it is a pro-drug that needs to ...
M.N. Cattaneo, G. Podda
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Responsiveness to P2Y12 receptor inhibitors
Current Opinion in Cardiology, 2011This review is aimed at describing the variability in response to P2Y12 inhibitor agents, and to focus on the main tests currently available to assess the responsiveness.There is high interindividual response variability to clopidogrel. Some patients do not respond to the drug; this condition can be due to patient-related factors (poor compliance ...
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P2Y12 receptors: structure and function
Journal of Thrombosis and Haemostasis, 2015The platelet P2Y12 receptor (P2Y12R) for adenosine 5'diphosphate (ADP) plays a central role in platelet function, hemostasis, and thrombosis. Patients with inherited P2Y12R defects display mild-to-moderate bleeding diatheses. Defects of P2Y12R should be suspected when ADP, even at high concentrations (≥ 10 μm), is unable to induce full, irreversible ...
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Pharmacology: Inhibitors of P2Y12
2017Dual antiplatelet treatment consisting of aspirin and a P2Y12 inhibitor represents the cornerstone of treatment in patients with acute coronary syndrome (ACS) and those undergoing percutaneous coronary intervention. P2Y12 inhibitors are broadly used worldwide to prevent and treat ischemic events in cardiac patients; however, understanding their ...
Lisa Gross, Dániel Aradi, Dirk Sibbing
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Switching P2Y12 Receptor Inhibiting Therapies
Interventional Cardiology Clinics, 2017Antiplatelet therapy with aspirin and a P2Y12 receptor inhibitor is the cornerstone of treatment of patients with atherothrombotic disease manifestations. Switching between P2Y12 inhibitors occurs commonly in clinical practice for a variety of reasons, including safety, efficacy, adherence, and economic considerations.
Fabiana, Rollini +2 more
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Heart, 2011
The management and prevention of arterial thrombosis has been transformed by the recognition of the role of platelets in this process and the development of effective antiplatelet drugs. The limited role of thromboxane A2 in platelet activation explains why aspirin therapy, which effectively inhibits release of thromboxane A2 by platelets, is ...
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The management and prevention of arterial thrombosis has been transformed by the recognition of the role of platelets in this process and the development of effective antiplatelet drugs. The limited role of thromboxane A2 in platelet activation explains why aspirin therapy, which effectively inhibits release of thromboxane A2 by platelets, is ...
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Thrombosis and Haemostasis, 2010
SummaryNovel P2Y12 inhibitors are in development to overcome the occurrence of atherothrombotic events associated with poor responsiveness to the widely used P2Y12 inhibitor clopidogrel. Cangrelor is an intravenously administered P2Y12 inhibitor that does not need metabolic conversion to an active metabolite for its antiplatelet action, and as a ...
Bouman, HJ +8 more
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SummaryNovel P2Y12 inhibitors are in development to overcome the occurrence of atherothrombotic events associated with poor responsiveness to the widely used P2Y12 inhibitor clopidogrel. Cangrelor is an intravenously administered P2Y12 inhibitor that does not need metabolic conversion to an active metabolite for its antiplatelet action, and as a ...
Bouman, HJ +8 more
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P2Y12 Inhibitors: Pharmacologic Mechanism and Clinical Relevance
Cardiovascular & Hematological Agents in Medicinal Chemistry, 2013Platelets play a critical role in the pathogenesis of atherothrombotic processes and inhibition of platelet aggregation by antiplatelet therapy is essential and really important in the acute coronary syndromes or in the setting of percutaneous coronary intervention.
SECCO, GIOEL GABRIO +9 more
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