New P2Y12 blockers.

作者: M. CATTANEO

DOI: 10.1111/J.1538-7836.2009.03382.X

关键词:

摘要: Summary.  A number of new antiplatelet agents currently in development are anticipated to improve clinical outcomes and safety benefits patients with acute coronary syndrome (ACS). This article reviews the pharmacology three these agents: prasugrel, cangrelor, ticagrelor. Prasugrel, a third-generation, oral thienopyridine, has been shown be superior clopidogrel, current gold standard, preventing ischemic events ACS undergoing percutaneous intervention (PCI), although bleeding rate was higher. Cangrelor, chemical analog adenosine triphosphate, is potent direct platelet P2Y12 antagonist. In as an intravenous agent, cangrelor being evaluated two phase III studies requiring PCI. Ticagrelor first class orally available antagonizing effects ADP mediated by P2Y12; it studied trial ACS.

参考文章(18)
Christopher P Cannon, Steen Husted, Robert A Harrington, Benjamin M Scirica, Håkan Emanuelsson, Gary Peters, Robert F Storey, DISPERSE-2 Investigators, Safety, Tolerability, and Initial Efficacy of AZD6140, the First Reversible Oral Adenosine Diphosphate Receptor Antagonist, Compared With Clopidogrel, in Patients With Non-ST-Segment Elevation Acute Coronary Syndrome Primary Results of the DISPERSE-2 Trial Journal of the American College of Cardiology. ,vol. 50, pp. 1844- 1851 ,(2007) , 10.1016/J.JACC.2007.07.053
A. SUGIDACHI, T. OGAWA, A. KURIHARA, K. HAGIHARA, J.A. JAKUBOWSKI, M. HASHIMOTO, Y. NIITSU, F. ASAI, The greater in vivo antiplatelet effects of prasugrel as compared to clopidogrel reflect more efficient generation of its active metabolite with similar antiplatelet activity to that of clopidogrel's active metabolite. Journal of Thrombosis and Haemostasis. ,vol. 5, pp. 1545- 1551 ,(2007) , 10.1111/J.1538-7836.2007.02598.X
Richard H Hongo, Jill Ley, Stuart E Dick, Rupsa R Yee, The effect of clopidogrel incombination with aspirin whengiven before coronary artery bypass grafting Journal of the American College of Cardiology. ,vol. 40, pp. 231- 237 ,(2002) , 10.1016/S0735-1097(02)01954-X
John T. Brandt, Christopher D. Payne, Stephen D. Wiviott, Govinda Weerakkody, Nagy A. Farid, David S. Small, Joseph A. Jakubowski, Hideo Naganuma, Kenneth J. Winters, A comparison of prasugrel and clopidogrel loading doses on platelet function: magnitude of platelet inhibition is related to active metabolite formation. American Heart Journal. ,vol. 153, ,(2007) , 10.1016/J.AHJ.2006.10.010
Sachin Yende, Richard G. Wunderink, Effect of clopidogrel on bleeding after coronary artery bypass surgery. Critical Care Medicine. ,vol. 29, pp. 2271- 2275 ,(2001) , 10.1097/00003246-200112000-00006
Adam B. Greenbaum, Cindy L. Grines, John A. Bittl, Richard C. Becker, Dean J. Kereiakes, Ian C. Gilchrist, Jane Clegg, Jill E. Stankowski, Donna R. Grogan, Robert A. Harrington, Hakan Emanuelsson, W. Douglas Weaver, Initial experience with an intravenous P2Y12 platelet receptor antagonist in patients undergoing percutaneous coronary intervention: Results from a 2-part, phase II, multicenter, randomized, placebo- and active-controlled trial American Heart Journal. ,vol. 151, pp. 689.e1- 689.e10 ,(2006) , 10.1016/J.AHJ.2005.11.014
LiQian Chen, Arthur W. Bracey, Rajko Radovancevic, John R. Cooper, Charles D. Collard, William K. Vaughn, Nancy A. Nussmeier, Clopidogrel and bleeding in patients undergoing elective coronary artery bypass grafting The Journal of Thoracic and Cardiovascular Surgery. ,vol. 128, pp. 425- 431 ,(2004) , 10.1016/J.JTCVS.2004.02.019
J. J.J van Giezen, Robert G Humphries, Preclinical and clinical studies with selective reversible direct P2Y12 antagonists. Seminars in Thrombosis and Hemostasis. ,vol. 31, pp. 195- 204 ,(2005) , 10.1055/S-2005-869525
Christopher D Payne, Ying Grace Li, David S Small, C Steven Ernest, Nagy A Farid, Joseph A Jakubowski, John T Brandt, Daniel E Salazar, Kenneth J Winters, Increased Active Metabolite Formation Explains the Greater Platelet Inhibition With Prasugrel Compared to High-dose Clopidogrel Journal of Cardiovascular Pharmacology. ,vol. 50, pp. 555- 562 ,(2007) , 10.1097/FJC.0B013E3181492209