Ticagrelor: a P2Y12 antagonist for use in acute coronary syndromes

被引:2
作者
Wijeyeratne, Yanushi Dullewe [1 ]
Joshi, Rashi [1 ]
Heptinstall, Stan [1 ]
机构
[1] Univ Nottingham, Queens Med Ctr, Nottingham NG7 2UH, England
基金
英国医学研究理事会;
关键词
acute coronary syndrome; antiplatelet therapy; clopidogrel; cyclopentyl-triazolo-pyrimidine; P2Y(12) antagonists; prasugrel; thienopyridine; thrombosis; ticagrelor; PLATO PLATELET INHIBITION; RECEPTOR ANTAGONIST; CLOPIDOGREL; OUTCOMES; ADENOSINE; AZD6140; SAFETY; ADP; PHARMACOKINETICS; PHARMACODYNAMICS;
D O I
10.1586/ECP.12.17
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Agents that inhibit platelet function are used routinely in the treatment and prevention of acute coronary syndromes. The main antiplatelet treatments used combine aspirin with one of the thienopyridine P2Y(12) antagonists, either clopidogrel or prasugrel. By blocking the synthesis of thromboxane A(2) in platelets and by blocking the effects of ADP, respectively, these agents reduce platelet activity, platelet aggregation and thrombus formation. Ticagrelor (marketed by AstraZeneca as Brilinta (TM) in the USA, and as Brilique (R) or Possia (R) in Europe) is a cyclopentyl-triazolo-pyrimidine, a new chemical class of P2Y(12) antagonist that is now approved for use in the wide spectrum of acute coronary syndromes. In this article we provide an overview of ticagrelor. We discuss the differences in mode of action compared with other P2Y(12) antagonists, examine its pharmacodynamic, pharmacokinetic and safety profile, and summarize the various clinical trials that have provided information on its efficacy in combination with aspirin. Ticagrelor appears to overcome some of the difficulties that have been encountered with other antiplatelet treatments, clopidogrel in particular.
引用
收藏
页码:257 / 269
页数:13
相关论文
共 69 条
  • [1] [Anonymous], MI SEC PREV SEC PREV
  • [2] [Anonymous], MORT STAT DEATHS REG
  • [3] [Anonymous], Coronary Heart Disease Statistics 2007
  • [4] [Anonymous], 2008, European Cardiovascular Disease Statistics
  • [5] ST-Elevation Acute Coronary Syndromes in the Platelet Inhibition and Patient Outcomes (PLATO) Trial Insights From the ECG Substudy
    Armstrong, Paul W.
    Siha, Hany
    Fu, Yuling
    Westerhout, Cynthia M.
    Steg, Ph. Gabriel
    James, Stefan K.
    Storey, Robert F.
    Horrow, Jay
    Katus, Hugo
    Clemmensen, Peter
    Harrington, Robert A.
    Wallentin, Lars
    [J]. CIRCULATION, 2012, 125 (03) : 514 - U131
  • [6] AstraZeneca, 2011, G BA ISS POS FIN MED
  • [7] AstraZeneca, 2011, BRIL TIC TABL HIGHL
  • [8] AstraZeneca, 2010, NEW OUTC STUD TIC BR
  • [9] Bleeding complications with the P2Y12 receptor antagonists clopidogrel and ticagrelor in the PLATelet inhibition and patient Outcomes (PLATO) trial
    Becker, Richard C.
    Bassand, Jean Pierre
    Budaj, Andrzej
    Wojdyla, Daniel M.
    James, Stefan K.
    Cornel, Jan H.
    French, John
    Held, Claes
    Horrow, Jay
    Husted, Steen
    Lopez-Sendon, Jose
    Lassila, Riitta
    Mahaffey, Kenneth W.
    Storey, Robert F.
    Harrington, Robert A.
    Wallentin, Lars
    [J]. EUROPEAN HEART JOURNAL, 2011, 32 (23) : 2933 - 2944
  • [10] Intravenous adenosine and dyspnea in humans
    Burki, NK
    Dale, WJ
    Lee, LY
    [J]. JOURNAL OF APPLIED PHYSIOLOGY, 2005, 98 (01) : 180 - 185