Pharmacology and clinical trials of reversibly-binding P2Y12 inhibitors

被引:35
作者
Storey, Robert F. [1 ]
机构
[1] Univ Sheffield, Dept Cardiovasc Sci, Sheffield S10 2RX, S Yorkshire, England
关键词
ADP receptors; antiplatelet agents; arterial thrombosis; platelet pharmacology; antiplatelet drugs; ACUTE CORONARY SYNDROMES; ELEVATION MYOCARDIAL-INFARCTION; RECEPTOR ANTAGONIST; PLATELET-AGGREGATION; DOUBLE-BLIND; CLOPIDOGREL RESPONSIVENESS; ADENOSINE-DIPHOSPHATE; ANTIPLATELET THERAPY; THROMBUS STABILITY; ACTIVE METABOLITE;
D O I
10.1160/THS10-12-0769
中图分类号
R5 [内科学];
学科分类号
1002 ; 100201 ;
摘要
The important role of the P2Y(12) receptor in amplification of platelet activation and associated responses and the limitations associated with clopidogrel therapy have led to the development of novel inhibitors of this receptor. Three reversibly-binding P2Y(12) inhibitors are in phase 3 development, ticagrelor, cangrelor and elinogrel. The pharmacology and clinical trial data for each of these inhibitors are discussed and compared with relevant data for the thienopyridines clopidogrel and prasugrel.
引用
收藏
页码:S75 / S81
页数:7
相关论文
共 65 条
  • [1] P2Y12 regulates platelet adhesion/activation, thrombus growth, and thrombus stability in injured arteries
    André, P
    Delaney, SM
    LaRocca, T
    Vincent, D
    DeGuzman, F
    Jurek, M
    Koller, B
    Phillips, DR
    Conley, PB
    [J]. JOURNAL OF CLINICAL INVESTIGATION, 2003, 112 (03) : 398 - 406
  • [2] Safety and feasibility of adjunctive antiplatelet therapy with intravenous elinogrel, a direct-acting and reversible P2Y12 ADP-receptor antagonist, before primary percutaneous intervention in patients with ST-elevation myocardial infarction: The Early Rapid ReversAl of Platelet ThromboSis with Intravenous Elinogrel before PCI to Optimize REperfusion in Acute Myocardial Infarction (ERASE MI) pilot trial
    Berger, Jeffrey S.
    Roe, Matthew T.
    Gibson, C. Michael
    Kilaru, Rakhi
    Green, Cynthia L.
    Melton, Laura
    Blankenship, James D.
    Metzger, D. Christopher
    Granger, Christopher B.
    Gretler, Daniel D.
    Grines, Cindy L.
    Huber, Kurt
    Zeymer, Uwe
    Buszman, Pawel
    Harrington, Robert A.
    Armstrong, Paul W.
    [J]. AMERICAN HEART JOURNAL, 2009, 158 (06) : 998 - U145
  • [3] Intravenous Platelet Blockade with Cangrelor during PCI.
    Bhatt, Deepak L.
    Lincoff, A. Michael
    Gibson, C. Michael
    Stone, Gregg W.
    McNulty, Steven
    Montalescot, Gilles
    Kleiman, Neal S.
    Goodman, Shaun G.
    White, Harvey D.
    Mahaffey, Kenneth W.
    Pollack, Charles V., Jr.
    Manoukian, Steven V.
    Widimsky, Petr
    Chew, Derek P.
    Cura, Fernando
    Manukov, Ivan
    Tousek, Frantisek
    Jafar, M. Zubair
    Arneja, Jaspal
    Skerjanec, Simona
    Harrington, Robert A.
    [J]. NEW ENGLAND JOURNAL OF MEDICINE, 2009, 361 (24) : 2330 - 2341
  • [4] Björkman JA, 2007, CIRCULATION, V116, P28
  • [5] Prospective Evaluation of the Prognostic Implications of Improved Assay Performance With a Sensitive Assay for Cardiac Troponin I
    Bonaca, Marc
    Scirica, Benjamin
    Sabatine, Marc
    Dalby, Anthony
    Spinar, Jindrich
    Murphy, Sabina A.
    Jarolim, Peter
    Braunwald, Eugene
    Morrow, David A.
    [J]. JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY, 2010, 55 (19) : 2118 - 2124
  • [6] Which platelet function test is suitable to monitor clopidogrel responsiveness? A pharmacokinetic analysis on the active metabolite of clopidogrel
    Bouman, H. J.
    Parlak, E.
    van Werkum, J. W.
    Breet, N. J.
    ten Cate, H.
    Hackeng, C. M.
    ten Berg, J. M.
    Taubert, D.
    [J]. JOURNAL OF THROMBOSIS AND HAEMOSTASIS, 2010, 8 (03) : 482 - 488
  • [7] BUCKLAND R, 2009, THROMB HAEMOST S2, V7
  • [8] Pharmacokinetics, pharmacodynamics, safety and tolerability of multiple ascending doses of ticagrelor in healthy volunteers
    Butler, Kathleen
    Teng, Renli
    [J]. BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 2010, 70 (01) : 65 - 77
  • [9] Safety, tolerability, and initial efficacy of AZD6140, the first reversivle oral adenosine diphosphate receptor antagonist, compared with clopidigrel, in patients with non-ST-segment elevation acute coronary syndrome - Primary results of the DISPERSE-2 trial
    Cannon, Christopher P.
    Husted, Steen
    Harrington, Robert A.
    Scirica, Benjamin M.
    Emanuelsson, Hakan
    Storey, Robert F.
    [J]. JOURNAL OF THE AMERICAN COLLEGE OF CARDIOLOGY, 2007, 50 (19) : 1844 - 1851
  • [10] Comparison of ticagrelor with clopidogrel in patients with planned invasive strategy for acute coronary syndromes (PLATO): a randomised double-blind study
    Cannon, Christopher P.
    Harrington, Robert A.
    James, Stefan
    Ardissino, Diego
    Becker, Richard C.
    Emanuelsson, Hakan
    Husted, Steen
    Katus, Hugo
    Keltai, Matyas
    Khurmi, Nardev S.
    Kontny, Frederic
    Lewis, Basil S.
    Steg, Philippe Gabriel
    Storey, Robert F.
    Wojdyla, Daniel
    Wallentin, Lars
    [J]. LANCET, 2010, 375 (9711) : 283 - 293