A brief review of the past and future of platelet P2Y12 antagonist

Coronary Artery Disease

Volumn 23, Issue 6, 2012, Pages 368-374

  Barn, Kulpreet ^a   Steinhubl, Steven R ^a  

^a GEISINGER MEDICAL CENTER   (United States)

Author keywords

ADP; P2Y12; platelet antagonist; thienopyridines

Indexed keywords

ANTITHROMBOCYTIC AGENT; CANGRELOR; CLOPIDOGREL; ELINOGREL; PRASUGREL; PURINERGIC P2Y12 RECEPTOR ANTAGONIST; TICAGRELOR; TICLOPIDINE; UNCLASSIFIED DRUG;

ANTICOAGULATION; DRUG ABSORPTION; DRUG DOSE INCREASE; DRUG EFFICACY; DRUG HYDROLYSIS; DRUG METABOLISM; HUMAN; LOADING DRUG DOSE; NEUTROPENIA; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); RECEPTOR BLOCKING; REVIEW; ST SEGMENT ELEVATION MYOCARDIAL INFARCTION; THROMBOCYTE AGGREGATION INHIBITION; THROMBOTIC THROMBOCYTOPENIC PURPURA; TREATMENT OUTCOME;

ACUTE CORONARY SYNDROME; ADENOSINE; ADENOSINE MONOPHOSPHATE; CORONARY ARTERY DISEASE; HUMANS; MYOCARDIAL INFARCTION; PIPERAZINES; PURINERGIC P2Y RECEPTOR ANTAGONISTS; QUINAZOLINONES; STENTS; SULFONAMIDES; THIOPHENES; THROMBOSIS; TICLOPIDINE;

EID: 84864861785     PISSN: 09546928     EISSN: 14735830     Source Type: Journal    
DOI: 10.1097/MCA.0b013e3283564930     Document Type: Review

References (36)

1. Fuster V, Badimon L, Badimon JJ, Chesebro JH. The pathogenesis of coronary artery disease and the acute coronary syndromes (1). N Engl J Med 1992; 326:242-250.
2. Cattaneo M. New P2Y(12) inhibitors. Circulation 2010; 121:171-179.
3. Becker RC, Gurbel PA. Platelet P2Y12 receptor antagonist pharmacokinetics and pharmacodynamics: a foundation for distinguishing mechanisms of bleeding and anticipated risk for platelet-directed therapies. Thromb Haemost 2010; 103:535-544.
4. Caplain H, Donat F, Gaud C, Necciari J. Pharmacokinetics of clopidogrel. Semin Thromb Hemost 1999; 25 (Suppl 2):25-28. (Pubitemid 29350288)
5. Von Beckerath N, Taubert D, Pogatsa-Murray G, Schomig E, Kastrati A, Schomig A. Absorption, metabolization, and antiplatelet effects of 300-, 600-, and 900-mg loading doses of clopidogrel: results of the ISARCHOICE (Intracoronary Stenting and Antithrombotic Regimen: Choose Between 3 High Oral Doses for Immediate Clopidogrel Effect) trial. Circulation 2005; 112:2946-2950. (Pubitemid 41612296)
6. Montalescot G, Sideris G, Meuleman C, Bal-dit-Sollier C, Lellouche N, Steg PG, et al. A randomized comparison of high clopidogrel loading doses in patients with non-ST-segment elevation acute coronary syndromes: the ALBION (Assessment of the Best Loading Dose of Clopidogrel to Blunt Platelet Activation, Inflammation and Ongoing Necrosis) trial. J Am Coll Cardiol 2006; 48:931-938. (Pubitemid 44292463)
7. Yusuf S, Zhao F, Mehta SR, Chrolavicius S, Tognoni G, Fox KK. Effects of clopidogrel in addition to aspirin in patients with acute coronary syndromes without ST-segment elevation. N Engl J Med 2001; 345:494-502. (Pubitemid 32758501)
8. Mehta SR, Yusuf S, Peters RJ, Bertrand ME, Lewis BS, Natarajan MK, et al. Effects of pretreatment with clopidogrel and aspirin followed by long-term therapy in patients undergoing percutaneous coronary intervention: the PCI-CURE study. Lancet 2001; 358:527-533. (Pubitemid 32772726)
9. Steinhubl SR, Berger PB, Mann JT IIII, Fry ET, DeLago A,Wilmer C, Topol EJ. Early and sustained dual oral antiplatelet therapy following percutaneous coronary intervention: a randomized controlled trial. JAMA 2002; 288:2411-2420. (Pubitemid 35340537)
10. Chen ZM, Jiang LX, Chen YP, Xie JX, Pan HC, Peto R, et al. Addition of clopidogrel to aspirin in 45,852 patients with acute myocardial infarction: randomised placebo-controlled trial. Lancet 2005; 366:1607-1621.
11. Sabatine MS, Cannon CP, Gibson CM, Lopez-Sendon JL, Montalescot G, Theroux P, et al. Addition of clopidogrel to aspirin and fibrinolytic therapy for myocardial infarction with ST-segment elevation. N Engl J Med 2005; 352:1179-1189. (Pubitemid 40397259)
12. Sabatine MS, Cannon CP, Gibson CM, Lopez-Sendon JL, Montalescot G, Theroux P, et al. Effect of clopidogrel pretreatment before percutaneous coronary intervention in patients with ST-elevation myocardial infarction treated with fibrinolytics: the PCI-CLARITY study. JAMA 2005; 294: 1224-1232. (Pubitemid 41352110)
13. Vlaar PJ, Svilaas T, Damman K, de Smet BJ, Tijssen JG, Hillege HL, Zijlstra F. Impact of pretreatment with clopidogrel on initial patency and outcome in patients treated with primary percutaneous coronary intervention for STsegment elevation myocardial infarction: a systematic review. Circulation 2008; 118:1828-1836.
14. Mehta SR, Bassand JP, Chrolavicius S, Diaz R, Eikelboom JW, Fox KA, et al. Dose comparisons of clopidogrel and aspirin in acute coronary syndromes. N Engl J Med 2010; 363:930-942.
15. Mehta SR, Tanguay JF, Eikelboom JW, Jolly SS, Joyner CD, Granger CB, et al. Double-dose versus standard-dose clopidogrel and high-dose versus low-dose aspirin in individuals undergoing percutaneous coronary intervention for acute coronary syndromes (CURRENT-OASIS 7): a randomised factorial trial. Lancet 2010; 376:1233-1243.
16. Cannon CP, Harrington RA, James S, Ardissino D, Becker RC, Emanuelsson H, et al. Comparison of ticagrelor with clopidogrel in patients with a planned invasive strategy for acute coronary syndromes (PLATO): a randomised double-blind study. Lancet 2010; 375:283-293.
17. Wiviott SD, Braunwald E, McCabe CH, Horvath I, Keltai M, Herrman JP, et al. Intensive oral antiplatelet therapy for reduction of ischaemic events including stent thrombosis in patients with acute coronary syndromes treated with percutaneous coronary intervention and stenting in the TRITONTIMI 38 trial: a subanalysis of a randomised trial. Lancet 2008; 371: 1353-1363.
18. Steinhubl SR. Genotyping, clopidogrel metabolism, and the search for the therapeutic window of thienopyridines. Circulation 2010; 121:481-483.
19. Steinhubl SR. The illusion of 'optimal' platelet inhibition. JACC Cardiovasc Interv 2012; 5:278-280.
20. Parodi G, Marcucci R, Valenti R, Gori AM, Migliorini A, Giusti B, et al. High residual platelet reactivity after clopidogrel loading and long-term cardiovascular events among patients with acute coronary syndromes undergoing PCI. JAMA 2011; 306:1215-1223.
21. Price MJ, Berger PB, Teirstein PS, Tanguay JF, Angiolillo DJ, Spriggs D, et al. Standard- vs high-dose clopidogrel based on platelet function testing after percutaneous coronary intervention: the GRAVITAS randomized trial. JAMA 2011; 305:1097-1105.
22. Niitsu Y, Jakubowski JA, Sugidachi A, Asai F. Pharmacology of CS-747 (prasugrel, LY640315), a novel, potent antiplatelet agent with in vivo P2Y12 receptor antagonist activity. Semin Thromb Hemost 2005; 31:184-194. (Pubitemid 40605193)
23. Brandt JT, Payne CD,Wiviott SD,Weerakkody G, Farid NA, Small DS, et al. A comparison of prasugrel and clopidogrel loading doses on platelet function: magnitude of platelet inhibition is related to active metabolite formation. Am Heart J 2007; 153:66e9-16.
24. Wiviott SD, Braunwald E, McCabe CH, Montalescot G, Ruzyllo W, Gottlieb S. Prasugrel versus clopidogrel in patients with acute coronary syndromes. N Engl J Med 2007; 357:2001-2015. (Pubitemid 350106708)
25. Kaul S, Shah PK, Diamond GA. Abstract 4014: timing of benefit with prasugrel in patients with acute coronary syndromes undergoing percutaneous coronary intervention: reanalysis of TRITON-TIMI 38 results. Circulation 2008; 118 (Suppl):S818-S819.
26. Wallentin L, Becker RC, Budaj A, Cannon CP, Emanuelsson H, Held C, et al. Ticagrelor versus clopidogrel in patients with acute coronary syndromes. N Engl J Med 2009; 361:1045-1057.
27. Kaul S, Diamond GA, Shah PK. Abstract 988: do high-risk characteristics (history of stroke or TIA, age 75 years, weight >60 kg) reliably predict bleeding in TRITON-TIMI 38? Circulation 2008; 118 (Suppl):S638-S639.
28. Montalescot G,Wiviott SD, Braunwald E, Murphy SA, Gibson CM, McCabe CH, Antman EM. Prasugrel compared with clopidogrel in patients undergoing percutaneous coronary intervention for ST-elevation myocardial infarction (TRITON-TIMI 38): double-blind, randomised controlled trial. Lancet 2009; 373:723-731.
29. Murphy SA, Antman EM,Wiviott SD,Weerakkody G, Morocutti G, Huber K, et al. Reduction in recurrent cardiovascular events with prasugrel compared with clopidogrel in patients with acute coronary syndromes from the TRITON-TIMI 38 trial. Eur Heart J 2008; 29:2473-2479.
30. Wiviott SD, Braunwald E, Angiolillo DJ, Meisel S, Dalby AJ, Verheugt FW, et al. Greater clinical benefit of more intensive oral antiplatelet therapy with prasugrel in patients with diabetes mellitus in the trial to assess improvement in therapeutic outcomes by optimizing platelet inhibition with prasugrel-thrombolysis in myocardial infarction 38. Circulation 2008; 118:1626-1636.
31. Chin CT, Roe MT, Fox KA, Prabhakaran D, Marshall DA, Petitjean H, et al. Study design and rationale of a comparison of prasugrel and clopidogrel in medically managed patients with unstable angina/non-ST-segment elevation myocardial infarction: the TaRgeted platelet Inhibition to cLarify the Optimal strateGy to medicallY manage Acute Coronary Syndromes (TRILOGY ACS) trial. Am Heart J 2010; 160:16.e1-22.e1.
32. Storey RF, Husted S, Harrington RA, Heptinstall S, Wilcox RG, Peters G, et al. Inhibition of platelet aggregation by AZD6140, a reversible oral P2Y12 receptor antagonist, compared with clopidogrel in patients with acute coronary syndromes. J Am Coll Cardiol 2007; 50:1852-1856. (Pubitemid 350017792)
33. Mahaffey KW, Wojdyla DM, Carroll K, Becker RC, Storey RF, Angiolillo DJ, et al. Ticagrelor compared with clopidogrel by geographic region in the Platelet Inhibition and Patient Outcomes (PLATO) trial. Circulation 2011; 124:544-554.
34. Akers WS, Oh JJ, Oestreich JH, Ferraris S, Wethington M, Steinhubl SR. Pharmacokinetics and pharmacodynamics of a bolus and infusion of cangrelor: a direct, parenteral P2Y12 receptor antagonist. J Clin Pharmacol 2010; 50:27-35.
35. Bhatt DL, Lincoff AM, Gibson CM, Stone GW, McNulty S, Montalescot G, et al. Intravenous platelet blockade with cangrelor during PCI. N Engl J Med 2009; 361:2330-2341.
36. Harrington RA, Stone GW, McNulty S,White HD, Lincoff AM, Gibson CM, et al. Platelet inhibition with cangrelor in patients undergoing PCI. N Engl J Med 2009; 361:2318-2329.