188
Views
16
CrossRef citations to date
0
Altmetric
Drug Profile

Ticagrelor: a P2Y12 antagonist for use in acute coronary syndromes

, &
Pages 257-269 | Published online: 10 Jan 2014

References

  • Centers for Disease Control and Prevention (CDC). Prevalence of coronary heart disease – United States, 2006–2010. Morb. Mortal. Wkly Rep.60(40), 1377–1381 (2011).
  • Leal J, Luengo-Fernández R, Gray AM et al. Economic burden of cardiovascular diseases in the enlarged EU. Eur. Heart J.27(3), 1610–1619 (2006).
  • Fox KAA, Dabbous OH, Goldberg RJ et al. Prediction of risk of death and myocardial infarction in the six months after presentation with acute coronary syndrome: prospective multinational observational study (GRACE). Br. Med. J.333(7578), 1091–1094 (2006).
  • Fox KAA, Carruthers KF, Dunbar DR et al. Underestimated and under-recognized: the late consequences of acute coronary syndrome (GRACE UK–Belgian study). Eur. Heart J.31(22), 2755–2764 (2010).
  • Tang EW, Wong CK, Herbison P. Global registry of acute coronary events (GRACE) hospital discharge risk score accurately predicts long-term mortality post acute coronary syndrome. Am. Heart J.153(1), 29–35 (2007).
  • Mehran R, Pocock S, Nikolsky E et al. Impact of bleeding on mortality after percutaneous coronary intervention results from a patient-level pooled analysis of the REPLACE-2 (Randomized Evaluation of PCI Linking Angiomax to Reduced Clinical Events), ACUITY (Acute Catheterization and Urgent Intervention Triage Strategy), and HORIZONS-AMI (Harmonizing Outcomes with Revascularization and Stents in Acute Myocardial Infarction) trials. JACC Cardiovasc. Interv.4(6), 654–664 (2011).
  • Wijeyeratne YD, Heptinstall S. Antiplatelet therapy: ADP receptor antagonists. Br. J. Clin. Pharmacol.72(4), 647–657 (2011).
  • Danchin N, Aïssaoui N. Pharmacologic therapy for non-ST-segment elevation acute coronary syndromes: focus on anti-thrombotic therapy. Cardiovasc. Drugs Ther.24(4), 325–330 (2010).
  • Fox SC, May JA, Shah A, Neubert U, Heptinstall S. Measurement of platelet P-selectin for remote testing of platelet function during treatment with clopidogrel and/or aspirin. Platelets20(4), 250–259 (2009).
  • Sofi F, Marcucci R, Gori AM et al. Clopidogrel non-responsiveness and risk of cardiovascular morbidity. An updated meta-analysis. Thromb. Haemost.103(4), 841–848 (2010).
  • Kunadian B, Thornley AR, Tanos M, Dunning J. Should clopidogrel be stopped prior to urgent cardiac surgery? Interact. Cardiovasc. Thorac. Surg.5(5), 630–636 (2006).
  • Wiviott SD, Braunwald E, McCabe CH et al. Prasugrel versus clopidogrel in patients with acute coronary syndromes. N. Engl. J. Med.357(20), 2001–2015 (2007).
  • van Giezen JJ, Nilsson L, Berntsson P et al. Ticagrelor binds to human P2Y(12) independently from ADP but antagonizes ADP-induced receptor signaling and platelet aggregation. J. Thromb. Haemost.7(9), 1556–1565 (2009).
  • Teng R, Oliver S, Hayes MA, Butler K. Absorption, distribution, metabolism, and excretion of ticagrelor in healthy subjects. Drug Metab. Dispos.38(9), 1514–1521 (2010).
  • Husted S, van Giezen JJ. Ticagrelor: the first reversibly binding oral P2Y12 receptor antagonist. Cardiovasc. Ther.27(4), 259–274 (2009).
  • Högberg C, Svensson H, Gustafsson R, Eyjolfsson A, Erlinge D. The reversible oral P2Y12 antagonist AZD6140 inhibits ADP-induced contractions in murine and human vasculature. Int. J. Cardiol.142(2), 187–192 (2010).
  • van Giezen JJ, Sidaway J, Glaves P, Kirk I, Björkman JA. Ticagrelor inhibits adenosine uptake in vitro and enhances adenosine-mediated hyperemia responses in a canine model. J. Cardiovasc. Pharmacol. Ther. doi:10.1177/1074248411410883 (2011) (Epub ahead of print).
  • Ohman J, Kudira R, Albinsson S et al. Ticagrelor induces adenosine triphosphate release from human red blood cells. Biochem. Biophys. Res. Commun.418(4), 754–758 (2012).
  • Burki NK, Dale WJ, Lee LY. Intravenous adenosine and dyspnea in humans. J. Appl. Physiol.98(1), 180–185 (2005).
  • Iyú D, Glenn JR, White AE, Fox SC, Heptinstall S. Adenosine derived from ADP can contribute to inhibition of platelet aggregation in the presence of a P2Y12 antagonist. Arterioscl. Thromb. Vasc. Biol.31(2), 416–422 (2011).
  • Husted S, Emanuelsson H, Heptinstall S et al. Pharmacodynamics, pharmacokinetics, and safety of the oral reversible P2Y12 antagonist AZD6140 with aspirin in patients with atherosclerosis: a double-blind comparison to clopidogrel with aspirin. Eur. Heart J.27(9), 1038–1047 (2006).
  • Cannon CP, Husted S, Harrington RA et al. 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. J. Am. Coll. Cardiol.50(19), 1844–1851 (2007).
  • Storey RF, Husted S, Harrington RA 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.50(19), 1852–1856 (2007).
  • Gurbel PA, Bliden KP, Butler K et al. Randomized double-blind assessment of the ONSET and OFFSET of the antiplatelet effects of ticagrelor versus clopidogrel in patients with stable coronary artery disease: the ONSET/OFFSET study. Circulation120(25), 2577–2585 (2009).
  • Gurbel PA, Bliden KP, Butler K et al. Response to ticagrelor in clopidogrel nonresponders and responders and effect of switching therapies: the RESPOND study. Circulation121(10), 1188–1199 (2010).
  • James S, Akerblom A, Cannon CP et al. Comparison of ticagrelor, the first reversible oral P2Y(12) receptor antagonist, with clopidogrel in patients with acute coronary syndromes: rationale, design, and baseline characteristics of the Platelet Inhibition and Patient Outcomes (PLATO) trial. Am. Heart J.157(4), 599–605 (2009).
  • Wallentin L, Becker RC, Budaj A et al. Ticagrelor versus clopidogrel in patients with acute coronary syndromes. N. Engl. J. Med.361(11), 1045–1057 (2009).
  • Storey RF, Angiolillo DJ, Patil SB et al. Inhibitory effects of ticagrelor compared with clopidogrel on platelet function in patients with acute coronary syndromes: the PLATO (Platelet Inhibition and Patient Outcomes) PLATELET substudy. J. Am. Coll. Cardiol.56(18), 1456–1462 (2010).
  • Butler K, Teng R. Pharmacokinetics, pharmacodynamics, safety and tolerability of multiple ascending doses of ticagrelor in healthy volunteers. Br. J. Clin. Pharmacol.70(1), 65–77 (2010).
  • Butler K. Pharmacokinetics, pharmacodynamics, and safety of ticagrelor in volunteers with severe renal impairment. J. Clin. Pharmacol. doi:10.1177/0091270011415526 (2011) (Epub ahead of print).
  • Teng R, Mitchell PD, Butler K. Lack of significant food effect on the pharmacokinetics of ticagrelor in healthy volunteers. J. Clin. Pharm. Ther. doi:10.1111/j.1365-2710.2011.01307.x (2011) (Epub ahead of print).
  • Disney BR, Watson RDS, Blann AD, Lip GYH, Anderson MR. Proton pump inhibitors with clopidogrel. Evidence for and against a clinically-important interaction. Aliment. Pharmacol. Ther.33(7), 758–767 (2011).
  • Goodman SG, Clare R, Pieper KS et al. Association of proton pump inhibitor use on cardiovascular outcomes with clopidogrel and ticagrelor: insights from PLATO. Circulation125(8), 978–986 (2012).
  • Serebruany VL. Viewpoint: paradoxical excess mortality in the PLATO trial should be independently verified. Thromb. Haemost.105(5), 752–759 (2011).
  • Wallentin L, Becker RC, James SK, Harrington RA. The PLATO trial reveals further opportunities to improve outcomes in patients with acute coronary syndrome. Thromb. Haemost.105(5), 760–762 (2011).
  • Ohman EM, Roe MT. Explaining the unexpected: insights from the Platelet Inhibition and Clinical Outcomes (PLATO) trial comparing ticagrelor and clopidogrel. Thromb. Haemost.105(5), 763–765 (2011).
  • Mahaffey KW, Wojdyla DM, Carroll K et al. Ticagrelor compared with clopidogrel by geographic region in the platelet inhibition and patient outcomes (PLATO) trial. Circulation124(5), 544–554 (2011).
  • Fox SC, Behan MWH, Heptinstall S. Inhibition of ADP-induced intracellular Ca2+ responses and platelet aggregation by the P2Y12 receptor antagonists AR-C69931MX and clopidogrel is enhanced by prostaglandin E1. Cell Calcium35(1), 39–46 (2004).
  • Cattaneo M, Lecchi A. Inhibition of the platelet P2Y12 receptor for adenosine diphosphate potentiates the antiplatelet effect of prostacyclin. J. Thromb. Haemost.5(3), 577–582 (2007).
  • Iyú D, Glenn JR, White AE, Fox SC, Dovlatova N, Heptinstall S. P2Y(12) and EP3 antagonists promote the inhibitory effects of natural modulators of platelet aggregation that act via cAMP. Platelets22(7), 504–515 (2011).
  • Cannon CP, Harrington RA, James S et al. Comparison of ticagrelor with clopidogrel in patients with a planned invasive strategy for acute coronary syndromes (PLATO): a randomised double-blind study. Lancet375(9711), 283–293 (2010).
  • Steg PG, James S, Harrington RA et al. Ticagrelor versus clopidogrel in patients with ST-elevation acute coronary syndromes intended for reperfusion with primary percutaneous coronary intervention: a Platelet Inhibition and Patient Outcomes (PLATO) trial subgroup analysis. Circulation122(21), 2131–2141 (2010).
  • Armstrong PW, Siha H, Fu Y et al. Elevation acute coronary syndromes in PLATO: insights from the ECG substudy. Circulation125(3), 514–521 (2012).
  • Held C, Asenblad N, Bassand JP et al. Ticagrelor versus clopidogrel in patients with acute coronary syndromes undergoing coronary artery bypass surgery: results from the PLATO (Platelet Inhibition and Patient Outcomes) trial. J. Am. Coll. Cardiol.57(6), 672–684 (2011).
  • James SK, Roe MT, Cannon CP et al. Ticagrelor versus clopidogrel in patients with acute coronary syndromes intended for noninvasive management: substudy from prospective randomised Platelet Inhibition and Patient Outcomes (PLATO) trial. Br. Med. J.342, D3527 (2011).
  • James S, Angiolillo DJ, Cornel JH et al. Ticagrelor vs clopidogrel in patients with acute coronary syndromes and diabetes: a substudy from the Platelet Inhibition and Patient Outcomes (PLATO) trial. Eur. Heart J.31(24), 3006–3016 (2010).
  • James S, Budaj A, Aylward P et al. Ticagrelor versus clopidogrel in acute coronary syndromes in relation to renal function: results from the Platelet Inhibition and Patient Outcomes (PLATO) trial. Circulation122(11), 1056–1067 (2010).
  • Becker RC, Bassand JP, Budaj A et al. Bleeding complications with the P2Y12 receptor antagonists clopidogrel and ticagrelor in the Platelet Inhibition and Patient Outcomes (PLATO) trial. Eur. Heart J.32, 2933–2944 (2011).
  • Storey RF, Becker RC, Harrington RA et al. Pulmonary function in patients with acute coronary syndrome treated with ticagrelor or clopidogrel (from the Platelet Inhibition and Patient Outcomes [PLATO] pulmonary function substudy). Am. J. Cardiol.108(11), 1542–1546 (2011).
  • Butler K, Teng R. Evaluation and characterization of the effects of ticagrelor on serum and urinary uric acid in healthy volunteers. Clin. Pharmacol. Ther.91(2), 264–271 (2012).
  • Zhou D, Andersson TB, Grimm SW. In vitro evaluation of potential drug–drug interactions with ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics. Drug Metab. Dispos.39(4), 703–710 (2011).

Websites

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.