Vorapaxar in the secondary prevention of atherothrombosis

References

• Gurbel PA, Kuliopulos A, Tantry US. G-protein-coupled receptors signaling pathways in new antiplatelet drug development. Arterioscler Thromb Vasc Biol. 2015;35:500–512.
   PubMed Web of Science ®Google Scholar
• Zhang P, Covic L, Kuliopulos A. Protease-activated receptors. In: Michelson AD, editor. Platelets. 3rd ed. San Diego (CA): Academic Press; 2013. p. 249–259.
   Google Scholar
• Wiviott SD, Braunwald E, McCabe CH, et al. TRITON-TIMI 38 Investigators. Prasugrel versus clopidogrel in patients with acute coronary syndromes. N Engl J Med. 2007;357:2001–2015.
   PubMed Web of Science ®Google Scholar
• Wallentin L, Becker RC, Budaj A, et al. Ticagrelor versus clopidogrel in patients with acute coronary syndromes. N Engl J Med. 2009;361:1045–1057.
   PubMed Web of Science ®Google Scholar
• Silvain J, Collet JP, Nagaswami C, et al. Composition of coronary thrombus in acute myocardial infarction. J Am Coll Cardiol. 2011;57:1359–1367.
   PubMed Web of Science ®Google Scholar
• Yunoki K, Naruko T, Sugioka K, et al. Erythrocyte-rich thrombus aspirated from patients with ST-elevation myocardial infarction: association with oxidative stress and its impact on myocardial reperfusion. Eur Heart J. 2012;33:1480–1490.
   PubMed Web of Science ®Google Scholar
• Ardissino D, Merlini PA, Bauer KA, et al. Coagulation activation and long-term outcome in acute coronary syndromes. Blood. 2003;102:2731–2735.
   PubMed Web of Science ®Google Scholar
• Undas A, Szułdrzyński K, Brummel-Ziedins KE, et al. Systemic blood coagulation activation in acute coronary syndromes. Blood. 2009;113:2070–2078.
   PubMed Web of Science ®Google Scholar
• Skeppholm M, Kallner A, Malmqvist K, et al. Is fibrin formation and thrombin generation increased during and after an acute coronary syndrome? Thromb Res. 2011;128:483–489.
   PubMed Web of Science ®Google Scholar
• Rothberg MB, Celestin C, Fiore LD, et al. Warfarin plus aspirin after myocardial infarction or the acute coronary syndrome: meta-analysis with estimates of risk and benefit. Ann Intern Med. 2005;143:241–250.
   PubMed Web of Science ®Google Scholar
• Komócsi A, Vorobcsuk A, Kehl D, et al. Use of new-generation oral anticoagulant agents in patients receiving antiplatelet therapy after an acute coronary syndrome: systematic review and meta-analysis of randomized controlled trials. Arch Intern Med. 2012;172:1537–1545.
   PubMed Web of Science ®Google Scholar
• Leger AJ, Jacques SL, Badar J, et al. Blocking the protease-activated receptor 1-4 heterodimer in platelet-mediated thrombosis. Circulation. 2006;113:1244–1254.
   PubMed Web of Science ®Google Scholar
• Gieseler F, Ungefroren H, Settmacher U, et al. Proteinase-activated receptors (PARs) - focus on receptor-receptor-interactions and their physiological and pathophysiological impact. Cell Commun Signal. 2013;11:86.
   PubMed Web of Science ®Google Scholar
• Ramachandran R, Noorbakhsh F, Defea K, et al. Targeting proteinase-activated receptors: therapeutic potential and challenges. Nat Rev Drug Discov. 2012;11:69–86.
   PubMed Web of Science ®Google Scholar
• Brass LF, Vassallo RR Jr, Belmonte E, et al. Structure and function of the human platelet thrombin receptor. Studies using monoclonal antibodies directed against a defined domain within the receptor N terminus. J Biol Chem. 1992;267:13795–13798.
   PubMed Web of Science ®Google Scholar
• Gurbel PA, Jeong YH, Tantry US. Vorapaxar: a novel protease-activated receptor-1 inhibitor. Expert Opin Investig Drugs. 2011;20:1445–1453.
   PubMed Web of Science ®Google Scholar
• Zhang P, Gruber A, Kasuda S, et al. Suppression of arterial thrombosis without affecting hemostatic parameters with a cell-penetrating PAR1 pepducin. Circulation. 2012;126:83–91.
   PubMed Web of Science ®Google Scholar
• FDA approves Zontivity to reduce the risk of heart attacks and stroke in high-risk patients [Internet; cited 2015 Oct 15]. Available from: http://www.fda.gov/newsevents/newsroom/pressannouncements/ucm396585.htm.
   Google Scholar
• Zhang C, Srinivasan Y, Arlow DH, et al. High-resolution crystal structure of human protease-activated receptor 1. Nature. 2012;492:387–392.
   PubMed Web of Science ®Google Scholar
• Ghosal A, Lu X, Penner N, et al. Identification of human liver cytochrome P450 enzymes involved in the metabolism of SCH 530348 (vorapaxar), a potent oral thrombin protease-activated receptor 1 antagonist. Drug Metab Dispos. 2011;39:30–38.
   PubMed Web of Science ®Google Scholar
• Chackalamannil S, Wang Y, Greenlee WJ, et al. Discovery of a novel, orally active himbacine-based thrombin receptor antagonist (SCH 530348) with potent antiplatelet activity. J Med Chem. 2008;51:3061–3064.
   PubMed Web of Science ®Google Scholar
• Fowkes FG, Price JF, Stewart MC, et al. Aspirin for asymptomatic atherosclerosis trialists. Aspirin for prevention of cardiovascular events in a general population screened for a low ankle brachial index: a randomized controlled trial. JAMA. 2010;303:841–848.
   PubMed Web of Science ®Google Scholar
• Hawes BE, Zhai Y, Hesk D, et al. In vitro pharmacological characterization of vorapaxar, a novel platelet thrombin receptor antagonist. Eur J Pharmacol. 2015;762:221–228.
   PubMed Web of Science ®Google Scholar
• Kosoglou T, Reyderman L, Tiessen RG, et al. Pharmacodynamics and pharmacokinetics of the novel PAR-1 antagonist vorapaxar (formerly SCH 530348) in healthy subjects. Eur J Clin Pharmacol. 2012;68:249–258.
   PubMed Web of Science ®Google Scholar
• Becker RC, Moliterno DJ, Jennings LK, et al. Safety and tolerability of SCH 530348 in patients undergoing non-urgent percutaneous coronary intervention: a randomised, double-blind, placebo-controlled phase II study. Lancet. 2009;373:919–928.
   PubMed Web of Science ®Google Scholar
• Cavender MA, Scirica BM, Bonaca MP, et al. Vorapaxar in patients with diabetes mellitus and previous myocardial infarction: findings from the thrombin receptor antagonist in secondary prevention of atherothrombotic ischemic events-TIMI 50 trial. Circulation. 2015;131:1047–1053.
   PubMed Web of Science ®Google Scholar
• Goto S, Yamaguchi T, Ikeda Y, et al. Safety and exploratory efficacy of the novel thrombin receptor (PAR-1) antagonist SCH530348 for non-ST-segment elevation acute coronary syndrome. J Atheroscler Thromb. 2010;17:156–164.
   PubMed Web of Science ®Google Scholar
• Tricoci P, Huang Z, Held C, et al. TRACER Investigators. Thrombin-receptor antagonist vorapaxar in acute coronary syndromes. N Engl J Med. 2012;366:20–33.
   PubMed Web of Science ®Google Scholar
• Valgimigli M, Tricoci P, Huang Z, et al. Usefulness and safety of vorapaxar in patients with non-ST-segment elevation acute coronary syndrome undergoing percutaneous coronary intervention (from the TRACER Trial). Am J Cardiol. 20141;114:665–673.
   PubMed Web of Science ®Google Scholar
• Cornel JH, Tricoci P, Lokhnygina Y, et al. Glycoprotein IIb/IIIa receptor inhibitors in combination with vorapaxar, a platelet thrombin receptor antagonist, among patients with non-st-segment elevation acute coronary syndromes (from the TRACER Trial). Am J Cardiol. 2015;115:1325–1332.
   PubMed Web of Science ®Google Scholar
• Held C, Tricoci P, Huang Z, et al. Vorapaxar, a platelet thrombin-receptor antagonist, in medically managed patients with non-ST-segment elevation acute coronary syndrome: results from the TRACER trial. Eur Heart J Acute Cardiovasc Care. 2014;3:246–256.
   PubMedGoogle Scholar
• Whellan DJ, Tricoci P, Chen E, et al. Vorapaxar in acute coronary syndrome patients undergoing coronary artery bypass graft surgery: subgroup analysis from the TRACER trial (thrombin receptor antagonist for clinical event reduction in acute coronary syndrome). J Am Coll Cardiol. 2014;63:1048–1057.
   PubMed Web of Science ®Google Scholar
• Jones WS, Tricoci P, Huang Z, et al. Vorapaxar in patients with peripheral artery disease and acute coronary syndrome: insights from thrombin receptor antagonist for clinical event reduction in acute coronary syndrome (TRACER). Am Heart J. 2014;168:588–596.
   PubMed Web of Science ®Google Scholar
• Tricoci P, Lokhnygina Y, Huang Z, et al. Vorapaxar with or without clopidogrel after non-ST-segment elevation acute coronary syndromes: results from the thrombin receptor antagonist for clinical event reduction in acute coronary syndrome trial. Am Heart J. 2014;168:869-77.e1.
   Web of Science ®Google Scholar
• Mahaffey KW, Huang Z, Wallentin L, et al. Association of aspirin dose and vorapaxar safety and efficacy in patients with non-ST-segment elevation acute coronary syndrome (from the TRACER Trial). Am J Cardiol. 2014;113:936–944.
   PubMed Web of Science ®Google Scholar
• Morrow DA, Braunwald E, Bonaca MP, et al. TRA 2P–TIMI 50 Steering Committee and Investigators. Vorapaxar in the secondary prevention of atherothrombotic events. N Engl J Med. 2012;366:1404–1413.
   PubMed Web of Science ®Google Scholar
• Bhatt DL, Flather MD, Hacke W, et al. CHARISMA investigators. Patients with prior myocardial infarction, stroke, or symptomatic peripheral arterial disease in the CHARISMA trial. J Am Coll Cardiol. 2007;49:1982–1988.
   PubMed Web of Science ®Google Scholar
• Magnani G, Bonaca MP, Braunwald E, et al. Efficacy and safety of vorapaxar as approved for clinical use in the United States. J Am Heart Assoc. 2015;4:e001505.
   PubMed Web of Science ®Google Scholar
• Scirica BM, Bonaca MP, Braunwald E, et al. TRA 2°P-TIMI 50 Steering Committee Investigators. Vorapaxar for secondary prevention of thrombotic events for patients with previous myocardial infarction: a prespecified subgroup analysis of the TRA 2°P-TIMI 50 trial. Lancet. 2012;380:1317–1324.
   PubMed Web of Science ®Google Scholar
• Bonaca MP, Scirica BM, Braunwald E, et al. Coronary stent thrombosis with vorapaxar versus placebo: results from the TRA 2° P-TIMI 50 trial. J Am Coll Cardiol. 2014;64:2309–2317.
   PubMed Web of Science ®Google Scholar
• Morrow DA, Alberts MJ, Mohr JP, et al. Thrombin receptor antagonist in secondary prevention of atherothrombotic ischemic events–TIMI 50 steering committee and investigators. efficacy and safety of vorapaxar in patients with prior ischemic stroke. Stroke. 2013;44:691–698.
   PubMed Web of Science ®Google Scholar
• Bonaca MP, Scirica BM, Braunwald E, et al. New ischemic stroke and outcomes with vorapaxar versus placebo: results from the TRA 2 °P-TIMI 50 trial. J Am Coll Cardiol. 2014;64:2318–2326.
   PubMed Web of Science ®Google Scholar
• Alonso-Coello P, Bellmunt S, McGorrian C, et al. American college of chest physicians. antithrombotic therapy in peripheral artery disease: antithrombotic therapy and prevention of thrombosis, 9th ed: American College of Chest Physicians evidence-based clinical practice guidelines. Chest. 2012;141(2 Suppl):e669S–e690S.
   PubMed Web of Science ®Google Scholar
• Bonaca MP, Scirica BM, Creager MA, et al. Vorapaxar in patients with peripheral artery disease: results from TRA20P-TIMI 50. Circulation. 2013;127:1522–1529.
   PubMed Web of Science ®Google Scholar
• Zontivity [Internet; cited 2015 Oct 15]. Available from: http://www.ema.europa.eu/ema/index.jsp?curl=pages/medicines/human/medicines/002814/human_med_001839.jsp&mid=WC0b01ac058001d124.
   Google Scholar