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Effects of genetic variation in protease activated receptor 4 after an acute coronary syndrome: Analysis from the TRACER trial.

Tricoci P, Neely M, Whitley MJ, Edelstein LC, Simon LM, Shaw C, Fortina P, Moliterno DJ, Armstrong PW, Aylward P, White H, Van de Werf F, Jennings LK, Wallentin L, Held C, Harrington RA, Mahaffey KW, Bray PF.

Blood Cells Mol Dis. 2018 Sep;72:37-43. doi: 10.1016/j.bcmd.2018.07.004. Epub 2018 Jul 21.


Protease-activated receptor-4 (PAR4) variant influences on platelet reactivity induced by PAR4-activating peptide through altered Ca2+ mobilization and ERK phosphorylation in healthy Japanese subjects.

Morikawa Y, Kato H, Kashiwagi H, Nishiura N, Akuta K, Honda S, Kanakura Y, Tomiyama Y.

Thromb Res. 2018 Feb;162:44-52. doi: 10.1016/j.thromres.2017.12.014. Epub 2017 Dec 24.


PAR1 antagonists inhibit thrombin-induced platelet activation whilst leaving the PAR4-mediated response intact.

Judge HM, Jennings LK, Moliterno DJ, Hord E, Ecob R, Tricoci P, Rorick T, Kotha J, Storey RF.

Platelets. 2015;26(3):236-42. doi: 10.3109/09537104.2014.902924. Epub 2014 Apr 21.


A function-blocking PAR4 antibody is markedly antithrombotic in the face of a hyperreactive PAR4 variant.

French SL, Thalmann C, Bray PF, Macdonald LE, Murphy AJ, Sleeman MW, Hamilton JR.

Blood Adv. 2018 Jun 12;2(11):1283-1293. doi: 10.1182/bloodadvances.2017015552.


Efficacy and Safety of Vorapaxar in Non-ST-Segment Elevation Acute Coronary Syndrome Patients Undergoing Noncardiac Surgery.

van Diepen S, Tricoci P, Podder M, Westerhout CM, Aylward PE, Held C, Van de Werf F, Strony J, Wallentin L, Moliterno DJ, White HD, Mahaffey KW, Harrington RA, Armstrong PW.

J Am Heart Assoc. 2015 Dec 15;4(12). pii: e002546. doi: 10.1161/JAHA.115.002546.


Common variants in the human platelet PAR4 thrombin receptor alter platelet function and differ by race.

Edelstein LC, Simon LM, Lindsay CR, Kong X, Teruel-Montoya R, Tourdot BE, Chen ES, Ma L, Coughlin S, Nieman M, Holinstat M, Shaw CA, Bray PF.

Blood. 2014 Nov 27;124(23):3450-8. doi: 10.1182/blood-2014-04-572479. Epub 2014 Oct 7.


Effect of age on efficacy and safety of vorapaxar in patients with non-ST-segment elevation acute coronary syndrome: Insights from the Thrombin Receptor Antagonist for Clinical Event Reduction in Acute Coronary Syndrome (TRACER) trial.

Armaganijan LV, Alexander KP, Huang Z, Tricoci P, Held C, Van de Werf F, Armstrong PW, Aylward PE, White HD, Moliterno DJ, Wallentin L, Chen E, Harrington RA, Strony J, Mahaffey KW, Lopes RD.

Am Heart J. 2016 Aug;178:176-84. doi: 10.1016/j.ahj.2016.05.012. Epub 2016 Jun 9.


The protease-activated receptor 4 Ala120Thr variant alters platelet responsiveness to low-dose thrombin and protease-activated receptor 4 desensitization, and is blocked by non-competitive P2Y12 inhibition.

Whitley MJ, Henke DM, Ghazi A, Nieman M, Stoller M, Simon LM, Chen E, Vesci J, Holinstat M, McKenzie SE, Shaw CA, Edelstein LC, Bray PF.

J Thromb Haemost. 2018 Dec;16(12):2501-2514. doi: 10.1111/jth.14318. Epub 2018 Nov 22.


Use of thienopyridine prior to presentation with non-ST-segment elevation acute coronary syndrome and association with safety and efficacy of vorapaxar: insights from the TRACER trial.

Harskamp RE, Clare RM, Ambrosio G, Held C, Lokhnygina Y, Moliterno DJ, White HD, Aylward PE, Armstrong PW, Mahaffey KW, Harrington RA, Van de Werf F, Wallentin L, Strony J, Tricoci P.

Eur Heart J Acute Cardiovasc Care. 2017 Mar;6(2):155-163. doi: 10.1177/2048872616633880. Epub 2016 Sep 20.


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).

Whellan DJ, Tricoci P, Chen E, Huang Z, Leibowitz D, Vranckx P, Marhefka GD, Held C, Nicolau JC, Storey RF, Ruzyllo W, Huber K, Sinnaeve P, Weiss AT, Dery JP, Moliterno DJ, Van de Werf F, Aylward PE, White HD, Armstrong PW, Wallentin L, Strony J, Harrington RA, Mahaffey KW.

J Am Coll Cardiol. 2014 Mar 25;63(11):1048-57. doi: 10.1016/j.jacc.2013.10.048. Epub 2013 Nov 21.


Thrombin-receptor antagonist vorapaxar in acute coronary syndromes.

Tricoci P, Huang Z, Held C, Moliterno DJ, Armstrong PW, Van de Werf F, White HD, Aylward PE, Wallentin L, Chen E, Lokhnygina Y, Pei J, Leonardi S, Rorick TL, Kilian AM, Jennings LH, Ambrosio G, Bode C, Cequier A, Cornel JH, Diaz R, Erkan A, Huber K, Hudson MP, Jiang L, Jukema JW, Lewis BS, Lincoff AM, Montalescot G, Nicolau JC, Ogawa H, Pfisterer M, Prieto JC, Ruzyllo W, Sinnaeve PR, Storey RF, Valgimigli M, Whellan DJ, Widimsky P, Strony J, Harrington RA, Mahaffey KW; TRACER Investigators.

N Engl J Med. 2012 Jan 5;366(1):20-33. doi: 10.1056/NEJMoa1109719. Epub 2011 Nov 13.


Effects of vorapaxar on platelet reactivity and biomarker expression in non-ST-elevation acute coronary syndromes. The TRACER Pharmacodynamic Substudy.

Storey RF, Kotha J, Smyth SS, Moliterno DJ, Rorick TL, Moccetti T, Valgimigli M, Dery JP, Cornel JH, Thomas GS, Huber K, Harrington RA, Hord E, Judge HM, Chen E, Strony J, Mahaffey KW, Tricoci P, Becker RC, Jennings LK.

Thromb Haemost. 2014 May 5;111(5):883-91. doi: 10.1160/TH13-07-0624. Epub 2014 Jan 9.


Enhanced potency of prasugrel on protease-activated receptors following bivalirudin treatment for PCI as compared to clopidogrel.

Kimmelstiel C, Stevenson R, Nguyen N, Van Doren L, Zhang P, Perkins J, Kapur NK, Weintraub A, Castaneda V, Kuliopulos A, Covic L.

Thromb Res. 2019 May;177:59-69. doi: 10.1016/j.thromres.2019.01.017. Epub 2019 Feb 13.


Genetic Variant in Human PAR (Protease-Activated Receptor) 4 Enhances Thrombus Formation Resulting in Resistance to Antiplatelet Therapeutics.

Tourdot BE, Stoveken H, Trumbo D, Yeung J, Kanthi Y, Edelstein LC, Bray PF, Tall GG, Holinstat M.

Arterioscler Thromb Vasc Biol. 2018 Jul;38(7):1632-1643. doi: 10.1161/ATVBAHA.118.311112. Epub 2018 May 10.


Protease-Activated Receptor 4 Variant p.Tyr157Cys Reduces Platelet Functional Responses and Alters Receptor Trafficking.

Norman JE, Cunningham MR, Jones ML, Walker ME, Westbury SK, Sessions RB, Mundell SJ, Mumford AD.

Arterioscler Thromb Vasc Biol. 2016 May;36(5):952-60. doi: 10.1161/ATVBAHA.115.307102. Epub 2016 Mar 10.


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).

Cornel JH, Tricoci P, Lokhnygina Y, Moliterno DJ, Wallentin L, Armstrong PW, Aylward PE, Clare RM, Chen E, Leonardi S, Van de Werf F, White HD, Held C, Strony J, Mahaffey KW, Harrington RA.

Am J Cardiol. 2015 May 15;115(10):1325-32. doi: 10.1016/j.amjcard.2015.02.043. Epub 2015 Feb 18.


Vorapaxar, a Protease-Activated Receptor-1 Antagonist, a Double-Edged Sword!

Bhandari B, Mehta B.

Recent Adv Cardiovasc Drug Discov. 2014;9(2):73-7. Review.


Safety and efficacy of protease-activated receptor-1 antagonists in patients with coronary artery disease: a meta-analysis of randomized clinical trials.

Capodanno D, Bhatt DL, Goto S, O'Donoghue ML, Moliterno DJ, Tamburino C, Angiolillo DJ.

J Thromb Haemost. 2012 Oct;10(10):2006-15. doi: 10.1111/j.1538-7836.2012.04869.x.


Pharmacokinetic drug evaluation of vorapaxar for secondary prevention after acute coronary syndrome.

Perez-Rivera JA, Monedero-Campo J, Cieza-Borrella C, Ruiz-Perez P.

Expert Opin Drug Metab Toxicol. 2017 Mar;13(3):339-350. doi: 10.1080/17425255.2017.1289175. Epub 2017 Feb 7. Review.


Inhibition of protease-activated receptor 4 impairs platelet procoagulant activity during thrombus formation in human blood.

French SL, Arthur JF, Lee H, Nesbitt WS, Andrews RK, Gardiner EE, Hamilton JR.

J Thromb Haemost. 2016 Aug;14(8):1642-54. doi: 10.1111/jth.13293. Epub 2016 Jun 22.

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