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image of Brilinta (Ticagrelor): A Comprehensive Review of its Pharmacology, Clinical Efficacy, and Safety Profile

Abstract

Brilinta, a recently introduced oral P2Y12 inhibitor, is widely used as a potent antiplatelet agent, especially in the management of acute coronary syndromes (ACS) and related thrombotic disorders. Unlike traditional thienopyridines such as clopidogrel, which irreversibly inhibit the P2Y12 receptor, Brilinta reversibly inhibits it, leading to more consistent and potent platelet aggregation suppression. This distinct pharmacokinetic and pharmacodynamic profile results in a rapid onset and offset of action, minimizing interpatient variability and addressing limitations seen with existing P2Y12 inhibitors. Beyond ACS, Brilinta is being evaluated for its potential benefits in ischemic stroke, peripheral artery disease, and post-coronary artery bypass grafting (CABG) management. One of its key advantages is its pleiotropic effects, particularly its ability to increase adenosine concentration, which may contribute to enhanced vascular protection and additional survival benefits not observed with conventional therapies. Brilinta belongs to the cyclopentyl-triazolo-pyrimidine class, which exhibits high resistance to enzymatic degradation. This characteristic is essential because it allows for more stable and effective P2Y12 receptor inhibition, overcoming the limitations of adenosine triphosphate (ATP) as a direct pharmacological competitor of adenosine diphosphate (ADP). Overall, Brilinta represents a significant advancement in antiplatelet therapy, offering enhanced efficacy, improved safety, and expanded clinical applications. By offering a reversible, potent, and consistent inhibition of platelet aggregation, Brilinta has demonstrated superiority over clopidogrel in ACS treatment and shows promise in expanding its clinical indications. Its unique mechanism of action, combined with its rapid onset and cessation of effects, positions Brilinta as a key advancement in antiplatelet therapy, with the potential to enhance results across a broader range of vascular and thrombotic conditions.

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2025-10-02
2025-12-15
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References

  1. Kubisa M. Jeżewski M.P. Gasecka A. Siller-Matula J. Postuła M. Ticagrelor – toward more efficient platelet inhibition and beyond. Ther. Clin. Risk Manag. 2018 14 129 140 10.2147/TCRM.S152369 29398917
    [Google Scholar]
  2. Zègre-Hemsey J.K. Asafu-Adjei J. Fernandez A. Brice J. Characteristics of prehospital electrocardiogram use in North Carolina using a novel linkage of emergency medical services and emergency department data. Prehosp. Emerg. Care 2019 23 6 772 779 10.1080/10903127.2019.1597230 30885071
    [Google Scholar]
  3. Alomari M. Bratton H. Musmar A. Al Momani L.A. Young M. Ticagrelor-induced diarrhea in a patient with acute coronary syndrome requiring percutaneous coronary artery intervention. Cureus 2019 11 1 e3874 10.7759/cureus.3874 30899625
    [Google Scholar]
  4. Kerneis M. Nafee T. Yee M.K. Most promising therapies in interventional cardiology. Curr. Cardiol. Rep. 2019 21 4 26 10.1007/s11886‑019‑1108‑x 30868280
    [Google Scholar]
  5. Voudris K.V. Kavinsky C.J. Advances in management of stable coronary artery disease: The role of revascularization? Curr. Treat. Options Cardiovasc. Med. 2019 21 3 15 10.1007/s11936‑019‑0720‑9 30854580
    [Google Scholar]
  6. Singh A. Museedi A.S. Grossman S.A. Acute coronary syndrome. StatPearls. Treasure Island, FL StatPearls Publishing 2025 29083796
    [Google Scholar]
  7. Husted S. Van Giezen J.J.J. Ticagrelor: The first reversibly binding oral P2Y12 receptor antagonist. Cardiovasc. Ther. 2009 27 4 259 274 10.1111/j.1755‑5922.2009.00096.x 19604248
    [Google Scholar]
  8. Capodanno D. Alfonso F. Levine G.N. Valgimigli M. Angiolillo D.J. ACC/AHA versus ESC guidelines on dual antiplatelet therapy. J. Am. Coll. Cardiol. 2018 72 23 2915 2931 10.1016/j.jacc.2018.09.057 30522654
    [Google Scholar]
  9. Roffi M. Patrono C. Collet J.P. 2015 ESC guidelines for the management of acute coronary syndromes in patients presenting without persistent ST-segment elevation. Eur. Heart J. 2016 37 3 267 315 ESC Scientific Document Group. 10.1093/eurheartj/ehv320 26320110
    [Google Scholar]
  10. Valgimigli M. Bueno H. Byrne R.A. 2017 ESC focused update on dual antiplatelet therapy in coronary artery disease developed in collaboration with EACTS. Eur. Heart J. 2018 39 3 213 260 ESC Scientific Document Group; ESC Committee for Practice Guidelines (CPG); ESC National Cardiac Societies 10.1093/eurheartj/ehx419 28886622
    [Google Scholar]
  11. Umińska J.M. Ratajczak J. Pstrągowski K. The impact of mild therapeutic hypothermia on platelet reactivity in comatose survivors of cardiac arrest with acute myocardial infarction treated with ticagrelor. Cardiol. J. 2024 31 3 472 478 10.5603/CJ.a2022.0029 35514087
    [Google Scholar]
  12. Vranckx P. Valgimigli M. Jüni P. Ticagrelor plus aspirin for 1 month, followed by ticagrelor monotherapy for 23 months vs aspirin plus clopidogrel or ticagrelor for 12 months, followed by aspirin monotherapy for 12 months after implantation of a drug-eluting stent: A multicentre, open-label, randomised superiority trial. Lancet 2018 392 10151 940 949 GLOBAL LEADERS Investigators. 10.1016/S0140‑6736(18)31858‑0 30166073
    [Google Scholar]
  13. Linden M.D. Jackson D.E. Platelets: Pleiotropic roles in atherogenesis and atherothrombosis. Int. J. Biochem. Cell Biol. 2010 42 11 1762 1766 10.1016/j.biocel.2010.07.012 20673808
    [Google Scholar]
  14. Li C. Liu M. Chen W. Jiang T. Ling L. Comparison of ticagrelor and clopidogrel on platelet function and prognosis in unstable angina. Eur. J. Clin. Pharmacol. 2022 78 12 1949 1958 10.1007/s00228‑022‑03401‑3 36245047
    [Google Scholar]
  15. Dutta S. Harlequin ichthyosis: A brief discussion. Res J Pharm Technol 2015 8 5 587 10.5958/0974‑360X.2015.00098.0
    [Google Scholar]
  16. Fuller R Chavez B. Ticagrelor (brilinta), An antiplatelet drug for acute coronary syndrome 2012 37 10 562 8 23115464
  17. Franzone A. McFadden E.P. Leonardi S. Ticagrelor alone or conventional dual antiplatelet therapy in patients with stable or acute coronary syndromes. EuroIntervention 2020 16 8 627 633 10.4244/EIJ‑D‑20‑00145 32482616
    [Google Scholar]
  18. Htun W.W. Steinhubl S.R. Ticagrelor: The first novel reversible P2Y 12 inhibitor. Expert Opin. Pharmacother. 2013 14 2 237 245 10.1517/14656566.2013.757303 23268703
    [Google Scholar]
  19. Wallentin L. Varenhorst C. James S. Prasugrel achieves greater and faster P2Y12receptor-mediated platelet inhibition than clopidogrel due to more efficient generation of its active metabolite in aspirin-treated patients with coronary artery disease. Eur. Heart J. 2007 29 1 21 30 10.1093/eurheartj/ehm545 18055486
    [Google Scholar]
  20. Bliden K.P. Tantry U.S. Storey R.F. The effect of ticagrelor versus clopidogrel on high on-treatment platelet reactivity: Combined analysis of the Onset/offset and respond studies. Am. Heart J. 2011 162 1 160 165 10.1016/j.ahj.2010.11.025 21742103
    [Google Scholar]
  21. Storey R.F. Angiolillo D.J. Patil S.B. 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. 2010 56 18 1456 1462 10.1016/j.jacc.2010.03.100 20832963
    [Google Scholar]
  22. Wei P. Wang X. Fu Q. Cao B. Progress in the clinical effects and adverse reactions of ticagrelor. Thromb. J. 2024 22 1 8 10.1186/s12959‑023‑00559‑3 38200557
    [Google Scholar]
  23. Liu Z. Liu Y. Mu G. Integrated pharmacokinetics/pharmacodynamics model and simulation of the ticagrelor effect on patients with acute coronary syndrome. Clin. Pharmacokinet. 2023 62 3 435 447 10.1007/s40262‑022‑01208‑0 36735213
    [Google Scholar]
  24. Spagnolo M. Angiolillo D.J. Capodanno D. Evaluating the pharmacokinetic and pharmacodynamic impact of different modes of ticagrelor administration. Expert Opin. Drug Metab. Toxicol. 2023 19 11 769 784 10.1080/17425255.2023.2272595 37849294
    [Google Scholar]
  25. Becker R.C. Bassand J.P. Budaj A. Bleeding complications with the P2Y12 receptor antagonists clopidogrel and ticagrelor in the platelet inhibition and patient Outcomes (PLATO) trial. Eur. Heart J. 2011 32 23 2933 2944 10.1093/eurheartj/ehr422 22090660
    [Google Scholar]
  26. Amsterdam E.A. Wenger N.K. Brindis R.G. 2014 AHA/ACC guideline for the management of patients with non-ST-elevation acute coronary syndromes: Executive summary: A report of the american college of cardiology/american heart association task force on practice guidelines. Circulation 2014 130 25 2354 2394 25249586
    [Google Scholar]
  27. Johnston S.C. Amarenco P. Albers G.W. Ticagrelor versus aspirin in acute stroke or transient ischemic attack. N. Engl. J. Med. 2016 375 1 35 43 SOCRATES Steering Committee and Investigators 10.1056/NEJMoa1603060 27160892
    [Google Scholar]
  28. Cattaneo M. Faioni E.M. Why does ticagrelor induce dyspnea? Thromb. Haemost. 2012 108 6 1031 1036 10.1160/TH12‑08‑0547 23070079
    [Google Scholar]
  29. Burki N.K. Lee L.Y. Mechanisms of dyspnea. Chest 2010 138 5 1196 1201 10.1378/chest.10‑0534 21051395
    [Google Scholar]
  30. van Giezen J.J.J. Sidaway J. Glaves P. Kirk I. Björkman J.A. Ticagrelor inhibits adenosine uptake in vitro and enhances adenosine-mediated hyperemia responses in a canine model. J. Cardiovasc. Pharmacol. Ther. 2012 17 2 164 172 10.1177/1074248411410883 21697355
    [Google Scholar]
  31. Wang K. Zhou X. Huang Y. Adjunctive treatment with ticagrelor, but not clopidogrel, added to tPA enables sustained coronary artery recanalisation with recovery of myocardium perfusion in a canine coronary thrombosis model. Thromb. Haemost. 2010 104 3 609 617 20694285
    [Google Scholar]
  32. Wiviott SD Braunwald E McCabe CH Prasugrel versus clopidogrel in patients with acute coronary syndromes N Engl J Med 2007 357 20 2001 15 TRITON-TIMI 38 Investigators 10.1056/NEJMoa0706482 17982182
    [Google Scholar]
  33. Cannon CP Husted S Harrington RA Safety, tolerability, and initial efficacy of AZD6140, the first reversible oral adenosine di-phosphate receptor antagonist, compared with clopidogrel, in pa-tients with non-ST-segment elevation acute coronary syndrome: Pri-mary results of the DISPERSE-2 trial J Am Coll Cardiol 2007 50 19 1844-51.DISPERSE 2 Investigators 10.1016/j.jacc.2007.07.053 17980250
    [Google Scholar]
  34. Scirica B.M. Cannon C.P. Emanuelsson H. The incidence of bradyarrhythmias and clinical bradyarrhythmic events in patients with acute coronary syndromes treated with ticagrelor or clopidogrel in the PLATO (Platelet Inhibition and Patient Outcomes) trial: Results of the continuous electrocardiographic assessment substudy. J. Am. Coll. Cardiol. 2011 57 19 1908 1916 PLATO Investigators 10.1016/j.jacc.2010.11.056 21545948
    [Google Scholar]
  35. Belardinelli L. Lerman B.B. Adenosine: Cardiac Electrophysiology. Pacing Clin. Electrophysiol. 1991 14 11 1672 1680 10.1111/j.1540‑8159.1991.tb02742.x 1721156
    [Google Scholar]
  36. Ding Z. Kim S. Dorsam R.T. Jin J. Kunapuli S.P. Inactivation of the human P2Y12 receptor by thiol reagents requires interaction with both extracellular cysteine residues, Cys17 and Cys270. Blood 2003 101 10 3908 3914 10.1182/blood‑2002‑10‑3027 12560222
    [Google Scholar]
  37. Gurbel P.A. Fox K.A.A. Tantry U.S. ten Cate H. Weitz J.I. Combination antiplatelet and oral anticoagulant therapy in patients with coronary and peripheral artery Disease. Circulation 2019 139 18 2170 2185 10.1161/CIRCULATIONAHA.118.033580 31034291
    [Google Scholar]
  38. Born G. Patrono C. Antiplatelet drugs. Br. J. Pharmacol. 2006 147 Suppl. 1 S241 S251 10.1038/sj.bjp.0706401 16402110
    [Google Scholar]
  39. Birkeland K. Parra D. Rosenstein R. Antiplatelet therapy in acute coronary syndromes: Focus on ticagrelor. In: J. Blood Med. 2010 1 Sep 197 219 10.2147/JBM.S9650 22282698
    [Google Scholar]
  40. Katus H.A. Giannitsis E. Antiplatelet therapy – ticagrelor. Hamostaseologie 2012 32 3 177 185 10.5482/HAMO‑12‑05‑0003 22739809
    [Google Scholar]
  41. Franchi F. Angiolillo D.J. Novel antiplatelet agents in acute coronary syndrome. Nat. Rev. Cardiol. 2015 12 1 30 47 10.1038/nrcardio.2014.156 25286881
    [Google Scholar]
  42. Levine G.N. Bates E.R. Bittl J.A. 2016 ACC/AHA guideline focused update on duration of dual antiplatelet therapy in patients with coronary artery disease. J. Am. Coll. Cardiol. 2016 68 10 1082 1115 10.1016/j.jacc.2016.03.513 27036918
    [Google Scholar]
  43. January C.T. Wann L.S. Calkins H. 2019 AHA/ACC/HRS focused update of the 2014 AHA/ACC/HRS guideline for the management of patients with atrial fibrillation: A report of the american college of cardiology/american heart association task force on clinical practice guidelines and the heart rhythm society in collaboration with the society of thoracic surgeons. Circulation 2019 140 2 e125 e151 30686041
    [Google Scholar]
  44. Turgeon R.D. Ackman M.L. Babadagli H.E. The role of direct oral anticoagulants in patients with coronary artery disease. J. Cardiovasc. Pharmacol. Ther. 2019 24 2 103 112 10.1177/1074248418795889 30122072
    [Google Scholar]
  45. Choxi R. Kapoor K. Mackman N. Jovin I.S. Direct oral anticoagulants and coronary artery disease. Arterioscler. Thromb. Vasc. Biol. 2022 42 5 553 564 10.1161/ATVBAHA.121.317171 35296151
    [Google Scholar]
  46. Kaddoura R. Orabi B. Yassin M.A. Omar A.S. Trends in off-label indications of non-vitamin k antagonist oral anticoagulants in acute coronary syndrome. Rev. Cardiovasc. Med. 2023 24 6 180 10.31083/j.rcm2406180 39077529
    [Google Scholar]
  47. Bassand J.P. Novel oral anticoagulants in acute coronary syndrome: Re-evaluating the thrombin hypothesis. EuroIntervention 2014 9 11 1333 1341 10.4244/EIJV9I11A224 24650773
    [Google Scholar]
  48. Ostrowska M. Kubica J. Adamski P. Stratified approaches to antiplatelet therapies based on platelet reactivity testing. Front. Cardiovasc. Med. 2019 6 176 10.3389/fcvm.2019.00176 31850373
    [Google Scholar]
  49. Guan B. Zhao L. Ma D. The effect of ticagrelor on endothelial function compared to prasugrel, clopidogrel, and placebo: A systematic review and meta-analysis. Front. Cardiovasc. Med. 2022 8 820604 10.3389/fcvm.2021.820604 35155620
    [Google Scholar]
  50. Tao L. Ren S. Zhang L. A review of the role of the antiplatelet drug ticagrelor in the management of acute coronary syndrome, acute thrombotic disease, and other diseases. Med. Sci. Monit. 2022 28 e935664 10.12659/MSM.935664 35570383
    [Google Scholar]
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