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 con-sistent and potent platelet aggregation suppression. This distinct pharmacokinetic and phar-macodynamic 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 dis-ease, and post-coronary artery bypass grafting (CABG) management. One of its key ad-vantages 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-pyrimi-dine class, which exhibits high resistance to enzymatic degradation. This characteristic is essential because it allows for more stable and effective P2Y12 receptor inhibition, over-coming the limitations of adenosine triphosphate (ATP) as a direct pharmacological com-petitor of adenosine diphosphate (ADP). Overall, Brilinta represents a significant advance-ment in antiplatelet therapy, offering enhanced efficacy, improved safety, and expanded clin-ical applications. By offering a reversible, potent, and consistent inhibition of platelet aggre-gation, 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 throm-botic conditions.

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Publication Details

Journal
Current Drug Therapy
Published
2025-10-02
DOI
https://doi.org/10.2174/0115748855407305250917214211
Primary Topic
Antiplatelet Therapy and Cardiovascular Diseases
Type
article
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article

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

Rukaiah Fatma Begum, N. Pavithra, Manisha Pathania, Ankul Singh S et al.
Current Drug Therapy
Antiplatelet Therapy and Cardiovascular Diseases
article

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

Rukaiah Fatma Begum, N. Pavithra, Manisha Pathania, Ankul Singh S, N. Harikrishnan, Thanga Ashwini S.
article en

Abstract

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 con-sistent and potent platelet aggregation suppression. This distinct pharmacokinetic and phar-macodynamic 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 dis-ease, and post-coronary artery bypass grafting (CABG) management. One of its key ad-vantages 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-pyrimi-dine class, which exhibits high resistance to enzymatic degradation. This characteristic is essential because it allows for more stable and effective P2Y12 receptor inhibition, over-coming the limitations of adenosine triphosphate (ATP) as a direct pharmacological com-petitor of adenosine diphosphate (ADP). Overall, Brilinta represents a significant advance-ment in antiplatelet therapy, offering enhanced efficacy, improved safety, and expanded clin-ical applications. By offering a reversible, potent, and consistent inhibition of platelet aggre-gation, 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 throm-botic conditions.

Current Drug TherapyVol. 20
Dr. M.G.R. Educational and Research Institute (IN), GLA University (IN)
Openalex Percentile: Top 58%
Antiplatelet Therapy and Cardiovascular Diseases
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