Ticagrelor: A Comprehensive Review of Pharmacology, Clinical Applications, and Future Perspectives

Abstract

Ticagrelor is a first-in-class oral platelet P2Y₁₂ receptor inhibitor belonging to the cyclopentyltriazolopyrimidine chemical class. Unlike traditional thienopyridine agents such as clopidogrel and prasugrel, ticagrelor binds reversibly to the P2Y₁₂ receptor and does not require hepatic metabolic activation. These unique pharmacological properties confer rapid onset of action, greater potency, and more consistent platelet inhibition with reduced interpatient variability. Ticagrelor is approved for use in patients with acute coronary syndromes (ACS), coronary artery disease, and low-to-moderate risk acute ischemic stroke or high-risk transient ischemic attack. The landmark PLATO trial established its superiority over clopidogrel in reducing cardiovascular events in ACS patients. However, subsequent studies have raised questions about the generalizability of these findings, and the higher bleeding risk associated with ticagrelor remains a significant clinical concern. This review comprehensively examines the chemistry, pharmacology, clinical trial evidence, safety profile, novel formulation strategies, and future research directions for ticagrelor, with particular emphasis on areas suitable for academic research.