Frontiers in Cardiovascular Drug Discovery

Volume: 3

P2Y12-Receptor Antagonists and the Concept of Tailored Strategy

Author(s): Marouane Boukhris, Salvatore D. Tomasello, Zied Ibn Elhadj and Alfredo R. Galassi

Pp: 3-61 (59)

DOI: 10.2174/9781681081632116030003

* (Excluding Mailing and Handling)


Platelet represents the cornerstone of both physiologic hemostasis and thrombosis acting via different pathways. Adenosine diphosphate (ADP) plays a crucial role in platelet activation and thrombus formation through its interaction with platelet P2Y12 receptor, making therefore this receptor an interesting therapeutic target for anti-thrombotic agents.

Around the world, millions of people affected by coronary artery disease are treated with anti-platelet agents. Indeed, dual anti-platelet therapy, consisting of a combination of aspirin and a P2Y12 receptor antagonist, is the recommended strategy in patients with acute coronary syndrome and those who underwent percutaneous coronary intervention with stent implantation. Furthermore, the introduction of different generations of P2Y12 receptor antagonists has immensely improved the clinical outcome, as well established through literature.

Although the concept to replace “one size fits all” paradigm to a more individualized approach in anti-platelet therapy seems to be rational, in the area of based evidence medicine, a clear prognostic impact of such a strategy is not yet clearly demonstrated.

In the current chapter, we tried to summarize the mechanisms of P2Y12 receptor antagonists anti-platelet action, to report clinical proofs regarding the efficacy/safety of new generations of this class of drugs, and to discuss the place of a tailored strategy and its impact on improving clinical outcome.

Keywords: Anti-aggregation therapy, Bleeding, Cangrelor, Clinical outcome, Clopidogrel, Coronary artery disease, Dual anti-platelet therapy, Elinogrel, Genetic testing, High on-treatment platelet reactivity, Ischemic event, Low ontreatment platelet reactivity, Percutaneous coronary intervention, Platelet aggregation, Platelet reactivity, Prasugrel, P2Y12 receptor, P2Y12 receptor inhibitors, Stent implantation, Ticagrelor.

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