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The first P2Y 12 inhibitors were of the thienopyridine family. They are indirect antagonists, which block the ADP-induced platelet aggregation and activation. The first drug of this class was ticlopidine and was discovered in 1972 at Porcor (now Sanofi). It was discovered while screening for a new anti-inflammatory drug based on tinoridine.
On the other hand, P2Y 12 inhibitors do not change the risk of death when given as a pretreatment prior to routine PCI in people who have had a non-ST-elevation myocardial infarction . Though, a P2Y 12 inhibitor in addition to aspirin should be administered for up to 12 months to most patients with non-ST-elevation acute coronary syndrome. They ...
Ticagrelor (Brilinta) is often listed with thienopyridine inhibitors and has similar indications for use but is not a thienopyridine. It is a cyclo-pentyltriazolo-pyrimidine that is distinct from the mechanism of the thienopyridines in that it reversibly (rather than irreversibly) inhibits the P2Y 12 receptor.
P2Y 12 structure as generated by PYMOL with color-coded helices. P2Y receptors are membrane proteins belonging to the class A family of G protein-coupled receptors (GPCRs). [5] [6] P2Y receptor proteins display large-scale structural domains typical of GPCRs, consisting of seven hydrophobic transmembrane helices connected by three short extracellular loops and three variably sized ...
Prasugrel, sold under the brand names Effient and Efient, is a medication used to prevent formation of blood clots.It is a platelet inhibitor and an irreversible antagonist of P2Y 12 ADP receptors and is of the thienopyridine drug class.
Anti-platelet drugs. Many anti-platelet drugs such as Prasugrel, Ticagrelor, and Ticlopidine are adenosine diphosphate (ADP) receptor inhibitors. Before the expiry of its patent, the P2Y12 receptor antagonist Clopidogrel (trade name: Plavix) was the second most prescribed drug in the world. In 2010 alone, it generated over US$9 billion in ...
Selatogrel is a P2Y 12 inhibitor [1] [2] that has been proposed as a treatment for acute myocardial infarction. [3] References
Cangrelor, sold under the brand name Kengreal among others, is a P2Y 12 inhibitor FDA approved as of June 2015 as an antiplatelet drug [5] for intravenous application. Some P2Y 12 inhibitors are used clinically as effective inhibitors of adenosine diphosphate-mediated platelet activation and aggregation. [5]