CANGRELOR

The Uses of CANGRELOR

Cangrelor is a P2Y12 inhibitor used as an antiplatelet drug for intravenous application.

The Uses of CANGRELOR

Anti-platelet agent.

Indications

For use as an adjunct to percutaneous coronary intervention (PCI) for reducing the risk of periprocedural myocardial infarction (MI), repeat coronary revascularization, and stent thrombosis (ST) in patients in who have not been treated with a P2Y12 platelet inhibitor and are not being given a glycoprotein IIb/IIIa inhibitor.

Background

Cangrelor is an intravenous, direct-acting, reversible P2Y12 inhibitor for patients undergoing percutaneous coronary intervention (PCI) who have not been yet treated by oral P2Y12 inhibitors. An advantage Cangrelor provides over oral P2Y12 inhibitors (such as prasugrel, ticagrelor, and clopidogrel) is that it is an active drug not requiring metabolic conversion therefore providing a rapid onset and offset of action. Cangrelor was approved by the FDA in June 2015 for intravenous application.

Definition

ChEBI: A nucleoside triphosphate analogue that is 5'-O-[({[dichloro(phosphono)methyl](hydroxy)phosphoryl}oxy)(hydroxy)phosphoryl]adenosine carrying additional 2-(methylsulfanyl)ethyl and (3,3,3-trifluoropropyl)sulfanyl substituents at positions N6 and C2 respectively. Used (in the form of its tetrasodium salt) as an intravenous antiplatelet drug that prevents formation of harmful blood clots in the coronary arteries.

Clinical Use

Direct P2Y12 platelet receptor antagonist:

Antiplatelet for patients undergoing a PCI

Metabolism

Cangrelor is deactivated rapidly in the circulation by dephosphorylation to its primary metabolite, a nucleoside, which has negligible anti-platelet activity. Cangrelor's metabolism is independent of hepatic function and it does not interfere with other drugs metabolized by hepatic enzymes.

Metabolism

Cangrelor is deactivated rapidly in the plasma by dephosphorylation to form its main metabolite, a nucleoside. Following a 2 micrograms/kg/min infusion of [3 H] cangrelor, 58% was found in urine and the remaining 35% was found in faeces, presumably following biliary excretion.