Background:

Ticagrelor is a novel antagonist of the P2Y12 receptor [1].

Ticagrelor has been reported to inhibit the prothrombotic effects of ADP on the platelet by against the P2Y12 receptor. Ticagrelor has shown the complete inhibition of platelet aggregation ex vivo. In addition Ticagrelor has suggested a dose-dependent inhibition of platelet aggregation in human being. Apart from these, Ticagrelor has also demonstrated an orally, actively, reversibly binding antagonist. Unlike other inhibitors, Ticagrelor has also reported to inhibit P2Y12 receptor without metabolic transformation. Besides that, Ticagrelor is the first thienopyridine anti-platelet agent and mainly metabolized by CYP3A4 and CYP2C19 [1][2].

参考文献:
[1] Zhou D1, Andersson TB, Grimm SW. In vitro evaluation of potential drug-drug interactions with ticagrelor: cytochrome P450 reaction phenotyping, inhibition, induction, and differential kinetics. Drug Metab Dispos. 2011 Apr;39(4):703-10.
[2] Li Y1, Landqvist C, Grimm SW. Disposition and metabolism of ticagrelor, a novel P2Y12 receptor antagonist, in mice, rats, and marmosets. Drug Metab Dispos. 2011 Sep;39(9):1555-67. doi: 10.1124/dmd.111.039669. Epub 2011 Jun 13.