Catalog No.S4079 Synonyms: AZD 6140
Molecular Weight(MW): 522.57
Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.
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Effect of antiplatelet drugs on platelet aggregation in healthy individuals. Samples from healthy individuals were preincubated with anti-platelet drugs (n = 3). Curves and columns show mean platelet aggregation and the relationship between platelet aggregation and drug concen-tration. Bars represent standard deviations. *P < 0.05 as compared with platelet aggregation with the same agonist but no drugs added; pairedStudent’s t-test. (A-C) The drugs tested were abciximab (A), ticagrelor (B), and vorapaxar (C).
J Thromb Haemost, 2017, 15(6):1191-1202. Ticagrelor purchased from Selleck.
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Choose Selective P2 Receptor Inhibitors
|Description||Ticagrelor is the first reversibly binding oral P2Y12 receptor antagonist with Ki of 2 nM.|
|Features||First-in-class of a new type of P2Y12 antagonist known as cyclopentyl-triazolo-pyrimidines.|
Ticagrelor is an active drug which, does not require metabolic activation after intestinal absorption. It does not compete directly with ADP at the ADP binding site but occupies an adjacent binding site and acts in an allosteric way, resulting in a reversible conformational change of the receptor. Ticagrelor binds reversibly to the receptor and exhibits rapid onset and offset of effect. Binding studies in rh-P2Y12 receptor-transfected CHO-K1 cells indicate that ticagrelor exhibits potent, rapid, and reversible binding, with a Kd of 10.5 nM, a kon (association constant) of 0.00011/(nM•s), a koff (dissociation constant) of 0.00087/s, and half-life values of 4 min for binding and 14 min for unbinding, indicating that the magnitude of platelet inhibition is dependent on concentrations of drug available to bind platelets.  Ticagrelor moderately inhibits CYP2C9 activity in human liver microsomes, while exhibiting little or no inhibition of CYP1A2, CYP2B6, CYP2C8, CYP2C19, CYP2D6, and CYP2E1. In human liver microsomes, ticagrelor inhibits midazolam 4-hydroxylation, while activating 1_-hydroxylation of midazolam. Evaluated in fresh human hepatocytes, ticagrelor is not an inducer of CYP1A2 or CYP3A4. 
|In vivo||Absorption of ticagrelor is rapid with t max of 1.3-2 h. And the Cmax and area under the plasma concentration-time curve from time 0 to infinity increases in an apparently dose-proportional manner over the dose range studied, indicating linear pharmacokinetics. The mean terminal-phase half-life (t1/2) is approximately 7-8.5 h for ticagrelor. Inhibition of platelet aggregation (IPA) is dose related and is nearly complete at 2 h at doses of 100-400 mg. Ticagrelor is well tolerated, with no serious or doserelated adverse events or notable changes in laboratory values observed. |
|In vitro||DMSO||100 mg/mL (191.36 mM)|
|Ethanol||53 mg/mL (101.42 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03027934||Not yet recruiting||Diabetes Mellitus||CirQuest Labs, LLC||February 28, 2017||Phase 4|
|NCT03016611||Not yet recruiting||Acute Coronary Syndrome|STEMI||Sheba Medical Center||February 2017||Phase 4|
|NCT02866175||Not yet recruiting||Atrial Fibrillation||Daiichi Sankyo Inc.|European Cardiovascular Research Institute|Kompetenznetz Vorhofflimmern e.V.|Chiltern International Inc.||February 2017||Phase 3|
|NCT02663713||Recruiting||Myocardial Infarction|Diabetes Mellitus|Renal Disease|Coronary Artery Disease||University of Patras|AstraZeneca||January 2017||Phase 4|
|NCT02617290||Not yet recruiting||Coronary Artery Disease|Myocardial Ischemia|Myocardial Infarction|Stent Thrombosis|Cardiovascular Diseases||Assistance Publique - Hôpitaux de Paris|Action Research Group||December 2016||Phase 3|
|NCT02989558||Not yet recruiting||Aortic Valve Stenosis||University of Athens||December 2016||Phase 3|
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