Ticagrelor CAS NO 274693-27-5 Inquire about Ticagrelor
Tecoland supplies Ticagrelor bulk active pharmaceutical ingredient (API) to the pharmaceutical industry. Our Ticagrelor is manufactured by cGMP compliant facility. Welcome to contact us for further details including current DMF status for the product and up to date regulatory status of the manufacturing facility. We look forward to assisting you with your research and development projects.
What is Ticagrelor ?
Ticagrelor is a platelet aggregation inhibitor produced by AstraZeneca. The drug was approved for use in the European Union by the European Commission on December 3, 2010. The drug was approved by the US Food and Drug Administration on July 20, 2011.
Ticagrelor contains ticagrelor, a cyclopentyltriazolopyrimidine, inhibitor of platelet activation and aggregation mediated by the P2Y12 ADP-receptor. Chemically it is (1S,2S,3R,5S)-3-[7-{[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino}-5-(propylthio)-3H-[1,p 2,3]-triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol. The empirical formula of ticagrelor is C23H28F2N6O4S and its molecular weight is 522.57.
Ticagrelor is a crystalline powder with an aqueous solubility of approximately 10 ?g/mL at room temperature.
Ticagrelor Drug Interactions
Effects of other drugs
Ticagrelor is predominantly metabolized by CYP3A4 and to a lesser extent by CYP3A5.
CYP3A inhibitors
Avoid use of strong inhibitors of CYP3A (e.g., ketoconazole, itraconazole, voriconazole, clarithromycin, nefazodone, ritonavir, saquinavir, nelfinavir, indinavir, atazanavir and telithromycin).
CYP3A inducers
Avoid use with potent inducers of CYP3A (e.g., rifampin, dexamethasone, phenytoin, carbamazepine and phenobarbital).
Aspirin
Use of Ticagrelor with aspirin maintenance doses above 100 mg reduced the effectiveness of Ticagrelor.
Effect of Ticagrelor on other drugs
Ticagrelor is an inhibitor of CYP3A4/5 and the P-glycoprotein transporter.
Simvastatin, lovastatin
Ticagrelor will result in higher serum concentrations of simvastatin and lovastatin because these drugs are metabolized by CYP3A4. Avoid simvastatin and lovastatin doses greater than 40 mg.
Digoxin
Digoxin: Because of inhibition of the P-glycoprotein transporter, monitor digoxin levels with initiation of or any change in Ticagrelor therapy.
Other Concomitant Therapy
Ticagrelor can be administered with unfractionated or low-molecular-weight heparin, GPIIb/IIIa inhibitors, proton pump inhibitors, beta-blockers, angiotensin converting enzyme inhibitors, and angiotensin receptor blockers.
Precautions before using Ticagrelor
- Like other antiplatelet agents, Ticagrelor increases the risk of bleeding.
- Use of Ticagrelor with maintenance doses of aspirin above 100 mg decreased the effectiveness of Ticagrelor.
- Moderate Hepatic Impairment: Consider the risks and benefits of treatment, noting the probable increase in exposure to ticagrelor.
- Dyspnea: Dyspnea was reported more frequently with Ticagrelor than with clopidogrel. Dyspnea resulting from Ticagrelor is self-limiting. Rule out other causes.
- Discontinuation of Ticagrelor: Premature discontinuation increases the risk of myocardial infarction, stent thrombosis, and death.
Ticagrelor Side effects
Most common adverse reactions are bleeding 12% and dyspnea 14%.
Ticagrelor Storage
Store at 25°C (77°F); excursions permitted to 15°-30°C (59°- 86°F) [see USP controlled room temperature].
Disclaimer:
Information on this page is provided for general information purposes. You should not make a clinical treatment decision based on information contained in this page without consulting other references including the package insert of the drug, textbooks and where relevant, expert opinion. We cannot be held responsible for any errors you make in administering drugs mentioned on this page, nor for use of any erroneous information contained on this page.