Cardiovascular Intervention and Therapeutics

, Volume 29, Issue 4, pp 324–333 | Cite as

Pharmacodynamics, pharmacokinetics and safety of ticagrelor in Asian patients with stable coronary artery disease

  • Y. Hiasa
  • R. Teng
  • H. Emanuelsson
Original Article


This randomized, active-controlled, double-blind study assessed the pharmacodynamics, pharmacokinetics and safety of ticagrelor in Japanese patients and a smaller cohort of non-Japanese Asian patients. The study recruited patients aged 20–80 years who had received aspirin 75–100 mg/day for ≥2 weeks and had percutaneous coronary intervention or acute coronary syndrome >3 months previously. Patients received 4 weeks’ treatment with ticagrelor 45 mg bid, ticagrelor 90 mg bid or clopidogrel 75 mg qd (all with aspirin). The inhibition of platelet aggregation (IPA, final-extent) and pharmacokinetics of ticagrelor were assessed on days 1 and 28. Overall, 139 Asian patients were randomized (ticagrelor 45 mg bid, n = 50; ticagrelor 90 mg bid, n = 43; clopidogrel, n = 46) of whom 118 were Japanese. Mean final-extent IPA was greater with ticagrelor 90 mg bid versus ticagrelor 45 mg bid and with both ticagrelor doses versus clopidogrel. At the end of the dosing interval on day 28, mean final-extent IPA was 10.0 % higher (95 % confidence interval 0.5–19.5 %) for ticagrelor 90 mg bid versus ticagrelor 45 mg bid, 15.1 % higher (5.8–24.4 %) for ticagrelor 45 mg bid versus clopidogrel, and 25.1 % higher (15.5–34.7 %) for ticagrelor 90 mg bid versus clopidogrel. In Japanese patients, exposure to ticagrelor and its active metabolite AR-C124910XX increased dose-proportionally. The safety profile of ticagrelor was consistent with previous studies. Ticagrelor was associated with enhanced IPA versus clopidogrel in Japanese patients.


Ticagrelor Pharmacokinetics Pharmacodynamics P2Y12 receptor antagonist Japanese 



Medical writing support was provided by Rick Flemming and David Evans at Gardiner Caldwell Communications and was funded by AstraZeneca. The authors acknowledge Takaaki Isshiki (Teikyo University School of Medicine), Hiroyuki Daida (Juntendo University Faculty of Medicine), Yasuo Ikeda (Waseda University School of Advanced Science and Engineering), Hisao Ogawa (Kumamoto University School of Medicine) and Makoto Takagi (Saiseikai Central Hospital), who were members of the data safety monitoring board. Technical training in the use of platelet aggregation equipment and the surveillance of aggregation curve accuracy was provided to staff from all sites by Laura West of the University of Sheffield. The authors would also like to thank all medical staff and patients involved in the study.


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Copyright information

© Japanese Association of Cardiovascular Intervention and Therapeutics 2014

Authors and Affiliations

  1. 1.Department of CardiologyTokushima Red Cross HospitalTokushimaJapan
  2. 2.AstraZenecaWilmingtonUSA
  3. 3.AstraZeneca R&DMölndalSweden

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