title: A single-dose study investigating the pharmacokinetics and pharmacodynamics of edoxaban at 30-90 mg in healthy Chinese volunteers.
abstract: 1. This study investigated the pharmacokinetics and pharmacodynamics of single-dose edoxaban in healthy Chinese subjects. 2. This single-centre, open-label, 3-occasion, cross-over study enrolled six males and six females. Subjects received a single-oral-dose of edoxaban 30-90 mg in each study occasion under fasting condition. Serial blood samples were collected to measure the plasma concentrations of edoxaban and its major active metabolite D21-2393. Meanwhile, PT, INR, aPTT were measured pre- and post-dose. Safety was assessed. 3. After administration, edoxaban was rapidly absorbed (median Tmax=1-2 h). With rapid transformation, peak concentration of D21-2393 was reached within 2-h post-dose. The elimination half-life of edoxaban was 5-20 h. The dose-exposure relationships were slightly lower-than-dose-proportional for both edoxaban and D21-2393. Although women had higher plasma exposure of edoxaban and D21-2393 than men, it was considered clinically insignificant. 4. The effects of edoxaban on all pharmacodynamic biomarkers were concentration-dependent and linearly-correlated to plasma level of the compound. Minor bleeding was the most commonly reported adverse events. 5. Single oral doses of edoxaban 30-90 mg were safe and well tolerated in healthy Chinese volunteers. 6. The pharmacokinetic and pharmacodynamic profiles of edoxaban in Chinese subjects were comparable to those observed in Caucasian and Japanese populations.
authors: a Phase I Unit , Beijing City Key Laboratory, Clinical Pharmacological Research Center, Peking Union Medical College Hospital , Beijing , China.
authors: Xia
authors: X
authors: Chen
authors: a Phase I Unit , Beijing City Key Laboratory, Clinical Pharmacological Research Center, Peking Union Medical College Hospital , Beijing , China.
authors: Dongyang
authors: D
authors: Liu
authors: a Phase I Unit , Beijing City Key Laboratory, Clinical Pharmacological Research Center, Peking Union Medical College Hospital , Beijing , China.
authors: Yiwen
authors: Y
authors: Wu
authors: a Phase I Unit , Beijing City Key Laboratory, Clinical Pharmacological Research Center, Peking Union Medical College Hospital , Beijing , China.
authors: Hanlin
authors: H
authors: Song
authors: a Phase I Unit , Beijing City Key Laboratory, Clinical Pharmacological Research Center, Peking Union Medical College Hospital , Beijing , China.
authors: Yang
authors: Y
authors: Liu
authors: a Phase I Unit , Beijing City Key Laboratory, Clinical Pharmacological Research Center, Peking Union Medical College Hospital , Beijing , China.
authors: Ji
authors: J
authors: Jiang
authors: a Phase I Unit , Beijing City Key Laboratory, Clinical Pharmacological Research Center, Peking Union Medical College Hospital , Beijing , China.
authors: Pei
authors: P
authors: Hu
mesh_terms: D000284:Administration, Oral; D000328:Adult; D044466:Asian People; D002681:China; D018592:Cross-Over Studies; D065427:Factor Xa Inhibitors / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D005260:Female; D064368:Healthy Volunteers; D006801:Humans; D008297:Male; D011725:Pyridines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D013844:Thiazoles / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*
chemical_list: D065427:Factor Xa Inhibitors; D011725:Pyridines; D013844:Thiazoles; C552171:edoxaban
keywords: Chinese; edoxaban; pharmacodynamics; pharmacokinetics; safety