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学科主题: 临床医学
题名:
Safety, pharmacokinetics and pharmacodynamics of single/multiple doses of the oral, direct Factor Xa inhibitor rivaroxaban in healthy Chinese subjects
作者: Zhao, Xia1; Sun, Peihong1; Zhou, Ying1; Liu, Yuwang1; Zhang, Huilin1; Mueck, Wolfgang3; Kubitza, Dagmar3; Bauer, Richard J.4; Zhang, Hong2; Cui, Yimin1
关键词: anticoagulant ; Chinese subjects ; Factor Xa inhibitor ; rivaroxaban
刊名: BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
发表日期: 2009-07-01
DOI: 10.1111/j.1365-2125.2009.03390.x
卷: 68, 期:1, 页:77-88
收录类别: SCI
文章类型: Article
WOS标题词: Science & Technology
类目[WOS]: Pharmacology & Pharmacy
研究领域[WOS]: Pharmacology & Pharmacy
关键词[WOS]: TOTAL HIP-REPLACEMENT ; DEEP-VEIN THROMBOSIS ; VENOUS THROMBOEMBOLISM ; BAY 59-7939 ; ATRIAL-FIBRILLATION ; BAY-59-7939 ; PREVENTION ; ANTICOAGULATION ; PREVALENCE ; ISSUES
英文摘要:

center dot Rivaroxaban is an oral, direct Factor Xa inhibitor in advanced clinical development for the prevention and treatment of thromboembolic disorders.

center dot In single- and multiple-dose Phase I studies in White subjects, rivaroxaban was safe and demonstrated predictable, dose-dependent pharmacokinetics and pharmacodynamics.

WHAT THIS STUDY ADDS

center dot The Phase III programme with rivaroxaban is being conducted worldwide.

center dot Therefore, it is necessary to determine whether the pharmacokinetics, pharmacodynamics and tolerability of rivaroxaban are altered in patients of different ethnic origins.

center dot Dose-escalation studies were conducted to determine the safety, pharmacokinetics and pharmacodynamics of single and multiple doses of rivaroxaban in healthy Chinese subjects.

AIMS

To investigate the safety, pharmacokinetics and pharmacodynamics of rivaroxaban, an oral, direct Factor Xa (FXa) inhibitor, in healthy, male Chinese subjects.

METHODS

Two randomized, single-blind, placebo-controlled, dose-escalation studies were conducted in healthy Chinese men aged 18-45 years. In the single-dose study, subjects received single, oral doses of rivaroxaban 2.5, 5, 10, 20 and 40 mg. In the multiple-dose study, oral rivaroxaban was administered in doses of 5, 10, 20 and 30 mg twice daily for 6 days.

RESULTS

Rivaroxaban, in single and multiple doses up to 60 mg, was well tolerated. Rapid absorption was observed in both studies (time to C(max) 1.25-2.5 h). In the multiple-dose study, rivaroxaban exposure increased dose-proportionally after the first dose and at steady state (for the 5-20-mg doses). The half-life of rivaroxaban was up to 7.9 h in the single-dose study. Maximal inhibition of FXa activity was achieved within 1-3 h of dosing in the single-dose study [at 20 mg FXa inhibition as a median percentage change from baseline, 45.92; 95% confidence interval (CI) 44.64, 50.70] and 2-3 h after administration at steady state in the multiple-dose study (at 20 mg median FXa inhibition as a median percentage change from baseline, 60.25; 95% CI 56.16, 63.05), in line with maximum rivaroxaban plasma concentrations.

CONCLUSIONS

Rivaroxaban demonstrated predictable pharmacokinetics and pharmacodynamics in healthy Chinese subjects, in line with findings observed previously in White subjects. This suggests that fixed doses of rivaroxaban may be administered to all patients, regardless of their ethnic origin.

语种: 英语
项目资助者: Bayer Schering Pharma AG
WOS记录号: WOS:000268050600009
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.bjmu.edu.cn/handle/400002259/50519
Appears in Collections:北京大学第一临床医学院_药剂科_期刊论文

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作者单位: 1.Bayer Schering Pharma AG, Clin Pharmacol, Wuppertal, Germany
2.Peking Univ, Hosp 1, Dept Pharm, Beijing 100034, Peoples R China
3.Bayer HealthCare Co Ltd, Dept Med, Beijing, Peoples R China
4.Bayer Schering Pharma AG, Med Affairs Asia Pacific, Wuppertal, Germany

Recommended Citation:
Zhao, Xia,Sun, Peihong,Zhou, Ying,et al. Safety, pharmacokinetics and pharmacodynamics of single/multiple doses of the oral, direct Factor Xa inhibitor rivaroxaban in healthy Chinese subjects[J]. BRITISH JOURNAL OF CLINICAL PHARMACOLOGY,2009,68(1):77-88.
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