Safety, pharmacokinetics and pharmacodynamics of single doses of rivaroxaban – an oral, direct factor Xa inhibitor – in elderly Chinese subjects

Ji Jiang; Yufang Hu; Jianyan Zhang; Jueling Yang; Wolfgang Mueck; Dagmar Kubitza; Richard J. Bauer; Ling Meng; Pei Hu

doi:10.1160/TH09-03-0196

Thrombosis and Haemostasis, Table of Contents

Thromb Haemost 2010; 103(01): 234-241
DOI: 10.1160/TH09-03-0196

New Technologies, Diagnostic Tools and Drugs

Schattauer GmbH

Safety, pharmacokinetics and pharmacodynamics of single doses of rivaroxaban – an oral, direct factor Xa inhibitor – in elderly Chinese subjects

Ji Jiang

¹The Clinical Pharmacology Research Center, Peking Union Medical College Hospital, P.R. China

,

Yufang Hu

¹The Clinical Pharmacology Research Center, Peking Union Medical College Hospital, P.R. China

,

Jianyan Zhang

¹The Clinical Pharmacology Research Center, Peking Union Medical College Hospital, P.R. China

,

Jueling Yang

¹The Clinical Pharmacology Research Center, Peking Union Medical College Hospital, P.R. China

,

Wolfgang Mueck

²Clinical Pharmacology, Bayer Schering Pharma AG, Wuppertal, Germany

,

Dagmar Kubitza

²Clinical Pharmacology, Bayer Schering Pharma AG, Wuppertal, Germany

,

Richard J. Bauer

³Medical Affairs Asia-Pacific, Bayer Schering Pharma AG, Wuppertal, Germany

,

Ling Meng

⁴Medical Department, Bayer HealthCare Company Ltd, Beijing, P.R. China

,

Pei Hu

¹The Clinical Pharmacology Research Center, Peking Union Medical College Hospital, P.R. China

› Author Affiliations

Abstract

Summary

Rivaroxaban is a novel, oral, direct factor Xa (FXa) inhibitor for the prevention and treatment of thromboembolic disorders. The aim of this study was to investigate the safety, pharmacokinetics (PK) and pharmacodynamics (PD) of rivaroxaban in healthy, elderly Chinese subjects. In this single-centre, single-blind, placebo-controlled, parallel-group, dose-escalation study, 79 subjects, aged 59–74 years (mean 62.8), were randomised to receive once-daily oral doses of rivaroxaban 5, 10, 20, 30 or 40 mg. Rivaroxaban was well tolerated: there was a low incidence of treatment-emergent adverse events and all events were of mild intensity. Rivaroxaban was absorbed rapidly, reaching maximum plasma concentrations within 2–4 hours. The PK of rivaroxaban were dose dependent over the dose range tested. Maximal inhibition of FXa occurred 2–3 hours after dosing and returned to baseline after 24–48 hours, reflecting rivaroxaban plasma concentrations. Inhibition of FXa was associated with dose-dependent effects on global clotting tests. There were no clinically relevant differences in rivaroxaban plasma concentrations between male and female subjects. In conclusion, rivaroxaban was well tolerated and was found to have predictable PK and PD in healthy, elderly Chinese subjects.

Keywords

Chinese subjects - factor Xa inhibitor - oral anticoagulant - rivaroxaban

Full Text

References

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