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Clin Pharmacol. 2013 Dec 6;5:177-84. doi: 10.2147/CPAA.S51981. eCollection 2013.

Single- and multiple-dose pharmacokinetics, pharmacodynamics, and safety of apixaban in healthy Chinese subjects.

Author information

  • 1Peking University First Hospital, Beijing, People's Republic of China.
  • 2Bristol-Myers Squibb, Princeton, NJ, USA.

Erratum in

  • Clin Pharmacol. 2014;6:61.

Abstract

BACKGROUND:

The pharmacokinetics (PK), pharmacodynamics (PD), and safety of apixaban were assessed in healthy Chinese subjects in this randomized, placebo-controlled, double-blind, single-sequence, single- and multiple-dose study.

SUBJECTS AND METHODS:

Eighteen subjects 18-45 years of age were randomly assigned (2:1 ratio) to receive apixaban or matched placebo. Subjects received a single 10 mg dose of apixaban or placebo on day 1, followed by 10 mg apixaban or placebo twice daily for 6 days (days 4-9). The PK and PD of apixaban were assessed by collecting plasma samples for 72 hours following the dose on day 1 and the morning dose on day 9, and measuring apixaban concentration and anti-Xa activity. Safety was assessed via physical examinations, vital sign measurements, electrocardiograms, and clinical laboratory evaluations.

RESULTS:

PK analysis showed similar characteristics of apixaban after single and multiple doses, including a median time to maximum concentration of ~3 hours, mean elimination half-life of ~11 hours, and renal clearance of ~1.2 L/hour. The accumulation index was 1.7, consistent with twice-daily dosing and the observed elimination half-life. Single-dose data predict multiple-dose PK, therefore apixaban PK are time-independent. The relationship between anti-Xa activity and plasma apixaban concentrations appears to be linear. Apixaban was safe and well tolerated, with no bleeding-related adverse events reported.

CONCLUSION:

Apixaban was safe and well tolerated in healthy Chinese subjects. Apixaban PK and PD were predictable and consistent with findings from previous studies in Asian and non-Asian subjects. The administration of apixaban does not require any dose modification based on race.

KEYWORDS:

apixaban; factor Xa inhibitor; oral anticoagulant; pharmacodynamics; pharmacokinetics

PMID:
24353445
[PubMed]
PMCID:
PMC3861362
Free PMC Article
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