Absence of QTc prolongation with betrixaban: a randomized, double-blind, placebo- and positive-controlled thorough ECG study

Expert Opin Pharmacother. 2013 Jan;14(1):5-13. doi: 10.1517/14656566.2013.753057. Epub 2012 Dec 10.

Abstract

Objective: To evaluate the effects of the anticoagulant betrixaban on individual heart rate-corrected QT (QTcI).

Research design and methods: Ninety-six healthy adults were randomly assigned to single-dose betrixaban 80 and 140 mg (therapeutic and supratherapeutic doses, respectively), placebo, and moxifloxacin 400 mg (positive control) in a four-period crossover study. Electrocardiograms were recorded at pre-dose and post-dose hours 1, 2, 3, 4, 5, 6, 8, 12, 16 and 24.

Main outcomes measures: An analysis of covariance determined the placebo-corrected, time-matched mean change from baseline QTcI at the 95% upper confidence interval (UCI; one-sided). The pre-specified clinically significant change for betrixaban-treated groups was > 10 ms (95% UCI, one-sided). Subjects were monitored for safety and tolerability.

Results: Mean QTcI change was < 10 ms for both betrixaban groups at all time points; expected changes were observed for moxifloxacin, establishing assay sensitivity. Correlation between betrixaban plasma concentration and QTcI duration confirmed the absence of effect on QT.

Conclusions: Betrixaban at therapeutic and supratherapeutic doses did not cause clinically relevant changes in QTcI intervals or other electrocardiographic parameters. Betrixaban was well tolerated.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Adolescent
  • Adult
  • Anti-Bacterial Agents / adverse effects
  • Anticoagulants / adverse effects
  • Anticoagulants / therapeutic use*
  • Aza Compounds / adverse effects
  • Benzamides / adverse effects
  • Benzamides / therapeutic use*
  • Cross-Over Studies
  • Double-Blind Method
  • Electrocardiography / drug effects*
  • Female
  • Fluoroquinolones
  • Heart Rate / drug effects*
  • Humans
  • Long QT Syndrome / prevention & control*
  • Male
  • Middle Aged
  • Moxifloxacin
  • Pyridines / adverse effects
  • Pyridines / therapeutic use*
  • Quinolines / adverse effects
  • Young Adult

Substances

  • Anti-Bacterial Agents
  • Anticoagulants
  • Aza Compounds
  • Benzamides
  • Fluoroquinolones
  • Pyridines
  • Quinolines
  • betrixaban
  • Moxifloxacin