Repeated supratherapeutic dosing of strontium ranelate over 15 days does not prolong QT(c) interval in healthy volunteers

Br J Clin Pharmacol. 2012 Aug;74(2):296-303. doi: 10.1111/j.1365-2125.2012.04190.x.

Abstract

Aims: The study was performed to assess the safety of strontium ranelate in accordance with the ICH, E14 guidelines for QT/QT(c) studies. Its primary objective was to compare supratherapeutic repeated dosing of strontium ranelate (4 g day⁻¹ for 15 days) with placebo on the largest time-matched mean QT(c) variation, from baseline to under treatment values, in healthy subjects.

Methods: Ninety-six healthy male and female subjects (27.7 ± 7.5 years) were included to receive 1 day of placebo followed by 15 days of supratherapeutic repeated dosing of strontium ranelate (4 g day⁻¹), in a 4 month, randomized, placebo (16 days) and positive-controlled (single dose of moxifloxacin 400 mg preceded by 15 days of placebo), double-blind, double dummy, crossover design. Measurement of QT interval was performed automatically on the ECGs with subsequent manual onscreen over-reading by cardiologists using electronic callipers.

Results: The largest time-matched difference in QT(c) I (individual QT correction for heart rate) between moxifloxacin 400 mg and placebo was observed at 2 h post dose (mean [95% CI] 10.62 [7.90, 13.35] ms). For strontium ranelate (4 g day⁻¹) the largest time-matched difference in QT(c) I compared with placebo was observed at 1 h post dose (mean [90% CI] 7.54 [5.17, 9.90] ms). No subject had a QT(c) greater than 480 ms during the study. Both moxifloxacin and strontium ranelate were well tolerated in healthy subjects.

Conclusions: The findings of this study demonstrate that the administration of supratherapeutic repeated oral doses of strontium ranelate (4 g day⁻¹ for 15 days) does not lead to a prolongation of the QT/QT(c) interval above the threshold of regulatory concern.

Publication types

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

MeSH terms

  • Administration, Oral
  • Adult
  • Anti-Infective Agents / administration & dosage
  • Aza Compounds / administration & dosage
  • Bone Density Conservation Agents / administration & dosage*
  • Bone Density Conservation Agents / adverse effects
  • Bone Density Conservation Agents / pharmacokinetics
  • Cross-Over Studies
  • Double-Blind Method
  • Drug Administration Schedule
  • Electrocardiography
  • Female
  • Fluoroquinolones
  • Heart Rate / drug effects*
  • Humans
  • Linear Models
  • London
  • Long QT Syndrome / chemically induced
  • Male
  • Moxifloxacin
  • Nonlinear Dynamics
  • Organometallic Compounds / administration & dosage*
  • Organometallic Compounds / adverse effects
  • Organometallic Compounds / pharmacokinetics
  • Patient Safety
  • Predictive Value of Tests
  • Quinolines / administration & dosage
  • Risk Assessment
  • Risk Factors
  • Thiophenes / administration & dosage*
  • Thiophenes / adverse effects
  • Thiophenes / pharmacokinetics
  • Young Adult

Substances

  • Anti-Infective Agents
  • Aza Compounds
  • Bone Density Conservation Agents
  • Fluoroquinolones
  • Organometallic Compounds
  • Quinolines
  • Thiophenes
  • strontium ranelate
  • Moxifloxacin