A repeat-dose thorough QT study of inhaled fluticasone furoate/vilanterol combination in healthy subjects

Br J Clin Pharmacol. 2014 Mar;77(3):466-79. doi: 10.1111/bcp.12243.

Abstract

Aims: This study was designed as a thorough QT (TQT) study to evaluate the effects of fluticasone furoate (FF)/vilanterol (VI) in healthy subjects. Supportive data from a TQT study conducted with FF are also presented.

Methods: This was a randomized, placebo- and positive-controlled, double-dummy, double-blind, four-way crossover study, in which healthy subjects (n = 85) were randomized to 7 days of once-daily treatment of FF/VI (200/25 or 800/100 μg) or placebo or single-dose oral moxifloxacin (single-blind, 400 mg). In the supportive TQT study, subjects (n = 40) were randomized to single-dose inhaled FF (4000 μg), oral moxifloxacin (400 mg) or placebo.

Results: There was a lack of effect of FF/VI (200/25 μg) on QTcF (Fridericia's correction); all time-matched mean differences from baseline relative to placebo (0-24 h) were <5 ms, with upper 90% confidence intervals (CI) of <10 ms. At 800/100 μg, FF/VI had no significant clinical effect on QTcF except at 30 min postdose when the 90% CI was >10 ms [mean (90% CI), 9.6 ms (7.2, 12.0)]. No effect on QTci (individually corrected) was observed at either strength of FF/VI, with mean time-matched treatment differences <5 ms at all time points [upper 90% CIs <10 ms (0-24 h)]. Assay sensitivity was confirmed; moxifloxacin prolonged QTcF and QTci, with time-matched mean differences from baseline relative to placebo of >10 ms (1-8 h postdose).

Conclusions: Repeat once-daily dosing of FF/VI (200/25 μg), which is the highest therapeutic strength used in phase III studies, is not associated with QTc prolongation in healthy subjects. Supratherapeutic strength FF/VI (800/100 μg) demonstrated a small transient effect on QTcF but not on QTci.

Trial registration: ClinicalTrials.gov NCT01209026.

Keywords: fluticasone furoate; healthy subjects; moxifloxacin; thorough QT; vilanterol.

Publication types

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

MeSH terms

  • Administration, Inhalation
  • Adolescent
  • Adult
  • Aged
  • Androstadienes / administration & dosage*
  • Androstadienes / adverse effects
  • Androstadienes / pharmacokinetics
  • Benzyl Alcohols / administration & dosage*
  • Benzyl Alcohols / adverse effects
  • Benzyl Alcohols / pharmacokinetics
  • Bronchodilator Agents / administration & dosage*
  • Bronchodilator Agents / adverse effects
  • Bronchodilator Agents / pharmacokinetics
  • Chlorobenzenes / administration & dosage*
  • Chlorobenzenes / adverse effects
  • Chlorobenzenes / pharmacokinetics
  • Cross-Over Studies
  • Double-Blind Method
  • Drug Administration Schedule
  • Drug Combinations
  • Female
  • Glucocorticoids / administration & dosage*
  • Glucocorticoids / adverse effects
  • Glucocorticoids / pharmacokinetics
  • Healthy Volunteers
  • Heart Rate / drug effects*
  • Humans
  • London
  • Long QT Syndrome / chemically induced
  • Long QT Syndrome / physiopathology
  • Male
  • Middle Aged
  • Risk Assessment
  • Young Adult

Substances

  • Androstadienes
  • Benzyl Alcohols
  • Bronchodilator Agents
  • Chlorobenzenes
  • Drug Combinations
  • Glucocorticoids
  • vilanterol
  • fluticasone furoate

Associated data

  • ClinicalTrials.gov/NCT01209026