QT effect of semagacestat at therapeutic and supratherapeutic doses

Int J Clin Pharmacol Ther. 2012 Apr;50(4):290-9. doi: 10.5414/cp201672.

Abstract

Objective: This thorough QT/ QT interval corrected for heart rate (QTc) study was designed to assess the potential of semagacestat, a functional gamma-secretase inhibitor, to delay cardiac repolarization.

Methods: In this Phase I, single-dose, randomized, 4-period crossover study, semagacestat was compared with placebo in 54 healthy male and female subjects between the ages of 19 and 63 years, inclusive. Each study period included single oral-dose administrations of semagacestat 140 mg, semagacestat 280 mg, moxifloxacin 400 mg, or placebo. Study subjects and the investigator were blinded to the identity of semagacestat and placebo; however, moxifloxacin was administered as open-label. Moxifloxacin was compared with placebo for assay sensitivity analysis. Pharmacokinetic parameters were also assessed.

Results: For each QTc, the upper bound of the 2-sided 90% confidence interval (CI) for the least squares mean difference between semagacestat (at both the 140- and 280-mg dose levels) and placebo was < 10 msec at all time points, and thus, within the limits set for clinical relevance in regulatory guidelines.

Conclusions: The results of this study indicate that single doses of 140 and 280 mg semagacestat did not prolong QTc to a clinically significant degree.

Publication types

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

MeSH terms

  • Administration, Oral
  • Adult
  • Aged
  • Alanine / administration & dosage
  • Alanine / adverse effects
  • Alanine / analogs & derivatives*
  • Alanine / pharmacokinetics
  • Amyloid Precursor Protein Secretases / antagonists & inhibitors*
  • Analysis of Variance
  • Arrhythmias, Cardiac / chemically induced
  • Arrhythmias, Cardiac / diagnosis
  • Arrhythmias, Cardiac / physiopathology
  • Aza Compounds / administration & dosage
  • Aza Compounds / adverse effects
  • Azepines / administration & dosage*
  • Azepines / adverse effects
  • Azepines / pharmacokinetics
  • Cross-Over Studies
  • Electrocardiography
  • England
  • Enzyme Inhibitors / administration & dosage*
  • Enzyme Inhibitors / adverse effects
  • Enzyme Inhibitors / pharmacokinetics
  • Female
  • Fluoroquinolones
  • Heart Rate / drug effects
  • Humans
  • Least-Squares Analysis
  • Male
  • Middle Aged
  • Moxifloxacin
  • Quinolines / administration & dosage
  • Quinolines / adverse effects
  • Risk Assessment
  • Risk Factors
  • Young Adult

Substances

  • Aza Compounds
  • Azepines
  • Enzyme Inhibitors
  • Fluoroquinolones
  • N2-((2S)-2-(3,5-difluorophenyl)-2-hydroxyethanoyl)-N1-((7S)-5-methyl-6-oxo-6,7-dihydro-5H-dibenzo(b,d)azepin-7-yl)-L-alaninamide
  • Quinolines
  • Amyloid Precursor Protein Secretases
  • Alanine
  • Moxifloxacin