A phase 3, double-blind, parallel-group study to evaluate the efficacy and safety of tezacaftor in combination with ivacaftor in participants 6 through 11 years of age with cystic fibrosis homozygous for F508del or heterozygous for the F508del-CFTR mutation and a residual function mutation

J Cyst Fibros. 2021 Jan;20(1):68-77. doi: 10.1016/j.jcf.2020.07.023. Epub 2020 Sep 21.

Abstract

Background: The CFTR modulator tezacaftor/ivacaftor was efficacious and generally safe and well tolerated in Phase 3 studies in participants ≥12 years of age with cystic fibrosis (CF) homozygous for the F508del-CFTR mutation or heterozygous with a residual function-CFTR mutation (F/F or F/RF respectively). We evaluated tezacaftor/ivacaftor's efficacy and safety over 8 weeks in participants 6 through 11 years of age with these mutations.

Methods: Participants were randomized 4:1 to tezacaftor/ivacaftor or a blinding group (placebo for F/F, ivacaftor for F/RF). The primary endpoint was within-group change from baseline in the lung clearance index 2·5 (LCI2·5) through Week 8. Secondary endpoints were change from baseline in sweat chloride (SwCl), cystic fibrosis questionnaire-revised (CFQ-R) respiratory domain score, and safety.

Results: Sixty-seven participants received at least one study drug dose. Of those, 54 received tezacaftor/ivacaftor (F/F, 42; F/RF, 12), 10 placebo, and 3 ivacaftor; 66 completed the study. The within-group change in LCI2·5 was significantly reduced (improved) by -0·51 (95% CI: -0·74, -0·29). SwCl concentration decreased (improved) by -12·3 mmol/L and CFQ-R respiratory domain score increased (improved, nonsignificantly) by 2·3 points. There were no serious adverse events (AEs) or AEs leading to tezacaftor/ivacaftor discontinuation or interruption. The most common AEs (≥10%) in participants receiving tezacaftor/ivacaftor were cough, headache, and productive cough.

Conclusions: Tezacaftor/ivacaftor improved lung function (assessed using LCI) and CFTR function (measured by SwCl concentration) in participants 6 through 11 years of age with F/F or F/RF genotypes. Tezacaftor/ivacaftor was safe and well tolerated; no new safety concerns were identified.

Keywords: Clinical trial; Cystic fibrosis; F508del-CFTR mutation; Ivacaftor; Lung clearance index; Residual function CFTR mutation; Tezacaftor.

Publication types

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

MeSH terms

  • Aminophenols / administration & dosage*
  • Aminophenols / adverse effects
  • Benzodioxoles / administration & dosage*
  • Benzodioxoles / adverse effects
  • Child
  • Chloride Channel Agonists / administration & dosage*
  • Chloride Channel Agonists / adverse effects
  • Cystic Fibrosis / drug therapy*
  • Cystic Fibrosis / genetics*
  • Cystic Fibrosis / physiopathology
  • Cystic Fibrosis Transmembrane Conductance Regulator / genetics*
  • Drug Combinations
  • Female
  • Heterozygote
  • Homozygote
  • Humans
  • Indoles / administration & dosage*
  • Indoles / adverse effects
  • Male
  • Mutation*
  • Quinolones / administration & dosage*
  • Quinolones / adverse effects
  • Treatment Outcome

Substances

  • Aminophenols
  • Benzodioxoles
  • Chloride Channel Agonists
  • Drug Combinations
  • Indoles
  • Quinolones
  • cystic fibrosis transmembrane conductance regulator delta F508
  • tezacaftor
  • Cystic Fibrosis Transmembrane Conductance Regulator
  • ivacaftor