Ataluren in cystic fibrosis: development, clinical studies and where are we now?

Expert Opin Pharmacother. 2017 Sep;18(13):1363-1371. doi: 10.1080/14656566.2017.1359255. Epub 2017 Aug 1.

Abstract

Cystic fibrosis (CF) is one of the most common genetically-acquired life-limiting conditions worldwide. The underlying defect is dysfunction of the cystic fibrosis transmembrane-conductance regulator (CFTR) which leads to progressive lung disease and other multi-system effects. Around 10% of people with CF have a class I nonsense mutation that leads to production of shortened CFTR due to a premature termination codon (PTC). Areas covered: We discuss the discovery of the small-molecule drug ataluren, which in vitro has been shown to allow read-through of PTCs and facilitate synthesis of full-length protein. We review clinical studies that have been performed involving ataluren in CF. Early-phase short-term cross-over studies showed improvement in nasal potential difference. A follow-up phase III randomised controlled trial did not show a significant difference for the primary outcome of lung function, however a post-hoc analysis suggested possible benefit in patients not receiving tobramycin. A further randomised controlled trial in patients not receiving tobramycin has been reported as showing no benefit but has not yet been published in full peer-reviewed form. Expert opinion: A small-molecule approach to facilitate read-through of PTCs in nonsense mutations makes intuitive sense. However, at present there is no high-quality evidence of clinical efficacy for ataluren in people with CF.

Keywords: Ataluren; CFTR; PTC 124; cystic fibrosis; nonsense mutation; read-through agent.

Publication types

  • Review

MeSH terms

  • Codon, Nonsense / genetics
  • Cystic Fibrosis / drug therapy*
  • Cystic Fibrosis / genetics
  • Cystic Fibrosis Transmembrane Conductance Regulator / biosynthesis*
  • Cystic Fibrosis Transmembrane Conductance Regulator / genetics
  • Drug Discovery*
  • Humans
  • Oxadiazoles / administration & dosage
  • Oxadiazoles / pharmacokinetics
  • Oxadiazoles / therapeutic use*
  • Randomized Controlled Trials as Topic
  • Treatment Outcome

Substances

  • CFTR protein, human
  • Codon, Nonsense
  • Oxadiazoles
  • Cystic Fibrosis Transmembrane Conductance Regulator
  • ataluren