Inhalation of the prodrug PI3K inhibitor CL27c improves lung function in asthma and fibrosis

Nat Commun. 2018 Dec 12;9(1):5232. doi: 10.1038/s41467-018-07698-6.

Abstract

PI3K activation plays a central role in the development of pulmonary inflammation and tissue remodeling. PI3K inhibitors may thus offer an improved therapeutic opportunity to treat non-resolving lung inflammation but their action is limited by unwanted on-target systemic toxicity. Here we present CL27c, a prodrug pan-PI3K inhibitor designed for local therapy, and investigate whether inhaled CL27c is effective in asthma and pulmonary fibrosis. Mice inhaling CL27c show reduced insulin-evoked Akt phosphorylation in lungs, but no change in other tissues and no increase in blood glycaemia, in line with a local action. In murine models of acute or glucocorticoid-resistant neutrophilic asthma, inhaled CL27c reduces inflammation and improves lung function. Finally, inhaled CL27c administered in a therapeutic setting protects from bleomycin-induced lung fibrosis, ultimately leading to significantly improved survival. Therefore, local delivery of a pan-PI3K inhibitor prodrug reduces systemic on-target side effects but effectively treats asthma and irreversible pulmonary fibrosis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Inhalation
  • Animals
  • Asthma / chemically induced
  • Asthma / drug therapy*
  • Asthma / pathology
  • Benzene Derivatives / administration & dosage
  • Benzene Derivatives / therapeutic use*
  • Bleomycin / toxicity
  • Disease Models, Animal
  • Enzyme Inhibitors / administration & dosage
  • Enzyme Inhibitors / therapeutic use*
  • Esters / administration & dosage
  • Esters / therapeutic use*
  • Mice
  • Mice, Inbred BALB C
  • Mice, Inbred C57BL
  • Ovalbumin / toxicity
  • Phosphoinositide-3 Kinase Inhibitors*
  • Phosphorylation / drug effects
  • Proto-Oncogene Proteins c-akt / metabolism
  • Pulmonary Fibrosis / chemically induced
  • Pulmonary Fibrosis / drug therapy*
  • Pulmonary Fibrosis / pathology

Substances

  • Benzene Derivatives
  • CL27c
  • Enzyme Inhibitors
  • Esters
  • Phosphoinositide-3 Kinase Inhibitors
  • Bleomycin
  • Ovalbumin
  • Proto-Oncogene Proteins c-akt