FGFR as potential target in the treatment of squamous non small cell lung cancer

Cancer Treat Rev. 2015 Jun;41(6):527-39. doi: 10.1016/j.ctrv.2015.04.011. Epub 2015 May 1.

Abstract

To date therapeutic options for squamous cell lung cancer patients remain scarce because no druggable targets have been identified so far. Aberrant signaling by FGFs (fibroblast growth factors) and FGFRs (fibroblast growth factors receptors) has been implicated in several human cancers and, particularly, in squamous non-small cell lung cancer (NSCLC). FGFR gene amplifications, somatic missense mutations, chromosomal translocations are the most frequent mechanisms able to induce aberrant activation of this pathway. Data from literature have established that the presence of an aberrant FGFR signaling has to be considered a possible negative prognostic factor but predictive of potential sensitivity to FGFR inhibitors. In the last years, clinical research efforts allowed to identify and evaluate promising FGFR inhibitors, such as monoclonal antibodies, ligand traps, non-selective or selective tyrosine kinase inhibitors. This review summarizes the current knowledge about FGFR alterations in NSCLC and the relative inhibitors in development, in particular in squamous NSCLC.

Keywords: FGF; FGFR; NSCLC; Squamous cell carcinoma; TKI.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Carcinoma, Non-Small-Cell Lung / drug therapy*
  • Carcinoma, Squamous Cell / drug therapy*
  • ErbB Receptors / antagonists & inhibitors*
  • ErbB Receptors / chemistry
  • ErbB Receptors / genetics
  • ErbB Receptors / physiology
  • Gene Amplification
  • Gene Fusion
  • Humans
  • Lung Neoplasms / drug therapy*
  • Mutation
  • Protein Kinase Inhibitors / therapeutic use*
  • Signal Transduction

Substances

  • Protein Kinase Inhibitors
  • ErbB Receptors