Fibroblast growth factor receptor inhibitors as a cancer treatment: from a biologic rationale to medical perspectives

Cancer Discov. 2013 Mar;3(3):264-79. doi: 10.1158/2159-8290.CD-12-0362. Epub 2013 Feb 15.

Abstract

The fibroblast growth factor/fibroblast growth factor receptor (FGF/FGFR) signaling pathway plays a fundamental role in many physiologic processes, including embryogenesis, adult tissue homeostasis, and wound healing, by orchestrating angiogenesis. Ligand-independent and ligand-dependent activation have been implicated in a broad range of human malignancies and promote cancer progression in tumors driven by FGF/FGFR oncogenic mutations or amplifications, tumor neoangiogenesis, and targeted treatment resistance, thereby supporting a strong rationale for anti-FGF/FGFR agent development. Efforts are being pursued to develop selective approaches for use against this pathway by optimizing the management of emerging, class-specific toxicity profiles and correctly designing clinical trials to address these different issues.

Publication types

  • Review

MeSH terms

  • Animals
  • Clinical Trials as Topic
  • Humans
  • Neoplasms / blood supply
  • Neoplasms / drug therapy*
  • Neoplasms / enzymology
  • Neovascularization, Pathologic / drug therapy
  • Neovascularization, Pathologic / enzymology
  • Protein Kinase Inhibitors / pharmacology*
  • Protein Kinase Inhibitors / therapeutic use*
  • Randomized Controlled Trials as Topic
  • Receptors, Fibroblast Growth Factor / antagonists & inhibitors*
  • Receptors, Fibroblast Growth Factor / genetics
  • Receptors, Fibroblast Growth Factor / metabolism
  • Signal Transduction

Substances

  • Protein Kinase Inhibitors
  • Receptors, Fibroblast Growth Factor