Future applications of FGF/FGFR inhibitors in cancer

Abstract

Deregulation of the fibroblast growth factor (FGF)/FGF receptor (FGFR) network occurs frequently in tumors due to gene amplification, activating mutations, and oncogenic fusions. Thus, the development of FGF/FGFR-targeting therapies is the focus of several basic, preclinical, and clinical studies. Areas covered: This review will recapitulate the status of current FGF/FGFR-targeted drugs. Expert commentary: Non-selective FGF/FGFR inhibitors have been approved for cancer treatment but evidence highlights various complications affecting their use in the clinical practice. It appears mandatory to identify FGF/FGFR alterations and appropriate biomarkers that may predict and monitor response to treatment, to establish the contribution of the FGF/FGFR system to the onset of mechanisms of drug resistance, and to develop effective combinations of FGF/FGFR inhibitors with other targeted therapies.

Keywords: FGF traps; Fibroblast growth factor; cancer; fibroblast growth factor receptor; monoclonal antibodies; tyrosine kinase inhibitors.