Future applications of FGF/FGFR inhibitors in cancer

ABSTRACT

Introduction: 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:

• Fibroblast growth factor
• fibroblast growth factor receptor
• cancer
• tyrosine kinase inhibitors
• monoclonal antibodies
• FGF traps

Declaration of interest

The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This work was supported by IG 18943 and MFAG 18459 grants from Associazione Italiana per la Ricerca sul Cancro (AIRC) and by Fondazione Cariplo grant 2016-0570.