Investigational fibroblast growth factor receptor 2 antagonists in early phase clinical trials to treat solid tumors.

Abstract

Introduction: Fibroblast growth factor receptor 2 (FGFR2) is a highly conserved transmembrane tyrosine kinase receptor. FGFR2 dysregulation occurs in numerous human solid tumors and overexpression is closely associated with tumor progression. FGFR2 has recently been reported as a therapeutic target for cancer. Several targeted therapies are being investigated to disrupt FGFR2 activity; these include multi-target tyrosine kinase inhibitors (TKIs), pan-FGFR targeted TKIs and FGFR2 monoclonal antibodies. Areas: This review examines FGFR2 regulation and function in cancer and its potential as a target for cancer treatment. Expert opinion: Highly specific FGFR2 blockers have not yet been developed and moreover, resistance to FGFR2-targeted therapies is a challenge. More sophisticated patient selection strategies would help improve FGFR2-targeted therapies and combination therapy is considered the most promising approach for cancer patients with FGFR2 alterations.

• Authors: Dan Wang, Li Yang, Weina Yu, Yi Zhang
• Journal: Expert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 28 Issue 10 Pg. 903-916 (Oct 2019) ISSN: 1744-7658 [Electronic] England
• PMID: 31560229 (Publication Type: Journal Article, Review)

Chemical References

• Antineoplastic Agents
• Protein Kinase Inhibitors
• FGFR2 protein, human
• Receptor, Fibroblast Growth Factor, Type 2

Topics

• Animals
• Antineoplastic Agents (administration & dosage, pharmacology)
• Drug Resistance, Neoplasm
• Humans
• Molecular Targeted Therapy
• Neoplasms (drug therapy, pathology)
• Patient Selection
• Protein Kinase Inhibitors (administration & dosage, pharmacology)
• Receptor, Fibroblast Growth Factor, Type 2 (antagonists & inhibitors)