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

Dan Wang1,2,3, Li Yang1,2,3, Weina Yu1,2,3

  • 1Biotherapy Center, The First Affiliated Hospital of Zhengzhou University , Zhengzhou , Henan , P.R. China.

Insights

Fibroblast growth factor receptor 2 (FGFR2) is a key target in cancer therapy. Developing specific FGFR2 blockers and improving patient selection are crucial for effective treatment.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Fibroblast growth factor receptor 2 (FGFR2) is a transmembrane tyrosine kinase receptor implicated in numerous human solid tumors.
  • FGFR2 dysregulation and overexpression correlate with tumor progression, establishing it as a significant therapeutic target in oncology.

Purpose of the Study:

  • This review critically examines the regulatory mechanisms and functional roles of FGFR2 in cancer development.
  • It evaluates the potential of FGFR2 as a therapeutic target for various human cancers.

Main Methods:

  • The review synthesizes current research on FGFR2's involvement in cancer.
  • It analyzes emerging targeted therapies, including multi-target tyrosine kinase inhibitors (TKIs), pan-FGFR TKIs, and FGFR2 monoclonal antibodies.

Main Results:

  • While FGFR2 is a promising target, highly specific blockers are still under development.
  • Resistance to current FGFR2-targeted therapies presents a significant clinical challenge.

Conclusions:

  • Improved patient stratification strategies are essential to enhance the efficacy of FGFR2-targeted therapies.
  • Combination therapy approaches are considered the most promising strategy for patients with FGFR2 alterations.

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