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Updated: Feb 8, 2026

Development of Inhibitors of Protein-protein Interactions through REPLACE: Application to the Design and Development Non-ATP Competitive CDK Inhibitors
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Future applications of FGF/FGFR inhibitors in cancer

Gaia Cristina Ghedini1, Roberto Ronca1, Marco Presta1

  • 1a Department of Molecular and Translational Medicine , University of Brescia , Brescia , Italy.

Expert Review of Anticancer Therapy
|June 26, 2018
PubMed
Abstract

Insights

Fibroblast growth factor (FGF)/FGF receptor (FGFR) inhibitors show promise for cancer treatment but face clinical challenges. Identifying biomarkers and developing combination therapies are crucial for effective use of these targeted drugs.

Area of Science:

  • Oncology
  • Molecular Biology
  • Pharmacology

Background:

  • Deregulation of the fibroblast growth factor (FGF)/FGF receptor (FGFR) signaling pathway is common in various cancers.
  • This deregulation occurs through mechanisms like gene amplification, mutations, and fusions, driving tumor development.
  • Targeting the FGF/FGFR network is a key strategy in cancer therapy development.

Purpose of the Study:

  • To review the current landscape of FGF/FGFR-targeted drugs in cancer treatment.
  • To discuss the clinical challenges associated with non-selective FGF/FGFR inhibitors.
  • To highlight the need for improved therapeutic strategies, including biomarker identification and combination therapies.

Main Methods:

  • Literature review of basic, preclinical, and clinical studies on FGF/FGFR-targeted therapies.
  • Analysis of approved non-selective FGF/FGFR inhibitors and their clinical outcomes.
  • Discussion of mechanisms of drug resistance and potential combination strategies.

Main Results:

  • Non-selective FGF/FGFR inhibitors have gained approval for cancer treatment.
  • Clinical use of these inhibitors is associated with significant complications.
  • The review identifies limitations in current therapeutic approaches.

Conclusions:

  • Accurate identification of FGF/FGFR alterations and predictive biomarkers is essential.
  • Understanding the FGF/FGFR system's role in drug resistance is critical.
  • Developing effective combination therapies involving FGF/FGFR inhibitors is a necessary next step for improving patient outcomes.
Keywords:
FGF trapsFibroblast growth factorcancerfibroblast growth factor receptormonoclonal antibodiestyrosine kinase inhibitors

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