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Anti-Cancer Agents in Medicinal Chemistry

Editor-in-Chief

ISSN (Print): 1871-5206
ISSN (Online): 1875-5992

Review Article

Fibroblast Growth Factor Receptor (FGFR): A New Target for Non-small Cell Lung Cancer Therapy

Author(s): Federica Biello, Giovanni Burrafato, Erika Rijavec, Carlo Genova, Giulia Barletta, Anna Truini, Simona Coco, Maria Giovanna Dal Bello, Angela Alama, Francesco Boccardo and Francesco Grossi

Volume 16, Issue 9, 2016

Page: [1142 - 1154] Pages: 13

DOI: 10.2174/1871520616666160204112347

Price: $65

Abstract

Lung cancer is still the leading cause of cancer related death worldwide. Fibroblast growth factor receptor (FGFR) is a tirosine-kinase receptor that is seen to be amplified or mutated in non-small cell lung cancer (NSCLC) and it plays a crucial role in tumour development and maintenance.

The authors analyzed the state of the art of FGFR by reviewing the current literature. Fibroblast growth factor (FGF)-FGFR pathway and their aberrations are described, with the evaluation of their possible prognostic role in NSCLC and in particular in squamous cell carcinomas, in which FGFR is more often amplified. New therapeutic agents targeting FGFR signaling have been developed and are now in clinical evaluation.

Dysregulation of FGF signaling in tumour cells is related to FGFR gene amplification or mutation, although it is still uncertain which of these aberrations represents a real predictor of response to specific inhibitors. However, recent evidence has questioned whether FGFR is a real target in squamous cell histology. The effectiveness of FGFR inhibitors is also still unclear since there are no clinical data on selected patients. Moreover, the management of specific side effects related to inhibition of the physiological role of FGF should be more thorough.

Keywords: fifbroblast growth factor receptor (FGFR), non-small-cell lung cancer (NSCLC), amplification, tumorigenic role, prognostic role, targeted inhibitors.

Graphical Abstract

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