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Inhibition of FGF‐FGFR and VEGF‐VEGFR signalling in cancer treatment
Authors:Guihong Liu  Tao Chen  Zhenyu Ding  Yang Wang  Yuquan Wei  Xiawei Wei
Institution:1. Laboratory of Aging Research and Cancer Drug Target, State Key Laboratory of Biotherapy, National Clinical Research Center for Geriatrics, West China Hospital, Sichuan University, Chengdu China ; 2. Cardiology Department, Chengdu NO.7 People’s Hospital, Chengdu Tumor Hospital, Chengdu China ; 3. Department of Biotherapy, State Key Laboratory of Biotherapy, Cancer Center, West China Hospital, Sichuan University, Chengdu China
Abstract:The sites of targeted therapy are limited and need to be expanded. The FGF‐FGFR signalling plays pivotal roles in the oncogenic process, and FGF/FGFR inhibitors are a promising method to treat FGFR‐altered tumours. The VEGF‐VEGFR signalling is the most crucial pathway to induce angiogenesis, and inhibiting this cascade has already got success in treating tumours. While both their efficacy and antitumour spectrum are limited, combining FGF/FGFR inhibitors with VEGF/VEGFR inhibitors are an excellent way to optimize the curative effect and expand the antitumour range because their combination can target both tumour cells and the tumour microenvironment. In addition, biomarkers need to be developed to predict the efficacy, and combination with immune checkpoint inhibitors is a promising direction in the future. The article will discuss the FGF‐FGFR signalling pathway, the VEGF‐VEGFR signalling pathway, the rationale of combining these two signalling pathways and recent small‐molecule FGFR/VEGFR inhibitors based on clinical trials.
Keywords:FGFR/VEGFR inhibitor  fibroblast growth factor  fibroblast growth factor receptor  vascular endothelial growth factor  vascular endothelial growth factor receptor
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