biostudies-literatureLiu Gthe National Natural Science Foundation Regional Innovation and Developmentthe National Major Scientific and Technological Special Project for "Significant New Drugs Development"the Development Program of Chinathe Excellent Youth Foundation of Sichuan Scientific Committee Grant in Chinae13009https://www.ebi.ac.uk/biostudies/studies/S-EPMC8016646biostudies-literatureUnknown54(4)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.Cell proliferationInhibition of FGF-FGFR and VEGF-VEGFR signalling in cancer treatment.PMC8016646U19A20032016YFA02014022018ZX097330012019JDJQ008Wei XDing ZWang YWei YLiu GChen TfalseInhibition of FGF-FGFR and VEGF-VEGFR signalling in cancer treatment.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.2021-01-01T00:00:00Z2021 Apr2022-02-09T14:27:02.339Z2022-02-09T14:27:02.339ZS-EPMC80166463365555610.1111/cpr.13009