Hepatocellular carcinoma (HCC) is the sixth most common type of cancer, with an increasing mortality rate. Aberrant expression of fibroblast growth factor 19–fibroblast growth factor receptor 4 (FGF19–FGFR4
) is reported to be an oncogenic-driver pathway for HCC patients. Thus, the FGF19–FGFR4
signaling pathway is a promising target for the treatment of HCC. Several pan-FGFR
(1–4) and FGFR4
-specific inhibitors are in different phases of clinical trials. In this review, we summarize the information, recent developments, binding modes, selectivity, and clinical trial phases of different available FGFR4
inhibitors. We also discuss future perspectives and highlight the points that should be addressed to improve the efficacy of these inhibitors.
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