A patent review of FGFR4 selective inhibition in cancer (2007-2018)

Area of Science:

• Oncology
• Molecular Biology
• Drug Discovery

Background:

• Fibroblast Growth Factor Receptor 4 (FGFR4) is a tyrosine kinase receptor involved in cell proliferation and apoptosis resistance.
• Dysregulation of FGFR4 and its ligand FGF19 is implicated in various cancers, notably hepatocellular carcinoma.
• FGFR4 signaling alterations are also observed in other solid tumors like lung, breast, and colon cancer.

Purpose of the Study:

• To review patent literature on specific FGFR4 inhibitors and their applications.
• To summarize developments in FGFR4 inhibition strategies for cancer treatment.
• To assess the current status and future potential of FGFR4 inhibitors in oncology.

Main Methods:

• Comprehensive review of patent literature concerning FGFR4 inhibitors.
• Analysis of reported preclinical results and applications of these inhibitors.
• Examination of early-phase clinical trial data for FGFR4-targeted therapies.

Main Results:

• A significant number of patents disclose diverse approaches for FGFR4 inhibition.
• These inhibitors have demonstrated promising preclinical efficacy across various cancer models.
• Several small molecule FGFR4 inhibitors are currently in early clinical trials, primarily for hepatocellular carcinoma.

Conclusions:

• FGFR4 inhibition is an emerging and relevant strategy in oncology.
• Positive clinical trial outcomes could expand the application of FGFR4 inhibitors to a broader range of tumors.
• Targeting FGFR4-FGF19 signaling dysregulation presents a promising therapeutic avenue for multiple cancer types.