Fibroblast growth factor receptor (FGFR) inhibitors: A review of a novel therapeutic class

Area of Science:

• Oncology
• Genomics
• Pharmacology

Background:

• Advanced cancers often lack effective treatment options, leading to reliance on genomic alterations for targeted therapies.
• Fibroblast growth factor receptor (FGFR) alterations, including amplifications, mutations, rearrangements, and fusions, are frequent in various cancers.

Purpose of the Study:

• To review the role of fibroblast growth factor receptor (FGFR) inhibitors in cancer therapeutics.
• To outline the current FDA-approved FGFR inhibitors, erdafitinib and pemigatinib, and their indications.
• To discuss the potential future applications of FGFR inhibitors in urothelial carcinoma, cholangiocarcinoma, and other malignancies.

Main Methods:

• Review of current literature on fibroblast growth factor receptor (FGFR) alterations and inhibitors in cancer treatment.
• Analysis of FDA-approved medications targeting FGFR alterations, including erdafitinib and pemigatinib.
• Exploration of ongoing research and pipeline candidates for FGFR inhibitors.

Main Results:

• Erdafitinib and pemigatinib are FDA-approved FGFR inhibitors for specific advanced cancers (metastatic urothelial carcinoma and unresectable cholangiocarcinoma, respectively).
• These inhibitors target specific FGFR alterations (FGFR2, FGFR3) and represent a promising drug class.
• Multiple FGFR inhibitors are in clinical development, suggesting expanded therapeutic roles and potential approvals for other cancer types.

Conclusions:

• Fibroblast growth factor receptor (FGFR) inhibitors are emerging as crucial targeted therapies for advanced cancers with specific genomic alterations.
• Current approvals for erdafitinib and pemigatinib highlight the clinical utility of FGFR inhibition in urothelial carcinoma and cholangiocarcinoma.
• The ongoing development of FGFR inhibitors indicates a promising future for personalized cancer treatment across a broader range of malignancies.