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Screening and Identification of Small Peptides Targeting Fibroblast Growth Factor Receptor2 using a Phage Display Peptide Library
Published on: September 30, 2019
Fibroblast Growth Factor Receptor (FGFR) Inhibitors in Urothelial Cancer
Rohan Garje1,2, Josiah An1,2, Mohammad Obeidat3
1Division of Hematology, Oncology, Blood & Marrow Transplantation, University of Iowa, Iowa City, Iowa, USA.
Abstract:
Dysregulated fibroblast growth factor receptor (FGFR) signaling is associated with several cancers, including urothelial carcinoma. Preclinical studies with FGFR inhibitors have shown significant antitumor activity, which has led to clinical evaluation of multiple FGFR inhibitors. Recently, erdafitinib was approved by the U.S. Food and Drug Administration for advanced urothelial carcinoma with FGFR gene alterations as the first molecularly targeted therapy. Additional ongoing clinical trials with other types of FGFR inhibitors have shown encouraging results. This review summarizes the oncogenic signaling of FGFR alterations, completed and ongoing clinical trials of FGFR inhibitors, and resistance patterns. IMPLICATIONS FOR PRACTICE: Dysregulated fibroblast growth factor receptor (FGFR) signaling is associated with several cancers, including urothelial carcinoma. Preclinical studies with FGFR inhibitors have shown significant antitumor activity, which has led to clinical evaluation of multiple FGFR inhibitors. Most recently, erdafitinib was approved by the U.S. Food and Drug Administration for advanced urothelial carcinoma with FGFR gene alterations as the first molecularly targeted therapy. Additional ongoing clinical trials with other types of FGFR inhibitors have shown encouraging results. This review summarizes the oncogenic signaling of FGFR alterations, completed and ongoing clinical trials of FGFR inhibitors, and resistance patterns.
Insights
Fibroblast growth factor receptor (FGFR) signaling dysregulation drives urothelial carcinoma. FGFR inhibitors, including the approved erdafitinib, show promise, with ongoing trials exploring their efficacy and resistance patterns.
Area of Science:
- Oncology
- Molecular Biology
- Cancer Therapeutics
Background:
- Dysregulated fibroblast growth factor receptor (FGFR) signaling is implicated in various cancers, notably urothelial carcinoma.
- Preclinical research demonstrated significant antitumor effects of FGFR inhibitors, prompting clinical investigations.
- Erdafitinib represents a breakthrough as the first targeted therapy approved for advanced urothelial carcinoma with FGFR alterations.
Purpose of the Study:
- To review the role of FGFR signaling in oncogenesis.
- To summarize the clinical trial landscape of FGFR inhibitors.
- To discuss emerging resistance mechanisms against FGFR-targeted therapies.
Main Methods:
- Literature review of preclinical and clinical studies on FGFR inhibitors.
- Analysis of oncogenic signaling pathways driven by FGFR alterations.
- Synthesis of data from completed and ongoing clinical trials.
Main Results:
- FGFR inhibitors have demonstrated substantial antitumor activity in urothelial carcinoma.
- Erdafitinib's FDA approval marks a significant advancement in targeted therapy for FGFR-altered tumors.
- Ongoing trials continue to yield encouraging results for various FGFR inhibitors.
Conclusions:
- Targeted inhibition of FGFR signaling is a viable therapeutic strategy for urothelial carcinoma.
- Understanding resistance patterns is crucial for optimizing long-term treatment outcomes.
- The development of FGFR inhibitors represents a paradigm shift in cancer treatment.
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