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GENE:

FGFR2 (Fibroblast growth factor receptor 2)

i
Other names: FGFR2, BEK, CD332, CEK3, CFD1, ECT1, JWS, K-SAM, KGFR, TK14, TK25, Fibroblast growth factor receptor 2
3d
Copy Number-Based Oncogene Dominance May Suggest ERBB2 Dependence and Trastuzumab Response in HER2-Positive Gastric Cancer. (PubMed, Target Oncol)
Copy number-based oncogene dominance may suggest tumor dependence and response to HER2-targeted therapy, highlighting a potential novel biomarker in HER2-positive gastric cancer.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • FGFR2 (Fibroblast growth factor receptor 2) • CCNE1 (Cyclin E1)
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HER-2 positive • HER-2 amplification • EGFR positive
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Herceptin (trastuzumab) • oxaliplatin • Teysuno (gimeracil/oteracil/tegafur)
3d
Lirafugratinib attenuates ABCG2-dependent drug efflux and restores chemosensitivity in multidrug-resistant nonsmall cell lung cancer cells. (PubMed, Drug Metab Dispos)
SIGNIFICANCE STATEMENT: This work identifies lirafugratinib, a highly selective fibroblast growth factor receptor 2 inhibitor, as a previously unrecognized suppressor of ABCG2-dependent MDR. By limiting efflux-mediated depletion of anticancer drugs while maintaining its own activity, lirafugratinib resensitizes resistant nonsmall cell lung cancer cells to cytotoxic agents, supporting its potential utility in combination regimens for tumors with elevated ABCG2 expression.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • ABCG2 (ATP Binding Cassette Subfamily G Member 2)
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lirafugratinib (RLY-4008)
4d
Comparison of the Efficacy of 35 Anticancer Drugs According to Genomic Profiling and Biological Characteristics of 14 Gastric Cancer Cell Lines. (PubMed, Int J Mol Sci)
This study provides a framework for selecting cell lines that are responsive to each of the 35 anticancer drugs and elucidating their underlying therapeutic mechanisms through follow-up studies. Ultimately, clinical studies are required to confirm the therapeutic efficacy of the selected drugs.
Clinical • Preclinical • Journal • PD(L)-1 Biomarker • IO biomarker
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • PD-L1 (Programmed death ligand 1) • FGFR2 (Fibroblast growth factor receptor 2) • CLDN18 (Claudin 18) • CDK12 (Cyclin dependent kinase 12) • CD44 (CD44 Molecule) • TGFB1 (Transforming Growth Factor Beta 1)
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PD-L1 overexpression • HER-2 overexpression • MET overexpression • FGFR2 overexpression
9d
Epidemiology, biomarkers, and therapeutic approach in early-stage biliary tract cancers. (PubMed, Chin Clin Oncol)
In recent years, studies of adjuvant chemotherapy with capecitabine or S-1 have shown improved survival compared to postoperative observation alone...The goal of these treatment strategies is to improve surgical outcomes and identify new modalities to reduce recurrence rates of early-stage BTCs. This review provides an overview of the current management landscape of early-stage BTC, presenting the epidemiology and risk factors, reviewing the current management paradigm, and highlighting emerging therapeutic strategies.
Review • Journal • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • FGFR2 (Fibroblast growth factor receptor 2) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • SMAD4 (SMAD family member 4)
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capecitabine
11d
Fibroblast Growth Factor Receptor (FGFR) Inhibitors for the Treatment of Cholangiocarcinoma: Key Therapeutic Developments and Knowledge Gaps. (PubMed, Drug Des Devel Ther)
Parallel translational work using cfDNA-based liquid biopsy has mapped a spectrum of secondary kinase-domain mutations that underlie acquired resistance, informing the development of next-generation FGFR2-selective inhibitors (eg, lirafugratinib) and combination strategies with EGFR/ERBB blockade. Collectively, these data underscore the need for comprehensive molecular profiling and innovative umbrella trial designs to optimise targeted therapy in this rare, biologically heterogeneous malignancy.
Review • Journal • MSi-H Biomarker
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EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2) • BRAF (B-raf proto-oncogene) • MSI (Microsatellite instability) • FGFR2 (Fibroblast growth factor receptor 2) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • FGFR (Fibroblast Growth Factor Receptor)
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BRAF V600E • MSI-H/dMMR • HER-2 amplification • BRAF V600 • IDH1 mutation • FGFR2 mutation • FGFR2 fusion • IDH mutation + BRAF V600E
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lirafugratinib (RLY-4008)
12d
Aptamer-Mediated Proximity Labeling (ApMPL) for Spatially Resolved Deciphering of Cell Membrane Protein Interactomes. (PubMed, Anal Chem)
Additionally, the versatility and adaptability of the platform have been confirmed on the PTK7 protein and the FGFR2 protein. The ApMPL platform will be valuable for discovering membrane protein interactions, elucidating critical signaling networks, and facilitating therapeutic target identification.
Journal
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FGFR2 (Fibroblast growth factor receptor 2) • PTK7 (Protein Tyrosine Kinase 7) • NCL (Nucleolin)
13d
FGFR rearrangements: oncogenic drivers and therapeutic targets. (PubMed, Trends Cancer)
It covers their mechanisms in driving cancer, their potential as biomarkers to predict treatment response, and the emerging challenges and opportunities for FGFR-targeted therapy. Ultimately, a deeper understanding of FGFR rearrangements is critical for advancing precision oncology and improving patient benefit.
Review • Journal
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FGFR2 (Fibroblast growth factor receptor 2) • FGFR (Fibroblast Growth Factor Receptor)
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FGFR2 fusion • FGFR fusion
13d
Systemic therapy for combined hepatocellular-cholangiocarcinoma: a comprehensive review of chemotherapy, immunotherapy, and targeted therapy. (PubMed, J Liver Cancer)
Retrospective data indicate that gemcitabine plus platinum-based chemotherapy achieves the most consistent efficacy among conventional regimens, with median overall survival (OS) of 10-16 months...For clinical settings where comprehensive genomic profiling is not feasible, we discuss a pragmatic surrogate-based approach using imaging characteristics and serum tumor markers to guide initial treatment selection. We also address post-progression treatment considerations, including phenotype-based regimen switching and the role of re-biopsy.
Journal • IO biomarker
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HER-2 (Human epidermal growth factor receptor 2) • FGFR2 (Fibroblast growth factor receptor 2) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1)
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EGFR mutation • HER-2 amplification • IDH1 mutation • FGFR2 mutation • FGFR2 fusion
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gemcitabine
15d
A Study of E7090 in Participants With Unresectable Advanced or Metastatic Cholangiocarcinoma With Fibroblast Growth Factor Receptor (FGFR) 2 Gene Fusion (clinicaltrials.gov)
P2, N=63, Completed, Eisai Co., Ltd. | Active, not recruiting --> Completed | Trial completion date: Mar 2026 --> Nov 2025 | Trial primary completion date: Mar 2026 --> Nov 2025
Trial completion • Trial completion date • Trial primary completion date
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FGFR2 (Fibroblast growth factor receptor 2)
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FGFR2 fusion
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Tasfygo (tasurgratinib)
18d
REFOCUS: A First-in-Human Study of Highly Selective FGFR2 Inhibitor, RLY-4008, in Patients With ICC and Other Advanced Solid Tumors (clinicaltrials.gov)
P1/2, N=490, Completed, Elevar Therapeutics | Active, not recruiting --> Completed | Trial completion date: Dec 2027 --> Sep 2025
Trial completion • Trial completion date • First-in-human
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FGFR2 (Fibroblast growth factor receptor 2) • FGF23 (Fibroblast Growth Factor 23) • CA 19-9 (Cancer antigen 19-9)
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FGFR2 mutation • FGFR2 fusion
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lirafugratinib (RLY-4008)
18d
Trial completion date • Trial primary completion date
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FGFR2 (Fibroblast growth factor receptor 2)
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FGFR2 fusion
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Tasfygo (tasurgratinib)
19d
Genomic Landscape of Poorly Differentiated Gastric Carcinoma: An AACR GENIE® Project. (PubMed, Life (Basel))
Metastatic enrichment of CDH1 and MLH1 supports their roles in invasion and therapeutic resistance. Together, these findings highlight candidate biomarkers and actionable pathways warranting validation in larger, multi-omic cohorts to refine precision treatment strategies for this aggressive gastric cancer subtype.
Journal
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HER-2 (Human epidermal growth factor receptor 2) • KRAS (KRAS proto-oncogene GTPase) • TP53 (Tumor protein P53) • FGFR2 (Fibroblast growth factor receptor 2) • PTEN (Phosphatase and tensin homolog) • CDKN2A (Cyclin Dependent Kinase Inhibitor 2A) • ERBB3 (V-erb-b2 avian erythroblastic leukemia viral oncogene homolog 3) • ARID1A (AT-rich interaction domain 1A) • CCNE1 (Cyclin E1) • MLH1 (MutL homolog 1) • KMT2D (Lysine Methyltransferase 2D) • CDKN2B (Cyclin Dependent Kinase Inhibitor 2B) • KMT2C (Lysine Methyltransferase 2C) • CDH1 (Cadherin 1) • FAT1 (FAT atypical cadherin 1) • POLD1 (DNA Polymerase Delta 1)
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TP53 mutation • ARID1A mutation • FGFR2 mutation