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    BIOMARKER:

    FGFR2 Y375C

    i
    Other names: FGFR2, BEK, CD332, CEK3, CFD1, ECT1, JWS, K-SAM, KGFR, TK14, TK25, Fibroblast growth factor receptor 2
    Entrez ID:
    2263
    Related biomarkers:
    Expression
    Mutation
    CNA
    Fusion
    Others
    3ms
    Activated FGFR2 signalling as a biomarker for selection of intrahepatic cholangiocarcinoma patients candidate to FGFR targeted therapies. (PubMed, Sci Rep)
    This last finding entails that also this setting of patients could benefit from FGFR targeted therapies, widening indication of these drugs for iCCA patients beyond current approval. Future clinical studies are therefore encouraged to confirm this hypothesis.
    Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGF10 (Fibroblast Growth Factor 10)
    |
    FGFR2 mutation • FGFR2 expression • FGFR2b expression • FGFR2 C382R • FGFR2 F276C • FGFR2 Y375C • FGFR wild-type • FGFR2 wild-type
    4ms
    NCCH2006/MK010 Trial (FORTUNE Trial) (clinicaltrials.gov)
    P2, N=46, Active, not recruiting, National Cancer Center, Japan | Recruiting --> Active, not recruiting
    Enrollment closed • Metastases
    |
    EGFR (Epidermal growth factor receptor) • KRAS (KRAS proto-oncogene GTPase) • BRAF (B-raf proto-oncogene) • ALK (Anaplastic lymphoma kinase) • NRAS (Neuroblastoma RAS viral oncogene homolog) • FGFR2 (Fibroblast growth factor receptor 2) • ROS1 (Proto-Oncogene Tyrosine-Protein Kinase ROS) • FGFR4 (Fibroblast growth factor receptor 4) • NTRK (Neurotrophic receptor tyrosine kinase)
    |
    EGFR mutation • BRAF mutation • NRAS mutation • BRAF V600 • FGFR1 amplification • FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR2 N549K • FGFR1 fusion • FGFR3 fusion • FGFR2 P253R • FGFR2 K310R • FGFR3 Y375C • FGFR2 C382R • FGFR2 N549D • FGFR2 N549H • FGFR2 S252W • FGFR2 Y375C • FGFR3 G380R • FGFR3 K650E • FGFR2 W290C
    |
    tasurgratinib (E7090)
    6ms
    Efficacy of futibatinib, an irreversible fibroblast growth factor receptor inhibitor, in FGFR-altered breast cancer. (PubMed, Sci Rep)
    Per institutional and public databases, FGFR2 mutations and amplifications had a population frequency of 1.1%-2.6% and 1.5%-2.5%, respectively, in breast cancer patients. FGFR2 alterations in breast cancer may represent infrequent but highly promising targets for futibatinib.
    Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR2 mutation • FGFR2 amplification • FGFR2 overexpression • FGFR1 expression • FGFR2 expression • FGFR3 Y375C • FGFR2 Y375C
    |
    Lytgobi (futibatinib)
    1year
    Clinical and translational findings of pemigatinib in previously treated solid tumors with activating FGFR1-3 alterations in the FIGHT-207 study (AACR 2023)
    In addition to cholangiocarcinoma, pemigatinib showed clinical activity in gliomas, gynecologic tumors, and pancreatic cancer and safety was consistent with prior reports. We observed responses in patients with previously unreported FGFR alterations, suggesting that a broader population of patients may benefit from FGFR inhibitors. Further correlative work to predict response to therapy is needed to better identify these patients.Table.
    Clinical
    |
    TP53 (Tumor protein P53) • FGFR2 (Fibroblast growth factor receptor 2) • FGFR1 (Fibroblast growth factor receptor 1) • BAP1 (BRCA1 Associated Protein 1)
    |
    HER-2 mutation • FGFR2 mutation • FGFR2 fusion • FGFR1 mutation • BAP1 mutation • FGFR1 fusion • FGFR3 fusion • FGFR1 rearrangement • FGFR2 C382R • FGFR2 Y375C • FGFR2 W290C
    |
    Pemazyre (pemigatinib)
    over2years
    Efficacy of futibatinib, an irreversible fibroblast growth factor receptor (FGFR) inhibitor, in breast cancer models with FGFR alterations (SABCS 2021)
    Futibatinib had single agent activity of selected breast cancer PDX models. FGFR2 activating mutations and amplification may represent rare but promising therapeutic targets to FGFR inhibition.
    Clinical • Preclinical
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4) • BICC1 (BicC Family RNA Binding Protein 1)
    |
    FGFR2 mutation • FGFR2 fusion • FGFR2 amplification • FGFR2-BICC1 fusion • FGFR1 expression • FGFR2 expression • FGFR2b expression • FGFR4 expression • FGFR3 Y375C • FGFR2 Y375C
    |
    Lytgobi (futibatinib)
    over2years
    The frequency and somatic mutation landscape of Fibroblast growth factor receptor ( FGFR ) alterations in breast cancer (SABCS 2021)
    High-level FGFR amplifications are observed in >11% of breast cancers, especially the ER+/HER2- subtype, while mutations/fusions are rare. These data support the ongoing studies evaluating targeted therapies for FGFR amplified ER + breast cancer. Correlations with clinical information (MC cohort) and associations with actionable alterations are ongoing and may inform potential combination strategies.
    Tumor Mutational Burden • BRCA Biomarker • MSi-H Biomarker
    |
    HER-2 (Human epidermal growth factor receptor 2) • ER (Estrogen receptor) • TP53 (Tumor protein P53) • PIK3CA (Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha) • TMB (Tumor Mutational Burden) • BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset) • MSI (Microsatellite instability) • FGFR2 (Fibroblast growth factor receptor 2) • PTEN (Phosphatase and tensin homolog) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • CCND1 (Cyclin D1) • TACC3 (Transforming acidic coiled-coil containing protein 3) • FGFR4 (Fibroblast growth factor receptor 4) • CDK4 (Cyclin-dependent kinase 4) • PIK3R1 (Phosphoinositide-3-Kinase Regulatory Subunit 1) • BAG4 (BAG Cochaperone 4) • EMSY (EMSY Transcriptional Repressor BRCA2 Interacting) • TACC1 (Transforming Acidic Coiled-Coil Containing Protein 1)
    |
    MSI-H/dMMR • HER-2 amplification • HER-2 negative • HER-2 mutation • FGFR1 amplification • FGFR2 mutation • FGFR2 fusion • FGFR mutation • FGFR fusion • FGFR2 N549K • FGFR1 fusion • FGFR3 fusion • FGFR3 Y375C • FGFR2 Y375C