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    BIOMARKER:

    FGFR3 G380R

    i
    Other names: FGFR3, ACH, CD333, CEK2, JTK4, Fibroblast growth factor receptor 3
    Entrez ID:
    2261
    Related biomarkers:
    Expression
    Mutation
    CNA
    Fusion
    Others
    3ms
    Discovery of TYRA-300: First Oral Selective FGFR3 Inhibitor for the Treatment of Urothelial Cancers and Achondroplasia. (PubMed, J Med Chem)
    The pan-FGFR inhibitor erdafitinib was approved for the treatment of mUC with FGFR3 alterations but is limited due to FGFR isoform off-target toxicities and the development of on-target gatekeeper resistance mutations. TYRA-300 (22) was conceived using a structure-based approach as a potent FGFR3-selective inhibitor to avoid the toxicities associated with inhibition of FGFR1, FGFR2, and FGFR4, and to be agnostic for the FGFR3 gatekeeper mutations. TYRA-300 is being evaluated in a Phase 1 clinical trial in urothelial cancers and solid tumors, with intention to initiate Phase 2 studies in urothelial cancers and achondroplasia.
    Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR4 (Fibroblast growth factor receptor 4)
    |
    FGFR2 mutation • FGFR3 mutation • FGFR mutation • FGFR3 G380R
    |
    Balversa (erdafitinib) • TYRA-300
    12ms
    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
    |
    Tasfygo (tasurgratinib)