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    DRUG:

    dabogratinib (TYRA-300)

    i
    Other names: TYRA-300
    Company:
    Tyra Biosci
    Drug class:
    FGFR3 inhibitor
    Related drugs:
    3d
    SURF303: Phase 2A/B Efficacy and Safety of Dabogratinib in Participants With Low Grade Upper Tract Urothelial Carcinoma (clinicaltrials.gov)
    P2, N=230, Recruiting, Tyra Biosciences, Inc | Not yet recruiting --> Recruiting
    Enrollment open
    |
    FGFR3 (Fibroblast growth factor receptor 3)
    |
    dabogratinib (TYRA-300)
    7d
    SURF301: Safety and Preliminary Anti-Tumor Activity of TYRA-300 in Advanced Urothelial Carcinoma and Other Solid Tumors With FGFR3 Gene Alterations (clinicaltrials.gov)
    P1/2, N=310, Active, not recruiting, Tyra Biosciences, Inc | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    FGFR3 mutation
    |
    dabogratinib (TYRA-300)
    2ms
    SURF303: Phase 2A/B Efficacy and Safety of Dabogratinib in Participants With Low Grade Upper Tract Urothelial Carcinoma (clinicaltrials.gov)
    P2, N=230, Not yet recruiting, Tyra Biosciences, Inc
    New P2 trial
    |
    FGFR3 (Fibroblast growth factor receptor 3)
    |
    dabogratinib (TYRA-300)
    3ms
    Dabogratinib (TYRA-300), an FGFR3 Isoform-Selective Inhibitor: Preclinical and Initial Clinical Evidence of Antitumor Activity. (PubMed, Mol Cancer Ther)
    In a xenograft model driven by an FGFR3S249C-activating mutation, dabogratinib treatment resulted in dose-dependent tumor growth inhibition with tumor regression observed at the highest doses. These preclinical findings are supported by the three case reports from the SURF301 study, which demonstrate early clinical activity in patients with advanced metastatic urothelial carcinoma with an FGFR3 fusion or activating mutation.
    Preclinical • Journal
    |
    FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR3 mutation
    |
    dabogratinib (TYRA-300)
    3ms
    Next-generation isoform-selective fibroblast growth factor receptor inhibitors. (PubMed, Trends Pharmacol Sci)
    Pan-FGFR-selective inhibitors (erdafitinib, pemigatinib, and futibatinib) have been developed in clinical practice...FGFR2-selective inhibitor lirafugratinib, FGFR3-selective inhibitors LOXO-435 and TYRA-300, FGFR2/3-selective inhibitor ABSK061, and FGFR4-selective inhibitors are in clinical development. Additionally, novel isoform-selective FGFR-targeting degraders, FGFR2b/FGFR3-selective antibodies, and de novo-designed 'c' isoform-selective proteins provide novel treatment strategies. This review provides an overview of the current FGFR-targeted therapeutics and limitations and evaluates next-generation inhibitor development to guide future research.
    Review • Journal
    |
    FGFR2 (Fibroblast growth factor receptor 2) • FGFR3 (Fibroblast growth factor receptor 3) • FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4)
    |
    Balversa (erdafitinib) • Lytgobi (futibatinib) • Pemazyre (pemigatinib) • lirafugratinib (RLY-4008) • dabogratinib (TYRA-300) • ABSK061 • vepugratinib (LY3866288)
    3ms
    Dabogratinib (TYRA-300), an FGFR3 isoform-selective inhibitor: preclinical and initial clinical evidence of anti-tumor activity. (PubMed, Mol Cancer Ther)
    In a xenograft model driven by an FGFR3 S249C activating mutation, dabogratinib treatment resulted in dose-dependent tumor growth inhibition with tumor regression observed at the highest doses. These preclinical findings are supported by the three case reports from the SURF301 study, which demonstrate early clinical activity in advanced mUC patients with an FGFR3 fusion or activating mutation.
    Preclinical • Journal
    |
    FGFR3 (Fibroblast growth factor receptor 3)
    |
    FGFR3 mutation
    |
    dabogratinib (TYRA-300)
    8ms
    SURF302: Efficacy and Safety of TYRA-300 in Participants With FGFR3 Altered Low Grade, Intermediate Risk Non-Muscle Invasive Bladder Cancer (clinicaltrials.gov)
    P2, N=90, Recruiting, Tyra Biosciences, Inc | Not yet recruiting --> Recruiting
    Enrollment open
    |
    dabogratinib (TYRA-300)
    8ms
    SURF302: Efficacy and Safety of TYRA-300 in Participants With FGFR3 Altered Low Grade, Intermediate Risk Non-Muscle Invasive Bladder Cancer (clinicaltrials.gov)
    P2, N=90, Not yet recruiting, Tyra Biosciences, Inc
    New P2 trial
    |
    dabogratinib (TYRA-300)
    10ms
    A Relative Bioavailability and Food Effect Study of TYRA-300-B01 Capsule and Tablet Formulations in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=60, Active, not recruiting, Tyra Biosciences, Inc | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    dabogratinib (TYRA-300)
    11ms
    A Study of TYRA-300 in Children With Achondroplasia: BEACH301 (clinicaltrials.gov)
    P2, N=92, Recruiting, Tyra Biosciences, Inc | Not yet recruiting --> Recruiting
    Enrollment open
    |
    dabogratinib (TYRA-300)
    11ms
    A Study of TYRA-300 in Children With Achondroplasia: BEACH301 (clinicaltrials.gov)
    P2, N=92, Not yet recruiting, Tyra Biosciences, Inc
    New P2 trial
    |
    dabogratinib (TYRA-300)
    12ms
    A Relative Bioavailability and Food Effect Study of TYRA-300-B01 Capsule and Tablet Formulations in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=60, Recruiting, Tyra Biosciences, Inc | Trial completion date: Jul 2024 --> Jul 2025 | Trial primary completion date: May 2024 --> May 2025
    Trial completion date • Trial primary completion date
    |
    dabogratinib (TYRA-300)