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    DRUG:

    dabogratinib (TYRA-300)

    i
    Other names: TYRA-300
    Company:
    Tyra Biosci
    Drug class:
    FGFR3 inhibitor
    Related drugs:
    1m
    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)
    1m
    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)
    2ms
    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)
    6ms
    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)
    6ms
    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)
    8ms
    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)
    9ms
    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)
    9ms
    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)
    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, 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)
    1year
    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) • dabogratinib (TYRA-300)
    over1year
    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 | N=36 --> 60 | Trial primary completion date: Jan 2024 --> May 2024
    Enrollment change • Trial primary completion date
    |
    dabogratinib (TYRA-300)
    almost2years
    A Relative Bioavailability and Food Effect Study of TYRA-300-B01 Capsule and Tablet Formulations in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=36, Recruiting, Tyra Biosciences, Inc
    Trial completion date • Trial primary completion date
    |
    dabogratinib (TYRA-300)