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    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
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    FGFR3 (Fibroblast growth factor receptor 3)
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    FGFR3 mutation
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    dabogratinib (TYRA-300)
    2ms
    FORAGER-2: A Study of Vepugratinib (LY3866288) in Participants With Cancer in the Urinary Tract (clinicaltrials.gov)
    P3, N=450, Not yet recruiting, Eli Lilly and Company
    New P3 trial
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    Keytruda (pembrolizumab) • Padcev (enfortumab vedotin-ejfv) • vepugratinib (LY3866288)
    2ms
    Interventional Study of Vosoritide for the Treatment of Children With Hypochondroplasia (clinicaltrials.gov)
    P3, N=80, Active, not recruiting, BioMarin Pharmaceutical | Enrolling by invitation --> Active, not recruiting
    Enrollment closed
    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)
    4ms
    NAT10 Increases Lysosomal Acidification to Promote Esophageal Cancer Metastasis via ac4C Acetylation of ATP6V0E1 mRNA. (PubMed, Adv Sci (Weinh))
    Furthermore, G-749 is screened and identified as a novel NAT10 inhibitor capable of effectively impeding lysosomal acidification and tumor metastasis by disrupting the NAT10-Ubiquitin-specific Peptidase 39 (USP39) interaction. Overall, the results unveil a novel role of ac4C modifications in regulating lysosomal acidification and propose a potential strategy by targeting NAT10 to inhibit esophageal cancer metastasis.
    Journal
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    CDH1 (Cadherin 1)
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    denfivontinib (SKI-G-801)
    5ms
    CANOPY-HCH-EXT: Long-Term Extension Study of Vosoritide to Treat Children With Hypochondroplasia (clinicaltrials.gov)
    P3, N=140, Enrolling by invitation, BioMarin Pharmaceutical
    New P3 trial
    6ms
    A Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of ABSK061 Mini-tablets in Healthy Adult Participants (clinicaltrials.gov)
    P1, N=42, Recruiting, Abbisko Therapeutics Co, Ltd
    New P1 trial
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    ABSK061
    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)
    6ms
    A Monotherapy in Subjects With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=42, Active, not recruiting, 3D Medicines (Beijing) Co., Ltd. | Trial completion date: Dec 2024 --> Dec 2026 | Trial primary completion date: Dec 2024 --> Dec 2025
    Trial completion date • Trial primary completion date
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    segigratinib (3D185)
    6ms
    Targeting the ZMYM2-ANXA9 Axis with FLT3 Inhibitor G749 Overcomes Oxaliplatin Resistance in Colorectal Cancer. (PubMed, Biomedicines)
    The ZMYM2-ANXA9 signaling axis drives chemoresistance and tumor progression in CRC. FLT3 inhibition by G749 effectively downregulates ANXA9 and sensitizes tumors to chemotherapy, highlighting a novel therapeutic approach for chemoresistant CRC.
    Journal
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    FLT3 (Fms-related tyrosine kinase 3) • ZMYM2 (Zinc Finger MYM-Type Containing 2)
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    oxaliplatin • denfivontinib (SKI-G-801)
    7ms
    Efficacy and Safety of 3D185 Monotherapy in Subjects With Previously Treated Locally Advanced or Metastatic Cholangiocarcinoma (clinicaltrials.gov)
    P2, N=50, Not yet recruiting, 3D Medicines (Beijing) Co., Ltd. | Trial completion date: Jun 2026 --> Jun 2028 | Trial primary completion date: Dec 2025 --> Dec 2027
    Trial completion date • Trial primary completion date
    |
    FGFR (Fibroblast Growth Factor Receptor)
    |
    segigratinib (3D185)