^
    5d
    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)
    9d
    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)
    22d
    HMPL-453 Tartrate in Advanced Intrahepatic Cholangiocarcinoma (clinicaltrials.gov)
    P2/3, N=235, Recruiting, Hutchmed | Phase classification: P2 --> P2/3 | N=128 --> 235 | Trial completion date: Dec 2025 --> Feb 2030 | Trial primary completion date: Jun 2025 --> Jun 2028
    Phase classification • Enrollment change • Trial completion date • Trial primary completion date
    |
    FGFR2 (Fibroblast growth factor receptor 2)
    |
    FGFR2 fusion
    |
    fanregratinib (HMPL-453)
    1m
    A Study of ABSK061 to Assess Safety, Tolerability, Pharmacokinetics, and Efficacy in Children With Achondroplasia (clinicaltrials.gov)
    P1/2, N=110, Not yet recruiting, Abbisko Therapeutics Co, Ltd
    New P1/2 trial
    |
    ABSK061
    1m
    FORAGER-2: A Study of Vepugratinib (LY3866288) in Participants With Cancer in the Urinary Tract (clinicaltrials.gov)
    P3, N=450, Recruiting, Eli Lilly and Company | Not yet recruiting --> Recruiting
    Enrollment open
    |
    Keytruda (pembrolizumab) • Padcev (enfortumab vedotin-ejfv) • vepugratinib (LY3866288)
    1m
    A Clinical Trial to Evaluate the Relative Bioavailability of New and Old ABSK-011 Capsules (clinicaltrials.gov)
    P1, N=40, Completed, Abbisko Therapeutics Co, Ltd | Recruiting --> Completed | N=73 --> 40 | Trial completion date: Dec 2024 --> Sep 2025 | Trial primary completion date: Dec 2024 --> Sep 2025
    Trial completion • Enrollment change • Trial completion date • Trial primary completion date
    |
    irpagratinib (ABSK011) • ABSK061
    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
    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
    |
    Keytruda (pembrolizumab) • Padcev (enfortumab vedotin-ejfv) • vepugratinib (LY3866288)
    3ms
    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
    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)
    6ms
    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
    |
    CDH1 (Cadherin 1)
    |
    denfivontinib (SKI-G-801)