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    DRUG CLASS:

    FGFR4 inhibitor

    Related drugs:
    6d
    Comprehensive multi-platform tyrosine kinase profiling reveals novel actionable FGFR aberrations across sarcomas affecting the young. (PubMed, Mol Cancer Ther)
    We demonstrate marked tumor growth inhibition in all FP-RMS PDXs treated with single agent FGF401 (FGFR4-specific inhibitor) and single agent lenvatinib (multi-kinase FGFR-inhibitor), and report a clinical response to lenvatinib in a relapsed metastatic FP-RMS patient. Altogether, we identified new sarcoma patients who may benefit from FGFR-inhibitors, most notably FP-rhabdomyosarcoma via FGFR4/FGF8 co-expression.
    Journal
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    FGFR1 (Fibroblast growth factor receptor 1) • FGFR (Fibroblast Growth Factor Receptor) • FGFR4 (Fibroblast growth factor receptor 4) • FOXO1 (Forkhead box O1) • FGF8 (Fibroblast Growth Factor 8) • PAX3 (Paired Box 3)
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    Lenvima (lenvatinib) • roblitinib (FGF401)
    8d
    IAPETUS: A Prospective Study to Evaluate the Safety and Efficacy of the Combination Therapy of Irpagratinib, Atezolizumab, and Bevacizumab in Patients With Hepatocellular Carcinoma (clinicaltrials.gov)
    P2, N=33, Recruiting, Asan Medical Center | Not yet recruiting --> Recruiting | Initiation date: Nov 2025 --> Mar 2026
    Enrollment open • Trial initiation date
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    FGF19 (Fibroblast growth factor 19)
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    Avastin (bevacizumab) • Tecentriq (atezolizumab) • irpagratinib (ABSK011)
    28d
    ABSK-011-201: A Phase 2, Open-Label Study of ABSK-011 Combined Atezolizumab or SOC in HCC Patients (clinicaltrials.gov)
    P2, N=118, Enrolling by invitation, Abbisko Therapeutics Co, Ltd | Recruiting --> Enrolling by invitation | N=62 --> 118 | Trial completion date: Oct 2024 --> Dec 2029 | Trial primary completion date: Jul 2024 --> Dec 2028
    Enrollment status • Enrollment change • Trial completion date • Trial primary completion date
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    FGF19 (Fibroblast growth factor 19)
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    Tecentriq (atezolizumab) • Loqtorzi (toripalimab-tpzi) • irpagratinib (ABSK011)
    1m
    A validated UHPLC-MS/MS method for determination of BPI-43487 and its metabolite BPI-43739 in human plasma and its application to a pharmacokinetic study in Chinese patients with advanced solid tumors. (PubMed, Bioanalysis)
    This method was further successfully applied to a pharmacokinetic study of BPI-43487 capsules in Chinese patients with advanced solid tumors. http://www.chinadrugtrials.org.cn is CTR20210565).
    PK/PD data • Journal
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    FGFR4 (Fibroblast growth factor receptor 4)
    2ms
    Novel FGFR4-Targeting Peptide for Single-Photon Emission Computed Tomography Imaging in Hepatocellular Carcinoma. (PubMed, J Med Chem)
    In this study, we designed a series of FGFR4-targeted peptide-radionuclide conjugates (PRCs) based on a high-affinity peptide ligand derived from the binding epitope of the monoclonal antibody U3-1784...In xenograft models, this probe demonstrated high uptake (1.89 ± 0.35% ID/g) and produced high-contrast images specifically in high-FGFR4-expressing tumors. These results indicate that 99mTc-HYNIC-FYQ-8 is a promising peptide-based radiotracer for clinical imaging of FGFR4-overexpressing tumors.
    Journal
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    FGFR4 (Fibroblast growth factor receptor 4)
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    U3-1784
    2ms
    Inhibition of neutrophil extracellular traps via the FGF19/ERK/IL-8 axis enhances immune therapy in MSS colorectal cancer. (PubMed, Clin Immunol)
    The FGF19/ERK/IL-8 pathway contributed to NET formation in this model. Targeting this pathway represents a promising strategy to boost immunotherapy in MSS CRC.
    Journal • PD(L)-1 Biomarker • IO biomarker
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    CD8 (cluster of differentiation 8) • FGF19 (Fibroblast growth factor 19) • FGFR4 (Fibroblast growth factor receptor 4) • CXCL8 (Chemokine (C-X-C motif) ligand 8)
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    BLU 9931
    3ms
    ABSK-011+BSC vs. Placebo+BSC in Previously Treated Advanced HCC With FGF19 Overexpression (clinicaltrials.gov)
    P2, N=141, Recruiting, Abbisko Therapeutics Co, Ltd
    New P2 trial
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    FGF19 (Fibroblast growth factor 19)
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    irpagratinib (ABSK011)
    3ms
    Cytotoxic and senescence-inducing effects of BLU554 in pancreatic ductal adenocarcinoma: an in vitro study. (PubMed, BMC Cancer)
    This two-step strategy may represent a novel therapeutic approach for the treatment of therapy-resistant PDAC through senescence induction and subsequent senolysis.
    Preclinical • Journal
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    FGFR4 (Fibroblast growth factor receptor 4) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
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    dasatinib • fisogatinib (BLU-554) • BLU 9931
    4ms
    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
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    irpagratinib (ABSK011) • lavengratinib (ABSK061)
    4ms
    Enhancing the antitumor efficacy using a combination of FGFR4 Inhibitor (H3B-6527) and oxaliplatin in gastric cancer. (PubMed, Neoplasia)
    These findings indicate that H3B-6527 enhances gastric cancer sensitivity to oxaliplatin by amplifying DNA damage and disrupting cell survival pathways. This study provides a rationale for clinical trials targeting FGFR4 in gastric cancer.
    Journal • PARP Biomarker • IO biomarker
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    BCL2 (B-cell CLL/lymphoma 2) • FGFR4 (Fibroblast growth factor receptor 4) • STAT3 (Signal Transducer And Activator Of Transcription 3) • CASP3 (Caspase 3) • CASP7 (Caspase 7)
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    oxaliplatin • H3B-6527
    4ms
    A Phase 2 Study of BB102 in Patients With Hepatocellular Carcinoma (clinicaltrials.gov)
    P2, N=60, Not yet recruiting, Broadenbio Ltd., Co.
    New P2 trial
    4ms
    BB102-ST-Ⅰ-02: A Phase 1 Study of BB102 in Participants With Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=78, Recruiting, Broadenbio Ltd., Co. | Trial completion date: Jul 2025 --> Dec 2026 | Trial primary completion date: Jan 2025 --> Dec 2026
    Trial completion date • Trial primary completion date