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    DRUG:

    KC1036

    i
    Other names: KC1036
    Company:
    Konruns Pharma
    Drug class:
    FLT3 inhibitor, VEGFR-2 inhibitor, Tyrosine kinase inhibitor, AXL inhibitor
    Related drugs:
    2ms
    KC1036 in ewing sarcoma: mechanistic insights and future directions for a multi-targeted therapeutic strategy. (PubMed, Angiogenesis)
    The primary challenges ahead lie in delineating its molecular mechanisms of action beyond angiogenesis, prospectively defining resistance pathways to guide combination therapies, and rigorously evaluating its safety profile to ensure successful clinical translation. This letter outlines these priorities to stimulate further research.
    Review • Journal
    |
    EWSR1 (EWS RNA Binding Protein 1) • FLI1 (Fli-1 Proto-Oncogene ETS Transcription Factor)
    |
    KC1036
    3ms
    KC1036, a multi-kinase inhibitor with anti-angiogenic activity, can effectively suppress the tumor growth of Ewing sarcoma. (PubMed, Angiogenesis)
    The novel anti-angiogenic inhibitor, KC1036, is effective in treating ES in the preclinical models.
    Journal
    |
    FGFR (Fibroblast Growth Factor Receptor) • AXL (AXL Receptor Tyrosine Kinase) • KDR (Kinase insert domain receptor) • FLT1 (Fms-related tyrosine kinase 1) • NPY1R (Neuropeptide Y Receptor Y1)
    |
    doxorubicin hydrochloride • pazopanib • Cabometyx (cabozantinib tablet) • KC1036
    1year
    To Evaluate KC1036 in the Patients with Advanced Digestive System Tumors (clinicaltrials.gov)
    P1/2, N=133, Recruiting, Beijing Konruns Pharmaceutical Co., Ltd. | Trial completion date: Apr 2025 --> Dec 2025 | Trial primary completion date: Apr 2024 --> Oct 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    KC1036
    1year
    A Study of KC1036 in Patients with Advanced Solid Tumors (clinicaltrials.gov)
    P1, N=207, Recruiting, Beijing Konruns Pharmaceutical Co., Ltd. | Trial completion date: Jul 2024 --> Dec 2025 | Trial primary completion date: Jul 2023 --> Oct 2025
    Trial completion date • Trial primary completion date • Metastases
    |
    KC1036
    over1year
    A Study of KC1036 in Adolescents With Advanced Ewing Sarcoma (clinicaltrials.gov)
    P2, N=30, Recruiting, Beijing Konruns Pharmaceutical Co., Ltd.
    New P2 trial • Metastases
    |
    KC1036
    over1year
    A Study of KC1036 Versus Investigator's Choice of Chemotherapy in Patients With Advanced Esophageal Cancer (clinicaltrials.gov)
    P3, N=490, Recruiting, Beijing Konruns Pharmaceutical Co., Ltd. | Not yet recruiting --> Recruiting
    Enrollment open • Metastases
    |
    docetaxel • irinotecan • Teysuno (gimeracil/oteracil/tegafur) • KC1036
    almost2years
    A Study of KC1036 Versus Investigator's Choice of Chemotherapy in Patients With Advanced Esophageal Cancer (clinicaltrials.gov)
    P3, N=490, Not yet recruiting, Beijing Konruns Pharmaceutical Co., Ltd.
    New P3 trial • Metastases
    |
    docetaxel • irinotecan • Teysuno (gimeracil/oteracil/tegafur) • KC1036
    2years
    A Food Effect Study of KC1036 in Healthy Subjects (clinicaltrials.gov)
    P1, N=12, Completed, Beijing Konruns Pharmaceutical Co., Ltd. | Active, not recruiting --> Completed
    Trial completion
    |
    KC1036
    over2years
    Establishment and characterization of a novel lung adenocarcinoma cell line HX-JCJ harboring MET ex14 skipping mutation (ESMO 2023)
    Results Drug screen showed that this cell line was extremely sensitive to KC1036 (IC50=4.8nm), which is a home-made small molecule inhibitor with strong anti-MET and anti-angiogensis activity. Conclusions In conclusion, we successfully established a novel NSCLC cell line (HX-JCJ) harboring MET ex14 skipping mutation from the primary tumor tissue, which may provide a promising cell model for further MET relevant research.
    Preclinical
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET exon 14 mutation • MET mutation
    |
    KC1036