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    DRUG:

    BPI-9016M

    i
    Other names: BPI-9016M, BPI-9016, BPI 9016, BPI9016M, BPI9016, BPI 9016M
    Company:
    Betta Pharma
    Drug class:
    c-MET inhibitor, AXL inhibitor
    Related drugs:
    over1year
    Safety, efficacy and pharmacokinetics of BPI-9016M in c-MET overexpression or MET exon 14 skipping mutation patients with locally advanced or metastatic non-small-cell lung cancer: a phase Ib study. (PubMed, BMC Cancer)
    BPI-9016M showed manageable safety profile in c-MET overexpression or MET exon 14 skipping mutation patients with locally advanced or metastatic NSCLC, but showed limited efficacy.
    P1 data • PK/PD data • Clinical Trial,Phase I • Journal • Metastases
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET exon 14 mutation • MET overexpression • MET exon 14 mutation + MET overexpression
    |
    BPI-9016M
    almost3years
    Radiosensitizing effect of c-Met kinase inhibitor BPI-9016M in esophageal squamous cell carcinoma cells in vitro and in vivo. (PubMed, Ann Transl Med)
    The radiosensitizing effects of BPI-9016M were due to increased apoptosis, such as the up-regulation of cleaved-caspase 3 and 9, down-regulation of mutant P53 and Bcl-2, the decreased of phosphorylation of ATR and ATM, and the inhibition of γ-H2AX accumulation in vitro and in vivo. These findings indicated that BPI-9016M exerts a radiosensitizing effect and enhances apoptosis by inhibiting homologous recombination DNA repair in irradiated ESCC cells.
    Preclinical • Journal • IO biomarker
    |
    TP53 (Tumor protein P53) • MET (MET proto-oncogene, receptor tyrosine kinase) • BCL2 (B-cell CLL/lymphoma 2) • HRD (Homologous Recombination Deficiency) • HGF (Hepatocyte growth factor) • CHEK2 (Checkpoint kinase 2) • CHEK1 (Checkpoint kinase 1) • CASP3 (Caspase 3) • CASP9 (Caspase 9)
    |
    TP53 mutation
    |
    BPI-9016M
    over3years
    Safety, Efficacy and Pharmacokinetic of BPI-9016M in Patients With c-Met- Dysregulated Advanced NSCLC (clinicaltrials.gov)
    P1, N=80, Recruiting, Betta Pharmaceuticals Co., Ltd. | Completed --> Recruiting | Trial completion date: Dec 2018 --> Nov 2024 | Trial primary completion date: Dec 2018 --> Nov 2024
    Clinical • Enrollment open • Trial completion date • Trial primary completion date
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    MET exon 14 mutation • MET expression
    |
    BPI-9016M
    almost5years
    First-in-human phase I study of BPI-9016M, a dual MET/Axl inhibitor, in patients with non-small cell lung cancer. (PubMed, J Hematol Oncol)
    BPI-9016M showed favorable safety and pharmacokinetic profiles, and no DLT was observed at doses up to 800 mg once daily. The promising antitumor activity in Chinese NSCLC patients supports further development of this tyrosine kinase inhibitor.
    Clinical • P1 data • Journal
    |
    MET (MET proto-oncogene, receptor tyrosine kinase)
    |
    BPI-9016M