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    DRUG:

    golvatinib (E7050)

    i
    Other names: E7050
    Company:
    Eisai
    Drug class:
    c-MET inhibitor, VEGFR-2 inhibitor, c-KIT inhibitor, Angiogenesis inhibitor, RON inhibitor, EPH receptor inhibitor
    Related drugs:
    12d
    An Effective and Systematic Strategy for Metabolic Profiling of Golvatinib In Vitro by Combining UHPLC-MS/MS and UHPLC-Q-Orbitrap-HRMS. (PubMed, J Sep Sci)
    Detection was carried out by multiple reaction monitoring mode using the transitions m/z 634.3→184.2 for golvatinib and m/z 650.3→200.2 for golvatinib N-oxide. Further study demonstrated that CYP3A4 was the principal enzyme involved in metabolizing golvatinib. To the best of our knowledge, this is the first report combining ultra-high-performance liquid chromatography-tandem MS (UHPLC-MS/MS) with UHPLC-Quadrupole-Orbitrap-HRMS for profiling golvatinib metabolism in vitro, thereby laying a foundation for subsequent pharmacokinetic study.
    Preclinical • Journal
    |
    CYP3A4 (Cytochrome P450, family 3, subfamily A, polypeptide 4)
    |
    larotinib (Z650) • golvatinib (E7050)
    almost3years
    E7050 Suppresses the Growth of Multidrug-Resistant Human Uterine Sarcoma by Inhibiting Angiogenesis via Targeting of VEGFR2-Mediated Signaling Pathways. (PubMed, Int J Mol Sci)
    E7050 treatment also decreased the expression of CD31 and p-VEGFR2 in MES-SA/Dx5 tumor tissue sections in comparison with the vehicle control. Collectively, E7050 may serve as a potential agent for the treatment of cancer and angiogenesis-related disorders.
    Journal
    |
    CD31 (Platelet and endothelial cell adhesion molecule 1) • PECAM1 (Platelet And Endothelial Cell Adhesion Molecule 1)
    |
    KDR expression • CD31 expression
    |
    golvatinib (E7050)
    over3years
    Blockade of c-Met-Mediated Signaling Pathways by E7050 Suppresses Growth and Promotes Apoptosis in Multidrug-Resistant Human Uterine Sarcoma Cells. (PubMed, Int J Mol Sci)
    E7050 treatment also decreased the expression of Ki-67 and p-Met, and increased the expression of cleaved caspase-3 in MES-SA/Dx5 tumor sections. Therefore, E7050 is a promising drug that can be developed for the treatment of multidrug-resistant uterine sarcoma.
    Journal • PARP Biomarker
    |
    MET (MET proto-oncogene, receptor tyrosine kinase) • CCND1 (Cyclin D1) • BIRC5 (Baculoviral IAP repeat containing 5) • BAX (BCL2-associated X protein) • CASP3 (Caspase 3) • CCNA2 (Cyclin A2) • CDKN1A (Cyclin-dependent kinase inhibitor 1A)
    |
    CCND1 expression • BIRC5 expression • BAX expression
    |
    golvatinib (E7050)