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    DRUG:

    ER121

    i
    Other names: ER121
    Company:
    University of Pennsylvania
    Drug class:
    HER2 inhibitor, EGFR C797S inhibitor
    Related drugs:
    14d
    Targeting erbB Pathways in Breast Cancer: Dual Kinase Inhibition for Brain Metastasis and Prevention of p185HER2/Neu Tumor Development. (PubMed, Breast Cancer (Dove Med Press))
    The Herceptin-resistant breast cancer cell line JIMT-1 was used in an in vivo tumor model, and MMTV-erbB2 (Fo5) transgenic mice models were used to evaluate the efficacy and safety of ER121 as neoadjuvant. ER121 is a non-toxic small-molecule erbB kinase inhibitor and holds promise as an oral and systemic therapeutic agent for treating progressive erbB-driven tumors in therapeutic settings. Moreover, ER121 shows potential as a preventive therapy in neoadjuvant settings for erbB2-associated tumors and when administered systemically can dramatically limit erbB2 brain metastases in animal models.
    Journal
    |
    EGFR (Epidermal growth factor receptor) • HER-2 (Human epidermal growth factor receptor 2)
    |
    EGFR mutation • HER-2 overexpression • EGFR overexpression • EGFR overexpression + HER-2 overexpression
    |
    Herceptin (trastuzumab) • ER121