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    DRUG:

    CH7C4

    i
    Other names: CH7C4
    Company:
    Sichuan University
    Drug class:
    HER2 degrader
    over3years
    Discovery of potent and selective HER2 PROTAC degrader based Tucatinib with improved efficacy against HER2 positive cancers. (PubMed, Eur J Med Chem)
    Moreover, CH7C4 had acceptable pharmacokinetic profiles with a half-life of 5.31 h, and significantly inhibited the growth of BT-474 xenografts in vivo with TGI of 73%. As the first selective HER2 PROTAC degrader with better activity in vitro and in vivo than Tucatinib, CH7C4 provides new insights into the development of new therapeutic strategy for HER2 positive cancer.
    Journal
    |
    HER-2 (Human epidermal growth factor receptor 2)
    |
    HER-2 positive
    |
    Tukysa (tucatinib) • CH7C4