APPLICATION OF GILTERITINIB TO VARIOUS MUTANTS

    公开(公告)号:US20250099461A1

    公开(公告)日:2025-03-27

    申请号:US18263947

    申请日:2022-02-10

    Inventor: Ryohei Katayama

    Abstract: Tumors having acquired resistance to ALK-TKIs were analyzed by use of various kinase inhibitors. As a result, it was found that gilteritinib, which is a therapeutic drug for FLT3 gene mutation-positive acute myeloid leukemia, has an effect on the tumors. Gilteritinib directly inhibits the kinase activity of ALK to have an effect on an ALK fusion gene mutation-positive tumor having a plurality of compound mutations for which effective therapeutic drugs have been not present. ALK-TKI-resistant cancer developed via a fusion gene such as NTRK, ROS1 and LTK, and via AXL can be effectively overcome by gilteritinib alone, and the resistance mediated through ALK-TKI resistance mechanism via a bypass pathway such as KRAS, BRAF and EGFR, can be overcome by combination therapy.

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