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    DRUG:

    PLD-102

    i
    Other names: PLD-102, PLM-102
    Company:
    PeLeMed
    Drug class:
    RET inhibitor, FLT3 inhibitor
    Related drugs:
    almost2years
    Discovery of PLM-102, a highly potent 3rd generation FLT3 inhibitor, in drug-resistant FLT3-ITD-TKD mutated acute myeloid leukemia (AACR 2023)
    In FLT3-ITD-positive cell lines (MV4-11, MOLM-13, MOLM-14, Ba/F3-ITD-D835Y, Ba/F3-ITD-F691L), PLM-102 shows about 18~25-fold higher anti-proliferative activities than Gilteritinib. These results are very encouraging because large tumors have a limited blood supply and high interstitial fluid pressure, leading to a poor absorption of anticancer drugs. Pharmacokinetics of PLM-102 displayed higher bone-marrow exposure indicating better target engagement and benefits in the clinical translation in AML.In conclusion, PLM-102 is a promising therapeutic candidate for the FLT3-ITD-mutated AML as well as the acquired resistance to current FLT3 inhibitors.
    PARP Biomarker
    |
    FLT3 (Fms-related tyrosine kinase 3) • CASP3 (Caspase 3)
    |
    FLT3-ITD mutation • FLT3 D835Y • FLT3 F691L • FLT3 D835
    |
    Xospata (gilteritinib) • PLD-102