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DRUG:

PLD-102

i
Other names: PLD-102, PLM-102
Company:
PeLeMed
Drug class:
RET inhibitor, FLT3 inhibitor
Related drugs:
over1year
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
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FLT3 (Fms-related tyrosine kinase 3) • CASP3 (Caspase 3)
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FLT3-ITD mutation • FLT3 D835Y • FLT3 F691L • FLT3 D835
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Xospata (gilteritinib) • PLD-102