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Lasmotinib (PHI-101) is an orally bioavailable small molecule inhibitor that targets checkpoint kinase 2 (Chk2) and FMS-like tyrosine kinase 3 (FLT3). It is being developed as a next-generation therapy for cancers with DNA repair deficiencies and FLT3 mutations. As a Chk2 inhibitor, lasmotinib impairs the DNA damage response pathway, potentially preventing tumor cells from repairing DNA damage caused by chemotherapeutic agents and leading to increased tumor cell apoptosis. As a FLT3 inhibitor, it demonstrates potent anti-leukemic activity in acute myeloid leukemia (AML), including cases resistant to other FLT3 inhibitors. Lasmotinib has shown clinical efficacy in relapsed/refractory AML with FLT3 mutations and is also under investigation for platinum-resistant recurrent ovarian cancer[1][2][4][5][6][8].
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