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Emilumenib is an orally available small-molecule menin inhibitor developed by Daiichi Sankyo Co., Ltd. It functions by binding to the nuclear protein menin (MEN1) and preventing its interaction with the menin-mixed lineage leukemia (MLL; KMT2A, lysine methyltransferase 2A) complex. This disruption of the menin-KMT2A interaction inhibits proleukemogenic signaling, leading to the differentiation and apoptosis of leukemic cells. Emilumenib is being investigated for the treatment of acute leukemias, specifically acute myeloid leukemia (AML) and acute lymphoblastic leukemia (ALL), particularly in cases with KMT2A rearrangements or NPM1 mutations.
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