molecules of the month


oral menin-MLL1 inhibitor

Ph. I/II candidate in leukemia

from HTS and SBDD

Mixed Lineage Leukemia 1 (MLL1)

Kura Oncology, San Diego, CA

Ziftomenib chemical structure oral menin-MLL1 inhibitor - Kura Oncology, San Diego, CA
5 mins read

Context. Ziftomenib (KO-539; UMich) is an oral menin inhibitor being developed for mixed-lineage leukemia 1 (MLL1)-rearranged or NPM1-mutated acute myeloid leukemia (AML). Although a tumor suppressor in endocrine glands, the scaffold protein menin is an essential cofactor for leukemogenesis in leukemia subsets driven by the rearrangement of MLL, a histone-lysine methyltransferase, and transcriptional regulator. Based on promising preclinical data and clinical complete responses, inhibitors targeting the MLL1-menin protein-protein interaction (PPI) have potential to become the next novel class of targeted therapy in leukemias, such as AML. Evaluation of synergistic combinations (e.g., w/ BCL-2 inhibitors) involving these menin inhibitors may mitigate the high risk of resistance while offering superior activity. Target. Menin, encoded by the MEN1 tumor suppressor, is an important…

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