On October 28, 2017 Kura Oncology, Inc. (Nasdaq:KURA), a clinical stage biopharmaceutical company focused on the development of precision medicines for oncology, reported new results for KO-539, the company’s potent and selective inhibitor of the menin-MLL protein-protein interaction, which is currently in preclinical development as a potential treatment for patients with genetically-defined subsets of acute leukemias (Press release, Kura Oncology, OCT 28, 2017, View Source [SID1234521274]). The results were featured in a late-breaking presentation today at the AACR (Free AACR Whitepaper)-NCI-EORTC AACR-NCI-EORTC (Free AACR-NCI-EORTC Whitepaper) International Conference on Molecular Targets and Cancer Therapeutics (EORTC-NCI-AACR) (Free ASGCT Whitepaper) (Free EORTC-NCI-AACR Whitepaper) in Philadelphia.
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Although KO-539 was originally designed as a potential therapy for the MLL-rearranged leukemias, the new results demonstrate significant activity in preclinical models of additional genetically-defined subsets of AML, including those with oncogenic driver mutations in NPM1, IDH1, IDH2 and DNMT3A. Preliminary pharmacodynamic data suggests that KO-539 exerts anti-leukemic activity by induction of myeloid differentiation in AML blasts, a mechanism that is distinct from and potentially complementary to existing cytotoxic and antiproliferative therapies. The menin-MLL complex appears to be a central node in epigenetic dysregulation driven by several distinct oncogenic driver mutations known to be important in diverse leukemias and myeloproliferative disorders.
“Although AML is a relatively common hematologic malignancy with a generally poor prognosis, the development of novel therapeutic approaches has been hampered by the many different genetic and clinical subgroups found in the disease and the relatively short durations of response,” said Yi Liu, Ph.D., Chief Scientific Officer, Kura Oncology. “We’re encouraged by the results presented today because they demonstrate that menin-MLL inhibitors have the potential to be active in subtypes representing approximately half of the patients with AML and drive robust and persistent responses in preclinical models.”
A copy of the poster, entitled “A novel small molecule menin-MLL inhibitor for potential treatment of MLL-rearranged leukemias and NPM1/DNMT3A-mutant AML,” is now available on the company’s website at www.kuraoncology.com.