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“We are progressing multiple programs aimed at addressing the urgent needs of cancer patients facing a poor prognosis and limited treatment options,” said
KO-947 is a potent and selective inhibitor of ERK1/2 kinases, which are critical components of the MAPK pathway. Aberrant signaling caused by mutations or dysregulation of the MAPK pathway are frequent contributors to the development of cancer and are associated with numerous tumor types, including lung, colorectal and pancreatic adenocarcinomas and squamous cell carcinomas. Although small molecule inhibitors of BRAF and MEK have demonstrated clinical activity in selected patients, duration of response has been limited, and resistance is often associated with reactivation of the MAPK signaling pathway. In preclinical studies presented at AACR, KO-947 demonstrated prolonged inhibition of the MAPK pathway. Durable tumor regression was observed in preclinical cell line and patient derived xenograft models, including KRAS- and BRAF-mutant adenocarcinomas and squamous cell carcinomas lacking BRAF/RAS mutations, when KO-947 was administered on schedules ranging from daily to once weekly. Kura anticipates initiating a Phase 1 clinical trial for KO-947 in 1H 2017.
KO-539 is a potent and selective inhibitor of the interaction between the menin protein and the MLL fusion proteins, which characterize MLL leukemias. MLL-rearranged leukemia patients typically have a poor prognosis with a 5-year survival rate estimated to be 40%. As the leukemogenic activity of MLL fusion proteins has been shown to be dependent on their direct interaction with menin, the development of small molecules that block the menin-MLL interaction is a promising therapeutic strategy for the treatment of this disease. In preclinical studies presented at AACR, KO-539 demonstrated robust, sustained tumor regressions in multiple aggressive models of MLL-rearranged leukemias that correlated with modulation of target gene expression. KO-539 has been nominated as a development candidate, and further efforts are currently underway to assess potential utility of menin-MLL inhibitors in additional hematological malignancies and solid tumor indications.
Forward Looking Statements
This news release contains certain forward-looking statements that involve risks and uncertainties that could cause actual results to be materially different from historical results or from any future results expressed or implied by such forward-looking statements. Such forward-looking statements include statements regarding, among other things, the potential activity, tolerability and utility of KO-947 and KO-539, the conduct, results and timing of pre-clinical studies and clinical trials and plans regarding future research and development activities. Factors that may cause actual results to differ materially include the risk that compounds that appeared promising in early research or clinical trials do not demonstrate safety and/or efficacy in later preclinical studies or clinical trials, the risk that
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