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dc.contributor.authorMaes, T
dc.contributor.authorMascaró, C
dc.contributor.authorTirapu, I
dc.contributor.authorEstiarte, A
dc.contributor.authorCiceri, F
dc.contributor.authorLunardi, S
dc.contributor.authorGuibourt, N
dc.contributor.authorPerdones, A
dc.contributor.authorLufino, M
dc.contributor.authorSomervaille, Tim C P
dc.contributor.authorWiseman, Daniel H
dc.contributor.authorDuy, C
dc.contributor.authorMelnick, A
dc.contributor.authorWillekens, C
dc.contributor.authorOrtega, A
dc.contributor.authorMartinell, M
dc.contributor.authorValls, N
dc.contributor.authorKurz, G
dc.contributor.authorFyfe, M
dc.contributor.authorCastro-Palomino, J
dc.contributor.authorBuesa, C
dc.date.accessioned2018-04-15T17:15:38Z
dc.date.available2018-04-15T17:15:38Z
dc.date.issued2018-03-12
dc.identifier.citationORY-1001, a potent and selective covalent KDM1A inhibitor, for the treatment of acute leukemia. 2018, 33(3): 495-511.e12 Cancer Cellen
dc.identifier.issn1878-3686
dc.identifier.pmid29502954
dc.identifier.doi10.1016/j.ccell.2018.02.002
dc.identifier.urihttp://hdl.handle.net/10541/620886
dc.description.abstractThe lysine-specific demethylase KDM1A is a key regulator of stem cell potential in acute myeloid leukemia (AML). ORY-1001 is a highly potent and selective KDM1A inhibitor that induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML. ORY-1001 exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of an AML xenograft model, and extends survival in a mouse PDX (patient-derived xenograft) model of T cell acute leukemia. Surrogate pharmacodynamic biomarkers developed based on expression changes in leukemia cell lines were translated to samples from patients treated with ORY-1001. ORY-1001 is a selective KDM1A inhibitor in clinical trials and is currently being evaluated in patients with leukemia and solid tumors.
dc.language.isoenen
dc.rightsArchived with thanks to Cancer cellen
dc.titleORY-1001, a potent and selective covalent KDM1A inhibitor, for the treatment of acute leukemia.en
dc.typeArticleen
dc.contributor.departmentOryzon Genomics, S.A. Carrer Sant Ferran 74, 08940 Cornella de Llobregat, Spainen
dc.identifier.journalCancer Cellen
html.description.abstractThe lysine-specific demethylase KDM1A is a key regulator of stem cell potential in acute myeloid leukemia (AML). ORY-1001 is a highly potent and selective KDM1A inhibitor that induces H3K4me2 accumulation on KDM1A target genes, blast differentiation, and reduction of leukemic stem cell capacity in AML. ORY-1001 exhibits potent synergy with standard-of-care drugs and selective epigenetic inhibitors, reduces growth of an AML xenograft model, and extends survival in a mouse PDX (patient-derived xenograft) model of T cell acute leukemia. Surrogate pharmacodynamic biomarkers developed based on expression changes in leukemia cell lines were translated to samples from patients treated with ORY-1001. ORY-1001 is a selective KDM1A inhibitor in clinical trials and is currently being evaluated in patients with leukemia and solid tumors.


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