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|Drug Name||Trade Name||Synonyms||Drug Classes||Drug Description|
|EPZ004777||EPZ4777||DOT1L Inhibitor 3||EPZ004777 is a small molecule that inhibits DOT1L, which results in decreased histone H3 lysine 79 dimethylation, and potentially leads to decreased tumor cell proliferation (PMID: 21741596, PMID: 27535106).|
|Molecular Profile||Indication/Tumor Type||Response Type||Therapy Name||Approval Status||Evidence Type||Efficacy Evidence||References|
|FLT3 exon 14 ins NPM1 mut||leukemia||predicted - sensitive||EPZ004777||Preclinical||Actionable||In a preclinical study, EPZ004777 inhibited growth and induced differentiation of murine leukemia cells expressing an NPM1 mutation and FLT3 internal tandem duplication in culture, and improved survival in mouse models (PMID: 27535106).||27535106|
|DOT1L positive||leukemia||predicted - sensitive||EPZ004777||Preclinical||Actionable||In a preclinical study, EPZ004777 inhibited DOT1L activity, resulting in decreased H3K27 methylation in leukemia cell lines in culture (PMID: 21741596).||21741596|
|NPM1 mutant||acute myeloid leukemia||predicted - sensitive||EPZ004777||Preclinical - Patient cell culture||Actionable||In a preclinical study, EPZ004777 decreased HOX gene expression, and reduced proliferation and increased differentiation of a human acute myeloid leukemia (AML) cell line and primary AML samples harboring NPM1 mutations in culture (PMID: 27535106).||27535106|
|NPM1 mutant||leukemia||predicted - sensitive||EPZ004777||Preclinical||Actionable||In preclinical study, treatment with EPZ004777 resulted in reduced proliferation and increased differentiation of murine leukemia cells expressing an NPM1 mutation, and improved survival in NPM1-mutant murine leukemia models (PMID: 27535106).||27535106|
|KMT2A - MLLT10||leukemia||sensitive||EPZ004777||Preclinical||Actionable||In a preclinical study, transformed cells expressing the fusion, KMT2A-MLLT10, demonstrated sensitivity to EPZ004777 in culture and in mouse models, resulting in cell cycle arrest, increased apoptotic activity, and inhibition of cell proliferation (PMID: 23138183).||23138183|
|Clinical Trial||Phase||Therapies||Title||Recruitment Status|