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Therapy Name EPZ004777
Synonyms
Therapy Description

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).

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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).

Filtering

  • Case insensitive filtering will display rows where any text in any cell matches the filter term
  • Simple literal full or partial string matches
  • Separate multiple filter terms with a spaces, order doesn't matter (a b c and c b a are equivalent )
  • Filtering will only apply to rows that are already loaded on the page, filtering has no impact on query parameters
  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

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  • Generally, the default sort order for tables is set to be first column ascending, however, specific tables may set a different default sort order.
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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

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  • Use quotes to match a longer phrase which contains spaces "mtor c1483f"

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Clinical Trial Phase Therapies Title Recruitment Status


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