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pinometostat

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Overview

NCI Definition [1]:
A small molecule inhibitor of histone methyltransferase with potential antineoplastic activity. Upon intravenous administration, EPZ-5676 specifically blocks the activity of the histone lysine-methyltransferase DOT1L, thereby inhibiting the methylation of nucleosomal histone H3 on lysine 79 (H3K79) that is bound to the mixed lineage leukemia (MLL) fusion protein which targets genes and blocks the expression of leukemogenic genes. This eventually leads to an induction of apoptosis in the leukemic cells bearing the MLL gene translocations. DOT1L, a non-SET domain-containing histone methyltransferase, specifically methylates H3K79 and plays a key role in normal cell differentiation and in the development of leukemia with MLL gene rearrangement on chromosome 11 and promotes the expression of leukemia-causing genes.

Clinical Trials

View Clinical Trials for pinometostat

Pinometostat has been investigated in 4 clinical trials, of which 1 is open and 3 are closed. Of the trials investigating pinometostat, 2 are phase 1 (0 open) and 2 are phase 1/phase 2 (1 open).

KMT2A Fusion, KMT2A-AFF1 Fusion, and KMT2A-ELL Fusion are the most frequent biomarker inclusion criteria for pinometostat clinical trials.

Acute myeloid leukemia, acute lymphoblastic leukemia, and myelodysplastic syndromes are the most common diseases being investigated in pinometostat clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Pinometostat
Top Biomarker Inclusion Criteria for Closed Clinical Trials Investigating Pinometostat
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating pinometostat and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
dot1l inhibitor epz-5676, epz-5676
Drug Categories [2]:
Histone methyltransferase inhibitors
Drug Target(s) [2]:
DOT1L
NCIT ID [1]:
C103179

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.