Drug General Information
Drug ID
D00EQL
Former ID
DIB016694
Drug Name
EPZ-6438
Drug Type
Small molecular drug
Indication Solid tumours [ICD9: 140-199, 210-229; ICD10:C00-D48] Phase 1/2 [532681], [542041]
Company
Epizyme
Structure
Download
2D MOL

3D MOL

Formula
C34H44N4O4
InChI
InChI=1S/C34H44N4O4/c1-5-38(29-10-14-41-15-11-29)32-20-28(27-8-6-26(7-9-27)22-37-12-16-42-17-13-37)19-30(25(32)4)33(39)35-21-31-23(2)18-24(3)36-34(31)40/h6-9,18-20,29H,5,10-17,21-22H2,1-4H3,(H,35,39)(H,36,40)
InChIKey
NSQSAUGJQHDYNO-UHFFFAOYSA-N
PubChem Compound ID
PubChem Substance ID
Drug Resistance Mutation (DRM)
DRM DRM Info
Target and Pathway
Target(s) Enhancer of zeste homolog 2 Target Info Inhibitor [532681]
KEGG Pathway MicroRNAs in cancer
NetPath Pathway IL2 Signaling Pathway
Reactome PRC2 methylates histones and DNA
Oxidative Stress Induced Senescence
PKMTs methylate histone lysines
WikiPathways Interactome of polycomb repressive complex 2 (PRC2)
Endoderm Differentiation
Integrated Pancreatic Cancer Pathway
Histone Modifications
Cell Differentiation - meta
miRs in Muscle Cell Differentiation
miR-targeted genes in muscle cell - TarBase
miR-targeted genes in lymphocytes - TarBase
miR-targeted genes in epithelium - TarBase
References
Ref 532681Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Mol Cancer Ther. 2014 Apr;13(4):842-54.
Ref 542041(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7011).
Ref 532681Selective inhibition of EZH2 by EPZ-6438 leads to potent antitumor activity in EZH2-mutant non-Hodgkin lymphoma. Mol Cancer Ther. 2014 Apr;13(4):842-54.

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