Drug General Information
Drug ID
D0C6GK
Former ID
DNCL003456
Drug Name
EPZ-5676
Drug Type
Small molecular drug
Indication Leukemia [ICD9: 208.9; ICD10:C90-C95] Phase 1 [524761], [542044]
Company
Epizyme
Structure
Download
2D MOL

3D MOL

Formula
C30H42N8O3
InChI
InChI=1S/C30H42N8O3/c1-16(2)37(13-22-25(39)26(40)29(41-22)38-15-34-24-27(31)32-14-33-28(24)38)19-10-17(11-19)6-9-23-35-20-8-7-18(30(3,4)5)12-21(20)36-23/h7-8,12,14-17,19,22,25-26,29,39-40H,6,9-11,13H2,1-5H3,(H,35,36)(H2,31,32,33)/t17-,19+,22-,25-,26-,29-/m1/s1
InChIKey
LXFOLMYKSYSZQS-LURJZOHASA-N
PubChem Compound ID
Target and Pathway
Target(s) DOT1L Target Info Modulator [544327]
KEGG Pathway Lysine degradation
Transcriptional misregulation in cancer
Reactome PKMTs methylate histone lysines
WikiPathways Histone Modifications
References
Ref 524761ClinicalTrials.gov (NCT02141828) Dose Escalation Study of EPZ-5676 in Pediatric Patients With Leukemias Bearing a Rearrangement of the MLL Gene. U.S. National Institutes of Health.
Ref 542044(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: 7019).
Ref 544327Potent inhibition of DOT1L as treatment of MLL-fusion leukemia. Blood. 2013 August 8; 122(6): 1017-1025.

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