General Information of Drug (ID: DR5609)
Drug Name
Tazemetostat
Synonyms
EPZ-6438; 1403254-99-8; EPZ6438; UNII-Q40W93WPE1; N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide; Q40W93WPE1; EPZ 6438; E7438; (1,1'-Biphenyl)-3-carboxamide, N-((1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(4-morpholinylmethyl)-
Indication Follicular lymphoma [ICD11: 2A80] Approved [1]
Brain cancer [ICD11: ICD11: 2A00] Phase 2 [2]
Mesothelioma [ICD11: ICD11: 2C51] Phase 2 [3]
Solid tumour/cancer [ICD11: ICD11: 2A00-2F9Z] Phase 2 [4]
Diffuse large B-cell lymphoma [ICD11: ICD11: 2A81] Phase 1/2 [5]
Synovial sarcoma [ICD11: ICD11: 2B5A] Phase 1 [6]
Structure
3D MOL 2D MOL
Pharmaceutical Properties Molecular Weight 572.7 Topological Polar Surface Area 83.1
Heavy Atom Count 42 Rotatable Bond Count 9
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 6
Cross-matching ID
PubChem CID
66558664
CAS Number
1403254-99-8
TTD Drug ID
D00EQL
Formula
C34H44N4O4
Canonical SMILES
CCN(C1CCOCC1)C2=CC(=CC(=C2C)C(=O)NCC3=C(C=C(NC3=O)C)C)C4=CC=C(C=C4)CN5CCOCC5
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
The Metabolic Roadmap of This Drug
The Full List of Drug Metabolites (DM) of This Drug
DM Name DM ID PubChem ID Reaction DM Level REF
EPZ006931 DM016298
70872290
Unclear - Unclear 1 [8]
Tazemetostat Desethyl Metabolite (EPZ-6930) DM005178
70872689
Unclear - Unclear 1 [7]
The Full List of Metabolic Reaction (MR) of This Drug
MR ID Reactant Product MR Type DME REF
MR008625 Tazemetostat Tazemetostat Desethyl Metabolite (EPZ-6930) Unclear - Unclear CYP3A4 [7]
MR008626 Tazemetostat EPZ006931 Unclear - Unclear Unclear [8]
Drug-Metabolizing Enzyme(s) (DME) Metabolizing This Drug
DME Name DME Info Species Uniprot ID EC Number REF
Cytochrome P450 3A4 (CYP3A4) DME0001 Homo sapiens
CP3A4_HUMAN
1.14.14.55
[7]
References
1 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health Human Services. 2020
2 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
3 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
4 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
5 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
6 Clinical pipeline report, company report or official report of the Pharmaceutical Research and Manufacturers of America (PhRMA)
7 Tazemetostat, an EZH2 inhibitor, in relapsed or refractory B-cell non-Hodgkin lymphoma and advanced solid tumours: a first-in-human, open-label, phase 1 study
8 Pharmacokinetics of Herb-Drug Interactions of Plumbagin and Tazemetostat in Rats by UPLC-MS/MS

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