Details of the Active Pharmaceutical Ingredient (API)

General Information of API (ID: D01463)
Name
Tazemetostat
Synonyms    Click to Show/Hide the Synonyms of This API
Tazemetostat; 1403254-99-8; EPZ-6438; EPZ6438; E7438; 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; UNII-Q40W93WPE1; EPZ 6438; E-7438; Q40W93WPE1; N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide; (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)-; Tazemetostat [INN]; Tazverik; [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)-; Tazemetostat [USAN]; Tazemetostat (USAN/INN); Tazemetostat [USAN:INN]; E 7438; Tazemetostat(EPZ-6438); Tazemetostat (EPZ-6438); GTPL7011; CHEMBL3414621; SCHEMBL13276848; SCHEMBL19325409; SCHEMBL22210809; EX-A509; HMS3653O07; HMS3747A09; AOB87748; BCP07409; EPZ-7438; 2399AH; ABP001111; MFCD24849415; NSC777109; NSC791066; s7128; AKOS026750211; ZINC100285161; ACN-029397; CCG-264672; CS-1758; DB12887; NSC-777109; NSC-791066; SB22955; NCGC00381562-01; NCGC00381562-10; AC-30931; AK317596; AS-55991; DA-34776; HY-13803; N-((4,6-Dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(oxan-4-yl)amino)-4-methyl-4'-((morpholin-4-yl)methyl)(1,1'-biphenyl)-3-carboxamide; QC-11696; FT-0700193; SW220030-1; A12712; D11444; J-690163; J-690164; Q27088941; EPZ-6438; EPZ 6438; E7438; Tazemetostat; E-7438; E 7438; (R,Z)-1-(1-(1-(ethylsulfonyl)piperidin-4-yl)ethyl)-N-((2-hydroxy-4-methoxy-6-methylpyridin-3-yl)methyl)-2-methyl-1H-indole-3-carbimi dic acid; 5-(Ethyl(tetrahydro-2H-pyran-4-yl)amino)-N-((2-hydroxy-4,6-dimethylpyridin-3-yl)methyl)-4-methyl-4'-(morpholinomethyl)-[1,1'-biphenyl]-3-carboxamide; 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; N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4'-(morpholinomethyl)biphenyl-3-carboxamide
Clinical Status
Approved
PubChem CID
66558664
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
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
   Click to Show/Hide the Molecular Data (Structure/Property) of This API
Structure
<iframe style="width: 300px; height: 300px;" frameborder="0" src="https://embed.molview.org/v1/?mode=balls&cid=66558664"></iframe>
3D MOL is unavailable 2D MOL
Physicochemical Properties Molecular Weight 572.7 Topological Polar Surface Area 83.1
XlogP 4.2 Complexity 992
Heavy Atom Count 42 Rotatable Bond Count 9
Hydrogen Bond Donor Count 2 Hydrogen Bond Acceptor Count 6
Full List of Drug Formulations (DFMs) Containing This API
          Tazemetostat 200 mg tablet Click to Show/Hide the Full List of Formulation(s):          1 Formulation(s)
             Drug Formulation 1 DFM Info click to show the detail info of this DFM
                   All DIGs    Click to Show/Hide the Full List of DIGs in This DFM
Hydroxypropyl Cellulose; Lactose Monohydrate; Low-Substituted Hydroxypropyl Cellulose; Magnesium Stearate; Sodium Starch Glycolate; Hypromellose; Polyethylene Glycol; Red Iron Oxide; Talc; Titanium Dioxide
                   Dosage Form Tablet
                   Company Epizyme
                   DIG(s) with
                   Biological Activity
DIG Name DIG Info Representative Biological Activity of This DIG REF
Hydroxypropyl cellulose DIG Info Mephenytoin 4-hydroxylase (EC50 = 89.5 uM) [1]
Hypromellose DIG Info Cytochrome P450 3A5 (IC50 = 19.4 uM) [1]
Magnesium stearate DIG Info Albendazole monooxygenase (Protein expression downregulation) [2]
Polyethylene glycol 4000 DIG Info Albendazole monooxygenase (Inhibition ratio < 40 %) [3]
References
1 Mediation of in vitro cytochrome p450 activity by common pharmaceutical excipients. Mol Pharm. 2013 Jul 1;10(7):2739-48.
2 Effects of commonly used excipients on the expression of CYP3A4 in colon and liver cells. Pharm Res. 2010 Aug;27(8):1703-12.
3 Pharmaceutical excipients inhibit cytochrome P450 activity in cell free systems and after systemic administration. Eur J Pharm Biopharm. 2008 Sep;70(1):279-88.

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