tazemetostat   Click here for help

GtoPdb Ligand ID: 7011

Synonyms: E-7438 | EPZ 6438 | EPZ-6438 | EPZ6438 | Tazverik®
Approved drug
tazemetostat is an approved drug (FDA (2020))
Compound class: Synthetic organic
Comment: Tazemetostat is an oral, potent, first-in-class inhibitor of the histone methyltransferase, enhancer of zeste 2 polycomb repressive complex 2 subunit (EZH2) that was developed by Epizyme as anovel drug for the treatment of solid tumours and lymphomas with speciific genetic alterations. Link to Epizyme's tazemetostat webpage here.
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2D Structure
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Physico-chemical Properties
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Hydrogen bond acceptors 7
Hydrogen bond donors 2
Rotatable bonds 10
Topological polar surface area 86.9
Molecular weight 572.34
XLogP 5.61
No. Lipinski's rules broken 1
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Canonical SMILES CCN(c1cc(cc(c1C)C(=O)NCc1c(C)cc([nH]c1=O)C)c1ccc(cc1)CN1CCOCC1)C1CCOCC1
Isomeric SMILES CCN(c1cc(cc(c1C)C(=O)NCc1c(C)cc([nH]c1=O)C)c1ccc(cc1)CN1CCOCC1)C1CCOCC1
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)
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Summary of Clinical Use Click here for help
Tazemetostat is being evaluated in clinical trials for its potential to treat advanced solid tumours (with certain molecularly defined genetic alterations; e.g. INI1 (SMARCB1)-negative tumours [1,3] or those with EZH2 gain-of-function mutations) and B-cell lymphomas (with and without EZH2 mutations). Click here to link to ClinicalTrials.gov's full list of tazemetostat studies.
In July 2019 the FDA accepted Epizyme's New Drug Application (NDA) for accelerated approval of tazemetostat, for the treatment of metastatic or locally advanced epithelioid sarcoma that is ineligible for curative surgery. Following FDA priority review of this NDA Tazemetostat was granted full FDA approval in January 2020, as a treatment for metastatic or locally advanced epithelioid sarcoma (ES) that is not eligble for complete resection. This approval was based on observation of clinically significant and durable responses, and favourable tolerability in the ES cohort of trial NCT02601950. In the EU, tazemetostat is permitted as a treatment for malignant mesothelioma, follicular lymphoma and diffuse large B-cell lymphoma under orphan designations (granted in 2018 by the EMA).