Tazemetostat
Tazemetostat is an oral inhibitor of EZH2, the catalytic subunit of the polycomb repressive complex 2 (PRC2), which trimethylates histone H3 at lysine 27 (H3K27me3) to silence tumor suppressor genes. It is approved for relapsed or refractory follicular lymphoma with EZH2 mutations and for epithelioid sarcoma, and is under investigation for other EZH2-driven malignancies including bladder and breast cancers. By restoring silenced tumor suppressor gene expression, it exerts antiproliferative and pro-apoptotic effects.
आणविक भार
572.7000 g/mol
LogP
4.20
TPSA
83.10 Ų
लिपिंस्की RO5
उत्तीर्ण
चिकित्सीय क्षेत्र
Pharmacokinetics (PK)
Pharmacodynamics (PD)
2D संरचना
Cite this structure
Embed this structure
SMILES
CCN(c1cc(-c2ccc(CN3CCOCC3)cc2)cc(C(=O)NCc2c(C)cc(C)[nH]c2=O)c1C)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)
Molecular Formula
C34H44N4O4
HBD / HBA
2 / 6
घूर्णनीय बंधन
9
भारी परमाणु
42
No targets recorded
Target interaction data is not yet available for this drug.
No interactions recorded
Drug interaction data is not yet available for this compound.
No side effects recorded
Side effect data is not yet available for this drug.
अक्सर पूछे जाने वाले प्रश्न
Tazemetostat is an oral inhibitor of EZH2, the catalytic subunit of the polycomb repressive complex 2 (PRC2), which trimethylates histone H3 at lysine 27 (H3K27me3) to silence tumor suppressor genes. It is approved for relapsed or refractory follicular lymphoma with EZH2 mutations and for epithelioid sarcoma, and is under investigation for other EZH2-driven malignancies including bladder and breast cancers. By restoring silenced tumor suppressor gene expression, it exerts antiproliferative and pro-apoptotic effects.
Yes, Tazemetostat is an approved drug. It has reached clinical phase 4. It is classified as a Small molecule.
References & Data Sources
- ChEMBL — European Bioinformatics Institute (EBI). CHEMBL3414621. Open-access bioactivity database.
- PubChem — National Center for Biotechnology Information (NCBI). CID 66558664. Chemical information database.
Data aggregated from publicly available pharmacological databases. Last updated 2026-03-28.
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