Tazemetostat

CHEMBL3414621 Phase 4 Disetujui Small molecule
Half-Life
Bioavailability
Protein Binding
Molecular Weight
572.7 g/mol
LogP
4.2
Phase
4

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.

Berat Molekul

572,7000 g/mol

LogP

4,20

TPSA

83,10 Ų

Lipinski RO5

Lulus

Area Terapeutik

Pharmacokinetics (PK)

Pharmacodynamics (PD)

Struktur 2D

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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

Ikatan yang Dapat Dirotasi

9

Atom Berat

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.

Pertanyaan yang Sering Diajukan

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 section for drug detail pages. Renders standard pharmacological database links plus the drug's data_sources field. #}

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.

Penyangkalan Medis

This content is for educational and informational purposes only. It is not a substitute for professional medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before making medication decisions.

Data sources: ChEMBL, PubChem, DailyMed.