Tazemetostat is a methyltransferase inhibitor indicated to treat patients 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection. Tazemetostat was first named in literature as EPZ-6438.
- Mechanism
- Curator reviewed · 13 references
EZH2 is a methyltransferase subunit of the polycomb repressive complex 2 (PRC2) which catalyzes multiple methylations of lysine 27 on histone H3 (H3K27). Trimethylation of this lysine inhibits the transcription of genes associated with cell cycle arrest. PRC2 is antagonized by the switch/sucrose non-fermentable (SWI/SNF) multiprotein complex. Abnormal activation of EZH2 or loss of function mutations in SWI/SNF lead to hyper-trimethylation of H3K27. Hyper-trimethylation of H3K27 leads to cancer cell de-differentiation, a gain of cancer stem cell-like properties. De-differentiation can allow for cancer cell proliferation.
Tazemetostat inhibits EZH2, preventing hyper-trimethylation of H3K27 and an uncontrollable cell cycle.
- Primary indication
- Tazemetostat is indicated to treat adult and pediatric patients 16 years and older with metastatic or locally advanced epithelioid sarcoma that is not eligible for complete resection.Curator reviewed · 6 structured indications
- Formula / weight
- C34H44N4O4 · 572.75 g/mol (avg)
- First approval
- United States, 2020
- Code names
- E-7438 · EPZ-6438 · IPN60200
- Brand names
Resolves to
NSQSAUGJQHDYNO-UHFFFAOYSA-NSMILESCCN(C1CCOCC1)C1=C(C)C(=CC(=C1)C1=CC=C(CN2CCOCC2)C=C1)C(=O)NCC1=C(C)C=C(C)NC1=OWhat you can answer from here — as of September 23, 2026
Which drugs share a target with Tazemetostat, and which of those have an active Phase 3 trial?
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