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Tazemetostat was the first EZH2 inhibitor, approved for epithelioid sarcoma and follicular lymphoma in 2020 and withdrawn worldwide in 2026 after secondary blood cancers.
Accelerated approvals in 2020 (epithelioid sarcoma; relapsed EZH2-mutant or option-less FL). Modest response rates (15% and ~35-69%) with good tolerability; SYMPHONY-1 combined it with lenalidomide-rituximab. Withdrawn worldwide in March 2026 over secondary haematologic malignancies (T-ALL, MDS), ending the EZH2 class in lymphoma for now.
SAM-competitive inhibitor of EZH2 methyltransferase (wild-type and mutant), reducing H3K27me3 and de-repressing differentiation genes. Connects to EZH2.
1.Tazemetostat slips into a pocket on EZH2.
Treatment of adults and pediatric patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection
Accelerated approval, epithelioid sarcoma
Treatment of adult patients with relapsed or refractory (R/R) follicular lymphoma (FL) whose tumors are positive for an EZH2 mutation as detected by an FDA-approved test and who have received at least 2 prior systemic therapies. Treatment of adult patients with R/R FL who have no satisfactory alternative treatment options
Accelerated approval, follicular lymphoma
Withdrawn over secondary haematologic malignancies
Treatment of adults and pediatric patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection
Withdrawn: the indication came off the label 6.4 years after its accelerated approval. source
Treatment of adult patients with relapsed or refractory (R/R) follicular lymphoma (FL) whose tumors are positive for an EZH2 mutation as detected by an FDA-approved test and who have received at least 2 prior systemic therapies. Treatment of adult patients with R/R FL who have no satisfactory alternative treatment options
Withdrawn: the indication came off the label 6.0 years after its accelerated approval. source
| Region | Year | Indication |
|---|---|---|
| US | 2020 | Epithelioid sarcoma; relapsed FL (EZH2-mutant after 2 lines; wild-type without alternatives) · Withdrawn March 2026 |
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Query for this drug: (TITLE:"Tazemetostat" OR ABSTRACT:"Tazemetostat" OR TITLE:"Tazverik" OR ABSTRACT:"Tazverik") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Tazemetostat, not a curated reading list.
Shares Tazemetostat in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With EZH2, SMARCB1, or SMARCA4 Gene Mutations (A Pediatric MATCH Treatment Trial), Poorly differentiated chordoma (SMARCB1-deficient), Epithelioid sarcoma, Atypical teratoid/rhabdoid tumour (ATRT).
Shares Epithelioid sarcoma, Chordoma, Epigenetic progenitor theory: cancer without a first mutation, Atypical teratoid/rhabdoid tumour (ATRT).
Shares Poorly differentiated chordoma (SMARCB1-deficient), Chordoma, Sarcomas (soft tissue, bone, GIST).
Shares Tazemetostat in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With EZH2, SMARCB1, or SMARCA4 Gene Mutations (A Pediatric MATCH Treatment Trial), NCI-COG Pediatric MATCH (APEC1621), EZH2, Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET).
Shares Tazemetostat with doxorubicin as front-line therapy for advanced epithelioid sarcoma (EZH-301 run-in), Epithelioid sarcoma.
Shares EZH2, Lineage plasticity & neuroendocrine transformation, Epigenetic therapy roadmap: loosening silenced genes → mutation-specific enzymes → editing the epigenome, Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET).
Shares Epigenetic progenitor theory: cancer without a first mutation, Epigenetic therapy roadmap: loosening silenced genes → mutation-specific enzymes → editing the epigenome, Epigenetic drugs (HDAC, DNMT, EZH2, IDH, menin, BET).
Shares EZH2 gain-of-function mutation (Tyr646, originally Tyr641), FLIPI, FLIPI2 and POD24 (follicular lymphoma risk), EZH2, Follicular lymphoma.