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Tazverik (tazemetostat)
Tazverik works by blocking the action of the EED protein, which is involved in the regulation of gene expression.
Tazverik (tazemetostat) is a small molecule methyltransferase inhibitor developed by Epizyme Inc, targeting the Polycomb protein EED. It was FDA-approved in 2020 for the treatment of epithelioid sarcoma and follicular lymphoma. Tazverik is a patented medication with no generic manufacturers available. The drug has a half-life of approximately 3.1 hours. Key safety considerations include its potential to cause infections, anemia, and thrombocytopenia.
At a glance
| Generic name | tazemetostat |
|---|---|
| Sponsor | Epizyme Inc |
| Drug class | Methyltransferase Inhibitor |
| Target | Polycomb protein EED |
| Modality | Small molecule |
| Therapeutic area | Oncology |
| Phase | FDA-approved |
| First approval | 2020 |
Mechanism of action
Tazemetostat is an inhibitor of the methyltransferase, EZH2, and some EZH2 gain-of-function mutations including Y646X, A682G, and A692V. Tazemetostat also inhibited EZH1 with half-maximal inhibitory concentration (IC50) of 392 nM, approximately 36 times higher than the IC50 for inhibition of EZH2.The most well-characterized function of EZH2 is as the catalytic subunit of the polycomb repressive complex (PRC2), catalyzing mono-, di-, and trimethylation of lysine 27 of histone H3. Trimethylation of histone H3 leads to transcriptional repression.SWItch/Sucrose Non-Fermentable (SWI/SNF) complexes can antagonize PRC2 function in the regulation of the expression of certain genes of patients with epithelioid sarcoma. Preclinical in vitro and in vivo models with the loss or dysfunction of certain SWI/SNF complex members (e.g., integrase interactor [INI1/SNF5/SMARCB1/BAF47], SMARCA4, and SMARCA2) can lead to aberrant EZH2 activity or expression and resulting oncogenic
Approved indications
- Epithelioid Sarcoma
- Relapsed or Refractory Follicular Lymphoma with EZH2 Mutation
- Relapsed or Refractory Follicular Lymphoma without Satisfactory Alternatives
Common side effects
- Pain
- Fatigue
- Nausea
- Decreased appetite
- Vomiting
- Constipation
- Upper respiratory tract infection
- Hemorrhage
- Dyspnea
- Headache
- Cough
- Diarrhea
Key clinical trials
- Testing the Addition of Tazemetostat to the Immunotherapy Drug, Pembrolizumab (MK-3475), in Advanced Urothelial Carcinoma (PHASE1,PHASE2)
- Tazemetostat in Treating Patients With Recurrent Ovarian or Endometrial Cancer (PHASE2)
- Testing of Tazemetostat in Combination With Topotecan and Pembrolizumab in Patients With Recurrent Small Cell Lung Cancer (PHASE1)
- Testing the Safety of the Anti-cancer Drugs Tazemetostat and Belinostat in Patients With Lymphomas That Have Resisted Treatment (PHASE1)
- Testing the Addition of the Anti-cancer Drug, Tazemetostat, to the Usual Treatment (Dabrafenib and Trametinib) for Metastatic Melanoma That Has Progressed on the Usual Treatment (PHASE1,PHASE2)
- Phase II Study of Tazemetostat in Solid Tumors Harboring an ARID1A Mutation (PHASE2)
- Tazemetostat and Palbociclib With CPX-351for R/R AML (PHASE1)
- A Study of Tazemetostat With Enzalutamide or Abiraterone/Prednisone in Participants With Advanced Prostate Cancer (PHASE1,PHASE2)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Tazverik CI brief — competitive landscape report
- Tazverik updates RSS · CI watch RSS
- Epizyme Inc portfolio CI