Tazemetostat

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 a half-maximal inhibitory concentration (IC 50 ) of 392 nM, approximately 36 times higher than the IC 50 for inhibition of EZH2.

• TAZVERIK is a methyltransferase inhibitor indicated for the treatment of: Adults and pediatric patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection. ( 1.1 ) Adult patients with relapsed or refractory follicular lymphoma 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.ICD-10: C85.90

• None. None.contraindicated

Recommended dosage is 800 mg taken orally twice daily with or without food. ( 2.2 ) 2.1 Patient Selection Select patients with R/R FL for treatment with TAZVERIK based on the presence of EZH2 mutation of codons Y646, A682, or A692 in tumor specimens [see Clinical Studies ( 14.2 )] . Information on FDA-approved tests for the detection of EZH2 mutation in relapsed or refractory follicular lymphoma is available at: http://www.fda.gov/CompanionDiagnostics. 2.2 Recommended Dosage The recommended dosage of TAZVERIK is 800 mg orally twice daily with or without food until disease progression or unacceptable toxicity. Swallow tablets whole. Do not cut, crush, or chew tablets. Do not take an additional dose if a dose is missed or vomiting occurs after TAZVERIK, but continue with the next scheduled dose. 2.3 Dosage Modifications for Adverse Reactions Table 1 summarizes the recommended dose reductions, and Table 2 summarizes the recommended dosage modifications of TAZVERIK for adverse reactions. Table 1. Recommended Dose Reductions of TAZVERIK for Adverse Reactions *Permanently discontinue TAZVERIK in patients who are unable to tolerate 400 mg orally twice daily. Dose Reduction Dosage First 600 mg orally twice daily Second 400 mg orally twice daily* Table 2. Recommended Dosage Modifications of TAZVERIK for Adverse Reactions Adverse Reaction Severity Dosage Modification Neutropenia [see Adverse Reactions ( 6.1 )] Neutrophil count less than 1 × 10 9 /L Withhold until neutrophil count is greater than or equal to 1 × 10 9 /L or baseline. For first occurrence, resume at same dose.

Secondary Malignancies : TAZVERIK increases the risk of developing secondary malignancies, including T-cell lymphoblastic lymphoma, myelodysplastic syndrome, acute myeloid leukemia, and B-cell acute lymphoblastic leukemia. Monitor patients long-term for the development of secondary malignancies. ( 5.1 ) Embryo-Fetal Toxicity : Can cause fetal harm. Advise patients of potential risk to a fetus and to use effective non-hormonal contraception. ( 5.2 ) 5.1 Secondary Malignancies The risk of developing secondary malignancies is increased following treatment with TAZVERIK. Across clinical trials of 758 adults who received TAZVERIK 800 mg twice daily as monotherapy, myelodysplastic syndrome (MDS), acute myeloid leukemia (AML), or B-cell acute lymphoblastic leukemia (B-ALL) occurred in 1.7% of patients. One pediatric patient developed T-cell lymphoblastic lymphoma (T-LBL). Monitor patients long-term for the development of secondary malignancies. 5.2 Embryo-Fetal Toxicity Based on findings from animal studies and its mechanism of action, TAZVERIK can cause fetal harm when administered to pregnant women. There are no available data on TAZVERIK use in pregnant women to inform the drug-associated risk. Administration of tazemetostat to pregnant rats and rabbits during organogenesis resulted in dose-dependent increases in skeletal developmental abnormalities in both species beginning at maternal exposures approximately 1.5 times the adult human exposure (area under the plasma concentration time curve [AUC 0-45h ]) at the 800 mg twice daily dose.

The following clinically significant adverse reactions are described elsewhere in labeling: Secondary Malignancies [see Warnings and Precautions ( 5.1 )]. The most common (≥20%) adverse reactions in patients with epithelioid sarcoma are pain, fatigue, nausea, decreased appetite, vomiting, and constipation. ( 6.1 ) The most common (≥20%) adverse reactions in patients with follicular lymphoma are fatigue, upper respiratory tract infection, musculoskeletal pain, nausea, and abdominal pain. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Epizyme at 855-463-5127 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . 6.1 Clinical Trial Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared with rates in the clinical trials of another drug and may not reflect the rates observed in practice. Epithelioid Sarcoma The safety of TAZVERIK was evaluated in a cohort (Cohort 5) of Study EZH-202 that enrolled patients with epithelioid sarcoma [see Clinical Studies ( 14.1 )]. Patients received TAZVERIK 800 mg orally twice daily (n=62). Among patients who received TAZVERIK, 44% were exposed for 6 months or longer and 24% were exposed for greater than one year. Serious adverse reactions occurred in 37% of patients who received TAZVERIK. Serious adverse reactions in ≥3% of patients who received TAZVERIK were hemorrhage, pleural effusion, skin infection, dyspnea, pain, and respiratory distress.

Lactation : Advise not to breastfeed. ( 8.2 ) 8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [see Clinical Pharmacology ( 12.1 )] , TAZVERIK can cause fetal harm when administered to pregnant women. There are no available data on TAZVERIK use in pregnant women to inform the drug-associated risk. Administration of tazemetostat to pregnant rats and rabbits during organogenesis resulted in dose-dependent increases in skeletal developmental abnormalities in both species beginning at maternal exposures approximately 1.5 times the adult human exposure [AUC 0-45h ] at the 800 mg twice daily dose (see Data ) . Advise pregnant women of the potential risk to a fetus. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Animal Data In pregnant rats, once daily oral administration of tazemetostat during the period of organogenesis from gestation day (GD) 7 through 17 resulted in no maternal adverse effects at doses up to 100 mg/kg/day (approximately 6 times the adult human exposure at 800 mg twice daily). Skeletal malformations and variations occurred in fetuses at doses of ≥50 mg/kg (approximately 2 times the adult human exposure at the 800 mg twice daily dose).

Metabolism

The systemic exposure of tazemetostat is approximately dose proportional over the dose range of 200 mg to 1600 mg twice daily of TAZVERIK (0.25 to 2 times the approved recommended dosage). Following TAZVERIK 800 mg orally twice daily, steady-state was reached by Day 15.

• Jan 23, 2020NDANDA211723Epizyme Inc

Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

• Tazverik, Tablet, 200 mg (NDC 72607-100-00)To be discontinued
  Sponsor: Epizyme, Inc. (An Ipsen Company)
  Updated Mar 27, 2026

1. 1Off Label Use33221%
2. 2Fatigue32521%
3. 3Disease Progression30019%
4. 4Nausea23115%
5. 5Product Dose Omission Issue21214%
6. 6Death1247.9%
7. 7Diarrhoea1187.5%
8. 8Decreased Appetite976.2%
9. 9Vomiting925.9%
10. 10Asthenia835.3%
11. 11Constipation795.0%
12. 12Headache734.6%
13. 13Covid-19724.6%
14. 14Alopecia694.4%
15. 15Pain684.3%

The 10 most recently updated of 60 ClinicalTrials.gov registrations naming Tazemetostat as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Testing the Addition of Tazemetostat to the Immunotherapy Drug, Pembrolizumab (MK-3475), in Advanced Urothelial Carcinoma
  Active not recruiting · Phase 1 · Phase 2 · Interventional · 30 enrolled · National Cancer Institute (NCI)
  NCT03854474updated 2026-06-11
• Tazemetostat in Malignant Peripheral Nerve Sheath Tumors
  Active not recruiting · Phase 2 · Interventional · 10 enrolled · University of Florida
  NCT04917042updated 2026-06-04
• A Study to Assess the Efficacy, Safety, Pharmacodynamics, and Pharmacokinetics of Tazemetostat in Combination With Lenalidomide Plus Rituximab Versus Placebo in Combination With Lenalidomide Plus Rituximab in Adult Patients at Least 18 Years of Age With Relapsed/Refractory Follicular Lymphoma.
  Active not recruiting · Phase 3 · Interventional · 599 enrolled · Epizyme, Inc.
  NCT04224493updated 2026-06-01
• Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial)
  Active not recruiting · Phase 2 · Interventional · 1,377 enrolled · National Cancer Institute (NCI)
  NCT03155620updated 2026-06-01
• Tazemetostat in Treating Patients With Recurrent Ovarian or Endometrial Cancer
  Active not recruiting · Phase 2 · Interventional · 62 enrolled · National Cancer Institute (NCI)
  NCT03348631updated 2026-05-29
• Testing of Tazemetostat in Combination With Topotecan and Pembrolizumab in Patients With Recurrent Small Cell Lung Cancer
  Active not recruiting · Phase 1 · Interventional · 18 enrolled · National Cancer Institute (NCI)
  NCT05353439updated 2026-05-13
• Testing the Safety of the Anti-cancer Drugs Tazemetostat and Belinostat in Patients With Lymphomas That Have Resisted Treatment
  Active not recruiting · Phase 1 · Interventional · 48 enrolled · National Cancer Institute (NCI)
  NCT05627245updated 2026-05-13
• Phase Ia/Ib Talazoparib + Tazemetostat for mCRPC
  Active not recruiting · Phase 1 · Interventional · 35 enrolled · Dana-Farber Cancer Institute
  NCT04846478updated 2026-05-12
• Pembrolizumab and Tazemetostat to Overcome Immune Tolerance Following ASCT or CAR T-cell Therapy in Patients With Aggressive B-Cell Non-Hodgkin's Lymphoma
  Active not recruiting · Phase 2 · Interventional · 32 enrolled · Northwestern University
  NCT06242834updated 2026-05-07
• Study of Tazemetostat in Adults With Follicular Lymphoma Previously Treated With at Least Two Therapies
  Withdrawn · Observational · 0 enrolled · Ipsen
  NCT07282548updated 2026-04-29

Frequently asked questions

How does Tazemetostat work?

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 a half-maximal inhibitory concentration (IC 50 ) of 392 nM, approximately 36 times higher than the IC 50 for inhibition of EZH2.

What is Tazemetostat used for?

According to FDA labeling, Tazemetostat carries indications including: TAZVERIK is a methyltransferase inhibitor indicated for the treatment of: Adults and pediatric patients aged 16 years and older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection. ( 1.1 ) Adult patients with relapsed or refractory follicular lymphoma 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Tazemetostat?

Tazemetostat is classified as Other antineoplastic agents, Methyltransferase Inhibitor, Enzyme Inhibitors, Methyltransferase Inhibitors, Multidrug and Toxin Extrusion Transporter 1 Inhibitors, Multidrug and Toxin Extrusion Transporter 2 K Inhibitors, Cellular Cycle Alteration.

What are the brand names for Tazemetostat?

Tazemetostat is marketed under brand names including Tazverik.

What are the contraindications for Tazemetostat?

Tazemetostat labeling lists contraindications including: None. None.. Always consult the full prescribing information and a clinician.