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FOR U.S. HEALTHCARE PROFESSIONALS ONLY

TAZVERIK® MECHANISM OF ACTION

NORMAL

RegulatedEZH2 activity (a histone methyltransferase)

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EZH2 plays a key role in the regulation of gene expression through appropriate and timely repression of genes involved in cell differentiation, and apoptosis. This allows for controlled cell growth and survival.1-3

EPITHELIOID SARCOMA

OveractiveEZH2 activity

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Overactive EZH2 causes dysregulated gene expression by inappropriately silencing target genesa and locking cells in a proliferative state.1-4

This can lead to tumor growth.1-4

TAZVERIK®

Reduced EZH2 activity

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Uniquely designed to target and inhibit EZH2 activity, TAZVERIK can help unlock gene expression to allow target genesa to be appropriately expressed.5

This information is derived from animal studies and does not demonstrate clinical efficacy and safety.

aTarget genes include tumor suppressor genes, differentiation markers, cell cycle regulators, and apoptotic machinery.

EZH2=enhancer of zeste homologue 2.

References: 1. Italiano A. Role of the EZH2 histone methyltransferase as a therapeutic target in cancer. Pharmacol Ther. 2016;165:26-31. 2. Gan L, Yang Y, Li Q, et al. Epigenetic regulation of cancer progression by EZH2: from biological insights to therapeutic potential. Biomark Res. 2018;6:10. 3. Siontis BL, Chugh R, and Schuetze SM. The potential of emerging therapeutics for epithelioid sarcoma. Expert Opin Orphan Drugs. 2017;5(12):983-989. 4. Shain AH, Giacomini CP, Matsukuma K, et al. Convergent structural alterations define SWItch/Sucrose NonFermentable (SWI/SNF) chromatin remodeler as a central tumor suppressive complex in pancreatic cancer. Proc Natl Acad Sci U S A. 2012;109(5):E252-E259. doi:10.1073/pnas.1114817109. 5. TAZVERIK. Prescribing information. Epizyme, Inc; 2020.

Learn more about epithelioid sarcoma.

EPITHELIOID SARCOMA

See the efficacy data of TAZVERIK.

EFFICACY DATA

IMPORTANT SAFETY INFORMATION AND INDICATION

Warnings and Precautions

  • 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.

  • 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 [AUC0‑45h]) at the 800 mg twice daily dose.

Advise pregnant women of the potential risk to a fetus. Advise females of reproductive potential to use effective contraception during treatment with TAZVERIK and for 6 months after the final dose. Advise males with female partners of reproductive potential to use effective contraception during treatment with TAZVERIK and for 3 months after the final dose.

Adverse Reactions

In 62 clinical study patients with epithelioid sarcoma receiving TAZVERIK 800 mg twice daily: Serious adverse reactions occurred in 37% of patients who received TAZVERIK. Serious adverse reactions occurring in ≥3% were hemorrhage, pleural effusion, skin infection, dyspnea, pain, and respiratory distress. The most common (≥20%) adverse reactions were pain (52%), fatigue (47%), nausea (36%), decreased appetite (26%), vomiting (24%), and constipation (21%).

Drug Interactions

Avoid coadministration of strong or moderate CYP3A inhibitors with TAZVERIK. If coadministration of moderate CYP3A inhibitors cannot be avoided, reduce TAZVERIK dose.

Avoid coadministration of moderate and strong CYP3A inducers with TAZVERIK, which may decrease the efficacy of TAZVERIK.

Coadministration of TAZVERIK with CYP3A substrates, including hormonal contraceptives, can result in decreased concentrations and reduced efficacy of CYP3A substrates.

Lactation

Because of the potential risk for serious adverse reactions from TAZVERIK in the breastfed child, advise women not to breastfeed during treatment with TAZVERIK and for one week after the final dose.

To report SUSPECTED ADVERSE REACTIONS, contact Ipsen Biopharmaceuticals, Inc. at 1-855-463-5127 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

INDICATION

TAZVERIK is 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.

This indication is approved under accelerated approval based on overall response rate and duration of response. Continued approval for this indication may be contingent upon verification and description of clinical benefit in a confirmatory trial(s).

Please see full Prescribing Information.