Epithelioid sarcoma, metastatic or locally advanced: Oral: 800 mg twice daily until disease progression or unacceptable toxicity (Stacchiotti 2019).
Follicular lymphoma, relapsed/refractory, EZH2 mutation- positive: Oral: 800 mg twice daily until disease progression or unacceptable toxicity (Morschhauser 2020).
Follicular lymphoma, relapsed/refractory, salvage therapy: Oral: 800 mg twice daily until disease progression or unacceptable toxicity (Morschhauser 2020).
Missed dose: If a dose is missed or vomited, do not take an additional dose; continue with the next scheduled dose.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
No dosage adjustment necessary.
Mild impairment (total bilirubin >1 to 1.5 times ULN or AST > ULN): No dosage adjustment necessary.
Moderate (total bilirubin >1.5 to 3 times ULN) or severe (total bilirubin >3 times ULN) impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
(For additional information see "Tazemetostat: Pediatric drug information")
Epithelioid sarcoma, metastatic or locally advanced: Adolescents ≥16 years: Oral: 800 mg twice daily until disease progression or unacceptable toxicity.
Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Dosage adjustment for toxicity:
Dose reductions:
First dose reduction: Oral: Tazemetostat 600 mg twice daily.
Second dose reduction: Oral: Tazemetostat 400 mg twice daily.
Note: Discontinue permanently if unable to tolerate tazemetostat 400 mg twice daily.
Dosage adjustment for neutropenia (neutrophil count <1 x 109/L): Hold tazemetostat until neutrophil count ≥1 x 109/L or baseline, then resume as follows:
If first occurrence: Resume tazemetostat at same dose.
For second or third occurrence: Resume tazemetostat at reduced dose.
After fourth occurrence: Permanently discontinue tazemetostat.
Dosage adjustment for thrombocytopenia (platelet count <50 x 109/L): Hold tazemetostat until platelet count ≥75 x 109/L or baseline, then resume as follows:
For first and second occurrence: Resume tazemetostat at reduced dose.
After third occurrence: Permanently discontinue tazemetostat.
Dosage adjustment for anemia (hemoglobin <8 g/dL): Hold tazemetostat until improved to least grade 1 or baseline, then resume at the same or reduced dose.
Dosage adjustment for other grade 3 adverse reactions: Hold tazemetostat until improved to at least grade 1 or baseline, then resume as follows:
For first and second occurrence: Resume tazemetostat at reduced dose.
After third occurrence: Permanently discontinue tazemetostat.
Dosage adjustment for other grade 4 adverse reactions: Hold tazemetostat until improved to at least grade 1 or baseline, then resume as follows:
For first occurrence: Resume tazemetostat at reduced dose.
After second occurrence: Permanently discontinue tazemetostat.
Adolescents ≥16 years:
Mild to severe impairment: No dosage adjustment needed.
End-stage renal disease: No dosage adjustment needed.
Adolescents ≥16 years:
Mild impairment (total bilirubin >1 to 1.5 x ULN or AST > ULN): No dosage adjustment necessary.
Moderate (total bilirubin >1.5 to 3 x ULN) or severe (total bilirubin >3 x ULN) impairment: There are no dosage adjustments provided in the manufacturer's labeling (has not been studied).
Refer to adult dosing.
Initial (usual) dose |
800 mg twice daily |
First dose reduction level |
600 mg twice daily |
Second dose reduction level |
400 mg twice daily |
Unable to tolerate 400 mg twice daily |
Permanently discontinue tazemetostat |
Toxicity |
Severity |
Tazemetostat Dose Modification |
---|---|---|
Neutropenia |
Neutrophil count <1,000/mm3 |
Withhold tazemetostat until neutrophils ≥1,000/mm3 or baseline. If first occurrence, resume at the same dose. For second and third occurrence, resume at a reduced dose. Permanently discontinue after fourth occurrence. |
Thrombocytopenia |
Platelet count <50,000/mm3 |
Withhold tazemetostat until platelets ≥75,000/mm3 or baseline. If first or second occurrence, resume at a reduced dose. Permanently discontinue after third occurrence. |
Anemia |
Hemoglobin <8 g/dL |
Withhold tazemetostat until improvement to at least grade 1 or baseline, then resume at the same or a reduced dose. |
Other adverse reactions |
Grade 3 |
Withhold tazemetostat until improvement to at least grade 1 or baseline. If first or second occurrence, resume at a reduced dose. Permanently discontinue after third occurrence. |
Grade 4 |
Withhold tazemetostat until improvement to at least grade 1 or baseline. If first occurrence, resume at a reduced dose. Permanently discontinue after second occurrence. |
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Tablet, Oral:
Tazverik: 200 mg
No
Tazemetostat is available through a specialty pharmacy and specialty distributors. For further information, contact 833-437-4669 or https://www.tazverik.com/Content/pdf/ordering-and-distribution-sheet.pdf.
An FDA-approved patient medication guide, which is available with the product information and as follows, must be dispensed with this medication:
Tazverik: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/213400s000lbl.pdf
Oral: May administer with or without food. Swallow tablets whole; do not cut, crush, or chew.
Oral: Swallow tablet whole; do not cut, crush, or chew. Administer without regard to food. Do not administer an additional dose for a missed dose or for vomiting; resume with next scheduled dose.
This medication is not on the NIOSH (2016) list; however, it may meet the criteria for a hazardous drug. Tazemetostat may cause carcinogenicity and teratogenicity.
Use appropriate precautions for receiving, handling, storage, preparation, dispensing, transporting, administration, and disposal. Follow NIOSH and USP 800 recommendations and institution-specific policies/procedures for appropriate containment strategy (NIOSH 2016; USP-NF 2020).
Note: Facilities may perform risk assessment of some hazardous drugs to determine if appropriate for alternative handling and containment strategies (USP-NF 2020). Refer to institution-specific handling policies/procedures.
Epithelioid sarcoma, metastatic or locally advanced: Treatment of metastatic or locally advanced epithelioid sarcoma not eligible for complete resection in adults and adolescents ≥16 years of age.
Follicular lymphoma, relapsed/refractory:
Treatment of relapsed or refractory follicular lymphoma in adults whose tumors are positive for an EZH2 mutation (as detected by an approved test) and who have received at least 2 prior systemic therapies.
Treatment of relapsed or refractory follicular lymphoma in adults who have no satisfactory alternative treatment options.
Tazemetostat may be confused with belinostat, panobinostat, vorinostat.
This medication is in a class the Institute for Safe Medication Practices includes among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.
Tazemetostat may cause dose-limiting bone marrow suppression; decreased hemoglobin (including anemia), decreased neutrophils, decreased platelet count, decreased white blood cell count, and lymphocytopenia have commonly been reported. Hematologic effects may be reversible following dosage modification, interruption of therapy, and/or discontinuation.
Mechanism: Dose-related; exact mechanism is unknown.
Onset: May occur at any time during treatment (Ref).
Tazemetostat may increase the risk of developing secondary malignancies. Myelodysplastic syndromes and acute myeloid leukemia have been reported rarely.
Mechanism: Time-related. Exact mechanism is unknown; impact of disease process and concurrent medications must be considered.
Onset: Delayed; myelodysplastic syndrome and acute myeloid leukemia were reported after >1 year of treatment with tazemetostat in one clinical trial (Ref).
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified.
>10%:
Dermatologic: Alopecia, skin rash
Endocrine & metabolic: Decreased serum albumin, decreased serum calcium, decreased serum glucose, decreased serum phosphate, decreased serum potassium, decreased serum sodium, increased serum glucose, increased serum potassium, increased serum triglycerides, weight loss
Gastrointestinal: Abdominal pain, constipation, decreased appetite, diarrhea, nausea, vomiting
Genitourinary: Urinary tract infection
Hematologic & oncologic: Decreased hemoglobin (including anemia), decreased neutrophils, decreased platelet count, decreased white blood cell count, hemorrhage (including cerebral hemorrhage, hemoptysis, pulmonary hemorrhage, rectal hemorrhage, wound hemorrhage), lymphocytopenia, prolonged partial thromboplastin time
Hepatic: Increased serum alanine aminotransferase, increased serum alkaline phosphatase, increased serum aspartate aminotransferase
Nervous system: Fatigue (includes asthenia), headache, pain
Neuromuscular & skeletal: Musculoskeletal pain
Renal: Increased serum creatinine
Respiratory: Cough, dyspnea, lower respiratory tract infection, upper respiratory tract infection
1% to 10%:
Dermatologic: Skin infection
Infection: Herpes zoster infection, sepsis
Respiratory: Pleural effusion, pneumonia, respiratory distress
Miscellaneous: Fever
<1%: Hematologic & oncologic: Myelodysplastic syndrome (Morschhauser 2020), myeloid leukemia (acute) (Morschhauser 2020), T-cell lymphoma
There are no contraindications listed in the manufacturer's labeling.
Other warnings/precautions:
• Appropriate use: Select patients for tazemetostat treatment of relapsed/refractory follicular lymphoma (excluding salvage therapy) based on the presence of EZH2 mutation of codons Y646, A682, or A692 in tumor specimens. Information on approved tests is available at http://www.fda.gov/CompanionDiagnostics.
Substrate of CYP3A4 (major), P-glycoprotein/ABCB1 (minor); Note: Assignment of Major/Minor substrate status based on clinically relevant drug interaction potential; Inhibits CYP2C8 (weak); Induces CYP3A4 (weak)
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Abrocitinib: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid combination
Baricitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Baricitinib. Risk X: Avoid combination
BCG Products: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of BCG Products. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of BCG Products. Risk X: Avoid combination
Brincidofovir: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Brincidofovir. Risk C: Monitor therapy
Cladribine: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Cladribine. Risk X: Avoid combination
Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk C: Monitor therapy
CloZAPine: CYP3A4 Inducers (Weak) may decrease the serum concentration of CloZAPine. Risk C: Monitor therapy
Coccidioides immitis Skin Test: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the diagnostic effect of Coccidioides immitis Skin Test. Management: Consider discontinuing these oncologic agents several weeks prior to coccidioides immitis skin antigen testing to increase the likelihood of accurate diagnostic results. Risk D: Consider therapy modification
COVID-19 Vaccine (Adenovirus Vector): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (Adenovirus Vector). Management: Administer a 2nd dose using an mRNA COVID-19 vaccine (at least 4 weeks after the primary vaccine dose) and a bivalent booster dose (at least 2 months after the additional mRNA dose or any other boosters). Risk D: Consider therapy modification
COVID-19 Vaccine (Inactivated Virus): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (Inactivated Virus). Risk C: Monitor therapy
COVID-19 Vaccine (mRNA): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (mRNA). Management: Give a 3-dose primary series for all patients aged 6 months and older taking immunosuppressive medications or therapies. Booster doses are recommended for certain age groups. See CDC guidance for details. Risk D: Consider therapy modification
COVID-19 Vaccine (Subunit): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (Subunit). Risk C: Monitor therapy
COVID-19 Vaccine (Virus-like Particles): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of COVID-19 Vaccine (Virus-like Particles). Risk C: Monitor therapy
CYP3A4 Inducers (Moderate): May decrease the serum concentration of Tazemetostat. Risk X: Avoid combination
CYP3A4 Inducers (Strong): May decrease the serum concentration of Tazemetostat. Risk X: Avoid combination
CYP3A4 Inhibitors (Moderate): May increase the serum concentration of Tazemetostat. Management: Avoid when possible. If combined, reduce tazemetostat dose from 800 mg twice daily to 400 mg twice daily, from 600 mg twice daily to 400 mg in AM and 200 mg in PM, or from 400 mg twice daily to 200 mg twice daily. Risk D: Consider therapy modification
CYP3A4 Inhibitors (Strong): May increase the serum concentration of Tazemetostat. Risk X: Avoid combination
Dengue Tetravalent Vaccine (Live): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Dengue Tetravalent Vaccine (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Dengue Tetravalent Vaccine (Live). Risk X: Avoid combination
Denosumab: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Management: Consider the risk of serious infections versus the potential benefits of coadministration of denosumab and immunosuppressants. If combined, monitor patients for signs/symptoms of serious infections. Risk D: Consider therapy modification
Deucravacitinib: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid combination
Fexinidazole: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Filgotinib: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid combination
Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Risk X: Avoid combination
Hormonal Contraceptives: Tazemetostat may decrease the serum concentration of Hormonal Contraceptives. Management: Individuals of childbearing potential should use a non-hormonal contraceptive method during treatment with tazemetostat and for 6 months after. Males with partners of childbearing potential should use contraception during treatment and for 3 months after. Risk D: Consider therapy modification
Inebilizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Inebilizumab. Risk C: Monitor therapy
Influenza Virus Vaccines: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Influenza Virus Vaccines. Management: Administer influenza vaccines at least 2 weeks prior to initiating immunosuppressants if possible. If vaccination occurs less than 2 weeks prior to or during therapy, revaccinate at least 3 months after therapy discontinued if immune competence restored. Risk D: Consider therapy modification
Leflunomide: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Leflunomide. Management: Increase the frequency of chronic monitoring of platelet, white blood cell count, and hemoglobin or hematocrit to monthly, instead of every 6 to 8 weeks, if leflunomide is coadministered with immunosuppressive agents. Risk D: Consider therapy modification
Natalizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Natalizumab. Risk X: Avoid combination
NiMODipine: CYP3A4 Inducers (Weak) may decrease the serum concentration of NiMODipine. Risk C: Monitor therapy
Ocrelizumab: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Ocrelizumab. Risk C: Monitor therapy
Ofatumumab: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Ofatumumab. Risk C: Monitor therapy
Pidotimod: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Pidotimod. Risk C: Monitor therapy
Pimecrolimus: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk X: Avoid combination
Pneumococcal Vaccines: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Pneumococcal Vaccines. Risk C: Monitor therapy
Poliovirus Vaccine (Live/Trivalent/Oral): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Poliovirus Vaccine (Live/Trivalent/Oral). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Poliovirus Vaccine (Live/Trivalent/Oral). Risk X: Avoid combination
Polymethylmethacrylate: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the potential for allergic or hypersensitivity reactions to Polymethylmethacrylate. Management: Use caution when considering use of bovine collagen-containing implants such as the polymethylmethacrylate-based Bellafill brand implant in patients who are receiving immunosuppressants. Consider use of additional skin tests prior to administration. Risk D: Consider therapy modification
Rabies Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Rabies Vaccine. Management: Complete rabies vaccination at least 2 weeks before initiation of immunosuppressant therapy if possible. If combined, check for rabies antibody titers, and if vaccination is for post exposure prophylaxis, administer a 5th dose of the vaccine. Risk D: Consider therapy modification
Repaglinide: CYP2C8 Inhibitors (Weak) may increase the serum concentration of Repaglinide. Risk C: Monitor therapy
Rubella- or Varicella-Containing Live Vaccines: May enhance the adverse/toxic effect of Immunosuppressants (Miscellaneous Oncologic Agents). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Rubella- or Varicella-Containing Live Vaccines. Risk X: Avoid combination
Ruxolitinib (Topical): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Ruxolitinib (Topical). Risk X: Avoid combination
Selpercatinib: CYP3A4 Inducers (Weak) may decrease the serum concentration of Selpercatinib. Risk C: Monitor therapy
Sipuleucel-T: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Sipuleucel-T. Management: Consider reducing the dose or discontinuing the use of immunosuppressants prior to initiating sipuleucel-T therapy. Risk D: Consider therapy modification
Sirolimus (Conventional): CYP3A4 Inducers (Weak) may decrease the serum concentration of Sirolimus (Conventional). Risk C: Monitor therapy
Sirolimus (Protein Bound): CYP3A4 Inducers (Weak) may decrease the serum concentration of Sirolimus (Protein Bound). Risk C: Monitor therapy
Sphingosine 1-Phosphate (S1P) Receptor Modulator: May enhance the immunosuppressive effect of Immunosuppressants (Miscellaneous Oncologic Agents). Risk C: Monitor therapy
Tacrolimus (Systemic): CYP3A4 Inducers (Weak) may decrease the serum concentration of Tacrolimus (Systemic). Risk C: Monitor therapy
Tacrolimus (Topical): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Tacrolimus (Topical). Risk X: Avoid combination
Talimogene Laherparepvec: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Talimogene Laherparepvec. Specifically, the risk of infection from the live, attenuated herpes simplex virus contained in talimogene laherparepvec may be increased. Risk X: Avoid combination
Tertomotide: Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Tertomotide. Risk X: Avoid combination
Tofacitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Tofacitinib. Risk X: Avoid combination
Typhoid Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Typhoid Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Typhoid Vaccine. Risk X: Avoid combination
Ubrogepant: CYP3A4 Inducers (Weak) may decrease the serum concentration of Ubrogepant. Management: Use an initial ubrogepant dose of 100 mg and second dose (if needed) of 100 mg when used with a weak CYP3A4 inducer. Risk D: Consider therapy modification
Upadacitinib: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the immunosuppressive effect of Upadacitinib. Risk X: Avoid combination
Vaccines (Inactivated/Non-Replicating): Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Vaccines (Inactivated/Non-Replicating). Management: Give inactivated vaccines at least 2 weeks prior to initiation of immunosuppressants when possible. Patients vaccinated less than 14 days before initiating or during therapy should be revaccinated at least 3 after therapy is complete. Risk D: Consider therapy modification
Vaccines (Live): Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Vaccines (Live). Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Vaccines (Live). Risk X: Avoid combination
Yellow Fever Vaccine: Immunosuppressants (Miscellaneous Oncologic Agents) may enhance the adverse/toxic effect of Yellow Fever Vaccine. Specifically, the risk of vaccine-associated infection may be increased. Immunosuppressants (Miscellaneous Oncologic Agents) may diminish the therapeutic effect of Yellow Fever Vaccine. Risk X: Avoid combination
Evaluate pregnancy status prior to use in females of reproductive potential. Females of reproductive potential should use effective nonhormonal contraception during therapy and for 6 months after the last tazemetostat dose. Males with female partners of reproductive potential should use effective contraception during therapy and for at least 3 months after the last dose of tazemetostat.
Based on the mechanism of action, and data from animal reproduction studies, in utero exposure to tazemetostat may cause fetal harm.
It is not known if tazemetostat is present in breast milk.
Due to the potential for serious adverse reactions in the breastfed infant, breastfeeding is not recommended by the manufacturer during therapy and for one week after the last tazemetostat dose.
EZH2 mutation status in tumor specimen (for relapsed/refractory follicular lymphoma, excluding salvage therapy). CBC with differential. Evaluate pregnancy status prior to use in females of reproductive potential. Monitor (long term) for development of secondary malignancies. Monitor adherence.
The American Society of Clinical Oncology hepatitis B virus (HBV) screening and management provisional clinical opinion (ASCO [Hwang 2020]) recommends HBV screening with hepatitis B surface antigen, hepatitis B core antibody, total Ig or IgG, and antibody to hepatitis B surface antigen prior to beginning (or at the beginning of) systemic anticancer therapy; do not delay treatment for screening/results. Detection of chronic or past HBV infection requires a risk assessment to determine antiviral prophylaxis requirements, monitoring, and follow-up.
Tazemetostat is a potent and selective inhibitor of histone methyltransferase EZH2 (enhancer of zeste homolog 2); it also inhibits some EZH2 gain-of-function mutations (including Y646X and A687V), as well as EZH1. EZH2 is overexpressed or mutated in many cancer types and plays a role in tumor proliferation. SWItch/Sucrose Non-Fermentable (SWI/SNF) complex aids in facilitating gene expression and terminal differentiation; altered EZH2 upregulation and loss-of-function mutations in SWI/SNF are oncogenic in many human cancers; tazemetostat has antitumor activity in EZH2-mutant cell lines (Italiano 2018). Tazemetostat suppressed B-cell lymphoma cell lines proliferation in vitro, and showed antitumor activity in an animal model of B-cell lymphoma with or without EZH2 gain-of-function mutations; tazemetostat demonstrated increased inhibition of lymphoma cell line proliferation with mutant EZH2.
Distribution: Vss/F: 1,230 L.
Protein binding: 88%.
Metabolism: Via CYP3A to form the inactive major metabolites M5 (EPZ-6930) and M3 (EPZ006931); M5 is further metabolized by CYP3A.
Bioavailability: ~33%.
Half-life elimination: 3.1 hours.
Time to peak: 1 to 2 hours.
Excretion: Feces: 79%; urine: 15%.
Clearance: 274 L/hour.
Tablets (Tazverik Oral)
200 mg (per each): $88.73
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