Adult: In patients not eligible for complete resection: 800 mg bid, continue until disease progression or unacceptable toxicity occurs. Dose reduction, dosing interruption, or discontinuation may be required according to the type and severity of adverse reactions (refer to detailed product guidelines). Child: ≥16 years Same as adult dose.
Adult: In patients who are positive for enhancer of zeste homolog-2 (EZH2) mutation and have received at least 2 prior systemic therapies, and patients who have no satisfactory alternative treatment options: 800 mg bid, continue until disease progression or unacceptable toxicity occurs. Dose reduction, dosing interruption, or discontinuation may be required according to the type and severity of adverse reactions (refer to detailed product guidelines).
Special Patient Group
Patients concomitantly taking moderate CYP3A inhibitors: If the current tazemetostat dose is 800 mg bid, reduce the dose to 400 mg bid. If current tazemetostat dose is 600 mg bid, reduce the dose to 400 mg for the 1st dose and 200 mg for the 2nd dose. If the current tazemetostat dose is 400 mg bid, reduce the dose to 200 mg bid. After discontinuing the concomitant moderate CYP3A inhibitor for 3 elimination half-lives, resume the tazemetostat dose taken before initiating the CYP3A inhibitor.
Administration
May be taken with or without food. Swallow whole & do not cut/crush/chew.
Special Precautions
Patients concomitantly taking moderate CYP3A inhibitors. Avoid concomitant use with strong CYP3A inhibitors. Pregnancy and lactation.
Adverse Reactions
Significant: Secondary malignancies (e.g. myelodysplastic syndromes, acute myeloid leukaemia, B-cell acute lymphoblastic leukaemia); haematologic effects (e.g. decreased Hb, lymphocytes, platelets, neutrophils, and WBC count). Gastrointestinal disorders: Nausea, vomiting, constipation, diarrhoea, abdominal pain. General disorders and administration site conditions: Pain, fatigue, fever. Investigations: Decreased weight; decreased Na, Ca, phosphate; decreased or increased K; decreased albumin; decreased or increased glucose; increased triglycerides; increased AST, ALT and alkaline phosphatase; increased serum creatinine; increased partial thromboplastin time. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Musculoskeletal pain. Nervous system disorders: Headache. Renal and urinary disorders: UTI. Respiratory, thoracic and mediastinal disorders: Cough, dyspnoea, URTI, lower respiratory tract infection. Skin and subcutaneous tissue disorders: Alopecia, rash. Vascular disorders: Haemorrhage.
PO: Z (Embryo-foetal death and malformations were observed in animal studies. Not recommended.)
Patient Counseling Information
Women of childbearing potential must use effective non-hormonal birth control method during treatment and for 6 months after the last dose. Men with female partners of childbearing potential must use effective birth control method during treatment and for 3 months after the last dose. Breastfeeding is not recommended during treatment and for 1 week after the last dose.
Monitoring Parameters
Evaluate pregnancy status before starting treatment in women of childbearing potential. Determine EZH2 mutation status (presence of mutation of codons Y646, A682 or A692) in tumour specimens of patients with relapsed or refractory follicular lymphoma who have received at least 2 previous systemic therapies. Monitor CBC with differential and for development of secondary malignancies (during and long-term after therapy).
Drug Interactions
May increase plasma concentration with strong or moderate CYP3A inhibitors (e.g. fluconazole). May reduce plasma concentration with strong or moderate CYP3A inducers. May reduce the concentrations and efficacy of CYP3A substrates (e.g. hormonal contraceptives, midazolam).
Food Interaction
May increase plasma concentration with grapefruit or grapefruit juice. May reduce plasma concentration with St. John's wort.
Action
Description: Mechanism of Action: Tazemetostat is an antineoplastic agent and a selective, potent inhibitor of histone methyltransferase enhancer of zeste homolog 2 (EZH2), which plays a role in tumour proliferation. It also inhibits some EZH2 gain-of-function mutations, including Y646X and A687V, along with EZH1. Pharmacokinetics: Absorption: Bioavailability: Approx 33%. Time to peak plasma concentration: 1-2 hours. Distribution: Plasma protein binding: 88%. Metabolism: Metabolised by CYP3A to form inactive major metabolites, M5 (EPZ-6930) and M3 (EPZ006931); the M5 metabolite is further metabolised by CYP3A. Excretion: Via urine (15%); faeces (79%). Elimination half-life: 3.1 hours.
Chemical Structure
Tazemetostat Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 66558664, Tazemetostat. https://pubchem.ncbi.nlm.nih.gov/compound/Tazemetostat. Accessed Mar. 28, 2025.
Storage
Store below 30°C. Follow applicable procedures for receiving, handling, administration, and disposal.
L01XX72 - tazemetostat ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
References
Brayfield A, Cadart C (eds). Tazemetostat. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 06/03/2025.Tazemetostat. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 07/03/2025.Tazemetostat. UpToDate Lexidrug, AHFS DI (Adult and Pediatric) Online. American Society of Health-System Pharmacists, Inc. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/03/2025.Tazemetostat. UpToDate Lexidrug, Lexi-Drugs Multinational Online. Waltham, MA. UpToDate, Inc. https://online.lexi.com. Accessed 06/03/2025.Tazverik Tablet, Film Coated (Epizyme, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 06/03/2025.Tazverik Tablets 200 mg (Hutchmed [Hong Kong] Limited). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 06/03/2025.
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