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The emergence of tazerestat provides patients with a new, well-tolerated treatment option that can significantly improve patients' objective response rate (ORR) and prolong the duration of response.
1. Generic name: Tazemetostat
2. Trade name: TAZVERIK®
1. Adults and adolescents over 16 years old: treatment of unresectable metastatic or locally advanced epithelioid sarcoma.
2. Adult relapsed/refractory follicular lymphoma:
EZH2 mutation-positive (tested by FDA approval) and have received at least 2 types of systemic therapy;
Those who have no satisfactory alternative treatment options.
200 mg film-coated tablets.
Active ingredient: tazerestat hydrobromide (each tablet contains 200 mg of tazerestat, equivalent to 228 mg of hydrobromide).
1. Standard dose: 800 mg orally, twice a day (about 12 hours apart), with or without meals.
2. How to take: Swallow the tablet whole. Do not break, crush or chew.
1. Adverse reaction adjustment :
Reduce the dose to 600 mg twice a day for the first time and to 400 mg twice a day for the second time. If 400 mg is not tolerated, the drug should be permanently discontinued.
Specific adjustments are based on the severity of neutropenia, thrombocytopenia, anemia, etc. (for example, grade 3 and above require suspension or reduction).
2. Drug interaction adjustment :
Avoid the combined use of strong/moderate CYP3A inhibitors (if combined use is necessary, reduce the dose by half).
Avoid combined use of strong/moderate CYP3A inducers.
1. Effect of diet : High-fat diet does not affect absorption, and there is no need to take it on an empty stomach or after a meal.
2. Missed dose/vomiting : If you miss a dose or vomit after taking the medicine, there is no need to take a supplementary dose. Take the next dose according to the original plan.
1. Pregnant women : There is a risk to the fetus and effective contraception is required (for women during treatment and 6 months after stopping the drug, for men 3 months after stopping the drug).
2. Lactation : Breastfeeding is prohibited during treatment and within 1 week after the last dose.
3. Children : Safety for children under 16 years old has not been established.
4. Liver and renal insufficiency : no adjustment is needed for mild to moderate liver damage; no data for severe liver damage (total bilirubin >3 times ULN).
1. Common reactions of epithelioid sarcoma (≥20%): pain, fatigue, nausea, decreased appetite, vomiting, constipation.
2. Common reactions of follicular lymphoma (≥20%): fatigue, upper respiratory tract infection, musculoskeletal pain, nausea, and abdominal pain.
3. Serious risks : secondary malignant tumors (such as leukemia), embryotoxicity.
There are no clear contraindications.
1. CYP3A inhibitor/inducer : significantly affects blood drug concentration (see dose adjustment for details).
2. CYP3A substrate drug (such as hormonal contraceptives): may reduce its efficacy, so you need to switch to non-hormonal contraceptives.
If it is not clearly stated, it is recommended to refer to the package label for dry storage at room temperature.