Tazemetostat Storage
Store at ≤30°C.
Mechanism of Action of Tazemetostat
(1) Tazemetostat is a potent and selective inhibitor of EZH2, including EZH2 with activating mutations such as Y646X, A682G, or A692V.
(2) EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2), which is responsible for promoting transcriptional silencing of target genes.
(3) In vitro and in vivo, loss or dysfunction of the chromatin remodeling complex SWI/SNF leads to aberrant EZH2 activity and confers dependence on EZH2 enzymatic activity in oncogenesis.
(4) In vivo, antitumor activity was shown in B‑cell lymphoma xenograft models with or without activating EZH2 mutations; stronger inhibitory effects were observed in lymphoma cell lines harboring EZH2 mutations.
(5) The half‑maximal inhibitory concentration (IC50) required to inhibit EZH1 is approximately 36 times that required to inhibit EZH2.
Important Safety Information
1. Risk of secondary malignancies
If you experience fatigue, easy bruising, fever, bone pain, or pallor, you should inform your doctor.
2. Fetal harm risk
(1) Females of reproductive potential should use effective non‑hormonal contraception during treatment with Tazemetostat and for 6 months after the last dose.
(2) Males receiving this drug should use effective contraception during treatment and for at least 3 months after the last dose.
(3) Female patients should inform their doctor if they are pregnant or plan to become pregnant.
(4) If a patient becomes pregnant while using this drug, or if a patient's partner becomes pregnant, the potential hazard to the fetus should be communicated.
3. Breastfeeding should be avoided during treatment and for one week after the last dose.
4. It is important to inform your doctor of all concomitant treatments you are taking or planning to take, including prescription drugs, over‑the‑counter medications, and dietary or herbal supplements (e.g., St. John's wort), as well as any concomitant diseases.
