What is tazemetostat?

Tazemetostat is indicated for the treatment of adults and pediatric patients 16 years of age and older with metastatic or locally advanced epithelioid sarcoma who are not candidates for complete resection. It is also indicated for the treatment of adult patients with relapsed or refractory follicular lymphoma whose tumors are positive for IZH2 mutations and who have received at least 2 prior systemic therapies. Additionally, it is indicated for adult patients with relapsed or refractory follicular lymphoma who have no satisfactory alternative treatment options.

Tazerestat inhibitsEZH2, and the SWItch/SNF complex can antagonize the role of PRC2 in the regulation of certain gene expressions in patients with epithelioid sarcoma. Preclinical in vitro and in vivo models with deletion or dysfunction of certain SWI/SNF complex members (e.g., integrase interacting factor 1 [INI1/SNF5/SMARCB1/BAF47], SMARCA4, and SMARCA2) can lead to aberrant EZH2 activity or expression and result in oncogenic dependence on EZH2. Tazetostat is a methyltransferase inhibitor that prevents hypertrimethylation of histones and inhibits cancer cell dedifferentiation. Tazerestat requires twice daily dosing, has a long duration of action, and physicians should inform patients of the risk of secondary malignancies and embryo-fetal toxicity.

The original drug of tazerestat is not yet available in the domestic market and is therefore not included in medical insurance. Tazerestat US version of the original drug, specification200mg*240 tablets, which is marketed overseas, may cost around 200,000 yuan per bottle (the price may fluctuate due to exchange rates), which is very expensive. At present, there are no generic drugs of tazerestat produced and launched. For more drug information and specific prices, please consult the medical consultant of the drug.