The functions and efficacy of Tazemetostat

Tazemetostat is the first oral EZH2 inhibitor approved by the U.S. Food and Drug Administration (FDA) for follicular lymphoma (FL) and epithelioid sarcoma (ES) . In follicular lymphoma, EZH2 activity is elevated due to the interaction of mutated EZH2 and WT EZH2 with oncogenes. Tazetostat inhibits mutant andWT EZH2 in follicular lymphoma. In addition, tazemetostat inhibits some EZH2 gain-of-function mutations, including Y646X and A687V. This inhibition suppressed B-cell lymphoma proliferation, with higher activity observed in mutant EZH2.

Most epithelioid sarcomas start in the soft tissue under the skin of the extremities, although it can start elsewhere in the body. When cancer is localized to one area of u200bu200bthe body, surgical removal is considered the primary treatment. Chemotherapy or radiation therapy may also be given. However, even with treatment, the disease has a high potential for local and regional spread, and approximately50% of patients have metastatic disease at diagnosis. On the other hand, epithelioid sarcomas can develop oncogenic dependence on EZH2 through dysfunction of members of the SWI/SNF complex, specifically loss of INI1, SMARCB1, or both. In addition to EZH2 inhibition, tazetostat can also inhibit EZH1 activity and prevent the growth of epithelioid sarcoma cells.

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.