What are the effects of Tazemetostat?

The U.S. Food and Drug Administration (FDA) approved the marketing of Tazemetostat in January 2020. Tazemetostat is a first-in-class EZH2 inhibitor. EZH2 plays a role in controlling the biology of germinal B cells. Overexpression or mutations of epigenetic regulators are associated with the malignant transformation of B cell malignancies. Preclinical data have demonstrated the potential synergistic anti-tumor activity of combinations of EZH2 inhibitors with lenalidomide and/or rituximab.

Tazerestat was marketed based on the results of a clinical trial that enrolled 62 subjects with metastatic or locally advanced epithelioid sarcoma. During the clinical trial, subjects received 800 milligrams (mg) of tazerestat twice daily until disease progression or subjects reached unacceptable levels of toxicity, with tumor response assessments performed every eight weeks. The trial measured how many subjects experienced complete or partial shrinkage (some degree) of their tumors during treatment (overall response rate). The study results showed that the overall response rate was 15%, of which 1.6% of subjects had complete remission and 13% of subjects had partial remission. Of the 9 subjects who responded, 6 (67%) had responses lasting 6 months or longer.

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.