他泽司他用药效果如何？

On January 23, 2020, the FDA approved Epizyme's new drug Tazverik (Tazemetostat) for the first time through the accelerated approval process for the treatment of metastatic or locally advanced epithelioid sarcoma in adults and adolescent patients aged 16 years and above. It is suitable for patients who cannot completely remove the tumor through surgery. It is an oral cofactor S-adenosyl-L-methionine (SAM) competitive EZH2 inhibitor that blocks EZH2 to prevent the methylation of histone H3K27 and reduces the growth of cancer cells with EZH2 mutations or overexpression. It is a new treatment option. So, how effective is tazerestat?

Effects of using tazetostat

Ribrag et al. reported a phase I study of tazemetostat (NCT01897571), studying the safety and activity of tazemetostat in patients with relapsed or refractory non-Hodgkin lymphoma (NHL), including diffuse large B-cell lymphoma (DLBCL), follicular lymphoma (FL) and marginal zone lymphoma (MZL) [1].

The specific administration method is oral administration of tazemetostat, twice a day. The experiment designed a total of 5 dose groups (100 mg, n = 6; 200 mg, n = 3; 400 mg, n = 3; 800 mg, n = 14; 1600 mg, n = 12) and a food-influenced group (400 mg, n = 7). Tumor response assessments were performed every 8 weeks. Among the 26 patients with solid tumors for whom reported results have been obtained, the incidence of adverse reactions was greater than 10%, including fatigue, loss of appetite, constipation, nausea, indigestion, vomiting and muscle cramps. It was also accompanied by 5 adverse reactions of grade 3 or above, including thrombocytopenia, neutropenia, hypertension, anorexia and elevated transaminases.

Among 15 evaluable NHL patients, 5 DL-BCL, 3 FL, and 1 MZL had objective responses, and most of the cases with objective responses were treated at a dose of 800 mg/d (bid). The study results indicate that tazemetostat is a relatively safe drug that can be administered long-term to patients, including those with wild-type EZH2 or mutant DLBCL.

References

[1] An Pengjiao, Yang Liping. Epigenetic drug for the treatment of epithelioid sarcoma and follicular lymphoma - Tazemetostat [J]. Journal of Clinical Drug Therapy, 2021, 19(02): 17-22.

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