他泽司他(Tazemetostat)美国获批治疗上皮样肉瘤(ES)

Epithelioid sarcoma (ES) is a clinically rare and extremely aggressive soft tissue sarcoma, accounting for approximately 1% of all soft tissue sarcomas. The first clinical case of ES was reported in 1970. Clinically, it is divided into "distal type" and "proximal type" according to the site of onset. On January 23, 2020, Epizyme announced that the FDA has accelerated the approval of Tazverik (tazemetostat) for the treatment of adult and pediatric patients 16 years and older with metastatic/locally advanced epithelioid sarcoma who are not suitable for complete resection.

Tazerestat is an inhibitor of histone methyltransferase (EZH2). If EZH2 is mutated or abnormally activated and overexpressed, it will lead to the disorder of genes that control cell proliferation, inhibit the transcriptional activity of tumor suppressor genes, and cause the rapid growth of various solid tumor cells. Tazetostat can inhibit the methylation of histone H3 lysine 27 (H3K27) and restore the expression of tumor suppressor genes.

The first phase I/II clinical trial of tazetostat for the treatment of advanced malignant tumors in humans (NCTO1897571) was officially launched in July 2013, aiming to initially evaluate the safety and effectiveness of tazetostat. ITALIANO et al. reported the results of the phased study of NCTO1897571. The study included 64 patients with malignant tumors (including 3 ES patients), of which 63 (98%) had disease progression after receiving relevant treatment (median third-line treatment). Among 3 ES patients who received Taz treatment, 2 (67%) patients with INI1 functional protein loss achieved durable (>20 months) stable disease (SD), while among 30 patients with solid tumors who had other clinical benefits, only 1 (3%) had SD>11 months.

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