tazemetostat

Tazemetostat is an oral, small molecule inhibitor of the histone methyltransferase EZH2 (Enhancer of Zeste Homolog 2). It competitively inhibits both wild-type and mutant forms of EZH2 by blocking S-adenosylmethionine (SAM) binding, thereby preventing trimethylation of histone H3 at lysine 27 (H3K27me3). This epigenetic modulation leads to decreased proliferation and survival in cancer cells with EZH2 mutations or overexpression. Tazemetostat was developed by Epizyme and is indicated for the treatment of adults and children aged 16 years or older with metastatic or locally advanced epithelioid sarcoma not eligible for complete resection, as well as adults with relapsed/refractory follicular lymphoma who have received at least two prior systemic therapies or have no alternative treatment options. The drug has been approved in the US, Japan, and other regions for these indications[1][2][3][5].

Brand names

Tazverik

Other names

他泽司他氢溴酸他泽司他tazemetostat hydrobromide