Drug Discoveries & Therapeutics
Online ISSN : 1881-784X
Print ISSN : 1881-7831
ISSN-L : 1881-7831
Valemetostat: First approval as a dual inhibitor of EZH1/2 to treat adult T-cell leukemia/lymphoma
Fangzhou DouZhenxue TianXu YangJing LiRuquan WangJianjun Gao
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2022 Volume 16 Issue 6 Pages 297-299


Adult T-cell leukemia/lymphoma (ATL) is a mature T-cell lymphoma with a poor prognosis. Accumulating trimethylation of histone H3 lysine 27 (H3K27me3) caused by upregulated function of either enhancer of zeste homologue 2 (EZH2) or its homolog EZH1 plays an essential role in the maintenance of transcriptional repression in ATL. Selective inhibition of EZH2 may complementarily induce EZH1 activation, so dual targeting EZH1/2 is a rational strategy in developing potent antitumor agents. Valemetostat is the first dual EZH1/2 inhibitor approved for treatment of aggressive ATL in Japan in September 2022. Several other dual EZH1/2 inhibitors such as HH2853, HM97594, and HM97662 have also demonstrated potential in treating malignant tumors. Dual targeting EZH1/2 may have promising antitumor action in hematological malignancies and solid tumors.

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