Valemetostat (Ezharmia)

Mechanism of action

From the NCI Drug Dictionary: The tosylate form of valemetostat, an orally available selective inhibitor of the histone lysine methyltransferases enhancer of zeste homolog 1 (EZH1) and 2 (EZH2), with potential antineoplastic activity. Upon oral administration, valemetostat selectively inhibits the activity of both wild-type and mutated forms of EZH1 and EZH2. Inhibition of EZH1/2 specifically prevents the methylation of lysine 27 on histone H3 (H3K27). This decrease in histone methylation alters gene expression patterns associated with cancer pathways, enhances transcription of certain target genes, and results in decreased proliferation of EZH1/2-expressing cancer cells.

Diseases for which it is used

• Adult T-cell leukemia-lymphoma

History of changes in PMDA indication

• 2022-09-26: Newly indicated for the treatment of relapsed or refractory adult T-cell leukemia/lymphoma. (Based on DS3201-A-J201)

Also known as

• Code name: DS-3201b
• Generic names: valemetostat tosilate, valemetostat tosylate
• Brand name: Ezharmia