Difference between revisions of "Valemetostat (Ezharmia)"
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(Created page with "==Mechanism of action== From the [https://www.cancer.gov/publications/dictionaries/cancer-drug/def/tazemetostat NCI Drug Dictionary]: The tosylate form of valemetostat, an ora...") |
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==History of changes in PMDA indication== | ==History of changes in PMDA indication== | ||
| − | *2022-09-26: Newly indicated for the treatment of relapsed or refractory [[Adult T-cell leukemia-lymphoma|adult T-cell leukemia/lymphoma]]. | + | *2022-09-26: Newly indicated for the treatment of relapsed or refractory [[Adult T-cell leukemia-lymphoma|adult T-cell leukemia/lymphoma]]. ''(Based on DS3201-A-J201)'' |
==Also known as== | ==Also known as== | ||
Latest revision as of 01:31, 13 January 2024
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
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