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Drug intelligence / Profile preview
valemetostat
- Development stage
- Phase 2
- Lead developer
- Daiichi Sankyo
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Valemetostat is a first-in-class, orally available, selective small molecule dual inhibitor of the histone lysine methyltransferases enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2). By inhibiting both wild-type and mutated forms of EZH1 and EZH2, valemetostat counteracts epigenetic dysregulation implicated in certain hematologic malignancies. It is primarily developed for the treatment of relapsed or refractory adult T-cell leukemia/lymphoma (ATL) and peripheral T-cell lymphoma (PTCL), with additional clinical development in B-cell lymphomas, non-small cell lung cancer, small cell lung cancer, and solid tumors. Valemetostat has received orphan drug designation for ATL and PTCL[3][4][5][6].
- Brand names
- Ezharmia
- Other names
- valemetostat tosylatevalemetostat tosilateEzh1/2 inhibitor ds-3201
02
Targets
EZH1EZH2 (Histone-lysine N-methyltransferase EZH2)
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