Valemetostat

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Valemetostat
Clinical data
Trade namesEzharmia
Other namesValemetostat tosilate (JAN); DS-3201; DS-3201b
Identifiers
  • (2R)-7-Chloro-2-[4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide
CAS Number
PubChem CID
UNII
KEGG
Chemical and physical data
FormulaC26H34ClN3O4
Molar mass488.03 g·mol−1

Valemetostat (trade name Ezharmia) is a drug used for the treatment of adult T-cell leukemia/lymphoma (ATL).

Valemetostat is an inhibitor of the enzymes enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2), which are implicated in the etiology of some forms of cancer including non-Hodgkin lymphomas.[1][2]

In Japan, valemetostat was approved in September 2022 for patients with relapsed or refractory adult T-cell leukemia/lymphoma.[3][4]

References

  1. ^ Ishitsuka K, Izutsu K, Maruyama D, Makita S, Jacobsen ED, Horwitz S, et al. (2021). "First-In-Human Study of the Ezh1 and Ezh2 Dual Inhibitor Valemetostat Tosylate (Ds-3201B) in Patients with Relapsed or Refractory Non-Hodgkin Lymphomas". Hematological Oncology. 39. doi:10.1002/hon.14_2879. S2CID 237853028.
  2. ^ Morishima S, Ishitsuka K, Izutsu K, Kusumoto S, Makiyama J, Utsunomiya A, et al. (2019). "First-in-Human Study of the EZH1/2 Dual Inhibitor Valemetostat in Relapsed or Refractory Non-Hodgkin Lymphoma (NHL) - Updated Results Focusing on Adult T-Cell Leukemia-Lymphoma (ATL)". Blood. 134: 4025. doi:10.1182/blood-2019-125507. S2CID 209291086.
  3. ^ Dou F, Tian Z, Yang X, Li J, Wang R, Gao J (October 2022). "Valemetostat: First approval as a dual inhibitor of EZH1/2 to treat adult T-cell leukemia/lymphoma". Drug Discoveries & Therapeutics. 16 (6): 297–299. doi:10.5582/ddt.2022.01085. PMID 36310058. S2CID 253189013.
  4. ^ "Japan Green Lights Valemetostat Tosilate for Relapsed/Refractory Adult T-cell Leukemia/Lymphoma". OncLive. September 26, 2022.
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