Valemetostat Explained

Tradename:	Ezharmia
Synonyms:	Valemetostat tosilate (JAN); DS-3201; DS-3201b
Cas Number:	1809336-39-7
Cas Supplemental:	(tosylate)
Pubchem:	126481870
Unii:	60RD0234VE
Kegg:	D11662
Iupac Name:	(2R)-7-Chloro-2-[4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1''H''-pyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide
C:	26
H:	34
Cl:	1
N:	3
O:	4

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]}

Notes and References

1. 10.1002/hon.14_2879 . First-In-Human Study of the Ezh1 and Ezh2 Dual Inhibitor Valemetostat Tosylate (Ds-3201B) in Patients with Relapsed or Refractory Non-Hodgkin Lymphomas . 2021 . Ishitsuka K, Izutsu K, Maruyama D, Makita S, Jacobsen ED, Horwitz S, Kusumoto S, Allen P, Porcu P, Imaizumi Y, Yamauchi N, Morishima S, Kawamata T, Foss FM, Utsunomiya A, Nosaka K, Serbest G, Kato K, Adachi N, Tsukasaki K, Tobinai K . Hematological Oncology . 39 . 237853028 . free .
2. 10.1182/blood-2019-125507 . 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) . 2019 . Morishima S, Ishitsuka K, Izutsu K, Kusumoto S, Makiyama J, Utsunomiya A, Nosaka K, Ishida T, Imaizumi Y, Yamauchi N, Araki K, Adachi N, Yamashita T, Atsumi R, Tsukasaki K, Tobinai K . Blood . 134 . 4025 . 209291086 . free .
3. Dou F, Tian Z, Yang X, Li J, Wang R, Gao J . Valemetostat: First approval as a dual inhibitor of EZH1/2 to treat adult T-cell leukemia/lymphoma . Drug Discoveries & Therapeutics . October 2022 . 16 . 6 . 297–299 . 36310058 . 10.5582/ddt.2022.01085 . 253189013 . free .
4. Web site: Japan Green Lights Valemetostat Tosilate for Relapsed/Refractory Adult T-cell Leukemia/Lymphoma . September 26, 2022 . OncLive .