別名

Diethyl-[6-(4-hydroxycarbamoyl-phenyl carbamoyloxymethyl)-naphthalen-2-yl methyl]-ammonium chloride,ITF2357,N-[4-[(Hydroxyamino)carbonyl]phenyl]-carbamic acid, [6-[(diethylamino)methyl]-2-naphthalenyl]methyl ester hydrochloride

應(yīng)用

Givinostat hydrochloride hydrate has been used as a histone deacetylase inhibitor to test its effect on the human immunodeficiency virus reactivation in CD4+ T-cell model.

生化/生理作用

Givinostat (ITF2357) is a hydroxamate HDAC inhibitor that inhibits class I and class II enzymes. Givinostat posseses a very promising activity profile in multiple myeloma and acute myelogenous leukemia in vitro and in vivo. Givinostat also has anti-inflammatory activity and inhibits the secretion of the tumor necrosis factor-alpha (TNF-α), IL-1, and IL-6. Givinostat has been in multiple Phase 2 studies for both inflammatory diseases (Duchenne Muscular Dystrophy , Juvenile arthritis, Polycythemia Vera) and blood cancers (myelomas and lymphomas). Givinostat is known to mediate the reduction of the human immunodeficiency virus release in macrophages.