RVX-028, also known as RVX-000222, is a potent BET bromodomain inhibitor. It_x000D_preferentially binds to the second bromodomain on BET proteins. It also stimulates_x000D_apolipoprotein (APO) AI gene expression, which increases apoA-I and HDL-C in vitro. In vivo,_x000D_RVX-208 enhances cholesterol efflux via different pathways and significantly increases serum_x000D_apoA-I and HDL-C in monkeys.