Nicodicosapent is a fatty acid niacin conjugate. It is also an inhibitor of the sterol regulatory element-binding protein (SREBP). The sterol regulatory element-binding protein (SREBP) is a key regulator of cholesterol metabolism proteins such as PCSK9, HMG-CoA reductase, ATP citrate lyase, and NPC1L1.

Nicodicosapent obviously suppresses ApoB secretion in a dose-dependent manner (IC50: 27 μM). Nicodicosapent displays a synergistic inhibition on secreted PCSK9 ( IC50: 17 μM). Nicodicosapent reduces the production of mature SREBP-2 protein in HepG2 cells but does not interact with the GPR109A receptor. Nicodicosapent causes time-dependent hydrolysis in HepG2 cells.

Nicodicosapent (100 mg/kg p.o.) produces high plasma levels of nicotinic acid in the plasma. ApoE*3-Leiden mice treated with Nicodicosapent display an obvious reduction in PCSK9 levels, LDL particles including VLDL and LDL cholesterol, and plasma triglycerides.