Lipoprotein lipase has long been a desirable target to treat atherosclerosis, but direct-acting activators of the enzyme have failed. Lipigon Pharmaceuticals AB is taking a different tack, developing small molecules that protect the enzyme from inactivation by endogenous inhibitors.

Lipoprotein lipase (LPL) plays a central role in blood lipid metabolism. It hydrolyzes triglycerides - resulting in formation of pre-beta HDL - and delivers free fatty acids to peripheral tissues for use as energy or storage. The enzyme also facilitates receptor-mediated uptake of atherogenic lipoproteins.