ly518674

LY-518674 is a highly potent and selective small molecule agonist of peroxisome proliferator-activated receptor alpha (PPARα). It was developed for the treatment of dyslipidemias with atherogenic potential and metabolic syndrome. Compared to existing fibrate drugs such as fenofibrate, LY-518674 demonstrates much greater potency and selectivity for PPARα. In clinical studies, it significantly reduced very low-density lipoprotein cholesterol (VLDL-C) and triglyceride levels by enhancing VLDL clearance through upregulation of lipoprotein lipase activity and downregulation of apolipoprotein C-III. It also increased the production rates of apolipoproteins A-I and A-II but did not change plasma HDL-C levels at tested doses. The drug was initially developed by Ligand Pharmaceuticals.