Xenalipin (4’-trifluoromethyl-2-biphenyl carboxylic acid) is a chemical compound which has been found to be an effective hypolipidemic agent in animal models. Significant reductions in serum cholesterol and triglycerides were observed in cholesterol-cholic acid-fed rats following oral doses of Xenalipin. Xenalipin was considerably more potent than clofibrate, nicotinic acid, and cholestyramine in the same model. Lipoprotein analysis showed that xenalipin reduced cholesterol and protein content in very low-density lipoprotein (VLDL), intermediate density lipoprotein (IDL), and low-density lipoprotein (LDL). Triglycerides were reduced in very low-density lipoprotein and intermediate density lipoprotein. Xenalipin was also effective in reducing serum cholesterol and triglyceride concentrations in normocholesterolemic rats. In diet-induced hypercholesterolemic African green monkeys, xenalipin reduced serum LDL-cholesterol concentrations. Xenalipin has a profile of activity which would be beneficial in therapy for hyperlipidemia.