Cerivastatin is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (Ki = 1.3 nM). It inhibits cholesterol synthesis in and growth of human arterial myocytes (IC50s = 0.4 and 4.6 nM, respectively). Cerivastatin inhibits proliferation of rat aorta smooth muscle cells and reduces fibrogen-induced migration of rat aortic myocytes in a concentration-dependent manner. In vivo, cerivastatin inhibits cholesterol biosynthesis in rats and dogs (ED50 = 0.002 mg/kg for both). It reduces serum levels of cholesterol, triglycerides, and low-density lipoprotein (LDL) in dogs in a dose-dependent manner. Cerivastatin (0.1 mg/kg) decreases cholesterol ester accumulation in arterial tissue of rabbits fed a 0.2% cholesterol diet. It also stabilizes plaques and delays progression into atherosclerotic disease in LDL-receptor deficient rabbits with hypercholesterolemia.