Cerivastatin (sodium salt)

Cerivastatin is an inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (K_i = 1.3 nM).^1,2 It inhibits cholesterol synthesis in and growth of human arterial myocytes (IC₅₀s = 0.4 and 4.6 nM, respectively).¹ Cerivastatin inhibits proliferation of rat aorta smooth muscle cells and reduces fibrinogen-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).² 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.³

WARNING This product is not for human or veterinary use.

1. Corsini, A., Arnaboldi, L., Raiteri, M., et al. Effect of the new HMG-CoA reductase inhibitor cerivastatin (BAY W 6228) on migration, proliferation and cholesterol synthesis in arterial myocytes. Pharmacol. Res. 33(1), 55-61 (1996).

2. Bischoff, H., Angerbauer, R., Bender, J., et al. Cerivastatin: Pharmacology of a novel synthetic and highly active HMG-CoA reductase inhibitor. Atherosclerosis 135(1), 119-130 (1997).

3. Shiomi, M., and Ito, T. Effect of cerivastatin sodium, a new inhibitor of HMG-CoA reductase, on plasma lipid levels, progression of atherosclerosis, and the lesional composition in the plaques of WHHL rabbits. Br. J. Pharmacol. 126(4), 961-968 (1999).