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Fluvastatin is an inhibitor of HMG-CoA reductase (Ki = 0.3 nM for the rat enzyme) that binds to the HMG-CoA binding site.1,2 It also inhibits the human cytochrome P450 (CYP) isoform CYP2C9 (IC50 = 100 nM).3 Fluvastatin (2 mg/kg per day) inhibits increases in serum cholesterol, triglycerides, phospholipids, and thiobarbituric acid-reactive substances (TBARS) levels, as well as vascular angiotensin converting enzyme (ACE) activity in rabbits fed a high-cholesterol diet.4 It increases survival in a mouse model of myocardial infarction when administered at a dose of 10 mg/kg per day.5 Formulations containing fluvastatin have been used in the treatment of hypercholesterolemia and the prevention of cardiovascular disease.

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