Cardiovascular diseases due to atherosclerosis are the leading causes of mortality in the Western world. Cholesterol-lowering therapy with 3-hydroxy-3-methylglutaryl coenzyme Areductase inhibitors (statins) has demonstrated a reduction in cardiovascular morbidity and mortality in diverse populations. Fluvastatin (Lescol, Novartis Pharmaceuticals) was the first totally synthetic 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor on the market and has recently become available in an extended-release formulation (Lescol XL, Novartis Pharmaceuticals). Data from several clinical outcome trials have shown substantial benefits from fluvastatin treatment in diverse populations. Fluvastatin exists primarily in its acid form and as inactive metabolites in vivo, while active metabolites as well as the lactone form are only present in small amounts. The demonstration of the safe use of fluvastatin in a wide range of patients may be associated with the predominant acid form of the drug in vivo, as well as its predominant metabolism via the cytochrome P450 2C9 pathway.