Because of their excellent tolerability and their positive impact on lipid parameters, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) have become the drugs of first choice for many patients with dyslipidemia. Rosuvastatin is an investigational statin in the U.S. with a number of favorable characteristics, which include low lipophilicity, high hepatocyte selectivity, minimal metabolism, and a low propensity for cytochrome P450 drug interactions. Rosuvastatin has been studied at doses ranging from 1 to 80 mg. In comparative clinical trials, rosuvastatin given at 5 to 10 mg/day reduced low-density lipoprotein cholesterol to a significantly greater extent than atorvastatin 10 mg/day, pravastatin 20 mg/day, and simvastatin 20 mg/day. In addition, rosuvastatin exhibited beneficial effects on other lipid parameters such as high-density lipoprotein cholesterol and triglycerides. Rosuvastatin's safety profile was demonstrated to be similar to those of other statins. Given its favorable pharmacokinetic and pharmacodynamic characteristics, rosuvastatin is likely to become a valuable addition to the statin drug class. The author reviews the pharmacologic and pharmacokinetic properties of this new statin.