Statins, super-statins and cholesterol absorption inhibitors.

An elevated level of low-density lipoprotein cholesterol (LDL-C) is an independent risk factor for premature coronary heart disease (CHD), with a value of > or = 160 mg/dl designated as high-risk by the National Cholesterol Education Program Adult Treatment Panels I, II and III. Current goals of therapy for all patients with elevated LDL-C include reducing levels to: (i) < 160 mg/dl in those with < or = 1 CHD risk factor; (ii) < 130 mg/dl in those with more than or equal to 2 CHD risk factors; and (iii) < 100 mg/dl in patients with established CHD or CHD risk equivalents, one of which is diabetes. The discovery of drugs that inhibit 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMGCR), the rate-limiting enzyme in cholesterol biosynthesis, constituted a major advance in the treatment of patients with elevated plasma concentrations of LDL-C. The efficacy of statins in LDL-lowering and CHD risk reduction has clearly been demonstrated in a number of primary and secondary intervention trials. Emerging options for the treatment of patients with elevated LDL-C include the super-statins rosuvastatin and pitavastatin, as well as the cholesterol absorption inhibitor ezetimibe. This article reviews large-scale clinical trials in which statins have been used to reduce LDL-C concentrations. Studies that have examined the efficacy and safety of rosuvastatin, pitavastatin and ezetimibe will also be discussed.