The statins have proved to be some of the most potent therapies for reducing elevated low-density lipoprotein (LDL) cholesterol and lessening the risk of coronary heart disease (CHD) and related events. Nonetheless, there are still questions about the clinical relevance of individual drug characteristics, such as chemical derivation, solubility properties, and metabolic route, in terms of tolerability or therapeutic benefit. At the same time, no clear explanation has emerged for the significantly steeper reductions in LDL cholesterol levels achieved with atorvastatin versus lovastatin, simvastatin, pravastatin, or fluvastatin, or, more recently, with rosuvastatin versus atorvastatin, although possible mechanisms have been suggested. More studies are needed to characterize the effects of statins on high-density lipoprotein (HDL) in different patient groups. Clearly, though, several statins have yielded significant reductions in CHD risk and have shown to be well tolerated in both primary and secondary prevention trials. The possibility that statins exert pronounced effects beyond lowering blood lipids is opening other avenues of research into the benefits of these drugs.