Lipid abnormalities are central among the risk factors for the development of cardiovascular disease and their correction remains a major target for the medical community. Inhibitors of 3-hydroxy-3-methyl glutaryl coenzyme A reductase (statins) are the most widely prescribed and best tolerated of the currently available lipid-modifying therapies. Newer agents in this class (e.g., rosuvastatin) have proven to be more effective at lowering levels of low-density lipoprotein cholesterol. New formulations of drugs such as nicotinic acid, which improve treatment regimens and reduce unpleasant side effects, may result in improved patient compliance with this therapy. The development of novel drugs such as cholesterol absorption inhibitors (e.g., ezetimibe) and acyl-coenzyme A cholesterol acyltransferase inhibitors (e.g., avasimibe) will provide clinicians with therapeutic options that exploit different pathways to those currently being utilised. By combining these agents with statins, greater improvements in the lipid profile than those seen to date could be produced. In addition, advances in our understanding of the pathophysiology of dyslipidaemia have enabled other novel therapeutic targets to be identified and studies with experimental drugs underscore the potential of these approaches.