Aggressive therapy with statins to lower the low density lipoprotein cholesterol decreases cardiovascular events. Nevertheless, administration of the highest approved statin dose only offers limited additional benefit at the expense of an increased incidence of side effects. Therefore, novel compounds that further reduce the low-density lipoprotein cholesterol and at the same time have beneficial effects on other lipid parameters when added to statin therapy are under investigation. Nicotinic acid lowers the levels of the low-density lipoprotein cholesterol and triglycerides while raising the concentration of the protective high-density lipoprotein cholesterol.

A significant inverse association exists between long-term intake of omega-3 fatty acids and cardiovascular mortality; these fish oils lower serum triglycerides levels. Fibrates substantially decrease triglycerides, increase high density lipoprotein cholesterol, and modestly decrease low-density lipoprotein cholesterol levels.

Ezetimibe selectively inhibits cholesterol absorption in the gut. Combined therapy with ezetimibe and a statin provides an incremental reduction in the low-density lipoprotein cholesterol levels.