Although HDL cholesterol is believed to have a protective effect against atherosclerosis by promoting reverse cholesterol transport and potentially through anti-inflammatory, anti-oxidative, antithrombotic and nitric oxide effects, HDL cholesterol remains a complex therapeutic target. New therapeutic strategies are currently being developed not only to increase plasma HDL levels but also to improve its function. Among them, niacin is the most effective agent currently available as it can increase HDL cholesterol by up to 35%. However, at the moment, use of niacin is limited by its tolerability. Inhibitors of cholesteryl ester transfer protein raise plasma HDL cholesterol levels substantially although the overall effect on atherosclerotic cardiovascular disease remains unknown and one agent of this new class has the adverse effect of increasing blood pressure. Apolipoprotein A-I upregulators and mimetic peptides may enhance HDL function without necessarily increasing plasma HDL cholesterol levels. Other alternatives are being examined to enhance macrophage reverse cholesterol transport with liver X receptor agonists. Thus, several approaches to increase plasma HDL levels or HDL function are being developed and may be useful alone or combined with available therapy to prevent and treat cardiovascular disease.
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