In the past decade, high-density lipoproteins (HDL) have emerged as a new potential therapeutic target for the treatment of cardiovascular disease. The key role of HDL as a carrier of excess cellular cholesterol in the reverse cholesterol transport pathway is believed to provide protection against atherosclerosis. In reverse cholesterol transport, peripheral tissues (e.g., vessel-wall macrophages) remove their excess cholesterol through the ATP-binding cassette transporter 1 (ABCA1) to poorly lipidated apolipoprotein A-I, forming pre-β-HDL. Lecithin–cholesterol acyltransferase then esterifies free cholesterol to cholesteryl esters, converting pre-β-HDL to mature spherical α-HDL (see Figure).

HDL cholesterol is transported to the liver by two pathways: . . .