Atherosclerotic cardiovascular disease remains the leading cause of morbidity and mortality in Western societies. A hallmark of the developing atherosclerotic lesion is the appearance of cholesterol-laden macrophages in the artery wall. A cell membrane transporter called ABCA1 mediates the removal of excess cholesterol from macrophages into the lipoprotein pathway. This makes ABCA1 a promising new therapeutic target for reducing cholesterol deposits in tissues, eliminating excess cholesterol from the body, and preventing cardiovascular disease.