Reverse cholesterol transport identifies a series of metabolic events
resulting in the transport of excess cholesterol from peripheral tissu
es to the liver. High-density lipoproteins (HDL) are the vehicle of ch
olesterol in this reverse transport, a function believed to explain th
e inverse correlation between plasma HDL levels and atherosclerosis. A
n attempt to stimulate, by the use of drugs, this transport process ma
y hold promise in the prevention and treatment of arterial disease. Am
ong the agents affecting lipoprotein metabolism, only probucol exerts
significant effects on reverse cholesterol transport, by stimulating t
he activity of the cholesteryl ester transfer protein and, consequentl
y, altering HDL subfraction composition/distribution. Another approach
to the stimulation of reverse cholesterol transport consists of raisi
ng plasma HDL levels; studies in animals, either by exogenous suppleme
ntation or by endogenous overexpression, have shown a consistent benef
it in terms of atherosclerosis regression and/or non-progression. Thus
, it is time to consider different future treatments of atherosclerosi
s, combining the classical lipid-lowering treatments with innovative m
ethods to promote cholesterol removal from the arterial wall.