Abstract: The present invention is directed to a method of inhibiting cholesterol transport through the intestinal lumen of a subject. The method comprises administering an intestinal alkaline phosphatase inhibitor to the subject. The inhibition of intestinal alkaline phosphatase prevents transport of exogenous cholesterol through the intestinal lumen and therefore decreases plasma levels of cholesterol. The invention further provides a method of screening for agents which inhibit cholesterol transport. This method comprises expressing intestinal alkaline phosphatase in a host cell, exposing the host cell to an agent and cholesterol, and determining whether the cholesterol is transported into the host cell. Since intestinal alkaline phosphatase mediates cholesterol transport into the cell, an agent that inhibits the expressed intestinal alkaline phosphatase (or inhibits the expression of intestinal alkaline phosphatase), will inhibit cholesterol transport.