The launch of ezetimibe, a novel cholesterol absorption inhibitor in 2003 may well herald the dawn of combination therapy in the management of dyslipidaemia. The recent identification of NPC 1L1 as the probable specific sterol permease involved in intestinal cholesterol absorption is an important breakthrough in the understanding of the mechanisms of cholesterol absorption. Combination of statin therapy with blockade of exogenous cholesterol absorption (the so called dual inhibition of cholesterol metabolism) is discussed together with the potential for tailoring therapy to the physiological profile of patients' cholesterol metabolism.
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