Lodazecar is a benzodiazepine derivative, which does not bind to the brain benzodiazepine receptor. The drug shares some similarity in tertiary structure with the cholesterol molecule. Oral administration of lodazecar in the cholesterol-fed rat is associated with significant changes in plasma lipoproteins and in key enzymes controlling hepatic cholesterol metabolism. In human the treatment reduced both the fractional and the absolute cholesterol absorption and increased fecal neutral sterol excretion by about 50%, serum plant sterol levels were reduced, most probably because of diminished sterol absorption. Biliary cholesterol secretion was unchanged.