AbstractSeveral of a series of linoleic acid amides have been reported to inhibit cholesterol‐induced atherosclerosis in rabbits. The three amides which have been studied to the greatest extent are (in order of increasing activity) N‐cyclohexyl linoleamide (AC23), N(α methylbenzyl) linoleamide (AC223), and N[α‐phenyl‐β‐(p‐tolyl) ethyl] linoleamide (AC485). We have found AC223 to inhibit cholesterol absorption in rats and to slightly inhibit exogenous but not endogenous cholesteremia in rabbits. In a fiber‐free diet, AC223 reduces serum cholesterol and liver triglyceride levels. Rats were also fed a basal semipurified diet with and without AC223. Fecal excretion of labeled exogenous (as [14C] cholesterol) or endogenous (as [14C] mevalonolactone) steroid was 44 and 43% higher in drug treated groups. The mechanism of hypocholesteremic action of the linoleamides appears to involve inhibition of cholesterol absorption.