The effect of Melinamide on the serum lipid and apolipoprotein was studied in the subjects with hypercholesterolemia. The significant decrease of serum cholesterol and phospholipid, and concomitant increase of HDL₂/HDL₃ ratio (p<0.05) were observed after Melinamide administration (2, 250mg/day, 16 weeks). The tendency of decrease in the levels of apo A-IV and B was demonstrated especially in the cases whose cholesterol reduced during therapy. These results suggested the serum apo A-IV might reflect the decrease of the exogenous cholesterol after Melinamide therapy.