For extending the uses of a compound represented by Chemical formula 1, the object of the present invention is to provide a derivative of cyclic tetrasaccharide whose physicochemical properties are changed from those of cyclic tetrasaccaride, a composition comprising the same, and a process for producing the same. The present invention solves the above object by providing a derivative of cyclic tetrasaccharide, which is produced by the steps of reacting a compound represented by Chemical formula 1 with a reactive reagent and substituting one ore more hydroxyl groups with substituents except hydroxyl group and O-glycosyl group; a composition comprising the same; and a process for producing the derivative of cyclic tetrasaccharide. ##STR00001##