Abstract: The present invention provides an immunosuppressive agent containing an effective amount of one or more of the macrolide antibiotics of the formula (I): ##STR1## (wherein each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4 is a methyl or ethyl group). The immunisuppressive agent has excellent immuno-suppressive activity and can be employed as an agent for suppressing rejection occurring after organ transplantation and as an agent for treating autoimmune diseases.