The present invention intends to provide a derivative of sphingosine analogue that is able to regulate the functions of sphigolipid, and its pharmaceutical compositions. The present invention is the derivatives of sphingosine analogues represented by the general formula (I) described below. ##STR1## In the formula, R.sup.1 and R.sup.2, which are the same or different each other, are hydrogen, alkyl groups having 1-4 carbon atoms, or acyl groups having 2-5 carbon atoms. R.sup.3 and R.sup.4, which are the same or different each other, are hydrogen or hydroxyl groups; or R.sup.3 and R.sup.4 make up a covalent bond. X.sup.1 is --(CH.sub.2).sub.n --CO--NH--CH(R.sup.5)--R.sup.6 or --(CH.sub.2).sub.m --O--CO--CH(R.sup.7)--R.sup.8.