The immunomodulatory drug fingolimod (FTY720, GilenyaR) was approved for oral treatmentof relapsing-remitting multiple sclerosis, due to its impressive efficacy and good tolerability.Pharmacologically, it acts as an unselective agonist of sphingosine 1-phosphate receptors(S1PR) and as a selective functional antagonist of the S1P1 subtype by induction of receptordownregulation. Since S1P1 is crucial for the regulation of lymphocyte trafficking, itsdownregulation causes redistribution of the immune cells to secondary lymphoid tissues,resulting in the depletion from the circulation and hence immunosuppression. Numerouspreclinical studies have since been performed with the aim to increase the spectrum ofpotential indications for fingolimod with emphasis on other autoimmune disorders and