receptors, is the first oral disease-modifying agent to be approved by the US FDA for the treatment of relapsing forms of multiple sclerosis (MS). Compared with other disease-modifying agents, fingolimod is unique in its mechanisms of action: it sequesters lymphocytes into lymph nodes without directly inhibiting effector functions, and it exerts pleiotropic actions on cultured oligodendrocytes and oligodendrocyte progenitors. Whether the latter contributes to the favorable response to this drug is currently being investigated. Results from Phase II and III clinical trials demonstrate that fingolimod is highly effective in relapsing-remitting MS. In this article, we review the background on MS therapy, the mechanisms and pharmacology of fingolimod and its benefit-risk profile as a novel therapy in MS.