This paper presents a summary of the current knowledge of the mechanism of action of fingolimod (FTY720; Gilenya®; Novartis Pharma Stein AG, Stein, Switzerland) and the phase 2 and 3 studies that have been performed on the drug. This study will discuss specific safety issues that should be considered when initiating this therapy. Multiple sclerosis (MS), an inflammatory disease of the central nervous system, is considered to be a leading cause of neurologic disability in young adults, and predominantly affects young women. The past two decades have seen significant growth in therapeutic options for relapsing forms of MS, including FTY720. Fingolimod (FTY720) is a sphingosine-1-phosphate receptor modulator, and currently the approved dosage is 0.5 mg daily. Notable side effects include bradycardia in the first hours after administration and macular edema. There may be an increased risk of herpetic infections (varicella zoster virus and herpes simplex virus) associated with this medication. This oral therapy has been shown to be effective in double-blind, placebo-controlled studies, and in trials comparing it to weekly interferon beta-1a therapy. However, the long-term efficacy and safety of this oral medication in relapsing MS, including the effect on reduction of disability progression and cognitive decline, remains to be established.