The 12-month, double-blind TRANSFORMS study compared two dose regimens of oral fingolimod (0.5 and 1.25 mg/day) with intramuscular (i.m.) interferon beta-1a (IFN-beta-1a) administered once weekly at dosage of 30 microg in a study population of 1292 patients with relapsing remitting multiple sclerosis. Both doses of fingolimod were shown to be superior to i.m. IFN-beta-1a in reducing relapse rate and disease activity as detected by magnetic resonance imaging, while no significant effect on disability progression was observed. Although about 90% of patients completed the study, a greater proportion receiving a higher dose of fingolimod discontinued treatment because of adverse events, such as herpes virus infections (fatal in two patients assigned to higher dose), dose-dependent bradyarrhytmias and lymphopenia, transient macular edema, skin cancer and liver enzyme increase. Because of these safety concerns, a long-term evaluation is required to define the risk-benefit ratio. The TRANSFORMS study clearly showed a superior efficacy of oral fingolimod over i.m. IFN-beta-1a, but it is still uncertain whether oral fingolimod could be used as first-line treatment, or as an alternative treatment for patients who have failed immunomodulating therapy.