Background: Multiple sclerosis (MS) is the most common inflammatory demyelinating disease of the CNS. There is a large unmet need for new disease-modifying therapies with improved convenience, safety and efficacy. Fingolimod is an oral sphingosine-1-phosphase (S1P) receptor modulator under clinical investigation for the treatment of relapsing-remitting and primary progressive MS.

Methods: This review provides an update on the mechanism of action, pharmacological properties and efficacy and safety of fingolimod in patients with relapsing MS, with a particular emphasis on clinical trials.

Results: The reader will gain a comprehensive overview of the mechanism of action of fingolimod, particularly how the drug inhibits lymphocyte egress from secondary lymphoid organs by modulation of S1P receptors, and its pharmacokinetic and pharmacodynamic properties. Results from Phase II studies and pivotal Phase III trials of fingolimod for relapsing MS are discussed in depth.

Conclusions: Randomized clinical trials have demonstrated the superior efficacy of fingolimod in reducing relapse rates and MRI measures of disease activity, as compared with placebo and intramuscular IFN-beta-1a. Fingolimod also lowered the risk of disability progression compared with placebo. Adverse events included bradycardia and atrioventricular block, respiratory and herpesvirus infections, increased liver enzyme levels, hypertension and macular edema. Fingolimod 0.5 mg seems to provide the best risk-benefit ratio.