Pharmacokinetic evaluation of fingolimod for the treatment of multiple sclerosis.

INTRODUCTION: Fingolimod is a sphingosine 1-phosphate receptor modulator with a novel mechanism of action and the first oral drug approved for the treatment of relapsing forms of multiple sclerosis (MS). Fingolimod reduces relapses more effectively than intramuscular interferon β1a and delays disability progression. Associated safety risks are bradyarrhythmia and atrioventricular block following the initial dose, requiring monitoring. AREAS COVERED: This article examines the characteristics of fingolimod, its pharmacokinetic properties and the efficacy and tolerability in MS. Information on the pharmacology and mechanisms of action is also provided. EXPERT OPINION: Fingolimod is an effective therapy for relapsing forms of MS in a convenient oral dose. Fingolimod may target not only inflammation but potentially also neurodegeneration. Antagonizing astrocyte sphingosine signaling may help explain the reduction in cerebral atrophy observed in Phase III trials. Long-term data about the safety of fingolimod are needed.