Fingolimod is the first oral treatment of relapsing-remitting mutiple sclerosis. It is the first-in-class sphingosin-1-phosphate (S1P) receptor modulator that binds to sphingosin-1-phosphate receptors on lymphocytes to prevent lymphocyte egress from lymphoid tissues into the circulation via down-regulation of S1P receptor expression.
By this mechanism, the infiltration of autoagressive lymphocytes into the central nervous system is reduced. Two large phase III studies have shown superior efficacy of fingolimod in two dosages compared to placebo and weekly intramuscular injections of interferon beta-1a used as the standard first-line treatment.
Transient bradycardia after starting fingolimod is among possible adverse effects and therefore the pulse rate and blood pressure need to be monitored for 6 hours following the first dose. During treatment, attention should be given to specific ifections, elevated liver enzymes and ophthalmologic changes