Siponimod (BAF-312)

Siponimod is an orally bioavailable agonist of the sphingosine-1-phosphate (S1P) receptor that is selective for S1P1 and S1P5 with EC₅₀ values of 0.39 and 0.98 nM respectively, in a GTPγS-binding assay. Siponimod (0.3 or 3 mg/kg/day mg/kg/day) reduces experimental autoimmune encephalomyelitis (EAE) symptoms in rats. It significantly attenuates demyelination in organotypic cerebellar slice cultures. It is used for the treatment of relapsing forms of multiple sclerosis.