Mechanism of action of oral fingolimod (FTY720) in multiple sclerosis

J Chun, HP Hartung - Clinical neuropharmacology, 2010 - journals.lww.com
Fingolimod (FTY720) is a first-in-class orally bioavailable compound that has shown efficacy
in advanced clinical trials for the treatment of multiple sclerosis (MS). In vivo, fingolimod is
phosphorylated to form fingolimod-phosphate, which resembles naturally occurring
sphingosine 1-phosphate (S1P), an extracellular lipid mediator whose major effects are
mediated by cognate G protein-coupled receptors. There are at least 5 S1P receptor
subtypes, known as S1P subtypes 1-5 (S1P 1-5), 4 of which bind fingolimod-phosphate …