Fingolimod was the first approved oral therapy for multiple sclerosis.
Fingolimod FTY720) is the prodrug of a S1P receptor agonist [4
]. When fingolimod binds to S1P1
R the complex is internalised and then degraded, so the drug acts as an indirect functional antagonist by preventing intracellular signalling. It acts as a lymphocyte migration inhibitor, promoting lymphocyte retention in lymphoid tissues, whilst preserving lymphocyte function [7
]. Clinical efficacy results from modulation of S1P1
receptors. Adverse effects are thought to be caused by fingolimod's off-target effects on other S1P receptor subtypes.
R agonists are being developed and investigated for immunomodulatory/immunosuppresant potential.
View more information in the IUPHAR Pharmacology Education Project: fingolimod