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Updated: Jun 12, 2026
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A Pipeline to Investigate the Structures and Signaling Pathways of Sphingosine 1-Phosphate Receptors
Published on: June 8, 2022
Fingolimod is a potential novel therapy for multiple sclerosis.
Orhan Aktas1, Patrick Küry, Bernd Kieseier
1Department of Neurology, Heinrich-Heine-University of Düsseldorf, 40225 Düsseldorf, Germany.
Nature Reviews. Neurology
|June 17, 2010
Summary
Fingolimod, an oral sphingosine-1-phosphate (S1P) receptor modulator, effectively reduces inflammation in relapsing-remitting multiple sclerosis (MS) by preventing lymphocyte infiltration. This therapy shows promise for treating MS and potentially promoting neural repair.
Area of Science:
- Immunology
- Neurobiology
- Pharmacology
Background:
- Fingolimod (FTY720) is an orally administered sphingosine-1-phosphate (S1P) receptor modulator with significant immunoregulatory effects.
- Phosphorylated fingolimod exhibits high affinity for S1P(1) receptors, modulating lymphocyte function.
Purpose of the Study:
- To review the immunological and neurobiological profile of fingolimod.
- To discuss clinical trial data for fingolimod in relapsing-remitting multiple sclerosis (MS).
- To provide an expert opinion on future S1P receptor modulators for MS therapy.
Main Methods:
- Review of mechanistic studies on fingolimod's action on S1P(1) receptors.
- Analysis of data from Phase III clinical trials (FREEDOMS and TRANSFORMS) in relapsing-remitting MS.
- Inclusion of preclinical study findings on neuroprotective potential.
Main Results:
- Fingolimod inhibits lymphocyte egress from lymph nodes by modulating S1P(1) receptors, thereby reducing CNS inflammatory lesions.
- Phase III trials confirm potent anti-inflammatory effects of fingolimod in relapsing-remitting MS.
- Preclinical data suggest fingolimod may promote in vivo neural repair.
Conclusions:
- Fingolimod represents a significant advancement as an orally available therapy for relapsing-remitting MS.
- Its immunomodulatory mechanism offers potent anti-inflammatory benefits.
- Further research into fingolimod and next-generation S1P receptor modulators holds promise for MS treatment and neural repair.
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