Which medications in the drug class Sphingosine 1-Phosphate Receptor Modulators are used in the treatment of Multiple Sclerosis?

Updated: Oct 08, 2019
  • Author: Christopher Luzzio, MD; Chief Editor: Jasvinder Chawla, MD, MBA  more...
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Answer

Sphingosine 1-Phosphate Receptor Modulators

Sphingosine-1-phosphate (S1P) receptor modulators bind with high affinity to S1P receptors 1 and 5. This action blocks lymphocytes to egress from lymph nodes, therefore reducing the number of lymphocytes in peripheral blood. The precise mechanism by which SP1 receptor modulators exert therapeutic effects in MS is unknown, but may involve reduction of lymphocyte migration into the central nervous system.

Siponimod (Mayzent)

Siponimod is indicated for treatment of adults with relapsing forms of MS, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease. The dose requires a brief upward titration to mitigate decreased HR associated with initial dosing. Titration and maintenance dose regimens are determined by CYP2C9 genotype.

Fingolimod (Gilenya)

Fingolimod is the first oral therapy for relapsing forms of MS approved by the FDA. Like other disease-modifying drugs (DMDs) for MS, fingolimod can reduce the frequency of clinical exacerbations and delay the accumulation of physical disability. The recommended dosage for fingolimod is 0.5 mg once a day.

The mechanism by which fingolimod exerts therapeutic effects in MS is unknown, but it appears to be fundamentally different from that of other MS medications. Its activity may involve a reduction of lymphocyte migration into the central nervous system.


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