S1P receptor modulators

What are S1P receptor modulators?

Some medications used in the treatment of IBD can be classified as receptor modulators. Receptor modulators are chemicals that bind to specific receptors (protein structures) found on the surface or inside cells to regulate their activity and therefore bring about a desired response.

An example of a sphingosine 1-phosphate (S1P) receptor modulator available on the market is ozanimod (Zeposia®).

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Who are S1P receptor modulators used for?

Ozanimod: Oral capsules

Ozanimod (brand name: Zeposia®) is used in the treatment of adults with moderate to severe, active ulcerative colitis who have had an inadequate response, loss of response, or were intolerant to either conventional therapy or a biologic medication.

It is also used to treat people with relapsing remitting multiple sclerosis (RRMS) to decrease the frequency of clinical complications.

Health Canada has not authorized the use of Zeposia® for people younger than 18 years old. 

As for people with colitis at/or greater than 65 years old, a limited number of them enrolled in the clinical trials for this medication. Within the group that participated, Zeposia® was found to be effective only to induce remission. Therefore, Health Canada has not authorized Zeposia® for maintenance therapy for people with ulcerative colitis who are 65 years old or older.

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How do S1P receptor modulators work?

These medications bind to two subtypes of receptors, or proteins, called sphingosine 1-phosphate (S1P). S1P receptors are found on the surface membranes of the immune cells, T cells and B cells. 

The binding action of ozanimod prevents these immune cells from being released in the blood. In turn, this reduces the level of inflammation in people with ulcerative colitis.

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How effective are S1P receptor modulators?

Ozanimod can be used to induce remission in adults with moderately to severely active ulcerative colitis.

Please consult your healthcare provider or IBD specialist for more information.

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Side effects and risks of use

General disclaimer

People with IBD may be advised to get a blood test done to monitor their blood counts prior to taking these medications. This is because the immunosuppressive properties of S1P receptor modulators may decrease your levels of white blood cells (cells that are part of the immune system) and as such, increase your risk of infections.  Your healthcare provider will review your medical history and inform you if you require additional testing. 


The side effects of Zeposia® may include higher levels of the liver enzyme ‘alanine aminotransferase’ (indicating inflammation or damage to liver cells), nasopharyngitis (inflammation of nasal passages and throat) and headache. These side effects are not common and Zeposia® is therefore considered a well tolerated medication.

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