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®).
Back to topWho 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.
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.
Etrasimod: Oral tablet
Etrasimod (brand name: Velsipity™) is used in the treatment of people 16 years of age or older with moderate to severe, active ulcerative colitis who have had an inadequate response, lost response, or were intolerant to either conventional therapy or an advanced treatment such as biologics.
Back to topHow 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.
Back to topHow 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.
Back to topSide 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.
Ozanimod
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.
Etrasimod
The side effects of Velsipity
™ may include higher levels of the liver enzymes, slower heart and irregular heart beat, increased infections, increased blood pressure, blurry vision caused by fluid buildup in the macula of the eye (macular oedema), and increased risk of herpes infection. These side effects were seen in a small minority of participants of the clinical trials, excluding infections. Up to 24.9% of the clinical trials participants experienced infections. However, almost the same number of participants (22.2%) in the control group (were given tablets without the drug) also experienced infections. The most common infection was urinary tract infections.
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