Is Zeposia (ozanimod) a biologic? How does it work?

Zeposia (ozanimod) is not a biologic, it is a conventional “small molecule” drug that belongs to the class of medicines called sphingosine 1-phosphate (S1P) receptor modulators. Zeposia does affect the immune system, although it does this in a different way to biologics which are drugs that have been derived from living organisms and contain components that control the action of other proteins, cellular processes, genes, or modify the immune system.

Zeposia is an oral prescription medicine that is approved to treat adults with moderately to severely active ulcerative colitis or relapsing forms of multiple sclerosis (MS) such as:

• clinically isolated syndrome,
• relapsing-remitting disease, and
• active secondary progressive disease.

Research has shown that people taking Zeposia for ulcerative colitis reported decreases in rectal bleeding and stool frequency, and were significantly more likely to experience clinical remission, clinical response, and endoscopic improvement compared to placebo.

People taking Zeposia for multiple sclerosis experienced significantly less disease progression, fewer relapses, and less brain atrophy than those who received standard care, with very few side effects.

How does Zeposia work?

Zeposia binds tightly and specifically to S1P receptors 1 and 5. S1P is a signaling lipid that helps to control many cellular processes including inflammation, the permeability of the blood vessels, cancer growth, and also adaptive immunity (also called acquired immunity), through the modulation of T-cell trafficking, and innate immunity, which is our first line of defense against infectious diseases. Compounds that target S1P receptors have long been of interest by researchers for the treatment of autoimmune diseases.

The first compound of this class discovered, fingolimod (brand name Gilenya) was approved in 2010 for relapsing forms of MS, but is not as specific as Zeposia, and binds to 4 out of 5 of the S1P receptors, and has a high risk of side effects, such as cardiac toxicity, macular edema, and pulmonary toxicity. Zeposia is a derivative of fingolimod that is more selective to S1P receptors.

By binding to these receptors, Zeposia is thought to block the ability of lymphocytes to escape from lymph nodes, which traps them in the lymph nodes and reduces their numbers in the blood, central nervous system, and in inflamed tissues. Exactly how Zeposia works in ulcerative colitis and multiple sclerosis is not known but is thought to be by a reduction in the migration of lymphocytes into the gut or central nervous system respectively.

Related questions

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• What are the new drugs used for multiple sclerosis (MS)?

How does Zeposia affect the immune system?

Zeposia affects the immune system by preventing the migration of lymphocytes from the lymph nodes into blood, the gut, the CNS, and inflamed tissues.

• Because Zeposia modulates the function of lymphocytes it can increase the risk of infection. Zeposia reduces the numbers of lymphocytes in the blood circulation to around 45% of baseline values. Although rare, life-threatening and fatal infections have occurred in patients receiving Zeposia.
• Use of Zeposia (ozanimod) with anticancer, non-corticosteroid immunosuppressive, or immune-modulating therapies is also expected to increase the risk of immunosuppression, and these treatments may be contraindicated.
• The use of live attenuated vaccines should also be avoided during and for 3 months after treatment with Zeposia. A full course of vaccination for antibody-negative patients with varicella vaccine is recommended before commencing treatment with ozanimod, This should be undertaken at least 4 weeks before ozanimod is initiated.