Ozanimod
Multiple sclerosis disease-modifying therapies
Multiple sclerosis disease-modifying therapies
An oral S1P receptor modulator that keeps lymphocytes inside lymph nodes. Used for relapsing MS and ulcerative colitis; it slows the heart at the start.
Quick facts
- Group
- Multiple sclerosis disease-modifying therapies
- Target
- Sphingosine-1-phosphate receptor 1 (S1PR1)
- Used for
- Relapsing forms of multiple sclerosis
- Key effects
- Upper respiratory and urinary infections · Back pain
- Monitor
- ECG before starting · Blood count · Blood pressure
- ATC
- L04AE02
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows ozanimod bound to the human S1P1 receptor coupled to its Gi protein.
Ozanimod acts directly (it is not a prodrug) and has high affinity for the S1P1 and S1P5 receptors. Like other S1P receptor modulators it behaves as a functional antagonist: it causes the S1P1 receptor to be internalized and degraded, so lymphocytes no longer follow the S1P signal that lets them leave lymph nodes. Fewer lymphocytes reach the brain or the colon.
- Ozanimod binds S1P1 on lymphocytes
- The receptor is internalized and degraded
- Lymphocytes stay trapped in lymph nodes
- Less inflammation in the CNS or the colon
Indications
- Relapsing forms of multiple sclerosis (including clinically isolated syndrome and active secondary progressive disease) Multiple sclerosis →
- Moderate to severe ulcerative colitis Ulcerative colitis →
Adverse effects
Common
- Upper respiratory and urinary infections
- Back pain
- Dizziness on standing, mainly at the start
- Raised liver enzymes
Contraindications
- Heart attack, unstable angina, stroke, TIA or heart failure in the previous 6 months
- Some heart rhythm disorders without a pacemaker
- Severe untreated sleep apnoea
- Active infection
Key interactions
- MAO inhibitors, opioids, SSRIs, SNRIs and tricyclic antidepressants
- Risk of a hypertensive reaction through the MAO-B-inhibiting metabolite
- Tyramine-rich foods (aged, smoked or fermented foods)
- Risk of a serious rise in blood pressure
- Medicines that slow the heart
- More bradycardia
- Live vaccines
- Not given during treatment and for 3 months after the last dose without the treating team's advice
What is monitored
- ECG before starting
- Blood count, liver tests and eye examination (macula) before and during treatment
- Blood pressure
- Skin checks for cancer
- Varicella immunity before starting
Administration and safety
- Oral capsule, raised over the first week
- Bradycardia is most likely in the first 8 days
Pregnancy and breastfeeding
It may harm the fetus; effective contraception is used during treatment and for 3 months after the last dose.
Nursing care
- Measure pulse and blood pressure, especially in the first week
- Teach to get up slowly at first (dizziness on standing)
- Give the tyramine-restricted food list
- Teach the signs of infection, which can occur up to 3 months after stopping
- Advise effective contraception during treatment and for 3 months after
Pharmacokinetics
- Absorption
- Oral, with good bioavailability
- Metabolism
- To several active metabolites, one of which inhibits MAO-B
- Half-life
- The effect lasts much longer than the parent drug because of its active metabolites
Test yourself
Think of the answer, then tap the question to see it.
How do S1P receptor modulators such as ozanimod reduce inflammation?
They internalize S1P1 receptors and keep lymphocytes trapped in lymph nodes.
Why must people on ozanimod watch tyramine and certain antidepressants?
One active metabolite inhibits MAO-B, which can cause hypertensive reactions.
Besides MS, which disease is ozanimod approved for?
Ulcerative colitis.
Connections
← Back to the class: Multiple sclerosis disease-modifying therapies
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: Ozanimod: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); ATCDDD - ATC/DDD Index (WHO Collaborating Centre for Drug Statistics Methodology, 2026); RCSB PDB - 7EW0: Cryo-EM structure of ozanimod -bound Sphingosine-1-phosphate receptor 1 in complex with Gi protein (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.