Sphingosine-1-phosphate receptor modulatorPrescription OnlyPregnancy Cat. Category X equivalent — contraindicated in pregnancy. Causes fetal harm in animal studies. Use effective contraception for at least 3 months after stopping (active metabolite half-life).FDA 2020
Ozanimod
ozanimod
Ozanimod is a sphingosine-1-phosphate (S1P) receptor 1 and 5 modulator approved for relapsing forms of multiple sclerosis (MS) and moderately to severely active ulcerative colitis. By functionally antagonizing S1P receptors on lymphocytes, it sequesters lymphocytes in lymph nodes, reducing circulating lymphocytes and their infiltration into the CNS and intestinal mucosa. It is an oral therapy offering convenience over injectable MS therapies and IV biologics for UC.
Medically reviewed by MedCentralHub Medical Review Board, Licensed Pharmacists & Physicians ·
Brand names:Zeposia
Quick Reference
Medicine ClassSphingosine-1-phosphate receptor modulator
FDA Approved2020
PregnancyCategory Category X equivalent — contraindicated in pregnancy. Causes fetal harm in animal studies. Use effective contraception for at least 3 months after stopping (active metabolite half-life).
FormsCapsules
Quick Facts
- Active ingredient
- ozanimod
- Medicine class
- Sphingosine-1-phosphate receptor modulator
- Brand names
- Zeposia
- Availability
- Prescription only (Rx)
- Pregnancy category
- Category X equivalent — contraindicated in pregnancy. Causes fetal harm in animal studies. Use effective contraception for at least 3 months after stopping (active metabolite half-life).
- Half-life
- Ozanimod: ~21 hours. Major active metabolite CC112273: ~10–13 days.
- Major interactions
- Anti-arrhythmics, beta-blockers, calcium channel blockers, digoxinMajor·MAO inhibitors (selegiline, rasagiline, phenelzine, tranylcypromine)Major·Tyramine-rich foods (aged cheese, cured meats, wine)Major·Live attenuated vaccinesMajor
- FDA approved
- 2020
What Is Ozanimod?
Ozanimod is a sphingosine-1-phosphate (S1P) receptor 1 and 5 modulator approved for relapsing forms of multiple sclerosis (MS) and moderately to severely active ulcerative colitis. By functionally antagonizing S1P receptors on lymphocytes, it sequesters lymphocytes in lymph nodes, reducing circulating lymphocytes and their infiltration into the CNS and intestinal mucosa. It is an oral therapy offering convenience over injectable MS therapies and IV biologics for UC.
Ozanimod (ozanimod) belongs to the Sphingosine-1-phosphate receptor modulator class of medications. It was first approved by the FDA in 2020. This medication requires a prescription from a licensed healthcare provider.
Key Safety Information
- •Always follow the dose recommended by your healthcare professional. Taking more than prescribed increases the risk of side effects including serious complications.
- •Seek emergency care if you experience signs of an allergic reaction — hives, swelling, difficulty breathing, or rash. Stop the medication and call your doctor immediately.
- •Some medications can increase the risk of cardiovascular events. Tell your doctor if you have high blood pressure, a history of heart attack or stroke, or any pre-existing health condition.
- •Avoid or limit alcohol while taking Ozanimod. Do not drink alcohol without first discussing it with your healthcare provider as it may increase adverse effects.
- •Take Ozanimod with food or a full glass of water if stomach upset occurs. Stop use and talk to your doctor if you experience persistent stomach pain or GI symptoms.
- •Tell your doctor about all medications, supplements, and vitamins you take. Some combinations significantly increase the risk of harm.
This is a summary only. Always read the full prescribing information and consult your healthcare provider for personalized medical advice.
Uses & Indications
Ozanimod is prescribed for the following conditions. Some uses are FDA-approved indications; others may be evidence-based off-label uses. Consult your healthcare provider for personalized guidance.
Relapsing forms of multiple sclerosis (including clinically isolated syndrome, relapsing-remitting MS, and active secondary progressive MS)
Moderately to severely active ulcerative colitis in adults
Dosage Guide
The following are general dosing guidelines only. Your actual dose should be determined by your healthcare provider based on your condition, renal/hepatic function, and other medications.
AD
Adult Dosage
MS: 0.23 mg orally once daily for 7 days, then 0.46 mg once daily for 7 days, then maintenance 0.92 mg once daily. UC: 0.23 mg once daily for 7 days, then 0.46 mg once daily for 7 days, then maintenance 0.92 mg once daily. Dose titration is mandatory to minimize first-dose cardiac effects.
PD
Pediatric Dosage
Not approved for patients under 18.
RI
Renal Impairment
No dose adjustment required for mild to moderate renal impairment. Not studied in severe renal impairment.
HI
Hepatic Impairment
Contraindicated in severe hepatic impairment (Child-Pugh C). No dose adjustment for mild/moderate hepatic impairment.
Available Forms
Capsules
Available Strengths
0.23 mg0.46 mg0.92 mg
Side Effects
Common
- Bradycardia and AV block (especially with first dose)
- Upper respiratory tract infections (URTI)
- Urinary tract infections
- Back pain and arthralgia
- Elevated liver enzymes (ALT/AST)
- Hypertension
- Abdominal pain (UC patients)
Serious
- Serious infections including opportunistic infections (PML — rare class risk)
- Bradycardia and AV block (first-dose cardiovascular effect — ECG monitoring required at initiation)
- Macular edema (screen for at baseline and if visual symptoms arise)
- Posterior reversible encephalopathy syndrome (PRES) — rare
- Malignancy (basal cell carcinoma reported)
- Rebound MS disease activity upon discontinuation (rare)
- Immune reconstitution inflammatory syndrome (IRIS) following discontinuation
Rare
- Cryptococcal meningitis and other invasive fungal infections
- Progressive multifocal leukoencephalopathy (PML) — rare class risk with S1P modulators
- Posterior reversible encephalopathy syndrome
- Allergic reactions
Medicine Interactions
Always inform your healthcare provider and pharmacist about ALL medications you take, including prescriptions, OTC medicines, vitamins, and supplements.
MajorModerateMinor
major
Anti-arrhythmics, beta-blockers, calcium channel blockers, digoxin
Additive bradycardic effects at first dose. Do not initiate ozanimod in patients on these medications without cardiology evaluation and monitoring. Extended first-dose observation required.
major
MAO inhibitors (selegiline, rasagiline, phenelzine, tranylcypromine)
Contraindicated. Ozanimod active metabolite inhibits MAO-B. Co-administration with MAO-A or non-selective MAO inhibitors may cause serotonin syndrome or hypertensive crisis.
major
Tyramine-rich foods (aged cheese, cured meats, wine)
Avoid excessive tyramine consumption. MAO-B inhibition by active metabolite may impair tyramine metabolism; large tyramine doses risk hypertensive crisis.
moderate
CYP2C8 inhibitors (gemfibrozil, clopidogrel)
May significantly increase ozanimod active metabolite exposure. Avoid combination.
major
Live attenuated vaccines
Avoid during treatment and for 3 months after discontinuation.
Warnings & Contraindications
Cardiovascular: do not initiate in patients with recent MI (within 6 months), unstable angina, stroke, TIA, decompensated heart failure, Class II–IV heart failure, history of Mobitz type II or third-degree AV block, sick sinus syndrome, or sinoatrial block (unless functioning pacemaker present). ECG required before first dose. First-dose observation period required (6 hours) in at-risk patients.
Infections: S1P modulators lower absolute lymphocyte count. Screen for varicella/VZV antibodies before initiation; vaccinate if seronegative. JC virus antibody status — monitor for PML risk.
Macular edema: ophthalmologic evaluation at baseline and with symptoms. Higher risk in diabetics and patients with prior uveitis.
Liver toxicity: monitor LFTs. Discontinue if significant elevation.
Pregnancy: teratogenic. Use effective contraception during treatment and for 3 months after stopping.
Immunosuppression: allow sufficient washout before starting other immunosuppressants.
How Ozanimod Works
Ozanimod acts as a functional antagonist at sphingosine-1-phosphate receptors 1 (S1P1) and 5 (S1P5). S1P1 is critical for lymphocyte egress from lymphoid tissues (lymph nodes, thymus, Peyer's patches). By binding S1P1, ozanimod causes receptor internalization and desensitization, trapping lymphocytes in lymphoid organs and reducing circulating T and B lymphocyte counts (predominantly CCR7+ naive and central memory T cells). This prevents autoreactive lymphocyte migration to the CNS in MS and to the intestinal mucosa in UC. S1P5 modulation additionally affects NK cell trafficking and CNS-resident cell populations.
Pharmacokinetics
Absorption
Oral bioavailability of ozanimod is approximately 26%. Active metabolites (CC112273 and CC1084037) have much higher exposure (~73x ozanimod). Peak concentration of active metabolite at approximately 6–8 hours post-dose.
Half-Life
Ozanimod: ~21 hours. Major active metabolite CC112273: ~10–13 days.
Metabolism
Extensively metabolized via MAO-B, aldehyde dehydrogenase, CYP3A4, and CYP2C8 to active metabolites. Active metabolites account for most pharmacodynamic activity.
Excretion
Fecal (~86%) and renal (~26%) excretion; primarily as metabolites.
Pregnancy & Breastfeeding Safety
Category X equivalent — contraindicated in pregnancy. Causes fetal harm in animal studies. Use effective contraception for at least 3 months after stopping (active metabolite half-life).
FDA Pregnancy Category Category X equivalent — contraindicated in pregnancy. Causes fetal harm in animal studies. Use effective contraception for at least 3 months after stopping (active metabolite half-life).
Consult your healthcare provider.
Full Pregnancy InformationBreastfeeding
Many medications pass into breast milk in varying amounts. Before using Ozanimodwhile breastfeeding, discuss the benefits and risks with your healthcare provider or pharmacist — they can weigh your dose, your infant's age, and available lactation safety data to find the safest option for you and your baby.
Storage & Handling
Store at room temperature, 68°F–77°F (20°C–25°C), in original container. Protect from moisture.
Frequently Asked Questions
1
Why is a dose titration required when starting ozanimod?
Dose titration (starting at 0.23 mg for 7 days, then 0.46 mg for 7 days, then maintenance 0.92 mg) is required because ozanimod causes transient bradycardia and AV conduction slowing with the first dose, mediated by S1P1 activation on cardiac nodal tissue. The gradual escalation minimizes the magnitude of the first-dose heart rate decrease. Patients with pre-existing cardiac conditions (bradycardia, AV block, use of antiarrhythmics) require extended monitoring (6 hours) after the first dose and medical evaluation before starting treatment.
2
How does ozanimod compare to fingolimod for multiple sclerosis?
Both are S1P receptor modulators, but ozanimod selectively activates S1P1 and S1P5, while fingolimod activates S1P1, S1P3, S1P4, and S1P5. Ozanimod's lack of S1P3 activity may reduce cardiac side effects (S1P3 mediates some negative chronotropic and AV conduction effects). However, ozanimod has a unique MAO-B inhibitory effect via its active metabolite, requiring dietary tyramine restriction and avoidance of MAO inhibitors. The SUNBEAM and RADIANCE Part B trials for MS showed ozanimod reduced annualized relapse rates by 48–52% vs. interferon beta-1a.
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Ozanimod and Anti-arrhythmics, beta-blockers, calcium channel blockers, digoxin interaction
Check the clinical significance of combining Ozanimod with Anti-arrhythmics, beta-blockers, calcium channel blockers, digoxin
- Interaction
Ozanimod and MAO inhibitors (selegiline, rasagiline, phenelzine, tranylcypromine) interaction
Check the clinical significance of combining Ozanimod with MAO inhibitors (selegiline, rasagiline, phenelzine, tranylcypromine)
Comprehensive Guide to Ozanimod
Ozanimod (Zeposia) is an oral sphingosine-1-phosphate (S1P) receptor 1 and 5 modulator approved by the FDA in March 2020 for relapsing forms of multiple sclerosis and in May 2021 for moderately to severely active ulcerative colitis. As the second S1P modulator approved for MS (after fingolimod) and the first approved for UC, ozanimod expands the oral therapeutic options in both conditions. Its mechanism — sequestering autoreactive lymphocytes in lymph nodes by preventing S1P1-mediated egress — reduces pathogenic lymphocyte trafficking to the CNS in MS and to the intestinal mucosa in UC. In the TRUE NORTH trial for UC, ozanimod achieved clinical remission in 18% (induction) and 37% (maintenance, week 52) vs. 6% and 18% for placebo, respectively. Its active metabolite's MAO-B inhibitory property distinguishes ozanimod from other S1P modulators and requires dietary precautions and avoidance of MAO inhibitors.
Sources & References
- • FDA Prescribing Information — Official labeling and package insert for Ozanimod
- • U.S. National Library of Medicine — MedlinePlus drug information
- • American Hospital Formulary Service (AHFS) — Clinical pharmacology monograph
- • PubMed / MEDLINE — View clinical studies
Last reviewed by MedCentralHub Medical Review Board · MedCentralHub Editorial Policy
Medical Disclaimer
The information on this page is for educational purposes only and is not intended as medical advice, diagnosis, or treatment. Always consult your doctor, pharmacist, or qualified healthcare provider before starting, stopping, or changing any medication.