Ozanimod

Ozanimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1 and 5. Ozanimod blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood.

• ZEPOSIA is indicated for the treatment of: relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. moderately to severely active ulcerative colitis (UC) in adults.ICD-10: G35, K51.90

• ZEPOSIA is contraindicated in patients who: In the last 6 months, have experienced a myocardial infarction, unstable angina, stroke, transient ischemic attack (TIA), decompensated heart failure requiring hospitalization, or Class III or IV heart failure [see Warnings and Precautions (5.3) ] Have the presence of Mobitz type II second-degree or third degree atrioventricular (AV) block, sick sinus syndrome, or sino-atrial block, unless the patient has a functioning pacemaker [see Warnings and Precautions (5.3) ] Have severe untreated sleep apnea [see Warnings and Precautions (5.3) ] Are taking a monoamine oxidase (MAO) inhibitor [see Drug Interactions (7) ] In the last 6 months, experienced myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or Class III or IV heart failure. ( 4 ) Presence of Mobitz type II second-degree or third degree atrioventricular (AV) block, sick sinus syndrome, or sino-atrial block, unless the patient has a functioning pacemaker.contraindicated

Assessments are required prior to initiating ZEPOSIA. ( 2.1 ) Titration is required for treatment initiation. ( 2.2 ) The recommended maintenance dosage is 0.92 mg orally once daily. ( 2.2 ) The recommended maintenance dosage in patients with mild or moderate chronic hepatic impairment (Child-Pugh class A or B) is 0.92 mg once every other day. ( 2.3 ) If a dose is missed within the first 2 weeks of treatment, reinitiate with the titration regimen. If a dose is missed after the first 2 weeks of treatment, continue treatment as planned. ( 2.4 ) 2.1 Assessments Prior to First Dose of ZEPOSIA Before initiation of treatment with ZEPOSIA, assess the following: Cardiac Evaluation Obtain an electrocardiogram (ECG) to determine whether preexisting conduction abnormalities are present. In patients with certain preexisting conditions, advice from a cardiologist should be sought [see Warnings and Precautions (5.3) ]. Complete Blood Count Obtain a recent (i.e., within the last 6 months or after discontinuation of prior MS or UC therapy) complete blood count (CBC), including lymphocyte count [see Warnings and Precautions (5.1) ]. Liver Function Tests Obtain recent (i.e., within the last 6 months) transaminase and bilirubin levels [see Warnings and Precautions (5.4) ]. Ophthalmic Assessment Obtain a baseline evaluation of the fundus, including the macula, near the start of treatment with ZEPOSIA [see Warnings and Precautions (5.8) ]. Skin Examination Obtain a baseline skin examination prior to or shortly after initiation of ZEPOSIA.

Infections : ZEPOSIA may increase the risk of infections. Obtain a complete blood count (CBC) before initiation of treatment. Monitor for infection during treatment and for 3 months after discontinuation. Do not start ZEPOSIA in patients with active infections. ( 5.1 ) Progressive Multifocal Leukoencephalopathy (PML) : Withhold ZEPOSIA at the first sign or symptom suggestive of PML. ( 5.2 ) Bradyarrhythmia and Atrioventricular Conduction Delays : ZEPOSIA may result in transient decrease in heart rate; titration is required for treatment initiation. Check an electrocardiogram (ECG) to assess for preexisting cardiac conduction abnormalities before starting ZEPOSIA. Consider cardiology consultation for conduction abnormalities or concomitant use with other drugs that decrease heart rate. ( 2.1 , 2.2 , 5.3 , 7 ) Liver Injury : Obtain liver enzyme results before initiation and periodically during treatment. Discontinue if there is evidence of liver injury without other cause. ( 5.4 ) Fetal Risk : Women of childbearing potential should use effective contraception during treatment and for 3 months after stopping ZEPOSIA. ( 5.5 , 8.3 ) Increased Blood Pressure (BP) : Monitor BP during treatment. ( 5.6 ) Respiratory Effects : May cause a decline in pulmonary function. Assess pulmonary function (e.g., spirometry) if clinically indicated. ( 5.7 ) Macular Edema : Increases the risk of macular edema. Obtain a baseline evaluation of the fundus, including the macula, near the start of treatment with ZEPOSIA.

The following serious adverse reactions are described elsewhere in the labeling: Infections [see Warnings and Precautions (5.1) ] Progressive Multifocal Leukoencephalopathy [see Warnings and Precautions (5.2) ] Bradyarrhythmia and Atrioventricular Conduction Delays [see Warnings and Precautions (5.3) ] Liver Injury [see Warnings and Precautions (5.4) ] Fetal Risk [see Warnings and Precautions (5.5) ] Increased Blood Pressure [see Warnings and Precautions (5.6) ] Respiratory Effects [see Warnings and Precautions (5.7) ] Macular Edema [see Warnings and Precautions (5.8) ] Cutaneous Malignancies [see Warnings and Precautions (5.9) ] Posterior Reversible Encephalopathy Syndrome [see Warnings and Precautions (5.10) ] Unintended Additive Immunosuppressive Effects from Prior Treatment with Immunosuppressive or Immune-Modulating Drugs [see Warnings and Precautions (5.11) ] Severe Increase in Multiple Sclerosis Disability after Stopping ZEPOSIA [see Warnings and Precautions (5.12) ] Immune System Effects after Stopping ZEPOSIA [see Warnings and Precautions (5.13) ] Most common adverse reactions (incidence ≥4%) are: Multiple Sclerosis : upper respiratory infection, hepatic transaminase elevation, orthostatic hypotension, urinary tract infection, back pain, and hypertension. ( 6.1 ) Ulcerative Colitis : liver test increased, upper respiratory infection, and headache. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Bristol-Myers Squibb at 1-800-721-5072 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch .

Hepatic Impairment : Use in severe hepatic impairment (Child-Pugh class C) is not recommended. ( 2.3 , 8.6 ) 8.1 Pregnancy Pregnancy Exposure Registry There is a pregnancy exposure registry that monitors pregnancy outcomes in women exposed to ZEPOSIA during pregnancy. Healthcare providers are encouraged to register patients on-line, or pregnant women may register themselves at https://www.zeposiapregnancyregistry.com/ or by calling 1-877-301-9314. Currently this registry is enrolling women with MS. Information regarding registration of pregnant women with UC will be made available in the future. Risk Summary There are no adequate data on the developmental risk associated with the use of ZEPOSIA in pregnant women . In animal studies, administration of ozanimod during pregnancy produced adverse effects on development, including embryolethality, an increase in fetal malformations, and neurobehavioral changes, in the absence of maternal toxicity. In rabbits, fetal blood vessel malformations occurred at clinically relevant maternal ozanimod and metabolite exposures (see Data) . The receptor affected by ozanimod (sphingosine1-phosphate) has been demonstrated to have an important role in embryogenesis, including vascular and neural development. In the U.S.

Metabolism

The steady state exposure parameters of ozanimod and its major active metabolite, CC112273 are summarized in Table 7. Population pharmacokinetic analysis indicated no meaningful differences in these pharmacokinetic parameters in patients with relapsing MS or UC.

• Mar 25, 2020NDANDA209899Bristol

1. 1Fatigue7319.1%
2. 2Multiple Sclerosis Relapse5777.2%
3. 3Drug Ineffective5426.7%
4. 4Headache5046.3%
5. 5Product Dose Omission Issue3564.4%
6. 6Dizziness3384.2%
7. 7Nausea2813.5%
8. 8Diarrhoea2613.2%
9. 9Colitis Ulcerative2523.1%
10. 10Pain2503.1%
11. 11Back Pain2122.6%
12. 12Adverse Event1862.3%
13. 13Fall1782.2%
14. 14Multiple Sclerosis1742.2%
15. 15Dyspnoea1531.9%

The 10 most recently updated of 67 ClinicalTrials.gov registrations naming Ozanimod as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• A Study Investigating Oral Ozanimod (RPC1063) in Pediatric Participants With Moderate to Severe Active Ulcerative Colitis
  Recruiting · Phase 2 · Phase 3 · Interventional · 120 enrolled · Bristol-Myers Squibb
  NCT05076175updated 2026-06-11
• A Study to Learn More About The Safety of Diroximel Fumarate (VUMERITY®) in Participants Who Took it During Pregnancy And About the Health of Their Babies
  Active not recruiting · Observational · 1,178 enrolled · Biogen
  NCT05688436updated 2026-06-04
• A Study to Describe the Persistence With Ozanimod Treatment in Relapsing-Remitting Multiple Sclerosis (RRMS) Participants
  Active not recruiting · Observational · 200 enrolled · Bristol-Myers Squibb
  NCT05811416updated 2026-05-29
• Effectiveness of Ozanimod in Patients With Steroid-Dependent Ulcerative Colitis
  Recruiting · Observational · 150 enrolled · Bristol-Myers Squibb
  NCT07271069updated 2026-05-18
• Describing Treatment Patterns and Creating an Updated Treatment Flow in an Ulcerative Colitis Population
  Active not recruiting · Observational · 4,000 enrolled · Pfizer
  NCT07177209updated 2026-05-14
• Predicting Disease Activity and Rebound Risk in MS Patients Treated With Sphingosine-1-phosphate Receptor Modulators (S1PRM)
  Terminated · Observational · 23 enrolled · Insel Gruppe AG, University Hospital Bern
  NCT05828901updated 2026-05-11
• Study to Evaluate the Effectiveness and Safety of Ozanimod Compared to Fingolimod in Children and Adolescents With Relapsing Remitting Multiple Sclerosis
  Recruiting · Phase 3 · Interventional · 194 enrolled · Bristol-Myers Squibb
  NCT06408259updated 2026-04-28
• Determine PK Profiles of Ozanimod and Its' Major Metabolites in Healthy Subjects
  Completed · Observational · 24 enrolled · Corium Innovations, Inc.
  NCT06528665updated 2026-02-25
• An Open-label Study of Ozanimod in Moderate to Severe Ulcerative Colitis in Clinical Practice
  Terminated · Phase 4 · Interventional · 139 enrolled · Bristol-Myers Squibb
  NCT05369832updated 2026-02-10
• An Extension Study of RPC1063 as Therapy for Moderate to Severe Ulcerative Colitis
  Completed · Phase 3 · Interventional · 877 enrolled · Celgene
  NCT02531126updated 2025-12-31

Frequently asked questions

How does Ozanimod work?

Ozanimod is a sphingosine 1-phosphate (S1P) receptor modulator that binds with high affinity to S1P receptors 1 and 5. Ozanimod blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood.

What is Ozanimod used for?

According to FDA labeling, Ozanimod carries indications including: ZEPOSIA is indicated for the treatment of: relapsing forms of multiple sclerosis (MS), to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease, in adults. moderately to severely active ulcerative colitis (UC) in adults.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Ozanimod?

Ozanimod is classified as Sphingosine-1-phosphate (S1P) receptor modulators, Sphingosine 1-phosphate Receptor Modulator, Monoamine Oxidase Inhibitors, Sphingosine 1-Phosphate Receptor Modulators, Decreased Lymphocyte Activation.

What are the brand names for Ozanimod?

Ozanimod is marketed under brand names including Zeposia.

What are the contraindications for Ozanimod?

Ozanimod labeling lists contraindications including: ZEPOSIA is contraindicated in patients who: In the last 6 months, have experienced a myocardial infarction, unstable angina, stroke, transient ischemic attack (TIA), decompensated heart failure requiring hospitalization, or Class III or IV heart failure [see Warnings and Precautions (5.3) ] Have the presence of Mobitz type II second-degree or third degree atrioventricular (AV) block, sick sinus syndrome, or sino-atrial block, unless the patient has a functioning pacemaker [see Warnings and Precautions (5.3) ] Have severe untreated sleep apnea [see Warnings and Precautions (5.3) ] Are taking a monoamine oxidase (MAO) inhibitor [see Drug Interactions (7) ] In the last 6 months, experienced myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or Class III or IV heart failure. ( 4 ) Presence of Mobitz type II second-degree or third degree atrioventricular (AV) block, sick sinus syndrome, or sino-atrial block, unless the patient has a functioning pacemaker.. Always consult the full prescribing information and a clinician.