What To Know About Zeposia (Ozanimod)

A Drug That Treats Relapses of Multiple Sclerosis

Table of Contents
View All
Table of Contents

 

Zeposia (ozanimod) is an oral medication prescribed for the prevention of multiple sclerosis (MS) relapses. Multiple sclerosis (MS) is a chronic demyelinating neurologic disease that occurs when the immune system attacks the protective covering surrounding neurons in the central nervous system.

Part of a class of drugs called sphingosine 1-phosphate receptor (S1PR) modulators, Zeposia prevents excess white blood cells from leaving the body's lymph nodes to reduce the damage they can cause.

Zeposia was approved by the US Food and Drug Administration in 2020. It is a disease-modifying therapy (DMT) and is taken at a maintenance dose of 0.92 milligrams (mg) per day.

Person with multiple sclerosis and support dog

Mark Hunt / Getty Images

 

Uses

Zeposia is approved for treating:

Before Taking

Before your doctor prescribes Zeposia, you will need tests to confirm your MS diagnosis and tests to ensure that you can safely take this medication.

Tests you may need include:

  • Complete blood count (CBC): This panel of tests determines the cellular composition of the blood, including the size and concentration of red blood cells, white blood cells, and platelets. Your doctors will pay special attention to your lymphocytes, a type of white blood cell that can be elevated when you have an infection.
  • Electrocardiogram (ECG): This non-invasive diagnostic test examines heart activity to determine whether there are any underlying problems that could contraindicate taking Zeposia.
  • Liver function testing: Since this drug can damage the liver, tests of liver enzyme levels and bilirubin need to be performed before treatment is started.
  • Ophthalmic assessment: Visual disturbances are often a symptom of MS. In these cases, doctors perform a full evaluation of the inner surface, or fundus, of the eye.
  • Assessment of medications: Your doctor will need to evaluate all the medications you’re taking currently to make sure there will be no dangerous interactions.
  • Blood testing: To assess whether a person has been properly vaccinated for varicella-zoster virus (VZV)—the kind that causes chickenpox and shingles—blood tests may be performed. If you haven't been vaccinated for varicella-zoster, vaccination is recommended at least one month before you start taking this medication.

 

Precautions and Contraindications

Due to its effects, Zeposia may not be safe for some people. There are several conditions and factors that contraindicate this drug’s use:

  • Recent heart problems: This includes a history of heart attack (myocardial infarction), unstable angina, heart failure, stroke, or other serious cardiac issues within the last six months.
  • Current heart problems: If you have a condition that affects your heart rhythm, such as second- or third-degree atrioventricular (AV) block, sick sinus syndrome, or sino-atrial block, you may only be able to use Zeposia if you have a pacemaker.
  • Sleep apnea: This breathing disorder is characterized by loud snoring and insufficient oxygen levels at night. Zeposia is not safe for those with severe, untreated sleep apnea.
  • Taking monoamine oxidase (MAO) inhibitor drugs: Antidepressants of the MAO type, such as Marplan (isocarboxazid), Nardil (phenelzine), and Parnate (tranylcypromine), are contraindicated with Zeposia.

Due to its effects on the body and interactions with other medications, Zeposia may be taken with caution if you have certain conditions.

These include:

  • Active infection: Because Zeposia suppresses immune function, it reduces your body’s ability to fight infections. If you have an active infection, you will need to be treated before starting treatment with Zeposia.  
  • Cryptococcal meningitis: A fungal infection that affects the brain, cryptococcal meningitis is severely disabling and can lead to death. If you are taking Zeposia, your doctors may have you stop taking it if you develop this infection.
  • Progressive multifocal leukoencephalopathy (PML): This is a very serious viral infection that affects regions throughout the brain. It's characterized by muscle-weakness on one or both sides of the body, impaired coordination, blurred vision, confusion or memory loss, and other symptoms. Your treatment would be discontinued if you develop PML.
  • Lacking vaccinations: Since Zeposia affects the immune system, patients who haven’t had updated vaccinations will need to get them at least four weeks prior to starting treatment. The efficacy of vaccines may also be impacted when taken within three months after your course of therapy. Live attenuated vaccines should be avoided during Zeposia treatment and for three months after treatment is stopped.
  • Heart problems: Those with a history of heart disease, heart attack, heart failure, un-managed hypertension (high blood pressure), and other conditions may also not be good candidates for Zeposia. If it is prescribed for you, your doctors will monitor your cardiac function throughout your treatment with Zeposia.
  • Liver disease: A history of liver disease may predispose to liver damage from Zeposia.
  • Fetal risk: There have not been enough studies determining whether Zeposia is safe to take during pregnancy. Women of childbearing potential should use effective contraception during treatment and for three months after stopping treatment.
  • Pediatric patients: The safety of Zeposia has not been established for children.
  • Breastfeeding: It has not been established whether this drug can be transmitted via breastmilk, but this is a potential risk. As such, patients may be counseled to stop breastfeeding while taking Zeposia.

 

Other S1PR Modulator Drugs

Zeposia is one of a class of drugs that modify the activity of S1PR modulator receptors. Some of the other drugs of this class are undergoing clinical trials.

  • Novartis (fingolimod) was the first S1PR modulator to be used to treat MS and was approved in 2010.
  • Mayzent (siponimod) is another MS treatment, approved in the U.S. market in 2019.
  • Ponesimod is currently going through clinical trials for safety and efficacy.
  • Laquinimod is a S1PR modulator that was not approved for use in the U.S. by the FDA in 2011, though it is used in some other countries.

 

Dosage

Zeposia comes in three strengths: 0.23 milligram (mg) doses are light-gray capsules; 0.46 mg strength capsules are half gray, half orange, and 0.92 mg, orange capsules.

Essential to a proper regimen of this treatment is that it’s started gradually.

According to the manufacturer, Celgene Corporation, standard dosing recommendations are the following:

  • Days 1-4: Initial dose of one 0.23 mg capsule a day
  • Days 5-7: Dosage of 0.46 mg a day
  • Day 8 and beyond: Standard dosage following initial titration is one 0.92 mg capsule per day

Your doctor may make adjustments to standard dosages.

 

Modifications

Dosage of Zeposia remains consistent, and there are no recommended modifications to it. However, if treatment with this drug is interrupted for two or more weeks, your doctor may instruct you to restart with a gradually increasing titration.

 How to Take and Store

As with all prescribed medications, bottles of Zeposia should be stored in a safe, secure location, out of reach of children. It’s best kept in temperatures between 68 and 77 Fahrenheit (20 to 25 Celsius).

How do you safely take this drug? Here are some quick guidelines:

  • Take one tablet a day of the prescribed strength
  • Tablets can be taken with or without food
  • Swallow tablets whole
  • Avoid foods high in tyramine (cured meats, red wine, aged cheeses, and others)

If you forget to take your medication for one or more days within the first 14 days on Zeposia, let your doctor know. You'll likely have to start with titration again. After that initial period, if you miss a dose, take the next scheduled one and get back on your daily routine.

Side Effects

If taking this drug, make sure to monitor how you’re feeling, and don’t hesitate to call your doctor or to get emergency medical help when needed.

Common

The common, manageable side-effects of taking Zeposia include:

  • Upper respiratory infection (bronchitis, laryngitis, pharyngitis, and other infections of upper airways).
  • High levels of liver transaminase enzymes
  • Orthostatic hypotension (decreases in blood pressure when standing up or sitting down)
  • Urinary tract infection.
  • Back pain.
  • Hypertension
  • Upper abdominal pain.

Severe

Severe, rare adverse side-effects, include:

  • Heart dysfunction: Especially within the first two weeks of treatment, some patients experience bradycardia (slower than normal heart rate). This drug can cause heart arrhythmias (irregular heartbeat), such as atrioventricular (AV) block, sick-sinus syndrome, and sinoatrial heart block. You may feel lightheaded, dizzy, or pass out if you have these side effects.
  • Liver failure: Zeposia can significantly impact liver function, potentially leading to liver failure. This may lead to a range of symptoms, including dark urine, nausea, jaundice (yellowing eyes and skin), and vomiting, among others.
  • Macular edema: Characterized as swelling or fluid retention in the macula, the small central portion of the retina towards the back of the eye, macular edema may become worse in those taking Zeposia. In particular, diabetes mellitus or uveitis (an infection of the middle eye) increases the risk of developing macular edema with this drug—so this side effect would be carefully monitored with periodic eye examinations.
  • Posterior reversible encephalopathy syndrome (PRES): This syndrome, arising due to increases in pressure on the brain, is characterized by headache, seizures, cognitive difficulties, and disturbances to vision. If these symptoms arise, evaluation and treatment are needed, and Zeposia use might be paused.
  • Worse symptoms after treatment: In some cases, MS patients who experience improvement with Zeposia will experience a significant relapse and even worsening of symptoms if the medication is discontinued.  
  • Weakened immune system: Given Zeposia’s effects on lymphocytes, patients following treatment will continue to have a weakened immune system for about 30 days after stopping the drug. Most patients, about 90%, have fully recovered immune function at about three months after stopping Zeposia.
  • Increased cancer risk: Patients following treatment are at an increased risk of developing certain types of cancer, including the most common skin cancer (basal cell carcinoma) and the most dangerous skin cancer (melanoma), as well as breast cancer, among others.
  • Hypersensitivity: Allergic reaction to Zeposia has been observed, typically leading to rash, hives, and shortness of breath. If you experience any of these symptoms, let your doctor know as soon as possible.

Warnings and Interactions

While not a comprehensive list, here are some prescription, over-the-counter medications, supplements, and herbs that can affect the efficacy and safety of this Zeposia:

  • Strong CYP2C8 inhibitors: Strong versions of this class of drug, like the cholesterol medication, Lopid (gemfibrozil), may increase the risk of side-effects when taken with Zeposia.
  • Strong CYP2C8 inducers: Drugs that induce more activity in the CYP2C8 receptors include the antibiotic, Rifadin (rifampin). They severely impact the efficacy of Zeposia.
  • Breast cancer resistance protein (BCRP) inhibitors: Use of drugs such as cyclosporine (which depresses immune activity), as well as Promacta (eltrombopang) (a bone marrow stimulant), can also increase Zeposia’s potency, so co-administration should be avoided. 
  • Immunosuppressive drugs: Three classes of drugs—anti-neoplastics (used in chemotherapy), immune-modulators (used to treat human immunodeficiency virus [HIV]), and immunosuppressives (as in corticosteroids, among others)—may cause serious problems if taken with Zeposia.
  • Medications for cardiac arrhythmia: Certain types of drugs that are taken to treat irregular heartbeat may be problematic when taken with Zeposia. These include quinidine, Pronestyl (procainamide), Nexterone (amiodarone), and Betapace (sotalol).
  • Opioids: Prescribed narcotic pain killers, such as Oxycontin, Percocet, and others may also interact poorly with this medication. Adverse reactions can lead to death.

When you are taking Zeposia, make sure to let your doctor know if there are any changes to other medications that you’re taking. Never make adjustments without talking to your doctor first, and be mindful of how you’re feeling throughout your course of treatment.

 

 

Was this page helpful?
Article Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
  1. Park S, Im D. Sphingosine 1-phosphate receptor modulators and drug discovery. Biomol Ther (Seoul). 2017;25(1):80-90. doi:10.4062/biomolther.2016.160

  2. National Multiple Sclerosis Society. Update: FDA-approved oral Zeposia® (ozanimod) for relapsing forms of MS now available for prescription. 2020.

  3. US Food and Drug Administration. Highlights of prescribing information: Zeposia. Updated March 2020.  

  4. Celgene Corporation. Medication guide: Zeposia. 2020.