Zeposia (Ozanimod) – Oral

What Is Zeposia?

Zeposia contains the active drug ozanimod. It is approved by the Food and Drug Administration (FDA) for managing relapsing forms of multiple sclerosis (MS). MS is a chronic inflammatory and neurodegenerative (nerve and brain) disease in which the body's immune cells start attacking the myelin covering that insulates nerves cells in the central nervous system (CNS) (brain and spinal cord).

Zeposia belongs to the class of medications called sphingosine-1-phosphate (S1P) receptor modulators, which work on S1P1 and S1P5 receptors (immune system cells). Zeposia has been proven effective and well-tolerated and helps decrease the number of relapses and prevent disability. In 2021, the FDA also approved Zeposia (ozanimod) for the treatment of ulcerative colitis.

Zeposia is a prescription medicine available as oral capsules of various strengths.

What Is Zeposia Used For?

FDA approved Zeposia to treat adults with relapsing forms of MS, including:

• Clinically isolated syndrome
• Relapsing-remitting disease
• Active secondary progressive disease

Zeposia doesn't cure MS but prevents or delays disability and reduces relapses (also called exacerbations, attacks, flares, or flare-ups), periods when new symptoms occur or old symptoms worsen.

It's also used for the treatment of ulcerative colitis. Inflammation from ulcerative colitis impacts the inner lining of large intestine and rectum. Symptoms of ulcerative colitis may vary but may include abdominal pain, blood in your stool, and diarrhea. In the United States, between 600,000 to 900,000 individuals have ulcerative colitis.

How to Take Zeposia

Before starting Zeposia, your healthcare provider will do specific medical/lab tests to monitor side effects. These tests include:

• Antibody tests for varicella-zoster virus (causes chicken pox and shingles): You may need a varicella-zoster virus vaccine before starting treatment with Zeposia. If you are not vaccinated, get vaccinations one month before treatment with Zeposia.
• Complete blood count (CBC): A CBC will measure lymphocytes (white blood cells that fight infections). A low level of lymphocytes means the presence of a disease.
• Heart tests: Tests such as an electrocardiogram (ECG) can determine abnormal heart rhythm. 
• Liver tests: These are used to check whether your liver enzyme levels are in the normal range and whether you have any damage to your liver. 
• Eye examination: An eye exam checks the pressure and fluid in people with a history of uveitis or macular edema.
  

The results of the lab tests will diagnose your condition. Your healthcare provider will prescribe the suitable dose for you accordingly.

Read the prescription label carefully and ask your healthcare provider about anything you don't understand.

Zeposia comes as an oral capsule of different strengths. Take it with or without food once daily. Take your medicine at around the same time every day to avoid missing the doses. Take exactly as prescribed. Don't take extra doses or fewer doses or more often than prescribed by your healthcare provider.

Swallow capsules whole; do not break, chew, or crush. Your healthcare provider may start you on a low dose of Zeposia and gradually increase the dosage over the first week.

Zeposia may interact with foods that contain tyramine and can cause a hypertensive crisis (a sudden, dangerous increase in blood pressure). Avoid foods with high levels of tyramine, such as aged cheeses, dried meats, sausages, preserved fish, pickles, yeast-containing products, beans, and red wine.

Zeposia may help control symptoms of MS and ulcerative colitis (an inflammatory bowel disease) but does not cure these diseases. Your healthcare provider may closely monitor post-drug use to see how well it works for you.

Storage

Store Zeposia capsules at room temperature (about 68 to 77 degrees Fahrenheit) and away from light and moisture.

Keep your medications tightly closed and out of the reach of children and pets, ideally locked in a cabinet or closet.

Avoid dumping unused and expired drugs down the drain or in the toilet. Ask your pharmacist or healthcare provider about the best ways to dispose of this medicine. Visit the FDA website to learn where and how to discard of unused and expired drugs. You may also find disposal boxes in your area. Ask your pharmacist or healthcare provider if you have any questions about the best ways to dispose of your medications.

If you plan to travel with Zeposia, become familiar with your final destination's regulations. In general, be sure to make a copy of your Zeposia prescription. Keep your medication in its original container from your pharmacy with your name on the label. If you have any questions about traveling with your medicine, ask your pharmacist or healthcare provider.

Off-Label Uses

Zeposia may be prescribed for the treatment of Crohn's disease, which is an inflammatory bowel disease.

Zeposia is undergoing a clinical trial for Crohn's disease.

What Are the Side Effects of Zeposia?

This is not a complete list of side effects and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your pharmacist or a healthcare provider. You may report side effects to the Food and Drug Administration (FDA) at fda.gov/medwatch or 800-FDA-1088.

Common Side Effects

Some of the common side effects of Zeposia are:

• Body aches, including back pain
• Elevated liver enzymes (hepatic transaminase)
• High blood pressure
• Feeling dizziness when standing up from the lying position (orthostatic hypotension)
• Difficulty breathing
• Loss of voice
• Cough or hoarseness
• Sore throat
• Light-colored stools
• Dark-colored urine
• Fatigue or weakness
• Headache

These side effects are mild and do not require any medical attention.

Severe Side Effects

Zeposia may cause some side effects that can be severe and need immediate medical attention.

Liver problems may result, with symptoms such as:

• Nausea
• Vomiting
• Abdominal pain
• Tiredness
• Loss of appetite
• Yellowing of the eyes or skin
• Dark-colored urine

Macular edema is a buildup of fluid in the macula of the eye, at the center of the retina. Its symptoms include:

• Blurred vision
• Shadows in the center of vision
• Sensitivity to light
• A blind spot
• Unusually colored vision

Posterior reversible encephalopathy syndrome (PRES) is a swelling and narrowing of blood vessels in the brain. Its symptoms include:

• Severe headache
• Neck stiffness
• Sudden confusion
• Loss of vision
• Seizures

Zeposia may increase the risk of a rare but severe and sometimes fatal brain infection called progressive multifocal leukoencephalopathy (PML). Symptoms of PML are like a worsening MS attack, such as:

• Weakness on one side of the body
• Clumsiness of the arms or legs 
• Changes in your thinking, memory, or balance
• Confusion
• Loss of strength

Weakening of the immune system (due to decreased lymphocytes and immune cells in the body) increases the chances of infections such as herpes simplex virus or bronchitis during the treatment and after three months. The common symptoms of infection are:

• Sore throat
• Difficulty breathing
• Fever or chills
• Cold or flu symptoms
• Sores or blisters

A severe allergic reaction to Zeposia is rare. However, immediately contact your healthcare provider or seek medical help if you have these problems.

Dosage: How Much Zeposia Should I Take?

Modifications

Zeposia may require a dose modification or limitation of use in specific populations, such as:

• People over age 65: Not enough data are available to determine if people over age 65 respond differently to the drug than younger people. In general, the dose selection for people above the age of 65 may need to be cautious regarding any decreased liver and kidney function, cardiac function, or the use of other drugs with Zeposia.
• Children: The safety and effectiveness of Zeposia have not been established in children.
• Breastfeeding: It is not known if Zeposia can pass into breast milk and harm a breastfed child. However, Zeposia should be avoided in breastfeeding people. 
• Pregnancy: Pregnant people should not take the drug as it may be fatal for the fetus.

Missed Dose

If you miss a dose of Zeposia within the first 14 days of the treatment, ask your healthcare provider before taking the next dose. You may need a dose adjustment and restart the therapy at a lower dose. 

If you miss the dose after 14 days of treatment, Keep taking the following doses as scheduled. Don't take a double dose to catch up for the missed one.

Overdose: What Happens If I Take Too Much Zeposia?

If you or someone has overdosed on Zeposia, watch for the symptoms of adverse effects and immediately seek medical help.

Precautions

What Are the Reasons I Should Not Take Zeposia?

Zeposia may not be suitable for people with certain medical conditions. These include:

• People who have had a heart attack, chest pain, stroke or ministroke, and decompensated heart failure requiring hospitalization in the last six months
• People with an irregular or abnormal heartbeat (arrhythmia) not corrected by a pacemaker
• People with severe, untreated sleep apnea
• People taking medicines called monoamine oxidase inhibitors (MAOIs) or with MAOI activity, including Marplan (isocarboxazid), Eldepryl (selegiline), Nardil (phenelzine), Parnate (tranylcypromine)
• People taking medicines with MAOI activity such as Zyvox (linezolid), an antibiotic with reversible MAOI activity (the effect goes away 24 hours after stopping the drug)
• Children
• Breastfeeding people: Your healthcare provider will help you determine whether the benefits of breastfeeding outweigh the risk to your breastfed child. Talk to your healthcare provider about different ways to feed your child. Otherwise, it may need to be avoided.
• People who can become pregnant: People who can become pregnant must consult their healthcare provider about the risk of Zeposia to the fetus and the need for contraception during their treatment. Contraception should be used while taking Zeposia and three months after discontinuing it. Giving your body time to eliminate the drug completely from the system will help avoid risks to the fetus after conception.
• People with hepatic impairment (liver disease)

What Other Medications Interact With Zeposia?

Zeposia can interact with some drugs. The use of these drugs with Zeposia may interfere with how these drugs or Zeposia works and may increase the risk of adverse effects.

Beta-blockers and/or calcium channel blockers:

• Tenormin (atenolol)
• Trandate (labetalol)
• Lopressor (metoprolol)
• Inderal (propranolol)
• Cardizem (diltiazem)
• Calan (verapamil)
  

Antineoplastic (cancer) drugs:

• Neoral (cyclosporine)

Strong CYP2C8 inhibitors:

• Lopid (gemfibrozil)
• Plavix (clopidogrel)

Medications for cardiac arrhythmias (irregular heartbeat) such as:

• Nexterone (amiodarone)
• Procainamide
• Nuedexta (quinidine)

Opioid drugs (narcotics):

• Demerol (meperidine)
• Dolophine (methadone)
• Tramadol

Strong CYP2C8 inducers:

• Rifampin
• Dilantin (phenytoin)

Selective serotonin reuptake inhibitors (SSRIs):

• Celexa (citalopram)
• Lexapro (escitalopram)
• Prozac (fluoxetine)
• Prozac (paroxetine)
• Zoloft (sertraline)

Serotonin and norepinephrine reuptake inhibitors (SNRIs):

• Khedezla (desvenlafaxine)
• Cymbalta (duloxetine)
• Savella (milnacipran)
• Effexor (venlafaxine)

Vaccines:

Live attenuated vaccines are not recommended while on treatment with Zeposia and three months after the treatment to reduce the risk of severe infections. 

Corticosteroids:

• Dexamethasone
• Medrol (methylprednisolone)
• Rayos (prednisone)

MAOIs (monoamine oxidase inhibitors) can cause severe hypertension if taken with Zeposia. It is advised to start using MAOIs at least 14 days after discontinuing treatment with Zeposia, including:

• Eldepryl (selegiline)
• Marplan (isocarboxazid)
• Nardil (phenelzine)
• Parnate (tranylcypromine)

Medicines with reversible MAOI activity:

• Zyvox (linezolid)

Immunosuppressant drugs:

• Campath (alemtuzumab)

This may not be a complete list of drugs that interact with Zeposia.

Talk with your healthcare provider about any other medicines you take or plan to take, including over-the-counter (nonprescription) products, vitamins, herbs, or plant-based medicines.

What Medications Are Similar?

Sphingosine 1-phosphate receptor (S1PR) modulators are a class of oral drugs with a novel mechanism to treat multiple sclerosis. Some other drugs belonging to this class of drugs approved by the FDA to treat multiple sclerosis are:

• Gilenya (fingolimod) 
• Mayzent (siponimod)
• Ponvory (ponesimod)

How Can I Stay Healthy While Taking Zeposia?

MS is a chronic immune-mediated disorder. This autoimmune condition can create a substantial burden on people, and the high cost of the available treatments makes it challenging to cope with the difficulties.

Zeposia is effective and well-tolerated in managing relapsing MS (when symptoms worsen or new symptoms arise). However, severe side effects are associated with the drug, such as the increased risk of infections, liver injury, fetal risk, increased blood pressure, respiratory effects, macular edema (swelling in the eye), and PERS.

Zeposia is effective in managing ulcerative colitis (UC). Living with UC can be challenging at times. Managing your symptoms and also keeping an eye on your nutrition are important since UC can cause anemia and other nutritional issues. Check out our guides for UC as well as recipe ideas to support your journey. Individuals with inflammatory bowel disease may also benefit from working with a registered dietitian nutritionist (RD or RDN). RDs can help you explore possible food triggers, and support building healthier habits through food, movement, medication, and more. Ask your healthcare provider for more information.

Always follow the guidelines of your prescriber to get the maximum benefit from the drug. Avoid taking Zeposia with tyramine-containing food to avoid hypertension. Do not stop taking Zeposia without having a discussion about this with your healthcare provider. You may have to take the medication on a long-term basis to manage the disease effectively.