What To Know About Zeposia (Ozanimod)

A Drug That Treats Relapses of Multiple Sclerosis

 

Zeposia (ozanimod) is a medication prescribed in cases of relapse of the progressive autoimmune disease, multiple sclerosis (MS). MS occurs when the body’s immune system attacks the myelin sheath, a protective layer surrounding neurons, preventing communication between brain and body.

Part of a class of drugs called sphingosine 1-phosphate receptor (S1PR) modulators, Zeposia acts on the white blood cells called lymphocytes, working to keep them within the lymph nodes. In turn, these cells aren’t able to cross into the brain or spine and damage neurons.

A therapy that was approved for the market in 2020, Zeposia is taken as capsules of varying strengths. A growing body of evidence has found this drug effective in taking on relapses of MS, so it’s important to get to know the basics of how Zeposia is used, and how to take it safely.

Person with multiple sclerosis and support dog

Mark Hunt / Getty Images

 

Uses

Zeposia is not a first-line treatment for MS. Rather, it’s indicated when symptoms, including muscle weakness, tingling, numbness, visual disturbances, and trouble balancing, return following initial treatment. The U.S. Food and Drug Administration (FDA) specifies several specific syndromes of MS that call for Zeposia:

  • Clinically isolated syndrome (CIS) is defined as a 24-hour period of one or more symptoms. For many patients, CIS becomes the first sign of MS, so when this develops after initial treatments, it represents a relapse.
  • Relapsing-remitting multiple sclerosis (RRMS) is a form of the disease, in which patients cycle through periods of increased symptoms, followed by those in which these subside. A majority of MS patients have this form of the disease.  
  • Secondary progressive multiple sclerosis (SPMS) refers to MS that, following initial periods of symptomology akin to RRMS, gets progressively more severe, with symptoms accumulating.

Before Taking

Before Zeposia is prescribed, it’s essential to get an accurate diagnosis. Clinical evaluation is key to this process, as it will also determine whether it’s safe for you to take this drug. These necessary tests include:

  • Complete blood count (CBC): This panel of tests determines the composition of the blood, breaking down the amounts of red and white blood cells. Particular important for doctors will be the number of lymphocytes, a type of white blood cell.
  • Electrocardiogram (ECG): This non-invasive diagnostic test examines heart activity to determine whether there are any underlying problems that could contraindicate prescription.
  • Liver function testing: Since the liver plays a major role in drug metabolism, assessment of its health is essential. Tests of liver enzyme levels and bilirubin need to be performed.
  • 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 as well as those you’ve taken in the past 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. Vaccination is recommended prior to therapy with Zeposia; however, it needs to occur at least one month before you start on the drug.

 

Precautions and Contraindications

Due to its effects on the body, Zeposia may not be safe for some patients to take. There are several conditions and factors that outright contraindicate this drug’s use:

  • Recent heart problems: This includes those who’ve had heart attack (myocardial infarction), unstable angina, heart failure, stroke, or other serious cardiac issues within the last six months.
  • Current heart problems: Those with problems affecting heartbeat, such as second- or third-degree atrioventricular (AV) block, sick sinus syndrome, or sino-atrial block can only use Zeposia if they 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 contraindicators for Zeposia.

Due to its effects on the body and interactions with other medications, Zeposia may also not be a safe option for several other cases. These include:

  • Active infection: Because Zeposia suppresses immune function, taking it greatly reduces your body’s ability to fight off infection. Those with an active infection will need to take have it taken care of before treatment begins.  
  • Cryptococcal meningitis: A fungal infection that affects the brain, cryptococcal meningitis is severely disabling and can lead to death. Doctors monitor for this condition, indicating Zeposia only after this has been managed, and calling for you to stop taking it if it crops up.
  • Progressive multifocal leukoencephalopathy (PML): This is a very serious viral infection of multiple brain regions that’s characterized by muscle-weakness on one or both sides of the body, impaired coordination, blurred vision, and confusion or memory loss, among others. Treatment is discontinued if PML and is not indicated if it’s present.
  • Lacking vaccinations: Since Zeposia affects the immune system, patients who haven’t had vaccinations will need to get these at least four weeks prior to starting administration. The efficacy of vaccines may also be impacted when taken within three months after your course of therapy.
  • Heart problems: Those with a history of heart disease, heart attack, heart failure, un-managed high blood pressure (hypertension), and other conditions may also not be good candidates for Zeposia. If prescribed, doctors ensure that cardiac health is carefully monitored.
  • Liver disease: A history of liver disease may predispose those taking Zeposia to experience severe effects on that organ.
  • Fetal risk: There have not been enough studies determining whether Zeposia is safe to take during pregnancy. There is a potential for the fetus to become damaged as a result, for this population is usually counseled to try an alternative. Pregnancy should be avoided and birth control should be used for three months following treatment.
  • Pediatric patients: The safety of Zeposia has not been established for children, so it’s typically not indicated for this population.
  • Breastfeeding: Doctors are unsure if this drug can be transmitted via breastmilk but note that 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 still undergoing the clinical trials necessary before they’re ready for the market. Here’s a quick breakdown:

  • Novartis (fingolimod) was the first S1PR modulator to be used to treat MS and was approved in 2010.
  • Mayzent (siponimod) is another MS treatment, cleared for sale on 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, something clinically referred to as “titration.”

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

  • Days 1-4: Initial dosages call for one 0.23 mg capsule a day.
  • Days 5-7: Dosage is doubled to 0.46 mg a day.
  • Day 8 and beyond: The standard dosage following titration is one 0.92 mg capsule per day.

When it comes to dosage of a drug like Zeposia, it’s important to remember that your doctor may make adjustments to standard dosages. It’s absolutely essential that you get a clear sense from them or your pharmacist about the proper amounts you should be taking.

 

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, patients will need to restart with 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 as you’ll have to start with titration again. After that initial period, if you miss a dose, just take the next scheduled one and get back on the routine.

Side Effects

Zeposia’s effects on the body, especially the immune system, are pervasive, and this can certainly lead to side-effects. The severity of these varies, with some being very dangerous and potentially deadly. If taking this drug, make sure to monitor how you’re feeling, and don’t hesitate to call your doctor or even emergency help when needed.

Common

The common, more 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
  • Drastic decreases in blood pressure when standing up or sitting down.
  • Urinary tract infection.
  • Back pain.
  • Hypertension (high blood pressure).
  • Upper abdominal pain.

Severe

In rarer cases, are a set of more adverse side-effects, including:

  • Affected heart function: Especially within the first two weeks of treatment, some patients experience bradycardia, or slower than normal heart rate. In addition, use can cause heart arrhythmias (irregular heartbeat), such as atrioventricular (AV) block, sick-sinus syndrome, and sinoatrial heart block.
  • Liver failure: Zeposia can significantly impact liver function, leading to liver failure. This leads 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, those who’ve had diabetes mellitus and uveitis (an infection of the middle eye) are at risk of developing edema, so, if treatment is undertaken, they are carefully evaluated.
  • 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 symptoms arise, evaluation and treatment are needed, and Zeposia use should be paused.
  • Worse symptoms after treatment: In some cases, MS patients finding improvement with Zeposia, will experience a significant relapse and even worsening of symptoms after the course of treatment is over.  
  • Weakened immune system: Given Zeposia’s effects on lymphocytes, patients following treatment will continue to have a weakened immune system for about 30 days. Most patients, about 90%, have fully recovered levels of this drug at about three months.
  • Increased cancer risk: Patients following treatment are at an increased risk of developing a couple of forms of cancer, including both the most common skin cancer (basal cell carcinoma) and the dangerous type (melanoma), as well as breast cancer, among some others.
  • Hypersensitivity: Allergic reaction to Zeposia has been observed, typically leading to rash and hives, among other symptoms. If you experience any of these symptoms, let your doctor know as soon as possible.

Warnings and Interactions

One of the major reasons doctors are so careful about prescribing drugs like Zeposia is to ensure that its usage won’t cause any unintended effects. This means evaluating everything you’re taking.

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

  • 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 alongside 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 alongside Zeposia.
  • Medications for cardiac arrhythmia: Certain types of drugs that are taken to treat irregular heartbeat also may be problematic alongside 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 here can lead to death.

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

 

 

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Article Sources
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  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. National Institutes of Health MedlinePlus. Multiple sclerosis. Updated 2014.

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

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