Zeposia: 7 things you should know
Medically reviewed by Carmen Pope, BPharm. Last updated on March 28, 2023.
1. How it works
- Zeposia is a brand (trade) name for ozanimod which may be used to treat relapsing forms of multiple sclerosis or moderately to severely active ulcerative colitis.
- Zeposia is a derivative of fingolimod that is more selective for S1P receptors. Zeposia works by binding tightly to two S1P receptors found on the surface of lymphocytes (a type of white blood cell) called S1P receptors 1 and 5. This prevents lymphocytes from leaving the lymph nodes and getting into the bloodstream, reducing their numbers in the blood, central nervous system, and inflamed tissue. The exact way Zeposia works in multiple sclerosis or ulcerative colitis is unknown, but is thought to be due to this decrease in the migration of lymphocytes from the lymph nodes into the central nervous system which lowers inflammation.
- Zeposia belongs to the class of medicines known as sphingosine-1-phosphate (S1P) receptor modulators. It may also be called a small molecule drug or a selective immunosuppressant.
- May be used to treat adults with relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease (RRMS), and active secondary progressive disease (SPMS with relapses).
- Also approved for moderately to severely active ulcerative colitis in adults.
- Taken orally once a day. There is a 7-day titration period, which starts with 0.23mg once a day for days 1 to 4, then 0.46mg once a day for days 5 to 7, then 0.92mg once a day on days 8 and thereafter. If one titration dose is missed for more than 24 hours during the first two weeks (14 days) of Zeposia treatment, then restart the titration regimen on day 1. If a dose is missed after the first 2 weeks of treatment, then continue with treatment as planned.
- Helps to decrease the frequency of relapse symptoms. Significantly slows down disability progression in people with active secondary progressive disease (SPMS with relapses), but does not cure MS.
- Unlike siponimod, testing for the CYP2C9 genotype is not required with Zeposia.
- Bristol Myers Squibb has a patient support program for people taking Zeposia. Call 1-800-721-8909 or visit BMS.com for more information. This program pairs you with a nurse coordinator who will help you start treatment, get the needed lab tests before treatment, and answer any insurance-related questions.
- May be taken with or without food.
- Available as 0.23mg, 0.46mg, and 0.92mg capsules.
- Zeposia is covered for 91% of people with private or commercial health insurance.
If you are between the ages of 18 and 60, take no other medication or have no other medical conditions, side effects you are more likely to experience include:
- Upper respiratory tract infections, elevated liver transaminases, orthostatic hypotension, urinary tract infections, back pain, headache, fever, nausea, joint pain, high blood pressure, and upper abdominal pain are the main side effects reported.
- Transient decreases in heart rate have been noted during the initiation of Zeposia, especially during the first 8 days. Zeposia may increase blood pressure with an average increase of 1-2 mm Hg noted at 3 months which persists with continued treatment.
- May cause respiratory effects in some people with reductions in forced expiratory volume (FEV1) and forced vital capacity (FVC) observed in Zeposia-treated patients at 3 months. The average decline in FEV1 was 60mL.
- Elevations in liver transaminases have been reported in 10% of people treated with Zeposia. 5.5% had elevations 3-fold the upper limit of normal (ULN) at 6 months. Most values return to less than 3-fold the ULN within 2 to 4 weeks of continued treatment.
- Macular edema (a build-up of fluid in the eyes that may affect your vision) has been reported in 0.3% to 0.4% of patients treated with Zeposia, compared to no patients receiving a placebo. This rate is less than with other S1P receptor modulators, but the risk may be increased in patients with a prior history of uveitis and diabetes mellitus.
- May increase the risk of skin cancer, such as basal cell carcinoma, melanoma, and possibly other cancers, such as breast and seminoma.
- Several tests are required before starting Zeposia, such as a complete blood count, an eye examination that includes an evaluation of the fundus (including the macula), recent (within 6 months) liver function tests (including transaminase and bilirubin levels), and a cardiac evaluation (including an ECG) to determine if preexisting conduction abnormalities are present.
- Not suitable for people who have experienced a heart attack, unstable angina, stroke, or certain other cardiovascular events in the past 6 months, with Mobitz type II second- or third-degree AV block or other cardiac conduction abnormalities, with severe untreated sleep apnea, or who are taking a monoamine oxidase (MAO) inhibitor.
- Zeposia needs to be titrated up slowly over 7 days to the recommended maintenance dose of 0.92 mg/day.
- Reduces lymphocyte count in peripheral blood to approximately 45% of baseline values. This increases the risk of infection, some of which may be serious or fatal, such as cryptococcal meningitis. Delay initiation of Zeposia in patients with a severe active infection until it resolves.
- S1P receptor modulators, such as Zeposia, have also been associated with Progressive multifocal leukoencephalopathy (PML), an opportunistic viral infection of the brain. Symptoms include progressive weakness on one side of the body, vision disturbances, confusion, and personality changes. Posterior reversible encephalopathy syndrome (PRES) has also been reported in people receiving an S1P receptor modulator. Symptoms include cognitive deficits, behavioral changes, or visual disturbances.
- Zeposia interacts with several other medications. Some may not be suitable for coadministration with Zeposia including drugs that could slow the heart rate or atrioventricular conduction, and antineoplastic, immunosuppressive, or immune-modulating treatments (or a prior history of use). See interactions below for more details.
- May cause reactivation of herpes viral infections. Patients should be tested for antibodies to the varicella-zoster virus before starting Zeposia treatment. Vaccinate antibody-negative patients before commencing treatment.
- Avoid administration of live attenuated vaccines while patients are taking Zeposia and for 3 months after stopping treatment. Other vaccines may be less effective if administered during Zeposia treatment. If live vaccines are required, administer them at least 1 month before Zeposia initiation.
- People with certain cardiovascular conditions (such as a slow heart rate of fewer than 55 beats per minute) or a history of heart attack or heart failure should be referred to a cardiologist before Zeposia is initiated as it has not been studied in these people.
- Safety in children has not been established.
- Zeposia may cause harm to a developing baby. All females of reproductive potential should use effective contraception to avoid pregnancy during and for 3 months after stopping Zeposia treatment. No data is available regarding Zeposia and breastfeeding so risks vs benefits need to be considered.
- Not available as a generic.
Note: In general, seniors or children, people with certain medical conditions (such as liver or kidney problems, heart disease, diabetes, seizures) or people who take other medications are more at risk of developing a wider range of side effects. View complete list of side effects
4. Bottom Line
Zeposia is an S1P receptor modulator that may be used to treat relapsing forms of multiple sclerosis or ulcerative colitis in adults. It requires a 7-day titration period and reduces lymphocyte counts to within 45% of baseline values. Upper respiratory tract infections and elevations in liver enzymes are 2 of the most common side effects reported, and effects may persist for up to 3 months after stopping it.
- You must take your medicine every day unless your doctor tells you otherwise. If your treatment is stopped for 1 or more days during the first 14 days of initiatingZeposia, or for more than 7 days between day 15 and day 28 of treatment, or for more than 145 consecutive days after day 28 of treatment then you must go back to the initial titration regimen. Talk to your doctor about this.
- Zeposia is taken once a day, with or without food. Do not split, crush, or chew Zeposia hard capsules.
- Before starting Zeposia your doctor will perform several tests such as a complete blood count, an eye examination, liver function tests, and an evaluation of your heart.
- Report any side effects of concern, such as vision problems, a racing or irregular heartbeat, shortness of breath, confusion, unexplained nausea, abdominal pain, dark urine, difficulty walking, or edema to your doctor.
- Zeposia interacts with several other medications. Talk to your doctor or pharmacist before taking any other medications, including over-the-counter and herbal supplements.
- May cause reactivation of herpes viral infections. Your doctor should test you for antibodies to the varicella-zoster virus before starting Zeposia treatment and will vaccinate you if you are antibody-negative.
- You should not get vaccinated with vaccines composed of live attenuated viruses during Zeposia treatment and for 3 months after stopping treatment.
- Zeposia is not safe to use during pregnancy and is not recommended during breastfeeding. If you are of child-bearing potential you may have to undertake a pregnancy test before starting Zeposia and use reliable contraception while taking it. If you inadvertently become pregnant during Zeposia treatment or within 3 months of stopping it, tell your doctor straight away. Breastfeeding is not recommended unless the benefits outweigh the risks.
- Zeposia may increase your risk of developing skin cancers such as basal cell carcinomas. Protect your skin from sunlight and wear protective clothing and use sunscreen with a high sun protection factor. Tell your doctor if you have any changes in the appearance of your skin, including changes in a mole or sores that do not heal.
- Once you stop taking Zeposia, its effects can persist for up to 3 months.
6. Response and effectiveness
- Zeposia works quickly in multiple sclerosis (MS), within a few months, although it may take up to a year for the full effects of significantly less disease progression, fewer relapses, and less brain atrophy than standard care to be seen.
- Research has shown that there was a trend towards a reduction in disease progression with Zeposia Vs interferon-beta-1a within 3 months of administration (7.6% of Zeposia patients had disease progression Vs 7.8% of patients assigned interferon, although this difference was not statistically significant)
- After one year of treatment, 78% of patients taking Zeposia were relapse-free, compared with 66% of patients taking interferon-beta-1a. After 2 years 76% of patients taking Zeposia remained relapse-free compared with 64% of those taking interferon
- The number of new or enlarging T2 hyperintense lesions seen on MRI was significantly lower with one year of Zeposia treatment compared to the number seen with interferon (a 48% relative reduction). The number of GdE lesions was also statistically significantly lower with Zeposia compared to interferon (a 63% relative reduction).
- In two-year studies, these significant results persisted, although the relative reductions were slightly less (46% for T2 lesions and 53% for GdE lesions).
- For people with moderately to severely active ulcerative colitis (UC), decreases in rectal bleeding and stool frequency were seen as early as week 2 and significant differences in clinical remission, clinical response, and endoscopic improvement compared to placebo were noted within 10 weeks of starting Zeposia.
- In True North, a phase 3 trial that compared Zeposia to placebo in adult patients with moderately to severely active UC, the primary endpoint of clinical remission was met by week 10 with 18% of people taking Zeposia in remission compared to only 6% of those taking placebo. Secondary endpoints were also met, including clinical response (48% versus 26%), endoscopic improvement (27% versus 12%), and endoscopic-histologic mucosal improvement (13% versus 4%) for Zeposia versus placebo, respectively. In the maintenance part of the trial the primary endpoint of clinical remission (37% versus 19%) as well as key secondary endpoints, including clinical response (60% versus 41%), endoscopic improvement (46% versus 26%), corticosteroid-free clinical remission (32% versus 17%) and endoscopic-histologic mucosal improvement (30% versus 14%) for Zeposia versus placebo, respectively, were maintained at week 52.
- Rarely, severe exacerbation of disease and disease rebound has been reported after discontinuation of an S1P receptor modulator, such as Zeposia.
- Zeposia has a long half-life of approximately 21 hours, and the half-life of its major active metabolites CC112273 and CC1084037 is 11 days. This means it can take up to 55 days for Zeposia to be eliminated from the body. Most experts suggest 3 months should be allowed after stopping Zeposia and being administered a live vaccine or becoming pregnant. Lymphocytes recover to the normal range within 30 days of stopping Zeposia with 90% reaching the normal range by 3 months.
Medicines that interact with Zeposia may either decrease its effect, affect how long it works, increase side effects, or have less of an effect when taken with Zeposia. An interaction between two medications does not always mean that you must stop taking one of the medications; however, sometimes it does. Speak to your doctor about how drug interactions should be managed.
Zeposia interacts with over 800 medications; the majority of these interactions are considered major or moderate. Common medications that may interact with Zeposia include:
- antibiotics such as azithromycin, ciprofloxacin, or norfloxacin
- antineoplastics, such as capecitabine, or cyclophosphamide
- antipsychotics, such as clozapine, aripiprazole, or haloperidol
- biologics, such as adalimumab, etanercept, golimumab, or infliximab
- breast cancer resistance protein inhibitors, such as cyclosporine or eltrombopag
- corticosteroids (such as prednisone or dexamethasone)
- CYP2C8 inhibitors, such as gemfibrozil, and CYP2C8 inducers, such as rifampin. Avoid
- heart medications, particularly Class Ia and Class III antiarrhythmics, known QT-prolonging drugs, and those that slow the heart rate, such as beta-blockers (eg, atenolol, sotalol), digoxin, amiodarone, or flecainide (may be associated with severe bradycardia or heart block)
- herbals, such as black cohosh or brewer's yeast
- HIV medications, such as atazanavir or zidovudine
- immunosuppressants such as azathioprine, cyclosporine, or tacrolimus
- live vaccines and some other vaccines, such as BCG, cholera, measles, hepatitis b vaccines, yellow fever, or live influenza vaccines (Zeposia reduces the immune response to vaccination if vaccines are given within 3 months of Zeposia or Zeposia is given 4 weeks after vaccination)
- medications that increase serotonin or noradrenaline (such as opioids, SSRIs, SSNRIs, or tricyclics)
- monoamine oxidase inhibitors (MAOI), such as selegiline, phenelzine, linezolid (may increase the risk for high blood pressure), or within 14 days of an MAOI. Avoid
- probiotics, such as lactobacillus
- tyramine-containing foods or beverages, for example, strong aged cheeses; cured, smoked, or processed meats; fish, soy, miso sauce, or yeast extracts; or beer (more than 150mg of tyramine could cause severe hypertension).
Initiation of Zeposia results in a decreased heart rate which may prolong the QT interval. Use of Class Ia (eg, quinidine, procainamide) and Class III medications (such as amiodarone or sotalol) has been associated with cases of Torsades de Pointes in patients with bradycardia. Consult with a cardiologist.
Zeposia may have additive immune-suppressing effects when given with any other medications such as anticancer drugs, immune-modulating, or immunosuppressive therapies, which may increase a person's risk for infection. Take this into account when switching from drugs with prolonged immune effects, such as natalizumab, teriflunomide, or mitoxantrone.
Note that this list is not all-inclusive and includes only common medications that may interact with Zeposia. You should refer to the prescribing information for Zeposia for a complete list of interactions.
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Related treatment guides
- Zeposia (ozanimod hydrochloride). Updated 11/2022. Celgene Corporation https://www.drugs.com/pro/zeposia.html
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