Skip to Content

Ozanimod

Class: Immunomodulatory Agents
- Sphingosine 1-Phosphate (S1P) Receptor Modulators
- Immunomodulators
Chemical Name: 5-[3-[(1S)-1-(2-hydroxyethylamino)-2,3-dihydro-1H-inden-4-yl]-1,2,4-oxadiazol-5-yl]-2-propan-2-yloxybenzonitrile
Molecular Formula: C23H24N4O3
CAS Number: 1306760-87-1
Brands: Zeposia

Medically reviewed by Drugs.com. Last updated on April 20, 2020.

Introduction

Ozanimod hydrochloride is an immunomodulatory agent.

Uses for Ozanimod

Ozanimod hydrochloride has the following uses:

Ozanimod hydrochloride is a sphingosine 1-phosphate receptor modulator 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.1

Ozanimod Dosage and Administration

General

Ozanimod hydrochloride is available in the following dosage form(s) and strength(s):

Capsules: 0.23 mg, 0.46 mg, and 0.92 mg (of ozanimod).1

Dosage

It is essential that the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:

Adults

Dosage and Administration
  • Assessments are required prior to initiating ozanimod hydrochloride.1

  • Titration is required for treatment initiation.1

  • The recommended maintenance dosage is 0.92 mg orally once daily.1

  • If a dose is missed within the first 2 weeks of treatment, reinitiate with the titration regimen.1

Cautions for Ozanimod

Contraindications

  • In the last 6 months, experienced myocardial infarction, unstable angina, stroke, transient ischemic attack (TIA), decompensated heart failure requiring hospitalization, or Class III or IV heart failure.1

  • 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.1

  • Severe untreated sleep apnea.1

  • Concomitant use of a monoamine oxidase (MAO) inhibitor.1

Warnings/Precautions

Infections

Risk of Infections

Ozanimod hydrochloride causes a mean reduction in peripheral blood lymphocyte count to 45% of baseline values because of reversible sequestration of lymphocytes in lymphoid tissues. Ozanimod hydrochloride may therefore increase the susceptibility to infections, some serious in nature. Life-threatening and rare fatal infections have occurred in patients receiving ozanimod hydrochloride.1

Obtain a recent (i.e., within 6 months or after discontinuation of prior MS therapy) complete blood count (CBC) including lymphocyte count before initiation of ozanimod hydrochloride.1

Delay initiation of ozanimod hydrochloride in patients with an active infection until the infection is resolved.1

In Study 1 and Study 2, the overall rate of infections and rate of serious infections in patients treated with ozanimod hydrochloride was similar to that in patients who received interferon (IFN) beta-1a (35% vs 34% and 1% vs 0.8%, respectively). Ozanimod hydrochloride increased the risk of viral upper respiratory tract infections, urinary tract infections, and herpes zoster.1

The proportion of patients who experienced lymphocyte counts less than 0.2 × 109/L was 3.3%. These values generally returned to greater than 0.2 × 109/L while patients remained on treatment with ozanimod hydrochloride. After discontinuing ozanimod hydrochloride 0.92 mg, the median time for peripheral blood lymphocytes to return to the normal range was 30 days, with approximately 90% of patients in the normal range within 3 months.1

Consider interruption of treatment with ozanimod hydrochloride if a patient develops a serious infection.1

Because the elimination of ozanimod hydrochloride after discontinuation may take up to 3 months, continue monitoring for infections throughout this period.1

Herpes Viral Infection: In Study 1 and Study 2, herpes zoster was reported as an adverse reaction in 0.6% of patients treated with ozanimod hydrochloride 0.92 mg and in 0.2% of patients who received IFN beta-1a. Herpes simplex encephalitis and varicella zoster meningitis have been reported with sphingosine 1-phosphate (S1P) receptor modulators. Patients without a healthcare professional-confirmed history of varicella (chickenpox), or without documentation of a full course of vaccination against varicella zoster virus (VZV), should be tested for antibodies to VZV before initiating ozanimod hydrochloride.1

Cryptococcal Infection: Cases of fatal cryptococcal meningitis (CM) and disseminated cryptococcal infections have been reported with S1P receptor modulators. Physicians should be vigilant for clinical symptoms or signs of CM. Patients with symptoms or signs consistent with a cryptococcal infection should undergo prompt diagnostic evaluation and treatment. Ozanimod hydrochloride treatment should be suspended until a cryptococcal infection has been excluded. If CM is diagnosed, appropriate treatment should be initiated.1

Progressive Multifocal Leukoencephalopathy: Progressive multifocal leukoencephalopathy (PML) is an opportunistic viral infection of the brain caused by the JC virus (JCV) that typically occurs in patients who are immunocompromised, and that usually leads to death or severe disability. Typical symptoms associated with PML are diverse, progress over days to weeks, and include progressive weakness on one side of the body or clumsiness of limbs, disturbance of vision, and changes in thinking, memory, and orientation leading to confusion and personality changes.1

PML has been reported in patients treated with S1P receptor modulators and other multiple sclerosis (MS) therapies and has been associated with some risk factors (e.g., immunocompromised patients, polytherapy with immunosuppressants). Physicians should be vigilant for clinical symptoms or MRI findings that may be suggestive of PML. MRI findings may be apparent before clinical signs or symptoms. If PML is suspected, treatment with ozanimod hydrochloride should be suspended until PML has been excluded by an appropriate diagnostic evaluation.1

If PML is confirmed, treatment with ozanimod hydrochloride should be discontinued.1

Prior and Concomitant Treatment with Antineoplastic, Immunosuppressive, or Immune-modulating Therapies

In clinical studies, patients who received ozanimod hydrochloride were not to receive concomitant treatment with antineoplastic, non-corticosteroid immunosuppressive, or immune-modulating therapies used for the treatment of MS. Concomitant use of ozanimod hydrochloride with any of these therapies would be expected to increase the risk of immunosuppression. Antineoplastic, immune-modulating, or immunosuppressive therapies (including corticosteroids) should be co-administered with caution because of the risk of additive immune system effects during such therapy. When switching to ozanimod hydrochloride from immunosuppressive medications, consider the duration of their effects and their mode of action to avoid unintended additive immunosuppressive effects.1

Vaccinations

Patients without a healthcare professional-confirmed history of chickenpox or without documentation of a full course of vaccination against VZV should be tested for antibodies to VZV before initiating ozanimod hydrochloride. A full course of vaccination for antibody-negative patients with varicella vaccine is recommended prior to commencing treatment with ozanimod hydrochloride, following which initiation of treatment with ozanimod hydrochloride should be postponed for 4 weeks to allow the full effect of vaccination to occur.1

No clinical data are available on the efficacy and safety of vaccinations in patients taking ozanimod hydrochloride. Vaccinations may be less effective if administered during ozanimod hydrochloride treatment.1

If live attenuated vaccine immunizations are required, administer at least 1 month prior to initiation of ozanimod hydrochloride. Avoid the use of live attenuated vaccines during and for 3 months after treatment with ozanimod hydrochloride.1

Bradyarrhythmia and Atrioventricular Conduction Delays

Since initiation of ozanimod hydrochloride may result in a transient decrease in heart rate and atrioventricular conduction delays, an up-titration scheme should be used to reach the maintenance dosage of ozanimod hydrochloride.1

Ozanimod hydrochloride was not studied in patients who had:1

  • A myocardial infarction, unstable angina, stroke, TIA, or decompensated heart failure requiring hospitalization within the last 6 months.1

  • New York Heart Association Class III/IV heart failure.1

  • Cardiac conduction or rhythm disorders, including sick sinus syndrome, significant QT prolongation (QTcF greater than 450 msec in males, greater than 470 msec in females), risk factors for QT prolongation, or other conduction abnormalities or cardiac condition that in the opinion of the treating investigator could jeopardize the patient's health.1

  • Other pre-existing stable cardiac conditions without clearance from a cardiologist.1

  • Severe untreated sleep apnea.1

  • A resting heart rate less than 55 beats per minute (bpm) at baseline.1

Reduction in Heart Rate

Initiation of ozanimod hydrochloride may result in a transient decrease in heart rate. In Study 1 and Study 2, after the initial dose of ozanimod hydrochloride 0.23 mg, the greatest mean decrease from baseline in heart rate of 1.2 bpm occurred at Hour 5 on Day 1, returning to near baseline at Hour 6. With continued up-titration, the maximal heart rate effect of ozanimod occurred on Day 8. The utility of performing first-dose cardiac monitoring when initiating ozanimod hydrochloride in patients with characteristics similar to those studied in the clinical trials of ozanimod hydrochloride is unclear. Heart rates below 40 bpm were not observed. Initiation of ozanimod hydrochloride without titration may result in greater decreases in heart rate.1

In Study 1 and Study 2, bradycardia was reported on the day of treatment initiation in 0.6% of patients treated with ozanimod hydrochloride compared to no patients who received IFN beta-1a. After Day 1, the incidence of bradycardia was 0.8% in patients treated with ozanimod hydrochloride compared to 0.7% of patients who received IFN beta-1a.1

Atrioventricular Conduction Delays

Initiation of ozanimod hydrochloride may result in transient atrioventricular conduction delays. At ozanimod hydrochloride exposures higher than the recommended dosage without dose titration, first- and second-degree type 1 atrioventricular blocks were observed in healthy volunteers; however, in Study 1 and Study 2 with dose titration, second- or third-degree atrioventricular blocks were not reported in patients treated with ozanimod hydrochloride.1

If treatment with ozanimod hydrochloride is considered, advice from a cardiologist should be sought for those individuals:1

  • With significant QT prolongation (QTcF greater than 450 msec in males, greater than 470 msec in females).1

  • With arrhythmias requiring treatment with Class 1a or Class III antiarrhythmic drugs.1

  • With ischemic heart disease, heart failure, history of cardiac arrest or myocardial infarction, cerebrovascular disease, and uncontrolled hypertension.1

  • With a history of second-degree Mobitz type II or higher AV block, sick sinus syndrome, or sinoatrial heart block.1

Liver Injury

Elevations of aminotransferases may occur in patients receiving ozanimod hydrochloride.1

Obtain transaminase and bilirubin levels, if not recently available (i.e., within 6 months), before initiation of ozanimod hydrochloride.1

In Study 1 and Study 2, elevations of ALT to 5-fold the upper limit of normal (ULN) or greater occurred in 1.6% of patients treated with ozanimod hydrochloride 0.92 mg and 1.3% of patients who received IFN beta-1a. Elevations of 3-fold the ULN or greater occurred in 5.5% of patients treated with ozanimod hydrochloride and 3.1% of patients who received IFN beta-1a. The median time to an elevation of 3-fold the ULN was 6 months. The majority (79%) of patients continued treatment with ozanimod hydrochloride with values returning to less than 3 times the ULN within approximately 2-4 weeks.1

In clinical trials, ozanimod hydrochloride was discontinued for a confirmed elevation greater than 5-fold the ULN. Overall, the discontinuation rate because of elevations in hepatic enzymes was 1.1% of patients treated with ozanimod hydrochloride 0.92 mg and 0.8% of patients who received IFN beta-1a.1

Patients who develop symptoms suggestive of hepatic dysfunction, such as unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, or jaundice and/or dark urine, should have hepatic enzymes checked, and ozanimod hydrochloride should be discontinued if significant liver injury is confirmed.1

Individuals with an AST or ALT greater than 1.5 times ULN were excluded from Study 1 and Study 2. Although there are no data to establish that patients with preexisting liver disease are at increased risk to develop elevated liver function test values when taking ozanimod hydrochloride, caution should be exercised when using ozanimod hydrochloride in patients with a history of significant liver disease.1

Fetal Risk

There are no adequate and well-controlled studies in pregnant women. Based on animal studies, ozanimod hydrochloride may cause fetal harm. Because it takes approximately 3 months to eliminate ozanimod hydrochloride from the body, women of childbearing potential should use effective contraception to avoid pregnancy during treatment and for 3 months after stopping ozanimod hydrochloride.1

Increased Blood Pressure

In Study 1 and Study 2, patients treated with ozanimod hydrochloride had an average increase of approximately 1 to 2 mm Hg in systolic pressure over patients who received IFN beta-1a, and no effect on diastolic pressure. The increase in systolic pressure was first detected after approximately 3 months of treatment and persisted throughout treatment. Hypertension was reported as an adverse reaction in 3.9% of patients treated with ozanimod hydrochloride 0.92 mg and in 2.1% of patients who received IFN beta-1a. Two patients treated with ozanimod hydrochloride in Study 1 and one patient treated with interferon (IFN) beta-1a in Study 2 experienced a hypertensive crisis that was not clearly influenced by a concomitant medication. Blood pressure should be monitored during treatment with ozanimod hydrochloride and managed appropriately.1

Certain foods that may contain very high amounts (i.e., more than 150 mg) of tyramine could cause severe hypertension because of potential tyramine interaction in patients taking ozanimod hydrochloride, even at the recommended doses. Because of an increased sensitivity to tyramine, patients should be advised to avoid foods containing a very large amount of tyramine while taking ozanimod hydrochloride.1

Respiratory Effects

Dose-dependent reductions in absolute forced expiratory volume over 1 second (FEV1) were observed in patients treated with ozanimod hydrochloride as early as 3 months after treatment initiation. In pooled analyses of Study 1 and Study 2, the decline in absolute FEV1 from baseline in patients treated with ozanimod hydrochloride compared to patients who received IFN beta-1a was 60 mL (95% CI: -100, -20) at 12 months. The mean difference in percent predicted FEV1 at 12 months between patients treated with ozanimod hydrochloride and patients who received IFN beta-1a was 1.9% (95% CI: -2.9, -0.8). Dose-dependent reductions in forced vital capacity (FVC) (absolute value and %-predicted) were also seen at Month 3 in pooled analyses comparing patients treated with ozanimod hydrochloride to patients who received IFN beta-1a (60 mL, 95% CI (-110, -10); 1.4%, 95% CI: (-2.6, -0.2)), though significant reductions were not seen at other timepoints. There is insufficient information to determine the reversibility of the decrease in FEV1 or FVC after drug discontinuation. One patient discontinued ozanimod hydrochloride because of dyspnea. Spirometric evaluation of respiratory function should be performed during therapy with ozanimod hydrochloride, if clinically indicated.1

Macular Edema

S1P modulators, including ozanimod hydrochloride, have been associated with an increased risk of macular edema.1

In Study 1 and Study 2, macular edema was observed in 0.3% of patients treated with ozanimod hydrochloride and in 0.3% of patients who received IFN beta-1a.1

An ophthalmic evaluation of the fundus, including the macula, is recommended in all patients at any time if there is any change in vision while taking ozanimod hydrochloride.1

Continuation of ozanimod hydrochloride therapy in patients with macular edema has not been evaluated. A decision on whether or not ozanimod hydrochloride should be discontinued needs to take into account the potential benefits and risks for the individual patient.1

Macular Edema in Patients with a History of Uveitis or Diabetes Mellitus

Patients with a history of uveitis and patients with a history of diabetes mellitus are at increased risk of macular edema during ozanimod hydrochloride therapy. The incidence of macular edema is also increased in MS patients with a history of uveitis. In addition to the examination of the fundus, including the macula, prior to treatment, MS patients with diabetes mellitus or a history of uveitis should have regular follow-up examinations.1

Posterior Reversible Encephalopathy Syndrome

Rare cases of posterior reversible encephalopathy syndrome (PRES) have been reported in patients receiving a S1P receptor modulator. In controlled clinical trials with ozanimod hydrochloride, one case of PRES was reported. Should an ozanimod hydrochloride-treated patient develop any unexpected neurological or psychiatric symptoms/signs (e.g., cognitive deficits, behavioral changes, cortical visual disturbances, or any other neurological cortical symptoms/signs), any symptom/sign suggestive of an increase of intracranial pressure, or accelerated neurological deterioration, the physician should promptly schedule a complete physical and neurological examination and should consider an MRI. Symptoms of PRES are usually reversible but may evolve into ischemic stroke or cerebral hemorrhage. Delay in diagnosis and treatment may lead to permanent neurological sequelae. If PRES is suspected, treatment with ozanimod hydrochloride should be discontinued.1

Unintended Additive Immunosuppressive Effects from Prior Treatment with Immunosuppressive or Immune-modulating Drugs

When switching from drugs with prolonged immune effects, the half-life and mode of action of these drugs must be considered to avoid unintended additive immunosuppressive effects while at the same time minimizing risk of disease reactivation, when initiating ozanimod hydrochloride.1

Initiating treatment with ozanimod hydrochloride after treatment with alemtuzumab is not recommended.1

Severe Increase in Disability After Stopping Ozanimod Hydrochloride

Severe exacerbation of disease, including disease rebound, has been rarely reported after discontinuation of a S1P receptor modulator. The possibility of severe exacerbation of disease should be considered after stopping ozanimod hydrochloride treatment. Patients should be observed for a severe increase in disability upon ozanimod hydrochloride discontinuation and appropriate treatment should be instituted, as required.1

Immune System Effects After Stopping Ozanimod Hydrochloride

After discontinuing ozanimod hydrochloride, the median time for peripheral blood lymphocytes to return to the normal range was 30 days, with approximately 90% of patients in the normal range within 3 months. Use of immunosuppressants within this period may lead to an additive effect on the immune system, and therefore caution should be applied when initiating other drugs 4 weeks after the last dose of ozanimod hydrochloride.1

Specific Populations

Pregnancy

Risk Summary: There are no adequate data on the developmental risk associated with the use of ozanimod hydrochloride 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. The receptor affected by ozanimod (sphingosine-1-phosphate) has been demonstrated to have an important role in embryogenesis, including vascular and neural development.1

In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. The background risk of major birth defects and miscarriage for the indicated population is unknown.1

Animal Data: Oral administration of ozanimod (0, 0.2, 1, or 5 mg/kg/day) to female rats during organogenesis resulted in a marked increase in embryofetal mortality, increased fetal malformations and skeletal variations (abnormal/delayed ossification), and reduced fetal body weight at the highest dose tested. No maternal toxicity was observed. At the no-effect dose (1 mg/kg/day) for adverse effects on embryofetal development, plasma ozanimod exposure (AUC) for ozanimod was approximately 60 times that in humans at the maximum recommended human dose (MRHD) of 0.92 mg/day. Plasma AUCs for major human metabolites, CC112273 and CC1084037, were similar to and less than, respectively, those in humans at the MRHD.1

Oral administration of ozanimod (0, 0.2, 0.6, or 2.0 mg/kg/day) to female rabbits during organogenesis resulted in a marked increase in embryofetal mortality at the highest dose tested and increased fetal malformations (malformed blood vessels) and skeletal variations at the mid and high doses. Maternal toxicity was not observed. At the no-effect dose (0.2 mg/kg/day) for adverse effects on embryofetal development in rabbit, plasma ozanimod exposure (AUC) was approximately 2 times that in humans at the MRHD; plasma AUCs for major human metabolites, CC112273 and CC1084037, were less than those in humans at the MRHD.1

Oral administration of ozanimod (0, 0.2, 0.7, or 2 mg/kg/day) to female rats throughout gestation and lactation resulted in persistent body weight reductions and long-term effects on reproductive (prolonged estrus cycle) and neurobehavioral (increased motor activity) function in offspring at the highest dose tested, which was not associated with maternal toxicity. At the no-effect dose (0.7 mg/kg/day) for adverse effects on pre- and postnatal development, plasma ozanimod exposure (AUC) was 30 times that in humans at the MRHD; plasma AUCs for major human metabolites, CC112273 and CC1084037, were less than those in humans at the MRHD.1

Lactation

Risk Summary: There are no data on the presence of ozanimod in human milk, the effects on the breastfed infant, or the effects of the drug on milk production. Following oral administration of ozanimod, ozanimod and/or metabolites were detected in the milk of lactating rat at levels higher than those in maternal plasma.1

The developmental and health benefits of breastfeeding should be considered along with the mother's clinical need for ozanimod hydrochloride and any potential adverse effects on the breastfed infant from ozanimod hydrochloride or from the underlying maternal condition.1

Females and Males of Reproductive Potential

Before initiation of ozanimod hydrochloride treatment, women of childbearing potential should be counseled on the potential for a serious risk to the fetus and the need for contraception during treatment with ozanimod hydrochloride. Because of the time it takes to eliminate the drug from the body after stopping treatment, the potential risk to the fetus may persist and women of childbearing age should also use effective contraception for 3 months after stopping ozanimod hydrochloride.1

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.1

Geriatric Use

Clinical studies of ozanimod hydrochloride did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. In general, dose selection for an elderly patient should be cautious, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.1

Hepatic Impairment

The effect of hepatic impairment on the pharmacokinetics of the ozanimod major active metabolites is unknown. Use of ozanimod hydrochloride in patients with hepatic impairment is not recommended.1

Common Adverse Effects

Most common adverse reactions (incidence greater than or equal to 4%): Upper respiratory infection, hepatic transaminase elevation, orthostatic hypotension, urinary tract infection, back pain, and hypertension.1

Drug Interactions

Specific Drugs

It is essential that the manufacturer's labeling be consulted for more detailed information on interactions with this drug, including possible dosage adjustments. Interaction highlights:

  • Vaccines: Avoid use of live attenuated vaccines during and for up to 3 months after treatment with ozanimod hydrochloride.1

  • Strong CYP2C8 inhibitors: Co-administration is not recommended.1

  • BCRP inhibitors: Co-administration is not recommended.1

  • Strong CYP2C8 inducers: Co-administration should be avoided.1

Actions

Mechanism of Action

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. The mechanism by which ozanimod exerts therapeutic effects in multiple sclerosis is unknown but may involve the reduction of lymphocyte migration into the central nervous system.1

Advice to Patients

Advise the patient to read the FDA-approved patient labeling (Medication Guide).1

Risk of Infections

Inform patients that they may be more likely to get infections, some of which could be life-threatening, when taking ozanimod hydrochloride and for 3 months after stopping it, and that they should contact their healthcare provider if they develop symptoms of infection. Inform patients that prior or concomitant use of drugs that suppress the immune system may increase the risk of infection. Advise patients that some vaccines containing live virus (live attenuated vaccines) should be avoided during treatment with ozanimod hydrochloride. If immunizations are planned, administer at least 1 month prior to initiation of ozanimod hydrochloride. Avoid the use of live attenuated vaccines during and for 3 months after treatment with ozanimod hydrochloride. Patients without a healthcare professional-confirmed history of chickenpox or without documentation of a full course of vaccination against VZV should be tested for antibodies to VZV before initiating ozanimod hydrochloride.1

Cardiac Effects

Advise patients that initiation of ozanimod hydrochloride treatment may result in a transient decrease in heart rate. Inform patients that to reduce this effect, dose titration is required. Advise patients that the dose titration is also required if a dose is missed for 1 day or more during the first 14 days of treatment.1

Liver Injury

Inform patients that ozanimod hydrochloride may increase liver enzymes. Advise patients that they should contact their healthcare provider if they have any unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, or jaundice and/or dark urine.1

Pregnancy and Fetal Risk

Inform patients that, based on animal studies, ozanimod hydrochloride may cause fetal harm. Discuss with women of childbearing age whether they are pregnant, might be pregnant, or are trying to become pregnant. Advise women of childbearing potential of the need for effective contraception during treatment with ozanimod hydrochloride and for 3 months after stopping ozanimod hydrochloride. Advise a female patient to immediately inform her healthcare provider if she is pregnant or planning to become pregnant.1

Respiratory Effects

Advise patients that they should contact their healthcare provider if they experience new onset or worsening dyspnea.1

Macular Edema

Advise patients that ozanimod hydrochloride may cause macular edema, and that they should contact their healthcare provider if they experience any changes in their vision. Inform patients with diabetes mellitus or a history of uveitis that their risk of macular edema may be increased.1

Posterior Reversible Encephalopathy Syndrome

Advise patients to immediately report to their healthcare provider any symptoms involving sudden onset of severe headache, altered mental status, visual disturbances, or seizure. Inform patients that delayed treatment could lead to permanent neurological consequences.1

Severe Increase in Disability After Stopping Ozanimod Hydrochloride

Inform patients that severe increase in disability has been reported after discontinuation of a S1P receptor modulator like ozanimod hydrochloride. Advise patients to contact their physician if they develop worsening symptoms of MS following discontinuation of ozanimod hydrochloride.1

Immune System Effects After Stopping Ozanimod Hydrochloride

Advise patients that ozanimod hydrochloride continues to have effects, such as lowering effects on peripheral lymphocyte count, for up to 3 months after the last dose.1

Additional Information

AHFSfirstRelease. For additional information until a more detailed monograph is developed and published, the manufacturer's labeling should be consulted. It is essential that the manufacturer's labeling be consulted for more detailed information on usual uses, dosage and administration, cautions, precautions, contraindications, potential drug interactions, laboratory test interferences, and acute toxicity.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Ozanimod Hydrochloride

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

0.23 mg (of ozanimod)

Zeposia

Celgene Corporation

0.46 mg (of ozanimod)

Zeposia

Celgene Corporation

0.92 mg (of ozanimod)

Zeposia

Celgene Corporation

Starter Pack

4 capsules, 0.23 mg (of ozanimod)

3 capsules, 0.46 mg (of ozanimod)

Zeposia 7-Day Starter Pack (available as blister package for first week of therapy)

Celgene Corporation

Starter Kit

4 capsules, 0.23 mg (of ozanimod)

3 capsules, 0.46 mg (of ozanimod)

30 capsules, 0.92 mg (of ozanimod)

Zeposia Starter Kit (available as blister package for first week of therapy and bottle of capsules for next 30 days of therapy)

Celgene Corporation

AHFS Drug Information. © Copyright 2021, Selected Revisions April 20, 2020. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

References

1. Celgene Corporation. Zeposia (ozanimod hydrochloride) oral capsules prescribing information. 2020 Apr. http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=93ce2fab-edfb-4804-8074-963071de51e4

Frequently asked questions