Ozanimod is developed and produced by Celgene Corporation in the United States. Ozanimod was first approved by the US Food and Drug Administration (FDA) on March 25, 2020, for the treatment of adult relapsing multiple sclerosis (RMS).

1、 Drug name

1. Common name: Ozanimod

2. Product Name: ZEPOSIA

2、 Indications

ZEPOSIA is suitable for treating adults:

1. Multiple sclerosis: Recurrent multiple sclerosis, including clinically isolated syndrome, relapsing remitting disease, and active secondary progressive disease.

2. Ulcerative colitis: moderate to severe active ulcerative colitis.

3、 Specifications and characteristics

1. Specification: Capsule, 0.92mg.

2. Appearance: 0.92mg Capsule: Orange opaque body/Orange opaque cap, with black "OZA" printed on the cap and black "0.92mg" printed on the body.

4、 Main components

Active ingredient: Ozanimod.

5、 Usage and dosage

1. Dose titration: The first use must undergo a 7-day dose titration to reduce the impact on heart rate. Please follow the doctor's advice for specific dosages.

2. Maintenance dose: After titration, the recommended maintenance dose is 0.92mg, taken orally once daily.

3. Usage: The capsule should be swallowed whole and can be taken with food or on an empty stomach.

6、 Dose adjustment

Patients with liver function impairment:

1. Mild or moderate injury (Child Pugh grade A or B): After completing the 7-day titration, adjust the maintenance dose to 0.92mg once every other day.

2. Severe injury (Child Pugh C grade): Not recommended for use.

7、 Medication precautions

1. Leakage handling:

Within the first 2 weeks of treatment: If one dose is missed, a titration regimen needs to be used to restart treatment.

After 2 weeks of treatment: If one dose is missed, continue taking the next dose as planned without the need for re titration.

2. Pre medication evaluation:

Before the first medication, electrocardiogram examination, complete blood cell count (including lymphocytes), liver function examination, fundus examination (including macula), and skin examination are required.

3. Vaccination:

During the medication period and within 3 months after discontinuation, vaccination with attenuated live vaccines should be avoided.

8、 Medication for special populations

1. Pregnant women: Based on animal research, it may cause harm to the fetus. Women of childbearing age must use effective contraceptive measures during treatment and within 3 months after discontinuing medication.

2. Breastfeeding women: It is not yet clear whether milk is secreted, and it is necessary to weigh the pros and cons before deciding whether to breastfeed or discontinue medication.

3. Child patients: Safety and efficacy have not been determined yet.

4. Elderly patients: Clinical studies did not include a sufficient number of patients aged 65 and above. Given the potential decline in heart and liver function in elderly individuals, close monitoring of adverse reactions to the heart and liver is necessary.

5. Renal dysfunction: No significant impact on pharmacokinetics, no need to adjust dosage.

9、 Adverse reactions

1. The most common adverse reactions (incidence ≥ 4%):

Multiple sclerosis: upper respiratory tract infection, elevated liver transaminase, orthostatic hypotension, urinary tract infection, back pain, hypertension.

Ulcerative colitis: abnormal liver function test, upper respiratory tract infection, headache.

2. Serious Warning and Precautions:

Risk of infection (including progressive multifocal leukoencephalopathy, herpes zoster, and cryptococcal infection).

Bradycardia with delayed atrioventricular conduction.

Liver injury (in rare cases requiring transplantation).

Elevated blood pressure.

Decreased respiratory function (FEV1 and FVC decrease).

Macular edema.

Malignant tumors of the skin (basal cell carcinoma, squamous cell carcinoma, melanoma).

Reversible posterior leukoencephalopathy syndrome.

Severe exacerbation of multiple sclerosis (disease rebound) after discontinuation of medication.

10、 Contraindications

ZEPOSIA is prohibited for the following patients:

1. Have experienced myocardial infarction, unstable angina, stroke, transient ischemic attack, decompensated heart failure requiring hospitalization, or grade III/IV heart failure within the past 6 months.

2. There is Mohs type II second or third degree atrioventricular block, sick sinus syndrome, or sinoatrial block (unless the patient has a functioning pacemaker).

3. Suffering from severe untreated sleep apnea.

4. Patients who are currently taking monoamine oxidase inhibitors (such as selegiline, phenylhydrazine, linezolid).

11、 Drug interactions

1. Antitumor, immunomodulatory, or non corticosteroid immunosuppressive therapy: cautious use may increase the risk of immunosuppression. It is not recommended to start using this product after treatment with Alenzumab.

2. Antiarrhythmic drugs, drugs that prolong QT interval, and heart rate lowering drugs: When using calcium channel blockers in combination with Class Ia or III antiarrhythmic drugs or beta blockers, it is necessary to consult a cardiologist.

3. Highly effective CYP2C8 inhibitors (such as gefitolozil): Not recommended for combination as they may increase exposure to active metabolites.

4. Strong CYP2C8 inducers (such as rifampicin) should be avoided in combination as they may reduce efficacy.

5. Monoamine oxidase inhibitors: Do not use in combination.

6. Vaccine: Avoid using attenuated live vaccines (during medication and within 3 months after discontinuation).

12、 Storage method

1. The storage temperature is between 20 ° C and 25 ° C, with a permissible fluctuation range of 15 ° C to 30 ° C.

2. Store in the original packaging and avoid contact with children.

ozanimodinformation