Repoxia Ozanimod Hydrochloride Capsules

1. Indications and Usage
Relapsing Form of Multiple Sclerosis (RFMS): Treatment of adult patients with relapsing forms of multiple sclerosis, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.
Ulcerative Colitis (UC): Treatment of adult patients with moderately to severely active ulcerative colitis.
2. Dosage and Administration
Route of Administration: Oral administration ONLY. Capsules can be taken with or without food.
Recommended Dosage: 0.92 mg once daily.
Titration Schedule: Initiate with a dose escalation regimen for the first 7 days to minimize cardiac effects (Day 1: 0.23 mg; Day 2-3: 0.46 mg; Day 4-7: 0.46 mg twice daily). From Day 8 onwards, take 0.92 mg once daily.
Missed Dose: If a dose is missed within the first 14 days, restart the titration schedule. If missed after Day 14, take the regular dose at the usual time; do not double up.
3. Mechanism of Action
S1P Receptor Modulation: Ozanimod is a selective modulator of sphingosine-1-phosphate (S1P) receptors 1 and 5.
Lymphocyte Sequestration: By binding to S1P1 receptors on lymphocytes, it prevents lymphocytes from exiting lymph nodes, thereby reducing the number of circulating lymphocytes.
Therapeutic Effect: This reduction in peripheral lymphocytes decreases the migration of immune cells into the central nervous system (in MS) and the gastrointestinal tract (in UC), reducing inflammation and tissue damage.
4. Safety and Warnings
Bradycardia and AV Block: Ozanimod can cause a transient decrease in heart rate and PR interval prolongation upon initiation. Baseline ECG and cardiac monitoring during the titration phase are required.
Infection Risk: Increased risk of infections due to lymphocyte reduction. Evaluate for active infections and screen for Varicella Zoster Virus (VZV) immunity prior to initiation.
Macular Edema: Risk of cystoid macular edema; patients with diabetes or history of uveitis should undergo baseline and periodic ophthalmologic monitoring.
Hepatotoxicity: Elevations in ALT and AST have been reported. Liver function tests should be performed prior to initiation and periodically during treatment.
Fetal Risk: May cause fetal harm. Effective contraception is required during and for 3 months after treatment.
5. Adverse Reactions and Clinical Research
Most Common Adverse Reactions: Nasopharyngitis, ALT increased, GGT increased, hypertension, headache, and lymphopenia.
Cardiovascular Effects: Bradycardia, hypotension, and hypertension may occur, particularly during the initial dose titration period.
Clinical Research Highlights: Phase 3 clinical trials (e.g., SUNBEAM, SOUL for MS; RADIATE, RUBY for UC) demonstrated significant efficacy in reducing relapse rates, disability progression, and endoscopic activity.
6. Drug Interations
MAO Inhibitors: Concomitant use with monoamine oxidase (MAO) inhibitors is not recommended due to potential pharmacokinetic interactions.
CYP2C8 Inhibitors/Inducers: Strong CYP2C8 inhibitors (e.g., gemfibrozil) may increase ozanimod exposure; strong CYP2C8 inducers (e.g., rifampin) may decrease exposure.
Vaccines: Live vaccines should be avoided during treatment and for 3 months after discontinuation due to the risk of infection.
7. Pharmaceutical Information
Chemical Composition: Active Ingredient: Ozanimod Hydrochloride.
Appearance: Hard gelatin capsules, available in 0.23 mg, 0.46 mg, and 0.92 mg strengths.
Packaging: Blister packaging or bottles.
Storage: Store at controlled room temperature (20°C to 25°C); protect from moisture.