Gilenya Fingolimod Hydrochloride Capsules

1. Indications and Usage
Relapsing Forms of Multiple Sclerosis (RMS): Treatment of patients (adults and pediatric patients 10 years of age and older) with relapsing forms of multiple sclerosis, to delay the accumulation of physical disability and reduce the frequency of clinical exacerbations .
2. Dosage and Administration
Administration: Oral administration. Capsules should be swallowed whole with water. Can be taken with or without food .
Standard Dose:
Recommended Dose: 0.5 mg once daily .
Dose Limit: Increasing the dose to 1.25 mg does not provide additional efficacy and is associated with a higher incidence of adverse reactions .
First-Dose Monitoring: Due to the risk of bradycardia and atrioventricular (AV) block, patients require monitoring for at least 6 hours after the first dose. Baseline ECG is required prior to dosing .
3. Mechanism of Action
Fingolimod is a sphingosine 1-phosphate (S1P) receptor modulator.
It binds to S1P receptors on lymphocytes, causing internalization of the receptor. This prevents lymphocytes from egressing from lymph nodes into the blood and CNS, thereby reducing inflammation and autoimmune damage in the CNS .
4. Safety and Warnings
Bradycardia and AV Block: Can cause a transient decrease in heart rate and AV block. Baseline ECG is mandatory. First-dose monitoring is required for all patients .
Macular Edema: May cause macular edema. A comprehensive eye exam is recommended prior to treatment and 3-4 months after initiation .
Infections: May increase the risk of infections (e.g., herpes virus, respiratory infections). Do not initiate in patients with active acute or chronic infections .
Hepatotoxicity: Monitor liver enzymes (ALT, AST) regularly. Discontinue if severe liver injury occurs .
Fetal Toxicity: May cause fetal harm. Pregnancy is contraindicated. Contraception is required during treatment and for at least 2 months after discontinuation .
5. Adverse Reactions
Common adverse reactions (incidence ≥10%) include:
Infections: Headache, influenza, nasopharyngitis.
Gastrointestinal: Diarrhea.
Musculoskeletal: Back pain, pain in extremities.
Laboratory Abnormalities: Increased liver enzymes (ALT, AST), decreased lymphocyte count .
6. Drug Interactions
Antiarrhythmic Drugs: Concomitant use with Class Ia (e.g., quinidine) or Class III (e.g., dofetilide) antiarrhythmics is contraindicated due to risk of fatal arrhythmias .
CYP3A Inhibitors: Co-administration with strong CYP3A inhibitors (e.g., ketoconazole) increases Fingolimod exposure; caution is advised .
Vaccines: Avoid live attenuated vaccines during treatment and for 2 months after discontinuation .
7. Pharmaceutical Information
Chemical Name: (2S)-2-[2-(4-octylphenyl)ethyl]-1-amino-1,3-propanediol hydrochloride .
Molecular Formula: C19H33NO2 · HCl .
Storage: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) .