Fingolimod

What it is and how it works

Mechanism of Action Fingolimod is metabolized by sphingosine kinase to the active metabolite, fingolimod-phosphate. Fingolimod-phosphate is a sphingosine 1-phosphate receptor modulator, and binds with high affinity to sphingosine 1-phosphate receptors 1, 3, 4, and 5. Fingolimod-phosphate blocks the capacity of lymphocytes to egress from lymph nodes, reducing the number of lymphocytes in peripheral blood. The mechanism by which fingolimod exerts therapeutic effects in multiple sclerosis is unknown, but may involve reduction of lymphocyte migration into the central nervous system.

Indications

Fingolimod capsules are 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 patients 10 years of age and older. Fingolimod capsules are 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 patients 10 years of age and older.

Dosage and administration (summary)

· Assessments are required prior to initiating fingolimod capsules. · Recommended dosage for adults and pediatric patients (10 years of age and older) weighing more than 40 kg: 0.5 mg orally once daily, with or without food. ( 2.2 , 2.3 ) · First-Dose Monitoring (including reinitiation after discontinuation greater than 14 days and dose increases): o Observe all patients for bradycardia for at least 6 hours; monitor pulse and blood pressure hourly. Electrocardiograms (ECGs) prior to dosing and at end of observation period required.

Contraindications

Fingolimod capsules are contraindicated in patients who have: in the last 6 months experienced myocardial infarction, unstable angina, stroke, transient ischemic attack (TIA), decompensated heart failure requiring hospitalization or Class III/IV heart failure a history or presence of Mobitz Type II second-degree or third-degree AV block or sick sinus syndrome, unless patient has a functioning pacemaker a baseline QTc interval ≥500 msec cardiac arrhythmias requiring anti-arrhythmic treatment with…

Warnings and precautions

• Infections: Fingolimod may increase the risk. Obtain a complete blood count (CBC) before initiating treatment. Monitor for infection during treatment and for 2 months after discontinuation. Do not start in patients with active infections. • Progressive Multifocal Leukoencephalopathy (PML): Withhold fingolimod at the first sign or symptom suggestive of PML. • Macular Edema : Increases the risk of macular edema. Obtain a baseline evaluation of the fundus, including the macula, near the start of treatment with fingolimod.

Pregnancy

Pregnancy Risk Summary Available observational pregnancy registry data suggest that use of fingolimod is associated with an increased prevalence of major birth defects in comparison to the general population. However, limitations in the number of exposed pregnant women and in the study design preclude definitive conclusions (see Data).

Storage and supply

How Supplied Fingolimod capsules 0.5 mg are supplied as follows: hard gelatin capsules with a white opaque body with two radial band imprinted with yellow ink and bright yellow cap imprinted with “FIG 0.5 mg” with black ink.

Source: Fingolimod Hydrochloride (Fingolimod) — US FDA prescribing information, 2026-03-27, DailyMed. Summarised and shortened; the full label governs. Iranian registration, indications and labelling may differ.