Section 04 · Monograph

Fingolimod

Reviewed Nov 2026FDA label

GilenyaS1P receptor modulator

Indications

Treatment of relapsing forms of multiple sclerosis (MS) in patients 10 years of age and older, to include clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive diseaseFDA-labeled

Fingolimod is metabolized by sphingosine kinase to the active metabolite fingolimod-phosphate
Fingolimod-phosphate binds with high affinity to sphingosine 1-phosphate (S1P) receptors 1, 3, 4, and 5 on lymphocytes and cardiac tissue
Causes internalization/degradation of S1P1 receptors, blocking the capacity of lymphocytes to egress from lymph nodes
Results in redistribution (not depletion) of lymphocytes, reducing circulating lymphocyte counts entering the CNS and reducing inflammatory damage
Cardiac S1P1 receptor engagement also underlies the transient first-dose bradycardia and AV conduction effects

First dose requires in-clinic observation for at least 6 hours with hourly pulse and blood pressure measurement, plus ECG before and at end of observation
Extend monitoring if heart rate <45 bpm (adults), <55 bpm (age ≥12), or <60 bpm (age 10–11), if ECG shows new-onset AV block, or if HR is at its lowest post-dose value at 6 hours
Overnight (extended) ECG monitoring recommended for patients with preexisting cardiac conditions, prolonged QTc, or concomitant QT-prolonging or heart-rate-lowering drugs
Same first-dose monitoring protocol recommended when restarting after a treatment interruption, depending on duration of interruption

Adults and pediatric patients >40 kg: 0.5 mg orally once daily, with or without food
Pediatric patients ≤40 kg: 0.25 mg orally once daily

Myocardial infarction, unstable angina, stroke, TIA, or decompensated heart failure (requiring hospitalization) in the last 6 months
Mobitz Type II second-degree or third-degree AV block, or sick sinus syndrome, unless patient has a functioning pacemaker
Baseline QTc interval ≥500 msec
Cardiac arrhythmia requiring treatment with a Class Ia or Class III anti-arrhythmic drug
Known hypersensitivity to fingolimod or any excipient

Ketoconazole (strong CYP3A4/P-gp inhibitor) increases fingolimod exposure by approximately 70%; use with caution
Concomitant heart-rate-lowering drugs (e.g., beta-blockers, calcium channel blockers, digoxin) may cause additive bradycardic effects — consider cardiology consult
Concomitant QT-prolonging drugs warrant extended (overnight) first-dose ECG monitoring
Class Ia and Class III anti-arrhythmic drugs are contraindicated with fingolimod
Live attenuated vaccines should be avoided during treatment and for 2 months after discontinuation
Other immunosuppressive or immune-modulating therapies (including corticosteroids) may have additive immunosuppressive effects

First-dose observation: 6 hours minimum with hourly HR/BP checks and pre/post ECG
Baseline ophthalmic (fundus) exam and follow-up at 3–4 months after starting; more frequent if diabetes or uveitis history
Complete blood count (lymphocytes) before initiation
Baseline and periodic liver function tests (ALT, AST, bilirubin) within 6 months prior to start and periodically thereafter
Varicella zoster virus antibody screening; vaccinate seronegative patients before starting and delay initiation 1 month post-vaccination
Skin examination prior to and periodically during treatment
Blood pressure monitoring during treatment
Monitor for signs/symptoms of infection during treatment and for 2 months after discontinuation
Monitor for symptoms suggestive of PML (progressive weakness, visual disturbance, cognitive/behavioral change) and withhold drug if suspected

May cause fetal harm; animal studies showed developmental toxicity at doses below the recommended human dose
Observational registry data suggest an increased rate of major birth defects (approximately 8.2–10.9%) compared with general population background rate (2–4%), including congenital heart defects, renal/urinary malformations, and limb abnormalities
Females of reproductive potential should use effective contraception during treatment and for 2 months after stopping, reflecting the drug's elimination half-life
No data on presence of fingolimod in human milk; weigh developmental/health benefits of breastfeeding against maternal need for therapy