Fingolimod
GILENYA
What it isSphingosine-1-phosphate receptor modulator trapping lymphocytes in nodes; relapsing multiple sclerosis.
Why this oneThe first oral disease-modifying therapy in MS, once daily.
What limits itFirst-dose bradycardia requires six hours of observation. Macular edema, lymphopenia, and severe rebound disease on stopping.
FDA-approved for
- relapsing multiple sclerosis (2010)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Relapsing forms of multiple sclerosis | Adults | 0.5 mg QD | 0.5 mg QD | 0.5 mg QD |
| Relapsing forms of multiple sclerosis | Peds ≥10y, >40 kg | 0.5 mg QD | 0.5 mg QD | 0.5 mg QD |
| Relapsing forms of multiple sclerosis | Peds ≥10y, ≤40 kg | 0.25 mg QD | 0.25 mg QD | 0.25 mg QD |
Renal Undefined
Hepatic No adjustment for mild-moderate impairment; closely monitor severe impairment
Instructions
- Take with or without food
- First-dose 6-hour cardiac monitoring (hourly pulse/BP; ECG before and after) at initiation, at reinitiation after >14-day interruption, and with pediatric dose increases
- Observe overnight if higher risk of symptomatic bradycardia, heart block, prolonged QTc, or on drugs with torsades risk
Contraindications
- Within prior 6 months: MI, unstable angina, stroke, TIA, decompensated HF requiring hospitalization, or Class III/IV HF
- History of Mobitz II 2nd-degree or 3rd-degree AV block or sick sinus syndrome, unless a pacemaker is present
- Baseline QTc ≥500 msec
- Cardiac arrhythmias requiring Class Ia or Class III antiarrhythmic drugs
Cautions
- Bradyarrhythmia and AV block (first-dose)
- Infections, incl. PML, cryptococcal, and herpes viral infections
- Macular edema
- Liver injury
- Posterior reversible encephalopathy syndrome (PRES)
- Fetal risk
- Severe increase in disability after stopping
- Increased blood pressure
- Malignancies (skin); baseline skin exam
Adverse reactions
- Headache
- Liver transaminase elevation
- Diarrhea
- Cough
- Influenza
- Sinusitis
- Back pain
- Abdominal pain
- Pain in extremity
Pregnancy May cause fetal harm; registry data suggest increased major birth defects. Stop 2 months before conception; use effective contraception during and for 2 months after.
Lactation No human data; present in rat milk. Weigh developmental/health benefits of breastfeeding against maternal need.
NO BOXED WARNINGS
Principal riskFirst-dose bradycardia; severe rebound on stopping
Cost, est. cash$1,000–$15,000+/month
Generic entry2019
Classes and tags
Clinical profile
Legacy pregnancy categoryNot assigned — PLLR-era drug
Defining liabilitySerious infection, cytopenias, hepatic injury and malignancy risk require laboratory and clinical monitoring.
Mechanism of action: Fingolimod ballicule
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Memory aids: mascots and interaction avatars
QT prolongation