Fingolimod
Multiple sclerosis disease-modifying therapies
Multiple sclerosis disease-modifying therapies
An oral S1P receptor modulator for relapsing multiple sclerosis that keeps lymphocytes in lymph nodes; the first dose can slow the heart.
Also called: Fingolimod hydrochloride
Quick facts
- Group
- Multiple sclerosis disease-modifying therapies
- Target
- Sphingosine 1-phosphate receptor 1 (S1P1; also S1P3, S1P4, S1P5)
- Used for
- Relapsing forms of multiple sclerosis
- Key effects
- Headache · Raised liver enzymes · Cough
- Monitor
- ECG before the first dose · Complete blood count
- ATC
- L04AE01
No doses: the clinician sets them by the current guideline.
Mechanism of action
The figure shows fingolimod-phosphate, the active form made in the body, bound to the human S1P1 receptor (in complex with its Gi protein).
Fingolimod is a prodrug: sphingosine kinase phosphorylates it to fingolimod-phosphate, which binds S1P receptors 1, 3, 4 and 5 with high affinity. On lymphocytes it causes lasting internalization and loss of S1P1 signalling, so the cells cannot leave lymph nodes. Fewer lymphocytes circulate and fewer reach the central nervous system. S1P receptors on heart cells explain the first-dose slowing of heart rate.
- Sphingosine kinase converts fingolimod to its phosphate
- Fingolimod-phosphate downregulates S1P1 on lymphocytes
- Lymphocytes stay trapped in lymph nodes
- Fewer immune cells reach the brain and spinal cord
Indications
- Relapsing forms of multiple sclerosis (clinically isolated syndrome, relapsing-remitting and active secondary progressive) from 10 years of age Multiple sclerosis →
Adverse effects
Common
- Headache, back pain and limb pain
- Raised liver enzymes
- Diarrhoea and abdominal pain
- Cough, influenza and sinusitis
Contraindications
- Myocardial infarction, unstable angina, stroke, TIA or decompensated heart failure in the last 6 months; class III/IV heart failure
- Mobitz II or third-degree AV block or sick sinus syndrome without a pacemaker
- Baseline QTc of 500 ms or more; arrhythmias treated with class Ia or III antiarrhythmics
- Hypersensitivity
Key interactions
- Beta-blockers, diltiazem, verapamil and other drugs that slow heart rate or AV conduction
- More bradycardia when treatment starts; experience is limited and monitoring is closer
- QT-prolonging drugs; class Ia and III antiarrhythmics
- Risk of serious arrhythmia
- Ketoconazole
- Raises fingolimod exposure
- Live attenuated vaccines
- Avoided during treatment and for 2 months after; responses to other vaccines are weaker
- Immunosuppressants, corticosteroids, other MS therapies (e.g., natalizumab, teriflunomide)
- Additive immunosuppression
What is monitored
- ECG before the first dose and after 6 hours; pulse and blood pressure every hour for 6 hours
- Complete blood count and liver enzymes before starting and periodically
- Varicella-zoster antibodies before starting (vaccinate if negative)
- Eye exam including the macula at baseline and 3 to 4 months later
- Blood pressure and skin checks during treatment
Administration and safety
- The first dose is given where symptomatic bradycardia can be managed
- First-dose monitoring is repeated after an interruption of treatment
- A pregnancy test is done before starting; contraception continues for 2 months after stopping
Pregnancy and breastfeeding
It may cause fetal harm; registry data suggest more major birth defects. Pregnancy is excluded before starting and effective contraception continues for 2 months after stopping.
Nursing care
- Record pulse and blood pressure every hour during the first 6 hours; report slow pulse, dizziness or chest discomfort
- Ask about heart disease, heart-slowing drugs and recent infections before the first dose
- Teach to report blurred vision, fever, rash or new neurological symptoms
- Warn that MS can worsen severely after stopping; doctors plan any switch
Pharmacokinetics
- Absorption
- Oral, once daily
- Metabolism
- Phosphorylated to the active form; metabolized mainly to inactive products excreted in the urine
- Half-life
- About 6 to 9 days; it takes about 2 months to leave the body
Test yourself
Think of the answer, then tap the question to see it.
What must happen to fingolimod before it acts?
It must be phosphorylated by sphingosine kinase to fingolimod-phosphate.
Why are patients monitored for 6 hours after the first fingolimod dose?
It can cause bradycardia and atrioventricular block.
Which eye complication is checked on fingolimod?
Macular oedema.
Which antibody test is done before starting fingolimod?
Varicella-zoster virus antibodies; seronegative patients are vaccinated first.
Connections
← Back to the class: Multiple sclerosis disease-modifying therapies
Educational content on how drugs work; not a prescribing guide and no substitute for a health professional's advice. No doses are given.
Sources: DailyMed - FINGOLIMOD capsule (DailyMed (U.S. National Library of Medicine), 2026); Fingolimod: MedlinePlus Drug Information (MedlinePlus (U.S. National Library of Medicine), 2026); RCSB PDB - 7VIF: Cryo-EM structure of Gi coupled Sphingosine 1-phosphate receptor bound with (S)-FTY720-P (RCSB Protein Data Bank, 2026).
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Representative model, for educational purposes only.