Fingolimod

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 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.ICD-10: G35

• 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 [see Warnings and Precautions ( 5.1 )] a baseline QTc interval ≥500 msec cardiac arrhythmias requiring anti-arrhythmic treatment with Class Ia or Class III anti-arrhythmic drugs had a hypersensitivity reaction to fingolimod or any of the excipients in fingolimod capsules. Observed reactions include rash, urticaria and angioedema upon treatment initiation [see Warnings and Precautions ( 5.14 )].contraindicated

· Assessments are required prior to initiating fingolimod capsules. ( 2.1 ) · 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. ( 2.4 ) o Monitor until resolution if heart rate < 45 beats per minute (bpm) in adults, < 55 bpm in patients aged 12 years and above, or < 60 bpm in pediatric patients aged 10 to below 12 years, atrioventricular (AV) block, or if lowest postdose heart rate is at the end of the observation period. ( 2.4 ) o Monitor symptomatic bradycardia with ECG until resolved. Continue overnight if intervention is required; repeat first-dose monitoring for second dose. ( 2.4 ) o Observe patients overnight if at higher risk of symptomatic bradycardia, heart block, prolonged QTc interval, or if taking drugs with known risk of torsades de pointes. ( 2.4 , 7.1 ) 2.1 Assessment Prior to Initiating Fingolimod Cardiac Evaluation Obtain a cardiac evaluation in patients with certain preexisting conditions [ see Warnings and Precautions ( 5.1 )] . Prior to starting treatment, determine whether patients are taking drugs that could slow heart rate or atrioventricular (AV) conduction [see Dosage and Administration ( 2.4 ), Drug Interactions ( 7.5 )] .

• 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. ( 5.2 ) • Progressive Multifocal Leukoencephalopathy (PML): Withhold fingolimod at the first sign or symptom suggestive of PML. ( 5.3 ) • 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. Conduct an evaluation of the fundus, including the macula, 3 to 4 months after treatment start, periodically while on therapy and any time there is a change in vision. Consider discontinuing fingolimod if macular edema develops. Diabetes mellitus and uveitis increase the risk. ( 5.4 ) • Liver Injury : Obtain liver enzyme results before initiation and periodically during treatment. Closely monitor patients with severe hepatic impairment. Discontinue if there is evidence of liver injury without other cause. ( 5.5 , 8.6 , 12.3 ) • Posterior Reversible Encephalopathy Syndrome (PRES): If suspected, discontinue fingolimod. ( 5.6 ) • Respiratory Effects: Evaluate when clinically indicated. ( 5.7 ) • Fetal Risk: May cause fetal harm. Advise females of reproductive potential of the potential risk to a fetus and to use an effective method of contraception during treatment and for 2 months after stopping fingolimod.

The following serious adverse reactions are described elsewhere in labeling: Bradyarrhythmia and Atrioventricular Blocks [see Warnings and Precautions ( 5.1 )] Infections [see Warnings and Precautions ( 5.2 )] Progressive Multifocal Leukoencephalopathy [see Warnings and Precautions ( 5.3 )] Macular Edema [see Warnings and Precautions ( 5.4 )] Liver Injury [ see Warnings and Precautions ( 5.5 ) ] Posterior Reversible Encephalopathy Syndrome [ see Warnings and Precautions ( 5.6 ) ] Respiratory Effects [ see Warnings and Precautions ( 5.7 ) ] Fetal Risk [see Warnings and Precautions ( 5.8 )] Severe Increase in Disability After Stopping Fingolimod [see Warnings and Precautions ( 5.9 )] Tumefactive Multiple Sclerosis [see Warnings and Precautions ( 5.10 )] Increased Blood Pressure [see Warnings and Precautions ( 5.11 )] Malignancies [see Warnings and Precautions ( 5.12 ) ] Immune System Effects Following fingolimod Discontinuation [see Warnings and Precautions ( 5.13 )] Hypersensitivity Reactions [see Warnings and Precautions ( 5.14 )] Most common adverse reactions (incidence ≥10% and greater than placebo): Headache, liver transaminase elevation, diarrhea, cough, influenza, sinusitis, back pain, abdominal pain, and pain in extremity. ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Ascend Laboratories, LLC at 1-877-272-7901 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

8.1 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). Data from prospective reports to the pregnancy registry are currently not sufficient to allow for an adequate assessment of the drug-associated risk for miscarriage. Based on findings from animal studies, fingolimod may cause fetal harm when administered to a pregnant woman. In oral studies conducted in rats and rabbits, fingolimod demonstrated developmental toxicity, including an increase in malformations (rats) and embryolethality, when given to pregnant animals. In rats, the highest no-effect dose was less than the recommended human dose of 0.5 mg/day on a body surface area (mg/m2) basis. The most common fetal visceral malformations in rats were persistent truncus arteriosus and ventricular septal defect. The receptor affected by fingolimod (sphingosine 1-phosphate receptor) is known to be involved in vascular formation during embryogenesis (see Data). Advise pregnant women of the potential risk to a fetus.

Metabolism

Absorption The T max of fingolimod is 12 to 16 hours. The apparent absolute oral bioavailability is 93%.

Fingolimod can induce bradycardia as well as AV conduction blocks (including complete AV block). The decline in heart rate usually starts within 1 hour of the first dose and is maximal within 6 hours in most patients [ see Warnings and Precautions ( 5.1 ) ] . In case of fingolimod overdosage, observe patients overnight with continuous ECG monitoring in a medical facility, and obtain regular measurements of blood pressure [ see Dosage and Administration ( 2.4 ) ] . Neither dialysis nor plasma exchange results in removal of fingolimod from the body.

• Sep 21, 2010NDANDA022527Novartis
• Dec 4, 2019ANDAANDA207979Biocon Ltd
• Dec 4, 2019ANDAANDA208014Sun Pharm
• May 18, 2020ANDAANDA207933Hetero Labs Ltd V
• Jun 18, 2020ANDAANDA207985Glenmark Pharms Ltd
• Jul 2, 2020ANDAANDA208008Teva Pharms Usa
• Oct 14, 2020ANDAANDA207994Zydus Pharms
• Dec 9, 2022NDANDA214962Cycle

1. 1Fatigue10,87713%
2. 2Multiple Sclerosis Relapse7,8029.0%
3. 3Headache7,3078.5%
4. 4Dizziness5,4136.3%
5. 5White Blood Cell Count Decreased4,0044.6%
6. 6Gait Disturbance3,8864.5%
7. 7Hypoaesthesia3,8044.4%
8. 8Lymphocyte Count Decreased3,5924.2%
9. 9Fall3,5074.1%
10. 10Nausea3,4514.0%
11. 11Drug Ineffective3,1703.7%
12. 12Malaise3,1483.6%
13. 13Memory Impairment2,9843.5%
14. 14Pain2,9533.4%
15. 15Central Nervous System Lesion2,9133.4%

Recent PubMed references pinned to Fingolimod as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Fingolimod increases cellular resistance to HIV-1 infection and limits viral reservoir size in peripheral CD4+ T-cells.
  PLoS pathogens · 2026 · Moraga E, Climent N, Sánchez-Molina A, et al.
  PMID 42234672DOI 10.1371/journal.ppat.1014266
• Investigating FTY720-NF immunomodulation of key lipid, gene, and protein mediators to enhance oral tissue regeneration.
  Biomaterials advances · 2026 · Toma AI, Shah DC, Duke VR, et al.
  PMID 42161013DOI 10.1016/j.bioadv.2026.214952
• Do apelin and ghrelin play a role in multiple sclerosis? The analysis of patients treated with immunomodulatory therapies.
  Frontiers in immunology · 2026 · Adamczyk B, Morawiec N, Rakoca M, et al.
  PMID 42131351DOI 10.3389/fimmu.2026.1701657
• Polypharmacologic phosphoinositide modulation by FTY720 triggers endomembrane trafficking collapse and metabolic starvation in cancer cells.
  Biochemical and biophysical research communications · 2026 · Kofuji S, Sumita K, Ikeda Y, et al.
  PMID 41924780DOI 10.1016/j.bbrc.2026.153671
• Comparative assessment of treatment switching in patients with multiple sclerosis receiving cladribine tablets versus fingolimod, dimethyl fumarate, and teriflunomide.
  Multiple sclerosis and related disorders · 2026 · Lobo C, Rey GG, Zhao X, et al.
  PMID 41894909DOI 10.1016/j.msard.2026.107143
• Therapeutic Potential of Fingolimod and Dimethyl Fumarate in Preclinical Pancreatic Cancer Models.
  Oncology research · 2026 · Gousseau P, Genest L, Froget G, et al.
  PMID 41799523DOI 10.32604/or.2025.072141
• Therapeutic effects of fingolimod through sphingosine-1-phosphate signaling in pulmonary arterial hypertension.
  Journal of pharmacological sciences · 2026 · Fujiwara M, Yamamura A, Kondo R, et al.
  PMID 41795957DOI 10.1016/j.jphs.2026.02.002
• FTY-720 pre-treatment attenuates acute lung injury following bilateral renal ischemia/reperfusion but not bilateral nephrectomy.
  Scientific reports · 2026 · Alebrahimdehkordi N, Karimi Z, Owji SM, et al.
  PMID 41730927DOI 10.1038/s41598-026-38140-3

The 10 most recently updated of 137 ClinicalTrials.gov registrations naming Fingolimod as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• Safety and Efficacy of Fingolimod in Pediatric Patients With Multiple Sclerosis
  Active not recruiting · Phase 3 · Interventional · 240 enrolled · Novartis Pharmaceuticals
  NCT01892722updated 2026-06-08
• A Study to Learn More About The Safety of Diroximel Fumarate (VUMERITY®) in Participants Who Took it During Pregnancy And About the Health of Their Babies
  Active not recruiting · Observational · 1,178 enrolled · Biogen
  NCT05688436updated 2026-06-04
• Safety and Efficacy Study of Fingolimod in Taiwanese Adults (≥ 20years) With Relapsing Remitting Multiple Sclerosis
  Recruiting · Phase 4 · Interventional · 30 enrolled · Novartis Pharmaceuticals
  NCT04480853updated 2026-05-29
• Efficacy and Safety of Ofatumumab and Siponimod Compared to Fingolimod in Pediatric Patients With Multiple Sclerosis
  Active not recruiting · Phase 3 · Interventional · 129 enrolled · Novartis Pharmaceuticals
  NCT04926818updated 2026-05-14
• Study to Assess Effects of Ublituximab in Pediatric Participants With Relapsing Forms of Multiple Sclerosis
  Not yet recruiting · Phase 2 · Phase 3 · Interventional · 240 enrolled · TG Therapeutics, Inc.
  NCT07220252updated 2026-05-12
• Study to Evaluate the Effectiveness and Safety of Ozanimod Compared to Fingolimod in Children and Adolescents With Relapsing Remitting Multiple Sclerosis
  Recruiting · Phase 3 · Interventional · 194 enrolled · Bristol-Myers Squibb
  NCT06408259updated 2026-04-28
• An Open-label Study Evaluating Ofatumumab Treatment Effectiveness and PROs in Subjects With RMS Transitioning From Fumarate-based RMS Approved Therapies or Fingolimod to Ofatumumab
  Completed · Phase 3 · Interventional · 562 enrolled · Novartis Pharmaceuticals
  NCT04353492updated 2026-04-09
• Phase 2 Study of Fingolimod in Lung Cancers
  Recruiting · Phase 2 · Interventional · 38 enrolled · Medical University of South Carolina
  NCT06424067updated 2026-03-30
• A Study to Learn About the Safety of Diroximel Fumarate (DRF) and Dimethyl Fumarate (DMF) and Their Effects on Relapses in Pediatric Participants With Relapsing Forms of Multiple Sclerosis (RMS)
  Not yet recruiting · Phase 3 · Interventional · 185 enrolled · Biogen
  NCT07483632updated 2026-03-19
• Study of the Mechanisms of Action of Cladribine in Multiple Sclerosis
  Completed · Interventional · 77 enrolled · University Hospital, Rouen
  NCT04821596updated 2026-02-18

Frequently asked questions

How does Fingolimod work?

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.

What is Fingolimod used for?

According to FDA labeling, Fingolimod carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Fingolimod?

Fingolimod is classified as Sphingosine-1-phosphate (S1P) receptor modulators, Sphingosine 1-phosphate Receptor Modulator, Sphingosine 1-Phosphate Receptor Modulators, Decreased Lymphocyte Activation.

What are the brand names for Fingolimod?

Fingolimod is marketed under brand names including Gilenya, Tascenso.

What are the contraindications for Fingolimod?

Fingolimod labeling lists contraindications including: 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 [see Warnings and Precautions ( 5.1 )] a baseline QTc interval ≥500 msec cardiac arrhythmias requiring anti-arrhythmic treatment with Class Ia or Class III anti-arrhythmic drugs had a hypersensitivity reaction to fingolimod or any of the excipients in fingolimod capsules. Observed reactions include rash, urticaria and angioedema upon treatment initiation [see Warnings and Precautions ( 5.14 )].. Always consult the full prescribing information and a clinician.