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Gilenya (FINGOLIMOD)
Gilenya works by binding to and blocking the S1P1 receptor, preventing immune cells from leaving the lymph nodes and reducing inflammation in the central nervous system.
Gilenya (Fingolimod) is a small molecule sphingosine 1-phosphate receptor modulator developed by Novartis, targeting the S1P1 receptor to treat relapsing-remitting multiple sclerosis. It was FDA-approved in 2010 and remains a branded product, with 17 generic manufacturers available. Gilenya has a half-life of 144 hours and 93% bioavailability. Key safety considerations include bradycardia and increased risk of infections. As a branded product, its commercial status is not off-patent.
At a glance
| Generic name | FINGOLIMOD |
|---|---|
| Sponsor | Novartis |
| Drug class | Sphingosine 1-phosphate Receptor Modulator |
| Target | Sphingosine 1-phosphate receptor 1 |
| Modality | Small molecule |
| Therapeutic area | Immunology |
| Phase | FDA-approved |
| First approval | 2010 |
Mechanism of action
Fingolimod is metabolized by sphingosine kinase to the active metabolite, fingolimod-phosphate. Fingolimod-phosphate is 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.
Approved indications
- Relapsing remitting multiple sclerosis
Common side effects
- Liver transaminase elevations
- Serum transaminase elevations
- Basal cell carcinoma
- Hemolytic anemia
- Thrombocytopenia
- Liver injury
- Cryptococcal infections
- Human papilloma virus (HPV) infection
- Progressive multifocal leukoencephalopathy
- Arthralgia
- Myalgia
- Posterior reversible encephalopathy syndrome
Drug interactions
- High Risk QT Prolonging Agents
- amiodarone
- atenolol
- betaxolol
- bisoprolol
- carvedilol
- diltiazem
- disopyramide
- dofetilide
- dronedarone
- esmolol
- flecainide
Key clinical trials
- 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) (PHASE3)
- Safety and Efficacy Study of Fingolimod in Taiwanese Adults (≥ 20years) With Relapsing Remitting Multiple Sclerosis (PHASE4)
- Study to Assess Effects of Ublituximab in Pediatric Participants With Relapsing Forms of Multiple Sclerosis (PHASE2,PHASE3)
- Efficacy and Safety of Ofatumumab and Siponimod Compared to Fingolimod in Pediatric Patients With Multiple Sclerosis (PHASE3)
- Study of the Mechanisms of Action of Cladribine in Multiple Sclerosis (NA)
- Study to Evaluate the Effectiveness and Safety of Ozanimod Compared to Fingolimod in Children and Adolescents With Relapsing Remitting Multiple Sclerosis (PHASE3)
- A Study to Evaluate Safety and Efficacy of Ocrelizumab in Comparison With Fingolimod in Children and Adolescents With Relapsing-Remitting Multiple Sclerosis (RRMS) (PHASE3)
- Study of Efficacy and Safety of Fingolimod (Gilenya) 0.5 mg in Chinese Patients With Relapsing Multiple Sclerosis (RMS) Patients (PHASE4)
Patents
| Patent | Expiry | Type |
|---|---|---|
Primary sources
Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.
| Source | Used for |
|---|---|
| FDA label | Mechanism, indications, dosing, boxed warnings, drug interactions |
| ClinicalTrials.gov | Trial enrolment, design, endpoints, results |
| FDA Orange Book | Patents + exclusivity |
Competitive intelligence
For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:
- Gilenya CI brief — competitive landscape report
- Gilenya updates RSS · CI watch RSS
- Novartis portfolio CI