Gilenya (Fingolimod) - Oral

What Is Gilenya?

Gilenya (fingolimod) is an immune modulator used to treat people with relapsing forms of multiple sclerosis (MS). It belongs to a class of medications called sphingosine 1-phosphate receptor modulators.

In MS, the immune system attacks your central nervous system (CNS), which causes your symptoms. Gilenya is metabolized to the active metabolite fingolimod-phosphate, which blocks lymphocytes from emerging from lymph nodes. Lymphocytes are a type of white blood cell released by the immune system to fight infection or disease. It's not clear how Gilenya exerts a therapeutic effect in MS, but it may be related to reducing lymphocyte migration into the CNS, thereby preventing lymphocytes from attacking the CNS.

Gilenya is available by prescription as an oral capsule.

Drug Facts

Generic Name: Fingolimod

Brand Name(s): Gilenya, Tascenso ODT

Drug Availability: Prescription

Administration Route: Oral

Therapeutic Classification: Immune modulator

Available Generically: Yes

Controlled Substance: N/A

Active Ingredient: Fingolimod

Dosage Form(s): Capsule

What Is Gilenya Used For?

The Food and Drug Administration (FDA) approved Gilenya to treat relapsing forms of MS, including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease in people 10 years of age and older.

How to Take Gilenya

Take Gilenya with or without food, exactly as prescribed (usually once a day). When starting Gilenya, your healthcare provider will observe you for six hours after the first dose to monitor for bradycardia (slower-than-normal heartbeat). This may require you to stay in the clinic or hospital for monitoring.

Storage

Store Gilenya capsules at room temperature, and protect them from light and moisture.

How Long Does Gilenya Take to Work?

Fingolimod begins to decrease peripheral lymphocyte count within five to six hours of the first dose. Lymphocyte counts continue to decrease over a two-week period and are maintained with daily dosing of Gilenya.

What Are the Side Effects of Gilenya?

This is not a complete list of side effects and others may occur. A healthcare provider can advise you on side effects. If you experience other effects, contact your pharmacist or a healthcare provider You may report side effects to the FDA at fda.gov/medwatch or 1-800-FDA-1088.

Common Side Effects

Common side effects of Gilenya include:

  • Abdominal pain
  • Diarrhea
  • Increased liver enzymes
  • Influenza (flu)
  • Back pain
  • Pain in extremities
  • Headache
  • Cough
  • Sinusitis

Severe Side Effects

Call your healthcare provider right away if you have serious side effects. Call 911 if your symptoms feel life-threatening or if you think you’re having a medical emergency. Serious side effects can include the following:

  • Bradycardia (abnormally slow heartbeat) or atrioventricular block
  • Skin cancer
  • Lymphocytopenia (low white blood cells)
  • Infections including herpes virus, human papillomavirus, cryptococcal meningitis
  • Progressive multifocal leukoencephalopathy (PML)
  • Macular edema
  • Liver injury

Long-Term Side Effects

Even after stopping Gilenya, its effects on lymphocytes may persist for up to two months after the last dose. Lymphocyte counts return to the normal range within one to two months after stopping the medication. During this time period, healthcare providers should use caution when prescribing other immune suppressing medications.

Report Side Effects

Gilenya may cause other side effects. Call your healthcare provider if you have any unusual problems while taking this medication. If you experience a serious side effect, you or your healthcare provider may send a report to the FDA's MedWatch Adverse Event Reporting Program or by phone (800-332-1088).

Dosage: How Much Gilenya Should I Take?

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The dose of this medicine will be different for different patients. Follow your doctor's orders or the directions on the label. The following information includes only the average doses of this medicine. If your dose is different, do not change it unless your doctor tells you to do so.

The amount of medicine that you take depends on the strength of the medicine. Also, the number of doses you take each day, the time allowed between doses, and the length of time you take the medicine depend on the medical problem for which you are using the medicine.

  • For oral dosage form (capsules):
    • For multiple sclerosis:
      • Adults and children 10 years of age and older weighing more than 40 kilograms (kg)—0.5 milligrams (mg) once a day.
      • Children 10 years of age and older weighing 40 kg or less—0.25 mg orally once a day.
      • Children younger than 10 years of age—Use and dose must be determined by your doctor.

Modifications

Safe use of Gilenya in pregnancy has not been established, and there is evidence of potential fetal harm based on nonhuman animal studies. Use effective contraception while taking Gilenya and for two months after stopping the medication. If you plan to become pregnant, stop using Gilenya at least two months before planned conception.   

It is not known if Gilenya is excreted in human breast milk, and there are no published reports of fingolimod use during breastfeeding. The expert opinion recommends avoiding this drug during breastfeeding as it is potentially toxic to breastfed infants, especially while nursing a preterm or newborn infant.

The safety and efficacy of Gilenya in children aged 10 to 17 years were established in one clinical trial. The safety profile was similar to that seen in adults, except more children who received Gilenya experienced seizures (5.6%) compared with the other group who received interferon beta-1a (0.9%). The safety and efficacy of Gilenya in children under the age of 10 is not known.

Clinical trials of Gilenya did not include enough older adults (aged 65 years and older) to determine if there is a difference in safety or efficacy in this age group. In general, use caution in older adults who may have decreased liver or kidney function. 

Missed Dose

Call your healthcare provider right away if you miss a dose of Gilenya. You may need to be observed by a healthcare provider for six hours when you restart Gilenya.

Overdose: What Happens If I Take Too Much Gilenya?

Overdoses of Gilenya should be treated symptomatically. Symptoms of overdose are expected to be similar to adverse effects and may include:

  • Slow heart rate (bradycardia)
  • Dizziness
  • Fainting
  • Difficulty breathing

Atropine or isoproterenol may be indicated for clinically significant bradycardia.

What Happens If I Overdose on Gilenya?

If you think you or someone else may have overdosed on Gilenya, call a healthcare provider or the Poison Control Center (800-222-1222).

If someone collapses or isn't breathing after taking Gilenya, call 911 immediately.

Precautions

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It is very important that your doctor check your or your child's progress at regular visits to make sure that this medicine is working properly. Blood and urine tests and tests for heart function may be needed to check for unwanted effects.

Using this medicine while you are pregnant can harm your unborn baby. Use an effective form of birth control to keep from getting pregnant. You should not become pregnant during treatment with this medicine and for 2 months after the last dose. If you think you have become pregnant while using the medicine, tell your doctor right away.

This medicine may cause your or your child's heart rate to slow down, especially after taking the first dose. You or your child will be observed in a hospital or clinic for 6 hours for signs and symptoms of bradycardia (slow heartbeat). Symptoms may include chest pain or discomfort, lightheadedness, dizziness, or fainting, slow or irregular heartbeat, or unusual tiredness.

Fingolimod can temporarily lower the number of white blood cells in your blood, increasing the chance of getting an infection (including a serious brain infection called progressive multifocal leukoencephalopathy), which could be life-threatening. Reported infections also include bronchitis, pneumonia, varicella zoster, or herpes simplex. This risk could last up to 2 months after you stop fingolimod treatment. If you can, avoid people with infections. Check with your doctor right away if you think you or your child have an infection or if you have a fever or chills, cough or hoarseness, lower back or side pain, or painful or difficult urination.

While you are being treated with fingolimod, and for 2 months after you stop treatment with it, do not have any immunizations (vaccines) without your doctor's approval. Your child should also have a complete immunization record before starting treatment with this medicine. Fingolimod may lower your or your child's body's resistance and the vaccine may not work as well or you might get the infection the vaccine is meant to prevent. In addition, you or your child should not be around other persons living in your household who receive live virus vaccines because there is a chance they could pass the virus on to you. Some examples of live vaccines include measles, mumps, influenza (nasal flu vaccine), poliovirus (oral form), rotavirus, and rubella. Do not get close to them and do not stay in the same room with them for very long. If you have questions about this, talk to your doctor.

This medicine may cause macular edema (swelling of the back of the eye), especially during the first 3 to 4 months of treatment. Check with your doctor right away if blurred vision, difficulty in reading, or any other change in vision occurs during or after treatment. Your doctor may want an eye doctor (ophthalmologist) to check your eyes.

This medicine may cause a rare condition called posterior reversible encephalopathy syndrome (PRES). Check with your doctor right away if you or your child have a sudden and severe headache, confusion, vision changes, or seizures with this medicine.

Check with your doctor right away if you or your child have difficult or labored breathing or tightness in the chest while using this medicine.

Check with your doctor right away if you or your child have pain or tenderness in the upper stomach, pale stools, dark urine, loss of appetite, nausea, unusual tiredness or weakness, or yellow eyes or skin. These could be symptoms of a serious liver problem.

This medicine may cause a severe increase in disability, including worsening of MS symptoms (eg, blurred vision, difficulty controlling your bladder or bowels, trouble walking, swallowing, or speaking, numbness or tingling in your arms, legs, or face, muscle spasms) for at least 12 to 24 weeks after stopping the medicine. Talk to your doctor if you have concerns about this.

This medicine may increase your risk of having skin cancer (eg, basal cell carcinoma, melanoma) or lymphoma. Tell your doctor right away if you notice any skin nodules, patches, or open sores that do not quickly heal. Avoid exposure to sunlight. Wear sunscreen with a high sun protection factor. Do not use sunlamps or tanning beds.

This medicine may cause serious allergic reactions, including angioedema, which can be life-threatening and require immediate medical attention. Tell your doctor right away if you or your child have a rash, hives or itching skin, or large, hive-like swelling on the face, eyelids, lips, tongue, throat, hands, legs, feet, or genitals.

Do not take other medicines unless they have been discussed with your doctor. This includes prescription or nonprescription (over-the-counter [OTC]) medicines and herbal or vitamin supplements.

What Are Reasons I Shouldn’t Take Gilenya?

Do not take Gilenya if you have:

  • Experienced myocardial infarction (heart attack), unstable angina, stroke, transient ischemic attack (TIA), heart failure requiring hospitalization, or Class III/IV heart failure in the last six months.
  • Past or current history of Mobitz Type II second-degree or third-degree AV block or sick sinus syndrome without a functioning pacemaker
  • Baseline QTc interval greater than or equal to 500 milliseconds
  • Cardiac arrhythmias requiring treatment with Class Ia or III antiarrhythmic drugs
  • Hypersensitivity reaction to fingolimod or any of the inactive ingredients in Gilenya

What Other Medications Interact With Gilenya?

The following medications may interact with Gilenya if taken together.

QT Prolonging Drugs

Gilenya slows the heart rate and may prolong the QT interval, which can lead to life-threatening arrhythmias. If you need to take QT prolonging drugs with Gilenya, you may need to be monitored overnight with continuous ECG in a medical facility.

QT prolong drugs include, but are not limited to:

  • Citalopram
  • Chlorpromazine
  • Haloperidol
  • Methadone
  • Erythromycin

Ketoconazole

Ketoconazole increases blood levels of Gilenya by 1.7-fold, so close monitoring is required due to the increased risk of side effects. 

Antineoplastic, Immunosuppressive, or Immune-modulating Therapies

When taken with Gilenya, these drugs have additive immune suppression and may further increase the risk of infection.

Drugs That Slow Heart Rate or Atrioventricular Conduction

These drugs have additional heart rate lowering effects when taken with Gilenya, resulting in severe bradycardia or heart block. Consider alternative cardiac medications or use overnight continuous ECG monitoring if the combination is indicated.

These drugs include:

Additionally, taking Gilenya can reduce the immune response to vaccinations. Vaccines may be less effective while taking Gilenya and for two months after stopping it. Avoid live vaccines while taking Gilenya due to the risk of infection. Children should be up to date on vaccinations before starting Gilenya. 

What Medications Are Similar?

Gilenya is a sphingosine 1-phosphate (S1P) receptor modulator used for relapsing forms of multiple sclerosis. People should only take one S1P receptor modulator at a time. Other S1P receptor modulators include:

  • Zeposia (ozanimod)
  • Ponvory (ponesimod)
  • Mayzent (siponimod)

Frequently Asked Questions

  • What is Gilenya used for?

    Gilenya is used to treat relapsing forms of multiple sclerosis.

  • How does Gilenya work?

    Gilenya is metabolized to the active metabolite fingolimod-phosphate, which blocks lymphocytes from emerging from lymph nodes, thereby reducing the number of lymphocytes in peripheral circulation. It’s not clear how fingolimod exerts a therapeutic effect in MS but may be related to decreasing the release of lymphocytes into the central nervous system.

  • What side effects can I expect while taking Gilenya?

    The most common side effects of Gilenya are abdominal pain, diarrhea, headache, cough, influenza, and other infections.

How Can I Stay Healthy While Taking Gilenya?

Take Gilenya as prescribed; do not stop taking it without first discussing it with your healthcare provider. Starting Gilenya temporarily decreases heart rate, and you will need to be monitored by a healthcare provider when starting, restarting after stopping, or increasing the dose of this medication. 

Gilenya can increase the risk of infections, some of which could be life-threatening. Contact your healthcare provider if you develop symptoms of infection. 

Other symptoms for which you should seek immediate evaluation by a healthcare provider include:

  • Progressive weakness on one side of the body or clumsiness of limbs
  • Visual disturbances
  • Changes in thinking, memory, or personality
  • Severe headache
  • Unexplained nausea
  • Vomiting
  • Jaundice
  • New or worsening breathing problems  

Basal cell carcinoma and melanoma are associated with Gilenya use. Have any suspicious skin lesions promptly evaluated by a healthcare provider. Limit exposure to sunlight and ultraviolet light to decrease the risk of skin cancer. Wear protective clothing and sunscreen. 

If you are a person of childbearing potential, discuss contraception options with your healthcare provider. 

Medical Disclaimer

Verywell Health's drug information is meant for educational purposes only and is not intended to replace medical advice, diagnosis, or treatment from a healthcare provider. Consult your healthcare provider before taking any new medication(s). IBM Watson Micromedex provides some of the drug content, as indicated on the page.

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3 Sources
Verywell Health uses only high-quality sources, including peer-reviewed studies, to support the facts within our articles. Read our editorial process to learn more about how we fact-check and keep our content accurate, reliable, and trustworthy.
  1. Food and Drug Administration. Gilenya prescribing information.

  2. Fingolimod. In: Drugs and Lactation Database (LactMed). National Library of Medicine (US);2006.

  3. Stephenson M, Wong A, Rotella JA, et al. Deliberate fingolimod overdose presenting with delayed hypotension and bradycardia responsive to atropine. J Med Toxicol. 2014;10(2):215-8. doi: 10.1007/s13181-013-0354-3