The information in this medication sheet has been adapted from the FDA-approved prescribing information for Gilenya.
Gilenya™ is a new class of medication called a sphingosine 1-phosphate receptor modulator, which is thought to act by retaining certain white blood cells (lymphocytes) in the lymph nodes, thereby preventing those cells from crossing the blood-brain barrier into the central nervous system (CNS). Preventing the entry of these cells into the CNS reduces inflammatory damage to nerve cells.
Gilenya was evaluated in two large-scale, phase III clinical trials involving people with relapsing-remitting MS:
- In a two-year study (FREEDOMS) comparing two doses of Gilenya to placebo, Gilenya (at the lower, 0.5mg dose) reduced relapses by 54% and reduced the risk of disability progression by 30% compared to placebo. Gilenya also reduced brain lesion activity as measured by MRI.
- In a one-year study (TRANSFORMS) comparing two doses of Gilenya to interferon beta-1a (Avonex), Gilenya (at the lower, 0.5mg dose) reduced relapses by 52% compared with Avonex; reduced disease activity as measured by the number of new and newly enlarged T2 lesions on MRI scans compared with Avonex (1.6 vs 2.6, respectively at one year); reduced brain lesion activity as measured by MRI.
In August 2011, the FDA approved an update in the prescribing information for Gilenya to include the MRI findings from both the TRANSFORMS and FREEDOMS studies. In both clinical trials, Gilenya showed a reduction in gadolinium-enhancing lesions, which indicate new MS activity. The data from the TRANSFORMS study indicated that at 12 months, the mean number of gadolinium-enhancing T1 lesions was significantly lower for patients treated with Gilenya at the 0.5 mg dose than for patients taking interferon beta-1a (Avonex), 0.2 vs 0.5 respectively. In the FREEDOMS trial, the mean number of gadolinium-enhancing T1 lesions was significantly lower at 24 months for the group treated with Gilenya (0.5 mg dose) than for the placebo group, 0.2 vs 1.1.
Gilenya has not been studied in people under the age of 18.
Approval by the U.S. Food and Drug Administration (FDA)
Gilenya was approved by the U.S. Food and Drug Administration (FDA) in 2010 for adults with relapsing forms of MS to reduce the frequency of clinical relapses and to delay the accumulation of physical disability.
In April, 2012, the FDA (along with the European Medicines Agency -- EMA) revised the prescribing information for Gilenya based on independent safety reviews initiated by the agencies after deaths had been reported among patients taking Gilenya. The revised prescribing information defines who should avoid using this MS therapy based on pre-existing medical conditions, and alters the recommended testing and heart monitoring that occurs when the first dose is given:
- All those starting treatment with Gilenya should have an electrocardiogram prior to dosing and after the 6-hour observation period. During the observation period, blood pressure and heart rate should be measured hourly.
- People whose first-dose monitoring indicates potentially unsafe heart events may require longer monitoring, and any who require treatment for low heart rate during the first-dose monitoring will need to be monitored overnight.
- Gilenya is not advisable for people who have had a history or presence of specific heart and vascular conditions, including heart attack, stroke, and heartbeat irregularities, and people taking heart rate-lowering medication.
- If anyone with a pre-existing heart condition is started on Gilenya, after the first dose the patient should be monitored overnight with continuous electrocardiogram in a medical facility.
- The heart function monitoring applies only to people initiating their first dose, and not to people who are already taking daily doses of Gilenya. There are also revised recommendations for people who re-initiate treatment after discontinuing Gilenya. People should not make changes to their Gilenya therapy without consulting their prescriber.
- Gilenya (0.5mg) is a capsule taken once per day by mouth.
- Higher doses of this medication are associated with a greater risk of adverse events without additional benefit.
The medication can be taken with or without food. Prior to starting this medication, the prescribing information for Gilenya recommends that your doctor do the following tests:
- A new or recent blood test to establish lymphocyte (immune cell) count;
- An eye (ophthalmologic) evaluation;
- A new or recent blood test to evaluate liver enzyme levels;
- A new or recent electrocardiogram in those using heart medications, those who have cardiac risk factors, or those who on examination have slow or irregular heart beat prior to starting Gilenya;
- Those who do not have a history of chickenpox or vaccination against varicella zoster virus (VZV) should be tested for VZV antibodies, and those who are negative should consider vaccination before starting treatment with Gilenya.
- Your first dose of the medication will be given in a doctor’s office, where you will be observed for six hours for signs and symptoms that may be associated with decreased heart rate and other possible heart effects.
- While on therapy, your doctor will probably evaluate your vision during routine visits.
- Do not stop taking the medication without talking with your doctor.
- If you re-start Gilenya after stopping for two or more weeks, you will need to take the first dose in the doctor’s office.
- Store the medication in a dry place at room temperature.
Warnings and Precautions
- Before starting Gilenya, it is important to tell your doctor about all of the medications you are taking, including medicines for heart problems or high blood pressure, vacines, other medications to control your immune system or treat cancer, or ketoconazole (an anti-fungal) by mouth.
- Before starting Gilenya, it is important to tell your doctor about any medical conditions you have, including irregular or abnormal heartbeat, a heart rate less than 55 beats a minute, a history of fainting, a fever or infection, eye problems (especially an inflammation of the eye called uveitis), diabetes, breathing problems, liver problems, high blood pressure.
- Gilenya may cause your heart rate to slow down, particularly right after the first dose, with the drop being most significant at about six hours after the dose is taken. Your doctor will monitor you during this six-hour period. Your heart rate is likely to return to normal within one month of starting the medication, but feelings of dizziness and tiredness, or a slowed or uneven heartbeat should be reported to your doctor.
- Because Gilenya lowers the number of lymphocytes in the blood, you may be at greater risk of infection. It is recommended that your doctor perform a blood test prior to treatment to determine your white blood cell count. After starting treatment, contact your doctor right away if you have fever, unusual tiredness, body aches, chills, nausea, or vomiting. White blood cell counts generally return to normal approximately two months after stopping this medication.
- Gilenya can cause a swelling of the macula (a spot in the center of retina of the eye), generally within 3-4 months of starting treatment. Macular swelling can cause symptoms similar to those that occur with an attack of optic neuritis, or may not be noticed at all. It is recommended that your doctor test your vision before starting treatment and then three to four months later, or any time that you notice any changes in your vision, including blurriness or shadows in the center of your vision, a blind spot in the center of your vision, sensitivity to light, or changes in your color vision.
- Gilenya may cause liver problems. Your physician will do a blood test to check your liver functions prior to starting treatment. Once you are on treatment, notify the doctor right away if you have nausea, vomiting, stomach pain, loss of appetite, unusual tireness, dark uring or a yellowish tint to your skin or the whites of your eyes.
- Gilenya may cause shortness of breath in some people. Contact your doctor immediately if you experience any difficulty breathing.
- Prior to treatment, your doctor may do a test to determine if you have ever had the chicken pox. If it cannot be confirmed that you have had the chicken pox in the past, your doctor may recommend that you get the chicken pox (varicelle) vaccine and wait one month before starting treatment with Gilenya.
- Women who are pregnant or considering becoming pregnant should discuss this with their doctor before starting treatment with Gilenya. This medication can cause harm to a fetus, so effective birth control should be used while on the medication and for two months after stopping the medication.
- It is not known whether Gilenya passes through breast milk. Because of the risk of serious reactions in nursing infants, women will need to discuss with their physician whether to discontinue the medication or discontinue nursing. You cannot do both.
Possible Side Effects
The most common side effects in the clinical trials of Gilenya were headache, influenza, diarrhea, back pain, abnormal liver tests, and cough.
For information about Gilenya, contact Novartis AG at 1-877-408-4974