Drug identification number (DIN): 02365480 / 0.5mg and 02482533 / 0.25mg
Novartis Pharmaceutical Canada Inc.
Gilenya is an oral disease modifying treatment for relapsing-remitting MS and the first in a new class of medications known as sphingosine 1-phosphate receptor (S1PR) modulators.
Indication and use
Gilenya is indicated as a monotherapy for the treatment of relapsing-remitting MS in individuals who have had an inadequate response to, or are unable to tolerate, one or more first-line therapies, to reduce the frequency of clinical exacerbations and to delay the progression of physical disability. Gilenya is indicated as monotherapy for the treatment of pediatric patients of 10 years to below 18 years of age with relapsing multiple sclerosis to reduce the frequency of clinical exacerbations.
It is not known if Gilenya is safe and effective in children under age 10 or adults over 65.
Gilenya is not approved for people with CIS or progressive MS. For information on CIS approved treatment options and treatments for progressive MS, please speak with your physician or contact the MS Society of Canada at 1-800-268-7582.
Gilenya is contraindicated in people: with certain heart-related conditions; are allergic (hypersensitive) to fingolimod or to any of the other ingredients in the formulation or component of the container; have a weakened immune system due to disease or medications or treatments that suppress the immune system; have a sever active infection or an active chronic infection such as hepatitis or tuberculosis; have an active cancer (except for a type of skin cancer called basal cell carcinoma); have severe liver disease; pregnant or nursing.
Administration and dose
Gilenya is a 0.5 mg capsule taken once a day, with or without food.
Gilenya is a 0.25mg capsule taken once a day, with or without food (pediatric indication).
Mechanism of action (MOA)
Gilenya reduces the frequency of MS relapses by preventing certain immune cells from reaching the central nervous system, where they could potentially attack myelin, the fatty substance that insulates nerves and helps them transmit impulses between the brain and the body.
Most common side effects: flu virus infection, headache, diarrhea, back pain, cough.Common side effects: sinusitis, fungal infections affecting skin, nails or hair, dizziness, migraine, weakness, skin rash, hair loss, itchy skin, weight loss, blurred vision, breathlessness, tingling or numbness, depression, eye pain.
In 2015 pharmaceutical company Novartis reported three cases of progressive multifocal leukoencephalopathy (PML) in individuals with multiple sclerosis who were being treated with Gilenya. In 2012 Novartis reported a case of PML in a patient that was taking Gilenya, noting that the PML may be associated with previous treatment with Tysabri.
Return of disease activity (rebound)
In the post-marketing setting, severe exacerbation of disease activity has been observed rarely in some patients stopping fingolimod. Patients should be monitored for development of high disease activity following discontinuation of Gilenya and begin appropriate treatment as needed.
This is not a comprehensive list of all possible side effects of Gilenya. Please see the Gilenya product monograph for a list of other potentially serious side effects. It is important that those with MS discuss side effects about any medication they are considering with their physician. (*Health Canada, product monograph for Gilenya.)
FREEDOMS Study Group1
A Placebo-Controlled Trial of Oral Fingolimod in Relapsing Multiple Sclerosis
Oral fingolimod, a sphingosine-1-phosphate–receptor modulator significantly improved relapse rates and end points measured on magnetic resonance imaging (MRI), as compared with either placebo or intramuscular interferon beta-1a, in phase 2 and 3 studies of multiple sclerosis.This 24-month, double-blind, randomized study, enrolled participants who had relapsing–remitting multiple sclerosis, who were 18 to 55 years of age, had a score of 0 to 5.5 on the Expanded Disability Status Scale (which ranges from 0 to 10, with higher scores indicating greater disability), and had had one or more relapses in the previous year or two or more in the previous 2 years. A total of 1033 of the 1272 patients completed the study. As compared with placebo, both doses of oral fingolimod improved the relapse rate, the risk of disability progression, and end points on MRI. These benefits will need to be weighed against possible long-term risks. (New England Journal of Medicine, 2010; 362: 387-401)
TRANSFORMS Study Group2
Oral Fingolimod or Intramuscular Interferon for Relapsing Multiple Sclerosis
In this 12-month, double-blind, double-dummy study, 1292 participants with relapsing– remitting multiple sclerosis who had a recent history of at least one relapse were randomly assigned to receive either oral fingolimod at a daily dose of either 1.25 or 0.5 mg or intramuscular interferon beta-1a (an established therapy for multiple sclerosis) at a weekly dose of 30 μg. The primary end point was the annualized relapse rate. Key secondary end points were the number of new or enlarged lesions on T2-weighted magnetic resonance imaging (MRI) scans at 12 months and progression of disability that was sustained for at least 3 months. A total of 1153 people completed the study. The annualized relapse rate was significantly lower in both groups receiving fingolimod than in the interferon group. MRI findings supported the primary results. No significant differences were seen among the study groups with respect to progression of disability. Two fatal infections occurred in the group that received the 1.25-mg dose of fingolimod: disseminated primary varicella zoster and herpes simplex encephalitis. This trial showed the superior efficacy of oral fingolimod with respect to relapse rates and MRI outcomes in patients with multiple sclerosis, as compared with intramuscular interferon beta-1a. Longer studies are needed to assess the safety and efficacy of treatment beyond 1 year. (New England Journal of Medicine, 2010; 362:402-415).
PARADIGMS Study Group4
The PARADIGMS study was a double-blind, randomized, active-controlled, parallel-group, multicenter study with flexible duration up to 24 months, to evaluate the efficacy and safety of fingolimod compared to interferon beta-1a in pediatric patients with multiple sclerosis, aged 10 to <18 years old. Patients were randomized to receive fingolimod or interferon beta-1a via the intramuscular route once weekly for up to 24 months. The primary endpoint, the annualized relapse rate, was significantly lower in patients treated with fingolimod than in patients who received interferon beta-1a (relative reduction in ARR of 81.9%). The key secondary endpoint, the annualized rate of the number of new or newly enlarged T2 lesions up to Month 24, was also significantly lower in patients treated with fingolimod than in patients who received interferon beta-1a. (New England Journal of Medicine, 2018; 379:1017-1027).
Gilenya is set at $33,000 per year. Much of the cost can be reimbursed through private and group health plans for people who meet the prescribing criteria, and through provincial drug programs for individuals who meet the prescribing criteria.
Drug support program
Go Program® : 1-866-841-5518. Please discuss any other questions about treatment options with your doctor.
1. Kappos L, et al. Oral fingolimod for relapsing multiple sclerosis. N Eng J Med. 2006; 355: 1124-1140.
2. Cohen J. et al. Oral fingolimod vs. intramuscular interferon in relapsing multiple sclerosis. N Eng J Med. 2010; 362(5): 402-15.
3. Kappos L, et al. Placebo-controlled study of oral fingolimod in relapsing multiple sclerosis. N Eng J Med. 2010; 362(5): 387-401.
4. Chitnis T, et al. Trial of Fingolimod versus Interferon Beta-1a in Pediatric Multiple Sclerosis. PARADIGMS Study Group. N Engl J Med. 2018 Sep 13;379(11):1017-1027.
Gilenya® is a registered trademark of Novartis Pharmaceuticals Canada Inc.