Fingolimod (Gilenya®)

 

Brand NameGilenya®
Scientific NameFingolimod
What is it?Gilenya is an immunosuppressant. It is disease-modifying oral agent that is indicated to reduce the frequency of MS exacerbations and to delay the progression of physical disability in patients with relapsing forms of MS.
What does it do?Gilenya is a disease-modifying drug used as monotherapy to reduce exacerbations and accumulation of disability in relapsing forms of MS.
How does it work?The exact mechanism is unknown, but Gilenya is thought to work by reducing the immune system's attack on the central nervous system by retaining certain white blood cells (lymphocytes) in the lymph nodes. It binds to receptors in the body that block progression of lymphocytes (white blood cells) into the blood and may reduce the movement of lymphocytes into the central nervous system (brain and spinal cord). Lymphocytes are part of the auto-immune response in MS; they play a role in inflammation and the demyelination (removal of protective covering) of axons.
Clinical Results and FDA approvalFDA approval of Gilenya was based on two clinical studies.

Kappos L, Radue EW, O'Connor P, Polman C, Hohlfeld R, Calabresi P, Selmaj K, Agoropoulou C, Leyk M, Zhang-Auberson L, Burtin P; FREEDOMS Study Group A placebo-controlled trial of oral fingolimod in relapsing multiple sclerosis. The New England Journal of Medicine 2010 Feb 4;362(5):387-401

Comi G, O'Connor P, Montalban X, Antel J, Radue EW, Karlsson G, Pohlmann H, Aradhye S, Kappos L; FTY720D2201 Study Group Phase II study of oral fingolimod (FTY720) in multiple sclerosis: 3-year results. Multiple Sclerosis 2010 Feb;16(2):197-207
How is it taken?Gilenya 0.5 mg orally once daily.
-Take the tablet whole. Do not break, crush, chew, or dissolve before swallowing as this may increase the risk for side effects.
-May be taken with or without food.
-Do not discontinue Gilenya without first talking to your physician.
-If you miss a dose, take when you remember, but if it is too close to the next dose, do not double up. You will be monitored for six hours after the first dose for signs of bradycardia (slow heart rate).
-If you are taking an anti-arrhythmic medication (including calcium channel blockers and beta-blockers) or have other cardiac risk factors such as congestive heart failure an EKG will be obtained prior to beginning therapy.
-If you have not had chickenpox before or a varicella zoster virus (VZV) vaccine, you may be tested for antibodies to VZV. If you do not have antibodies to VZV, you may be asked to receive the vaccination prior to starting therapy.
-A complete blood count, bilirubin, and liver function tests will be obtained before initiation of therapy.
-An eye exam will be administered before initiation of therapy and 3-4 months into therapy.
What are the side effects ?Common side effects include :
-Headache
-Influenza (flu)
-Diarrhea
-Back pain
-Cough
-Increase in liver enzymes


Serious side effects include:
-Infections
-AV block and bradyarrhythmia
-Macular Edema
-Leuokopenia

Here is an infomercial by Novartis about Gilenya.