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Initial U.S. Approval: 2010
Fingolimod is a sphingosine 1-phosphate receptor modulator.
Chemically, fingolimod is 2-amino-2-[2-(4-octylphenyl)ethyl]propan-1,3-diol hydrochloride.
Fingolimod hydrochloride is a white to practically white powder that is freely soluble in water and alcohol and soluble in propylene glycol. It has a molecular weight of 343.93.
GILENYA is provided as 0.5 mg hard gelatin capsules for oral use. Each capsule contains 0.56 mg of fingolimod hydrochloride, equivalent to 0.5 mg of fingolimod.
Each GILENYA 0.5 mg capsule contains the following inactive ingredients: gelatin, magnesium stearate, mannitol, titanium dioxide, yellow iron oxide.
Mechanism of Action
Fingolimod is metabolized by sphingosine kinase to the active metabolite, fingolimod-phosphate. Fingolimod-phosphate is a 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.
|GILENYA is a sphingosine 1-phosphate receptor modulator indicated for the treatment of patients with relapsing forms of multiple sclerosis to reduce the frequency of clinical exacerbations and to delay the accumulation of physical disability.|
WARNINGS AND PRECAUTIONS
Class Ia or Class III antiarrhythmic drugs: Because of a risk of serious rhythm disturbances, carefully monitor patients on Class Ia or Class III antiarrhythmic drugs during initiation of therapy.
Beta blockers: Because of a risk of additive effect on heart rate, carefully monitor patients on beta blockers during initiation of therapy.
Ketoconazole: Monitor patients closely, as GILENYA exposure is increased by70% during concomitant use with systemic ketoconazole, and risk of adverse reactions is greater.
Vaccines: Avoid live attenuated vaccines during, and for 2 months after stopping GILENYA treatment, due to risk of infection.
USE IN SPECIFIC POPULATIONS
Pregnancy: Based on animal data, may cause fetal harm. Pregnancy registry available.
Pediatric patients: Safety and effectiveness have not been established.
Hepatic impairment: Monitor patients with severe hepatic impairment closely, as GILENYA exposure is doubled, and risk of adverse reactions is greater.
|Most common adverse reactions (incidence 10% and > placebo): Headache, influenza, diarrhea, back pain, liver transaminase elevations and cough.|
The recommended dose of GILENYA is 0.5 mg orally once daily.
Patients should be observed for 6 hours after the first dose to
monitor for signs and symptoms of bradycardia [see Warnings and
Precautions]. Fingolimod doses higher than 0.5 mg are associated
with a greater incidence of adverse reactions without additional
GILENYA can be taken with or without food.
GILENYA is available as 0.5 mg hard capsules with a white opaque
body and bright yellow cap imprinted with “FTY 0.5 mg” on the
cap and two radial bands imprinted on the capsule body with
Package Insert data:
GILENYA is a trademark of Novartis AG.
Novartis Pharma Stein AG
Novartis Pharmaceuticals Corporation
East Hanover, New Jersey 07936
July 2011/September 2010
National Institutes of Health, U.S. National Library of Medicine,
Provides access to the latest drug monographs submitted to the Food and Drug Administration (FDA). Please review the latest applicable package insert for additional information and possible updates. A local search option of this data can be found here.
Listed dosages are for - Adult patients ONLY. PLEASE READ THE
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David F. McAuley, Pharm.D., R.Ph. GlobalRPh Inc.