Gilenya Generic Name & Formulations
Legal Class
General Description
Pharmacological Class
How Supplied
Manufacturer
Generic Availability
Gilenya Indications
Indications
Gilenya Dosage and Administration
Adults and Children
Renal Impairment
The blood level of some Gilenya metabolites is increased (up to 13-fold) in patients with severe renal impairment. The toxicity of these metabolites has not been fully explored. The blood level of these metabolites has not been assessed in patients with mild or moderate renal impairment.
Hepatic Impairment
Because fingolimod, but not fingolimod-phosphate, exposure is doubled in patients with severe hepatic impairment, patients with severe hepatic impairment should be closely monitored, as the risk of adverse reactions may be greater.
No dose adjustment is needed in patients with mild or moderate hepatic impairment.
Other Modifications
Females and Males of Reproductive Potential
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Pregnancy Testing: The pregnancy status of females of reproductive potential should be verified prior to starting treatment with Gilenya.
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Contraception: Counsel patients on the potential for a serious risk to the fetus and the need for effective contraception during treatment with Gilenya before initiation. Since it takes approximately 2 months to eliminate the compound from the body after stopping treatment, the potential risk to the fetus may persist and women should use effective contraception during this period.
Gilenya Contraindications
Contraindications
Gilenya Boxed Warnings
Not Applicable
Gilenya Warnings/Precautions
Warnings/Precautions
Gilenya Pharmacokinetics
Absorption
The Tmax of fingolimod is 12–16 hours. The apparent absolute oral bioavailability is 93%. Food intake does not alter Cmax or (AUC) of fingolimod or fingolimod-phosphate. Therefore, Gilenya may be taken without regard to meals. Steady-state blood concentrations are reached within 1 to 2 months following once-daily administration and steady-state levels are approximately 10-fold greater than with the initial dose.
Distribution
Fingolimod highly (86%) distributes in red blood cells. Fingolimod-phosphate has a smaller uptake in blood cells of < 17%. Fingolimod and fingolimod-phosphate are > 99.7% protein bound. Fingolimod and fingolimod-phosphate protein binding is not altered by renal or hepatic impairment. Fingolimod is extensively distributed to body tissues with a volume of distribution of about 1200 ± 260 L.
Elimination
Fingolimod blood clearance is 6.3 ± 2.3 L/h, and the average apparent terminal half-life (t1/2) is 6 to 9 days. Blood levels of fingolimod-phosphate decline in parallel with those of fingolimod in the terminal phase, yielding similar half-lives for both. After oral administration, about 81% of the dose is slowly excreted in the urine as inactive metabolites. Fingolimod and fingolimod-phosphate are not excreted intact in urine but are the major components in the feces with amounts of each representing less than 2.5% of the dose.
Gilenya Interactions
Interactions
Gilenya Adverse Reactions
Adverse Reactions
Gilenya Clinical Trials
Gilenya Note
Notes
Gilenya Patient Counseling
Cost Savings Program
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