FINGOLIMOD HYDROCHLORIDE

AbsorptionThe T max of fingolimod is 12 to 16 hours. The apparent absolute oral bioavailability is 93%. Food intake does not alter C max or (AUC) of fingolimod or fingolimod-phosphate. Therefore, fingolimod capsules 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.

DistributionFingolimod highly (86%) distributes in red ...

14.1 Adults The efficacy of fingolimod hydrochloride was demonstrated in 2 studies that evaluated once-daily doses of fingolimod hydrochloride 0.5 mg and 1.25 mg in patients with relapsing-remitting MS (RRMS). Both studies included patients who had experienced at least 2 clinical relapses during the 2 years prior to randomization or at least 1 clinical relapse during the 1 year prior to randomization, and had an Expanded Disability Status Scale (EDSS) score from 0 to 5.5. Study 1 was a 2-year randomized, double-blind, placebo-controlled study in patients with RRMS who had not received any inte...

The following serious adverse reactions are described elsewhere in labeling: Bradyarrhythmia and Atrioventricular Blocks [see Warnings and Precautions (5.1) ] Infections [see Warnings and Precautions (5.2) ] Progressive Multifocal Leukoencephalopathy [see Warnings and Precautions (5.3) ] Macular Edema [see Warnings and Precautions (5.4) ] Liver Injury [see Warnings and Precautions (5.5) ] Posterior Reversible Encephalopathy Syndrome [see Warnings and Precautions (5.6) ] Respiratory Effects...

Fingolimod capsules are contraindicated in patients who have: in the last 6 months experienced myocardial infarction, unstable angina, stroke, transient ischemic attack (TIA), decompensated heart failure requiring hospitalization or Class III/IV heart failure a history or presence of Mobitz Type II second-degree or third-degree AV block or sick sinus syndrome, unless patient has a functioning pace...

Infections: Fingolimod hydrochloride may increase the risk. Obtain a complete blood count (CBC) before initiating treatment. Monitor for infection during treatment and for 2 months after discontinuation. Do not start in patients with active infections. ( 5.2 ) Progressive Multifocal Leukoencephalopathy (PML): Withhold fingolimod hydrochloride at the first sign or symptom suggestive of PML. ( 5.3 ) Macular Edema: Examine the fundus before and 3 to 4 months after treatment start. Diabetes mellitus...

7 DRUG INTERACTIONS Systemic Ketoconazole: Monitor during concomitant use. ( 7.2 , 12.3 ) Vaccines: Avoid live attenuated vaccines during, and for 2 months after stopping fingolimod hydrochloride treatment. ( 5.2 , 7.3 ) 7.1 QT Prolonging Drugs Fingolimod hydrochloride has not been studied in patients treated with drugs that prolong the QT interval. Drugs that prolong the QT interval have been ass...