Generic Name and Formulations:
Fingolimod (as HCl) 0.25mg, 0.5mg; hard gel caps.
Novartis Pharmaceuticals Corp
Indications for GILENYA:
Relapsing forms of multiple sclerosis (MS).
Adults and Children:
<10yrs: not established. ≥10yrs (>40kg): 0.5mg once daily; (≤40kg): 0.25mg once daily. First dose monitoring for bradycardia: see Warnings/Precautions. Re-initiation of therapy after discontinuation for >14 days: within first 2 weeks, first dose procedures are recommended after interruption of 1 day or more; during week 3 and 4, first dose procedures are recommended after interruption of more than 7 days. Children: observe first dose monitoring when dose increased.
Recent (within the last 6 months) occurrence of: MI, unstable angina, stroke, TIA, decompensated heart failure requiring hospitalization, Class III/IV heart failure. History or presence of Mobitz Type II 2nd degree or 3rd degree AV block or sick sinus syndrome, unless paced. Baseline QTc interval ≥500ms. Concomitant Class Ia or Class III antiarrhythmic drug.
Risk of bradyarrhythmia; observe all patients for bradycardia for at least 6hrs after first dose with hourly pulse and BP measurement. Obtain ECG prior to dosing and at the end of observation period. If heart rate (HR) <45bpm (adults), <55bpm (≥12yrs) or <60bpm (10–11yrs), or new onset 2nd degree or higher AV block; monitor until resolution, those at the lowest post-dose HR should be monitored until HR increases. Symptomatic bradycardia: begin continuous ECG monitoring until resolved; if pharmacological intervention necessary, continue ECG monitoring overnight, and first dose monitoring procedures should be repeated for 2nd dose. Pre-existing cardiac conditions (eg, ischemic heart disease, history of MI, cardiac arrest or symptomatic bradycardia, cerebrovascular disease, CHF, uncontrolled hypertension, recurrent syncope, untreated sleep apnea, AV block, sino-atrial block), QT prolongation risk (eg, hypokalemia, hypomagnesemia, congenital long-QT syndrome): monitor ECG overnight after first dose. Monitor BP during treatment. Increased risk of infections (may be fatal). Obtain recent CBC before starting treatment. Consider suspending therapy if serious infection develops; continue monitoring for 2 months after discontinuation. Active acute or chronic infection: do not start treatment until infection resolved. Test for antibodies to varicella zoster virus; consider immunization before starting fingolimod. Immunosuppressed. Diabetes, history of uveitis: increased risk of macular edema. Monitor visual acuity and for visual disturbances. Do ophthalmic exam at baseline, and at 3–4 months after starting therapy. Renal or severe hepatic impairment. Recent LFTs (eg, within 6 months) should be available; monitor; discontinue if liver injury occurs. Respiratory dysfunction; obtain spirometry and DLCO when needed. Withhold and evaluate at first sign/symptom of progressive multifocal leukoencephalopathy (PML). Perform periodic skin exam (esp. with risk factors); monitor for suspicious skin lesions and evaluate if observed. Elderly. Pregnancy; use effective contraception during and for 2 months after discontinuation. Nursing mothers.
Sphingosine 1-phosphate receptor modulator.
Concomitant QT prolonging drugs (eg, citalopram, chlorpromazine, haloperidol, methadone, erythromycin): risk of torsades de pointes; monitor. Potentiated by ketoconazole; monitor if receiving systemic therapy. Concomitant β-blockers, digoxin, diltiazem, verapamil may be associated with severe bradycardia or heart block; consider alternatives. Avoid live virus vaccines during treatment and for 2 months after discontinuing fingolimod; may have suboptimal response. Antineoplastic, immunosuppressant or immunomodulating therapies may increase risk of immunosuppression; use caution when switching from long-acting immunotherapies (eg, natalizumab, teriflunomide, mitoxantrone).
Headache, increased liver transaminases, diarrhea, cough, influenza, sinusitis, back pain, abdominal pain, pain in extremity; bradyarrhythmia, AV blocks, hypertension, increased infection risk, macular edema, decreased pulmonary function, basal cell carcinoma/melanoma, hypersensitivity reactions; rare: posterior reversible encephalopathy syndrome (discontinue if suspected), PML.
Enroll pregnant patients in the Gilenya pregnancy registry by calling Outcome at (877) 598-7237.
Hepatic (major: CYP4F2, minor: CYP2D6, 2E1, 3A4, 4F12); >99.7% protein bound.
Renal, fecal (minor).
Caps—30; Blister cards—7