• Relapsing forms of multiple sclerosis (MS), including clinically isolated syndrome, relapsing-remitting disease, and active secondary progressive disease.

Contraindicated in:

• Hypersensitivity
• MI, unstable angina, stroke, transient ischemic attack, or class III or IV HF within previous 6 mo
• 2nd- or 3rd-degree heart block or sick sinus syndrome (in the absence of a pacemaker)
• QT interval ≥500 msec
• Cardiac arrhythmias requiring use of class Ia or III antiarrhythmics
• Active acute/chronic untreated infections
• OB: Pregnancy.

Use Cautiously in:

• Concurrent use of beta blockers, diltiazem, verapamil, or digoxin (↑ risk of bradycardia/heart block)
• History of ischemic heart disease, MI, HF, cerebrovascular disease, uncontrolled hypertension, AV or SA heart block, symptomatic bradycardia, recurrent syncope, cardiac arrest, or severe untreated sleep apnea (↑ risk of bradycardia/heart block)
• QT interval prolongation before doing or during observation period (>450 msec in adult and pediatric males, >470 msec in adult females, >460 msec in pediatric females), hypokalemia, hypomagnesemia, congenital long QT syndrome, or concurrent use of QT interval prolonging medications (↑ risk of QT interval prolongation)
• Severe hepatic impairment (↑ blood levels and risk of adverse reactions)
• Diabetes mellitus/history of uveitis (↑ risk of macular edema)
• Negative history for chickenpox or vaccination against varicella zoster virus (VZV) vaccination
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Rep: Women of reproductive potential
• Pedi: Children <10 yr (safety and effectiveness not established)
• Geri: Risk of adverse reactions may be ↑ in older adults; consider age-related ↓ in cardiac/renal/hepatic function, chronic illnesses, and concurrent drug therapy.

CV: QT interval prolongation, asystole, bradycardia, heart block, hypertension, syncope.

Derm: BASAL/SQUAMOUS CELL CARCINOMA, MELANOMA.

EENT: blurred vision, eye pain, macular edema.

GI: ↑ liver enzymes, diarrhea, HEPATOTOXICITY.

Hemat: leukopenia, lymphopenia.

MS: back pain.

Neuro: headache, posterior reversible encephalopathy syndrome (pres), progressive multifocal leukoencephalopathy (pml), tumefactive MS.

Resp: cough, ↓ pulmonary function.

Misc: hypersensitivity reactions (including angioedema), IMMUNE RECONSTITUTION INFLAMMATORY SYNDROME (IRIS), INFECTION (INCLUDING BACTERIAL, VIRAL AND FUNGAL), LYMPHOMA.

Drug-Drug:

• Class Ia or class III antiarrhythmics may ↑ risk of serious arrhythmias; concurrent use contraindicated.
• Concurrent use of beta blockers, diltiazem, verapamil, ivabradine, clonidine, or digoxin may ↑ risk of bradycardia; careful monitoring recommended.
• Concurrent use of QT-interval prolonging medications may ↑ risk of QT interval prolongation and torsades de pointes.
• Concurrent use of ketoconazole may ↑ blood levels and risk of adverse reactions.
• ↑ risk of immunosuppression with antineoplastics, immunosuppressants, or immune modulating therapies.
• Live-attenuated vaccines ↑ risk of infection.

(Generic available)

• Capsules: 0.25 mg; 0.5 mg;
• Orally disintegrating tablets: 0.25 mg; 0.5 mg;

• PO (Adults and Children ≥10 yr and >40 kg): 0.5 mg once daily.
• PO (Children ≥10 yr and ≤40 kg): 0.25 mg once daily.

Gilenya, Tascenso ODT

• Converted by sphingosine kinase to the active metabolite fingolimod-phosphate, which binds to sphingosine 1–phosphate receptors, resulting in ↓ migration of lymphocytes into peripheral blood. This may ↓ lymphocyte migration into the CNS.

• ↓ frequency of relapses/delayed accumulation of disability.

Therapeutic Classification: anti-multiple sclerosis agents

Pharmacologic Classification:

Absorption: Well absorbed (93%) following oral administration.

Distribution: Extensively distributed to body tissues; 86% of parent drug distributes into red blood cells; active metabolite uptake 17%.

Metabolism/Excretion: Converted to its active metabolite, then metabolized mostly by the CYP4F2 enzyme system, with further degradation by other enzyme systems. Most inactive metabolites excreted in urine (81%); <2.5% excreted as fingolimod and fingolimod-phosphate in feces.

Protein Binding: >99.7%.

Half-life: 6–9 days.

*Time to steady state plasma concentrations, peak plasma concentrations after a single dose at 12–16 hr.

†Time for complete elimination.

• Instruct patient to take fingolimod as directed. If a dose is missed, contact health care professional before taking next dose; may need to be observed by a health care professional for at least 6 hrs after taking next dose. Do not discontinue therapy without consulting health care professional, may cause severe increase in disability. Advise patient to read the Medication Guide prior to starting therapy and with each Rx refill in case of changes.
• Advise patient to notify health care professional if signs and symptoms of liver dysfunction (unexplained nausea, vomiting, abdominal pain, fatigue, anorexia, jaundice, dark urine), infection, PML, new onset of dyspnea, PRES (sudden headache, confusion, seizures, loss of vision, weakness), hypersensitivity reactions (rash or itchy hives, swelling of lips, tongue, or face), skin nodules (shiny pearly nodules), patches or open sores that do not heal within weeks, or changes in vision develop.
• Instruct patient not to receive live-attenuated vaccines during and for 2 mo after treatment due to risk of infection. Patients who have not had a health care professional confirmed history of chickenpox or documentation of a full course vaccination should be tested for antibodies to VZV virus before starting therapy. Antibody-negative patients should receive vaccination prior to starting therapy, then postpone start of fingolimod for 1 mo to allow for full effect of vaccination.
• Advise patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to consult with health care professional before taking other medications.
• May cause basal cell carcinoma, melanoma, and lymphoma. Caution patient to use sunscreen with a high protection factor, wear protective clothing, and limit exposure to sunlight and ultraviolet light.
• Rep: May cause fetal harm. Advise female patients to use contraception during and for at least 2 mo after discontinuation of therapy and to notify health care professional immediately if pregnancy is planned or suspected or if breastfeeding. Inform pregnant patients of pregnancy exposure registry that monitors pregnancy outcomes in women exposed to fingolimod during pregnancy. To enroll patient in the pregnancy registry, call 1-877-598-7237 or visit .

fin-GO-li-mod

NDC Code^*

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0607- Gilenya
    • 0078-0607-15- 30 CAPSULE in 1 BOTTLE (0078-0607-15)

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0607- Gilenya
    • 0078-0607-89- 7 CAPSULE in 1 CARTON (0078-0607-89)

• 0078- Novartis Pharmaceuticals Corporation
  • 0078-0965- Gilenya
    • 0078-0965-89- 7 CAPSULE in 1 CARTON (0078-0965-89)

• 64980- Rising Pharmaceuticals, Inc.
  • 64980-449- fingolimod
    • 64980-449-03- 30 CAPSULE in 1 BOTTLE (64980-449-03)

• 64980- Rising Pharmaceuticals, Inc.
  • 64980-449- fingolimod
    • 64980-449-07- 7 CAPSULE in 1 CARTON (64980-449-07)

• 64980- Rising Pharmaceuticals, Inc.
  • 64980-449- fingolimod
    • 64980-449-28- 28 CAPSULE in 1 CARTON (64980-449-28)

• 64980- Rising Pharmaceuticals, Inc.
  • 64980-449- fingolimod
    • 64980-449-97- 7 CAPSULE in 1 BLISTER PACK (64980-449-97)