section name header

Indications ⬇

REMS


Contraind./Precautions ⬆ ⬇

Contraindicated in:

Use Cautiously in:

Adv. Reactions/Side Effects ⬆ ⬇

CV: asystole, bradycardia, heart block, QT interval prolongation, 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

Interactions ⬆ ⬇

Drug-drug:

Availability ⬆ ⬇

(Generic available)

Route/Dosage ⬆ ⬇

US Brand Names ⬆ ⬇

Gilenya, Tascenso ODT

Action ⬆ ⬇

  • 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.
Therapeutic effects:
  • ↓frequency of relapses/delayed accumulation of disability.

Classifications ⬆ ⬇

Therapeutic Classification: anti-multiple sclerosis agents

Pharmacologic Classification: receptor modulators

Pharmacokinetics ⬆ ⬇

Absorption: 93% absorbed following oral administration.

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

Protein Binding: >99.7%.

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

Half-Life: 6–9 days.

Time/Action Profile ⬆ ⬇

ROUTEONSETPEAKDURATION
POunknown1–2 mo*2 mo‡

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

‡Time for complete elimination.

Patient/Family Teaching ⬆ ⬇

Pronunciation ⬆ ⬇

fin-GO-li-mod

Code ⬆

NDC Code