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Pharmacology: Pharmacodynamics: Fingolimod-phosphate, active metabolite of Fingolimod, binds to sphingosine 1-phosphate receptors 1, 3, 4, and 5. Fingolimod-phosphate blocks the lymphocytes' ability to emerge from lymph nodes; therefore, the amount of lymphocytes available to the central nervous system is decreased, which reduces central inflammation.
Pharmacokinetics: Distribution: Vd: ~1,200 L: distributes into red blood cells (86%).
Protein binding: >99.7% (Fingolimod and Fingolimod-phosphate).
Metabolism: Hepatic via CYP4F2 to Fingolimod-phosphate (active) and other metabolites (inactive); CYP2D6, 2E1, 3A4, and 4F12 also contribute to metabolism.
Bioavailability: 93%.
Half-life elimination: 6 to 9 days; prolonged by approximately 50% in patients with moderate or severe hepatic impairment.
Time to peak, plasma: 12 to 16 hours.
Excretion: Urine (~81 % as inactive metabolites); feces (Fingolimod and Fingolimod phosphate; <2.5% of dose).
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