Fingolimod, sometimes also called FTY720, is marketed as under the name Gilenya as of early 2012 as oral second line therapy for multiple sclerosis (MS). It is a partial sphingosine-1-phosphate (S1P) receptor agonist .
Fingolimod was originally developed to prevent organ rejection following a transplant, although it failed in this indication and is no longer being investigated for this purpose [2,3].
Fingolimod is thought to work in MS by removing T cells (also known as T lymphocytes) from the circulation, which limits their movement into the central nervous system (CNS) and prevents them from attacking neurones and causing the symptoms associated with MS [4,5].
Fingolimod also enters the CNS where it is thought to affect the blood–brain barrier – the membrane that protects the vulnerable brain tissues from substances and foreign bodies in the blood. Fingolimod may also have direct effects on the cells and tissues of the brain and spinal cord [1,5–7].
Fingolimod is currently undergoing medical research in phase III clinical trials as a potential new oral MS treatment. Fingolimod is currently not approved as a therapy for use in patients with MS.
Learn More About Fingolimod
- Mechanism of Action of Fingolimod
- Clinical Development of Fingolimod in Multiple Sclerosis
- Horga A, Montalban X. FTY720 (fingolimod) for relapsing multiple sclerosis. Expert Rev Neurotherapeutics 2008;8(5): 699−714.
- Salvadori M, Budde K, Charpentier B, et al. FTY720 versus MMF with cyclosporine in de novo renal transplantation: a 1-year, randomized controlled trial in Europe and Australasia. Am J Transplant. 2006;6(12): 2912−21.
- Tedesco-Silva H, Pescovitz MD, Cibrik D, et al. Randomized controlled trial of FTY720 versus MMF in de novo renal transplantation. Transplantation. 2006;82(12): 1689-97.
- Kappos L, Antel J, Comi G, et al. Oral fingolimod (FTY720) for relapsing multiple sclerosis. N Engl J Med. 2006;355(11): 1124−40.
- Miron VE, Schubart A, Antel JP. Central nervous system-directed effects of FTY720 (fingolimod). J Neurol Sci. 2008;274(1−2): 13−7.
- Coelho RP, Payne SG, Bittman R. The immunomodulator FTY720 has a direct cytoprotective effect in oligodendrocyte progenitors. J Pharmacol Exp Ther. 2007;323(2): 626−35.
- Foster CA, Howard LM, Schweitzer A,et al. Brain penetration of the oral immunomodulatory drug FTY720 and its phosphorylation in the central nervous system during experimental autoimmune encephalomyelitis: consequences for mode of action in multiple sclerosis. J Pharmacol Exp Ther. 2007;323(2): 469−75.