Description
Fingolimod is an inhibitor of sphingosine 1-phosphate receptors that is used clinically as a treatment for autoimmune diseases such as multiple sclerosis; this compound prevents movement of autoreactive lymphocytes from the lymph nodes into circulation. Fingolimod exhibits immunosuppressive, neuroprotective, and anticancer chemotherapeutic benefits. In Treg cells, fingolimod increases levels of TGF- β1 and Foxp3. In in vitro and in vivo models of Alzheimer’s disease, this compound decreases production of amyloid-β (Aβ) proteins. Additionally, fingolimod inhibits expression of sphingosine kinase 2 and increases cell death in neuroblastoma cells. Fingolimod inhibits growth of cancerous xenografts in vivo as well.
References
Li MH, Hla T, Ferrer F. FTY720 inhibits tumor growth and enhances the tumor-suppressive effect of topotecan in neuroblastoma by interfering with the sphingolipid signaling pathway. Pediatr Blood Cancer. 2013 Sep;60(9):1418-23. PMID: 23704073.
Takasugi N, Sasaki T, Ebinuma I, et al. FTY720/fingolimod, a sphingosine analogue, reduces amyloid-β production in neurons. PLoS One. 2013 May 7;8(5):e64050. PMID: 23667698.
Groves A, Kihara Y, Chun J. Fingolimod: direct CNS effects of sphingosine 1-phosphate (S1P) receptor modulation and implications in multiple sclerosis therapy. J Neurol Sci. 2013 May 15;328(1-2):9-18. PMID: 23518370.
Willis MA, Cohen JA. Fingolimod therapy for multiple sclerosis. Semin Neurol. 2013 Feb;33(1):37-44. PMID: 23709211.
Liu Y, Jiang J, Xiao H, et al. The sphingosine-1-phosphate receptor agonist FTY720 and its phosphorylated form affect the function of CD4+CD25+ T cells in vitro. Int J Mol Med. 2012 Jul;30(1):211-9. PMID: 22576630.
Spijkers LJ, Alewijnse AE, Peters SL. FTY720 (fingolimod) increases vascular tone and blood pressure in spontaneously hypertensive rats via inhibition of sphingosine kinase. Br J Pharmacol. 2012 Jun;166(4):1411-8. PMID: 22251137.
