Fingolimod

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Fingolimod
Systematic (IUPAC) name
2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol
Identifiers
CAS number	?
ATC code	?
PubChem	107969
Chemical data
Formula	C₁₉H₃₃N O₃
Mol. mass	307.471 g/mol
Pharmacokinetic data
Bioavailability	?
Metabolism	?
Half life	?
Excretion	?
Therapeutic considerations
Pregnancy cat.	?
Legal status
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Fingolimod (rINN, codenamed FTY720) is a novel immunosuppressant drug that causes lymphopenia by preventing egress of lymphocytes from lymph nodes. It is a sphingosine-1-phosphate receptor 1 modulator.

It is a chemical modification of the Myriocin (ISP-1) metabolite of the fungus Isaria sinclairii (Dong Chong Xia Cao). It is a structural analogue of sphingosine and gets phosphorylated by sphingosine kinases in the cell (most importantly sphingosine kinase 2).^[1]^[2] The molecular biology of this biological function lies in FTY720's activity at one of the five sphingosine-1-phosphate receptors, S1P1.^[3]] It is currently in phase III clinical trials as monotherapy for relapsing-remitting multiple sclerosis.^[4] In a previous phase III trial of kidney transplantation, FTY720 was found to be no better than the existing standard of care.^{[citation needed]}

In a Phase III clinical trial for MS, FTY720 was effective in preventing relapses in more than 60 percent of patients who took the pill for three years.^{[citation needed]}

[edit] See also

Laquinimod

[edit] References

^ Paugh SW, Payne SG, Barbour SE, Milstien S, Spiegel S (2003). "The immunosuppressant FTY720 is phosphorylated by sphingosine kinase type 2". FEBS Lett 554 (1–2): 189–93. doi:10.1016/S0014-5793(03)01168-2. PMID 14596938.
^ Billich A, Bornancin F, Dévay P, Mechtcheriakova D, Urtz N, Baumruker T (2003). "Phosphorylation of the immunomodulatory drug FTY720 by sphingosine kinases". J Biol Chem 278 (48): 47408–15. doi:10.1074/jbc.M307687200. PMID 13129923. Free full text
^ Hla T, Lee MJ, Ancellin N, Paik JH, Kluk MJ (2001). "Lysophospholipids--receptor revelations". Science 294 (5548): 1875–8. doi:10.1126/science.1065323. PMID 11729304.
^ Efficacy and Safety of Fingolimod in Patients With Relapsing-Remitting Multiple Sclerosis. ClinicalTrials.gov (2007-08-20). Retrieved on 2007-11-06.