Fingolimod

Drugbox
IUPAC_name = 2-amino-2- [2-(4-octylphenyl)ethyl] propane-1,3-diol


CAS_number = 162359-55-9
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PubChem = 107969
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C=19 | H=33 | N=1 | O=2
molecular_weight = 307.471 g/mol
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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). [cite journal |author=Paugh SW, Payne SG, Barbour SE, Milstien S, Spiegel S |title=The immunosuppressant FTY720 is phosphorylated by sphingosine kinase type 2 |journal=FEBS Lett |volume=554 |issue=1–2 |pages=189–93 |year=2003 |pmid=14596938 |doi=10.1016/S0014-5793(03)01168-2] [cite journal |author=Billich A, Bornancin F, Dévay P, Mechtcheriakova D, Urtz N, Baumruker T |title=Phosphorylation of the immunomodulatory drug FTY720 by sphingosine kinases |journal=J Biol Chem |volume=278 |issue=48 |pages=47408–15 |year=2003 |pmid=13129923 |doi=10.1074/jbc.M307687200 [http://www.jbc.org/cgi/content/full/278/48/47408 Free full text] ] The molecular biology of this biological function lies in FTY720's activity at one of the five sphingosine-1-phosphate receptors, S1P1. [cite journal |author=Hla T, Lee MJ, Ancellin N, Paik JH, Kluk MJ |title=Lysophospholipids--receptor revelations |journal=Science |volume=294 |issue=5548 |pages=1875–8 |year=2001 |pmid=11729304 |doi=10.1126/science.1065323] ] .

In a previous phase III trial of kidney transplantation, FTY720 was found to be no better than the existing standard of care.Fact|date=November 2007

It is currently in phase III clinical trials as monotherapy for relapsing-remitting multiple sclerosis. [ [http://www.clinicaltrials.gov/ct/show/NCT00289978 Efficacy and Safety of Fingolimod in Patients With Relapsing-Remitting Multiple Sclerosis.] ClinicalTrials.gov (2007-08-20). Retrieved on 2007-11-06.] . 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.Fact|date=April 2008

ee also

*Laquinimod

References