Fingolimod (Molecule of the Month for May 2017)
Fingolimod is an immunomodulating drug, mostly used for treating multiple sclerosis (MS).It has reduced the rate of relapses in relapsing-remitting multiple sclerosis by approximately one-half over a two-year period. Fingolimod is a sphingosine-1-phosphate receptor modulator, which sequesters lymphocytes in lymph nodes, preventing them from contributing to an autoimmune reaction.
ngolimod is used in the treatment of the relapsing form of multiple sclerosis. Its effect in those with primary progressive MS is not clear. May also be used in chronic inflammatory demyelinating polyneuropathy. It was originally proposed as an antirejection medication indicated after transplantation but it failed to show any significant benefit in post-transplantation clinical trials.
It is a structural analogue of sphingosine and is phosphorylated by sphingosine kinases in the cell (most importantly sphingosine kinase The molecular biology of phospho-fingolimod is thought to lie in its activity at one of the five sphingosine-1-phosphate receptors, S1PR1. Phospho-fingolimod causes the internalization of S1P receptors, which sequesters lymphocytes in lymph nodes, preventing them from moving to the central nervous system and cause a relapse in multiple sclerosis.
Formal Chemical Name (IUPAC)
Update by Karl Harrison
(Molecule of the Month for May 2017 )
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