Sunday, April 24, 2011

Gilenya: A Novel First in Class Oral Drug Approved for Multiple Sclerosis Treatment


A natural product inspired/derived first in class oral drug fingolimod (Gilenya) was approved by FDA for treating multiple sclerosis. This drug pocess novel mechanism of action compared to other drugs with immuno modulation. It is a structural analogue of myriocin, a sphingosine metabolite isolated from the fungus Isaria sinclairii. Fingolimod get phosphorylated with sphingosine kinases mainly sphingosine kinase-2 and binds to extra cellular G-protein coupled receptors mainly sphingosine-1-phosphate receptor S1PR1. It then prevents sequester lymphocytes in lymph node and preventing them from moving into central nervous system and stops the damage. A complete story was published on fingolimod in a recent Journal of Natural Products article