What is/are Fingolimod?
Fingolimod (rINN, trade name Gilenya, Novartis) is an immunomodulating drug, approved for treating multiple sclerosis. It has reduced the rate of relapses in relapsing-remitting multiple sclerosis by over half. Fingolimod is a sphingosine 1-phosphate receptor modulator, which sequesters lymphocytes in lymph nodes, preventing them from contributing to an autoimmune reaction.
Structure and mechanism
It is derived from the myriocin (ISP-1) metabolite of the fungus Isaria sinclairii. It is a structural analogue of sphingosine and gets phosphorylated by sphingosine kinases in the cell (most importantly sphingosine kinase 2). The molecular biology of phosphofingolimod is thought to lie in its activity at one of the five sphingosine-1-phosphate receptors, S1PR1. It can sequester lymphocytes in lymph nodes, preventing them from moving to the central nervous system for autoimmune responses in multiple sclerosis, and was originally proposed as an antirejection medication indicated after transplantation. It has been reported to stimulate the repair process of glial cells and precursor cells after injury. Fingolimod has also been reported to be a cannabinoid receptor antagonist, a cPLA2 inhibitor and a ceramide synthase inhibitor.
Fingolimod has been associated with potentially fatal infections, bradycardia and, recently, a case of hemorrhaging focal encephalitis, an inflammation of the brain with bleeding. Two subjects died: one due to brain herpes infection, and a second one due to zoster. It is unclear whether the drug was responsible for the events.
The most common side effects of fingolimod have been head colds, headache, and fatigue, but a few cases of skin cancer have been reported, which has also been reported in patients taking natalizumab (Tysabri), an approved MS drug.
Fingolimod has also been known to cause macular edema, resulting in decreased vision.
This article uses material from the Wikipedia article Fingolimod, which is released under the Creative Commons Attribution-Share-Alike License 3.0.