Catalog No.S5950 Synonyms: FTY-720A, FTY-720
Molecular Weight(MW): 307.47
Fingolimod is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
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|Description||Fingolimod is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.|
The main immunomodulatory mechanism of action of fingolimod is based on its effect on lymphocyte homing. It reversibly redistributes T and B cells from the circulation to secondary lymphoid organs like peripheral and mesenteric lymph nodes and Peyer's patches, thereby causing a state of peripheral lymphopenia.
SphK2 is the only enzyme which activates fingolimod in vivo,since only Sphk2 knockout mice are resistant to fingolimod-induced lymphopenia. A major advantage of fingolimod as a therapeutic agent is the possibility of its oral application. Absorption is food-independent and slow (maximal plasma concentration after 12-16 h), but extensive, and its bioavailability is high (93%). It reaches steady state concentrations after 1-2 months during daily intake. Fingolimod shows high plasma protein binding (>99.7%), mainly to albumin, and in contrast to S1P, there is no evidence for fingolimod binding to ApoM/HDL. It has a large volume of distribution of approx. 20L/kg and shows slow blood clearance (6.3±2.3 L/h), resulting in a half-life of 6-9 days. Fingolimod alleviates disease burden in immune-mediated animal models of multiple sclerosis.
|In vitro||DMSO||13 mg/mL (42.28 mM)|
|Ethanol||5 mg/mL (16.26 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03345940||Recruiting||Drug: Fingolimod|Drug: Dimethyl Fumarate||Relapsing Remitting Multiple Sclerosis||Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta|Patient-Centered Outcomes Research Institute|Universita degli Studi di Genova||April 30 2017||Phase 4|
|NCT02575365||Terminated||Drug: 05 mg Fingolimod||Cognition|Brain Volume Loss||Novartis Pharmaceuticals|Novartis||February 16 2016||Phase 4|
|NCT02490930||Completed||Drug: Fingolimod||Glioblastoma|Anaplastic Astrocytoma||Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins||July 2015||Early Phase 1|
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