A potent and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis

Citations of this article
Mendeley users who have this article in their library.


Lymphocyte trafficking is critically regulated by the Sphingosine 1-phosphate receptor-1 (S1P1), a G protein-coupled receptor that has been highlighted as a promising therapeutic target in autoimmunity. Fingolimod (FTY720, Gilenya) is a S1P1 receptor agonist that has recently been approved for the treatment of multiple sclerosis (MS). Here, we report the discovery of NIBR-0213, a potent and selective S1P1 antagonist that induces long-lasting reduction of peripheral blood lymphocyte counts after oral dosing. NIBR-0213 showed comparable therapeutic efficacy to fingolimod in experimental autoimmune encephalomyelitis (EAE), a model of human MS. These data provide convincing evidence that S1P1 antagonists are effective in EAE. In addition, the profile of NIBR-0213 makes it an attractive candidate to further study the consequences of S1P1 receptor antagonism and to differentiate the effects from those of S1P1 agonists. © 2012 Elsevier Ltd.




Quancard, J., Bollbuck, B., Janser, P., Angst, D., Berst, F., Buehlmayer, P., … Bigaud, M. (2012). A potent and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. Chemistry and Biology, 19(9), 1142–1151. https://doi.org/10.1016/j.chembiol.2012.07.016

Register to see more suggestions

Mendeley helps you to discover research relevant for your work.

Already have an account?

Save time finding and organizing research with Mendeley

Sign up for free