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Autoimmune disease

Multiple sclerosis (MS)

Sphingosine 1-phosphate
receptor 1
(S1PR1; S1P1; EDG1)

Mouse and cell culture studies suggest the S1P1-selective antagonist NIBR-0213 could help treat MS. In vitro, NIBR-0213 selectively inhibited S1P1 with an IC50 value of 2.5 nM and was inactive against S1P2 (S1PR2; EDG5), S1P3 (S1PR3; EDG3) and S1P4 (S1PR4; EDG6). In a mouse model of experimental autoimmune encephalitis (EAE), NIBR-0213 decreased disease scores compared with vehicle and showed efficacy comparable to that of the marketed S1PR agonist Gilenya fingolimod, which acts by downregulating the receptor. Next steps could include evaluating NIBR-0213 in additional mouse MS models.
Mitsubishi Tanabe Pharma Corp. and Novartis AG market Gilenya to treat MS.
Exelixis Inc. has XL541, an S1P1 antagonist, in preclinical development to treat cancer.
Noxxon Pharma AG's NOX-S91, an l-aptamer that antagonizes sphingosine 1-phosphate, is in preclinical development to treat age-related macular degeneration (AMD).

SciBX 5(39); doi:10.1038/scibx.2012.1023
Published online Oct. 4, 2012

Patent application filed; licensing status unavailable

Quancard, J. et al. Chem. Biol.; published online Sept. 21, 2012;
Contact: Jean Quancard, Novartis Institutes for BioMedical Research, Basel, Switzerland