Thursday, October 4, 2012
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Multiple sclerosis (MS)
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
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).
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
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