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Autoimmune disease

Multiple sclerosis (MS)

Endothelin 1 (EDN1; ET1);
endothelin receptor

Patient studies suggest antagonizing ET1 signaling could be useful for treating MS. In patients with MS, ET1 levels in circulation and in plaque-associated astrocytes were higher than those in healthy controls. Patients with MS treated with the ET1 receptor antagonist Tracleer bosentan showed increased cerebral blood flow, which is known to be decreased in MS, compared with untreated patients. Next steps include studying the mechanism of ET1 upregulation in astrocytes and evaluating the effect of ET1 receptor antagonists on MS progression in a clinical trial.
Tracleer is marketed by Actelion Ltd. to treat pulmonary arterial hypertension (PAH).
At least three other endothelin receptor antagonists are marketed for cardiovascular indications.

SciBX 6(15); doi:10.1038/scibx.2013.357
Published online April 18, 2013

Unpatented; licensing status not applicable

D'haeseleer, M. et al. Proc. Natl. Acad. Sci. USA; published online
March 18, 2013;
Contact: Jacques De Keyser, University Hospital Brussels, Brussels, Belgium