Drug intelligence / Profile preview

amiselimod

Development stage
Discontinued
Lead developer
Salix Pharmaceuticals
Modality
Small Molecules
Administration
Oral
01

Overview

Amiselimod is an orally active, selective sphingosine 1-phosphate receptor modulator developed primarily for the treatment of autoimmune diseases such as multiple sclerosis and ulcerative colitis. It acts as a functional antagonist at the sphingosine 1-phosphate receptor 1 (S1P1), sequestering lymphocytes in lymph nodes and thereby reducing their migration to sites of inflammation. Amiselimod was designed to avoid S1P3 receptor agonism, which is associated with cardiac side effects seen in similar drugs like fingolimod. Its active metabolite, amiselimod phosphate, is generated more slowly than that of fingolimod, potentially resulting in a better cardiac safety profile. The drug has shown efficacy in reducing disease activity in preclinical models and clinical trials for relapsing-remitting multiple sclerosis and ulcerative colitis[1][4][5][6]. Development has been discontinued for several indications but continues for ulcerative colitis.

Other names
amiselimod hydrochloride
02

Targets

S1PR5 (Sphingosine-1-phosphate receptor 5)

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