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Synonyms: SB-683699 | SB683699
Compound class: Synthetic organic
Comment: Firategrast (SB-683699) is an orally bioavailable, short-acting small molecule α4-integrin antagonist. It was designed to reduce α4β1/α4β7 integrin-mediated trafficking of lymphocytes into the central nervous system (CNS). Anti-α4-integrin natalizumab is currently approved to treat MS, but its long half-life is problematic, and it has to be administered by infusion. This short acting small molecule was developed as an alternative to antibody therapy.
|α4β1 integrins are regarded as a highly relevant molecular target in multiple sclerosis. Antagonising α4 integrins reduces migration of leucocytes to sites of inflammation and across biological barriers, such as into the CNS .|