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Firategrast is an orally bioavailable small molecule antagonist of the α4β1 and α4β7 integrins, developed as a potential treatment for multiple sclerosis (MS) and other immune-mediated diseases. By blocking these integrins, firategrast inhibits the trafficking of lymphocytes into the central nervous system (CNS), thereby reducing inflammation associated with MS. It was designed as a short-acting alternative to monoclonal antibody therapies like natalizumab, aiming to reduce risks such as progressive multifocal leukoencephalopathy (PML). Firategrast reached phase II clinical trials for relapsing-remitting MS but development was discontinued for other indications including Crohn’s disease, asthma, and rheumatoid arthritis. The drug was originally developed by Mitsubishi Tanabe Pharma and licensed to GlaxoSmithKline for further development[1][3][5][6][8].
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