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Synonyms: AJM-300 | AJM300
Compound class: Synthetic organic
Comment: Carotegrast methyl (AJM300) is an orally administered esterified prodrug α4 integrin inhibitor/antagonist that was developed by EA Pharma for anti-inflammatory potential .
|Carotegrast methyl (AJM300) is a small-molecule anti-integrin prodrug. Its active metabolite, carotegrast, produces the same functional outcome as the anti-α4 antibody natalizumab, but with the benefits associated with small-molecule drugs [2-4]. Specifically, carotegrast blocks interactions between α4β1 and α4β7 integrins with their counter-receptors (VCAM-1 and MAdCAM-1 respectively) and fibronectin, and this mechanism limits transmigration of leukocytes into sites of inflammation.|