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Carotegrast is a small-molecule α4-integrin antagonist approved for the treatment of moderate ulcerative colitis in patients who have an inadequate response or intolerance to 5-aminosalicylates. Carotegrast methyl is a prodrug that is hydrolyzed in the liver to carotegrast, the active metabolite, which blocks the interaction between α4β1 or α4β7 integrins and their ligands VCAM-1 and MAdCAM-1. This inhibition prevents the adhesion and transmigration of inflammatory cells, effectively reducing chronic gastrointestinal inflammation. Developed by EA Pharma (formerly Ajinomoto Pharmaceuticals) and Kissei Pharmaceutical, carotegrast methyl is marketed under the brand name Carogra and became clinically available in Japan in March 2022[1][5][3].
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