Carotegrast methyl

Carotegrast methyl (trade name Carogra) is a drug used for the treatment of ulcerative colitis.

Carotegrast methyl is a prodrug that has little pharmacological activity itself. The methyl ester, which is designed to enhance oral bioavailability, is hydrolyzed to a carboxylic acid, carotegrast, by the enzyme carboxylesterase 1 in the liver. Carotegrast is an α4-integrin antagonist which prevents the chronic inflammation affecting the gastrointestinal tract in individuals with ulcerative colitis.


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Carotegrast methyl received approval in Japan in March 2022 for the treatment of moderate ulcerative colitis in patients who had inadequate response to mesalazine.