Carotegrast methyl
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Trade names | Carogra |
Other names | AJM 300 |
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Formula | C28H26Cl2N4O5 |
Molar mass | 569.44 g·mol−1 |
Carotegrast methyl (trade name Carogra) is a drug used for the treatment of ulcerative colitis.[1]
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.[2] Carotegrast is an α4-integrin antagonist which prevents the chronic inflammation affecting the gastrointestinal tract in individuals with ulcerative colitis.[3]
Carotegrast methyl received approval in Japan in March 2022 for the treatment of moderate ulcerative colitis in patients who had inadequate response to mesalazine.[4]
References
- ^ "Carotegrast methyl - EA Pharma". Adis Insight.
- ^ Fukase H, Kajioka T, Oikawa I, Ikeda N, Furuie H (March 2020). "Food Effect on a Single High Dose of Carotegrast Methyl, an Oral Antagonist of α4-Integrin, in Healthy Male Subjects: A Randomised, Placebo-Controlled, Double-Blind Study". Clinical Drug Investigation. 40 (3): 237–247. doi:10.1007/s40261-019-00879-1. PMC 7035301. PMID 31965548.
- ^ Matsuoka K, Watanabe M, Ohmori T, Nakajima K, Ishida T, Ishiguro Y, et al. (July 2022). "AJM300 (carotegrast methyl), an oral antagonist of α4-integrin, as induction therapy for patients with moderately active ulcerative colitis: a multicentre, randomised, double-blind, placebo-controlled, phase 3 study". The Lancet. Gastroenterology & Hepatology. 7 (7): 648–657. doi:10.1016/S2468-1253(22)00022-X. PMID 35366419. S2CID 247847704.
- ^ Dhillon S (June 2022). "Carotegrast Methyl: First Approval". Drugs. 82 (9): 1011–1016. doi:10.1007/s40265-022-01732-0. PMID 35723803. S2CID 249854654.