Chemistry:Carotegrast methyl
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Short description: Chemical compound
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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. https://adisinsight.springer.com/drugs/800019529.
- ↑ "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. March 2020. doi:10.1007/s40261-019-00879-1. PMID 31965548.
- ↑ "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. July 2022. doi:10.1016/S2468-1253(22)00022-X. PMID 35366419.
- ↑ "Carotegrast Methyl: First Approval". Drugs 82 (9): 1011–1016. June 2022. doi:10.1007/s40265-022-01732-0. PMID 35723803. https://figshare.com/articles/online_resource/Carotegrast_Methyl_First_Approval/19790860.
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