Carotegrast methyl explained
| Tradename: | Carogra |
| Legal Status: | Rx in Japan |
| Synonyms: | AJM 300 |
| Cas Number: | 401905-67-7 |
| Chemspiderid: | 8048469 |
| Pubchem: | 9872780 |
| Unii: | OYK17DYO9M |
| Drugbank: | DB16119 |
| Iuphar Ligand: | 10510 |
| Kegg: | D09799 |
| Iupac Name: | methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-yl]phenyl]propanoate |
| C: | 28 |
| H: | 26 |
| Cl: | 2 |
| N: | 4 |
| O: | 5 |
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]
Notes and References
- Web site: Carotegrast methyl - EA Pharma . Adis Insight .
- Fukase H, Kajioka T, Oikawa I, Ikeda N, Furuie H . 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 . 31965548 . 7035301 . 10.1007/s40261-019-00879-1 .
- Matsuoka K, Watanabe M, Ohmori T, Nakajima K, Ishida T, Ishiguro Y, Kanke K, Kobayashi K, Hirai F, Watanabe K, Mizusawa H, Kishida S, Miura Y, Ohta A, Kajioka T, Hibi T . 6 . 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 . 35366419 . 10.1016/S2468-1253(22)00022-X . 247847704 .
- Dhillon S . Carotegrast Methyl: First Approval . Drugs . 82 . 9 . 1011–1016 . June 2022 . 35723803 . 10.1007/s40265-022-01732-0 . 249854654 .
