Chemical structure of the active metabolite carotegrast
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]
^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. PMC7035301. 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.
carotegrast, methyl, trade, name, carogra, drug, used, treatment, ulcerative, colitis, clinical, datatrade, namescarograother, namesajm, 300legal, statuslegal, statusrx, japanidentifiersiupac, name, methyl, dichlorobenzoyl, amino, dimethylamino, methyl, dioxoq. Carotegrast methyl trade name Carogra is a drug used for the treatment of ulcerative colitis 1 Carotegrast methylClinical dataTrade namesCarograOther namesAJM 300Legal statusLegal statusRx in JapanIdentifiersIUPAC name methyl 2S 2 2 6 dichlorobenzoyl amino 3 4 6 dimethylamino 1 methyl 2 4 dioxoquinazolin 3 yl phenyl propanoateCAS Number401905 67 7PubChem CID9872780IUPHAR BPS10510DrugBankDB16119ChemSpider8048469UNIIOYK17DYO9MKEGGD09799CompTox Dashboard EPA DTXSID60193189Chemical and physical dataFormulaC 28H 26Cl 2N 4O 5Molar mass569 44 g mol 1Carotegrast 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 a4 integrin antagonist which prevents the chronic inflammation affecting the gastrointestinal tract in individuals with ulcerative colitis 3 Chemical structure of the active metabolite carotegrastCarotegrast 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 edit 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 a4 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 a4 integrin as induction therapy for patients with moderately active ulcerative colitis a multicentre randomised double blind placebo controlled phase 3 study The Lancet Gastroenterology amp 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 nbsp This drug article relating to the gastrointestinal system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Carotegrast methyl amp oldid 1194222277, wikipedia, wiki, book, books, library,
