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Carotegrast methyl
Clinical data
Trade names	Carogra
Other names	AJM 300
Legal status
Legal status	Rx in Japan;
Identifiers
	IUPAC name methyl (2S)-2-[(2,6-dichlorobenzoyl)amino]-3-[4-[6-(dimethylamino)-1-methyl-2,4-dioxoquinazolin-3-yl]phenyl]propanoate;
CAS Number	401905-67-7;
PubChem CID	9872780;
IUPHAR/BPS	10510;
DrugBank	DB16119;
ChemSpider	8048469;
UNII	OYK17DYO9M;
KEGG	D09799;
CompTox Dashboard (EPA)	DTXSID60193189 ;
Chemical and physical data
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]

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]

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.

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[1] "Carotegrast methyl - EA Pharma". Adis Insight.

[2] 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.

[3] 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.

[4] Dhillon S (June 2022). "Carotegrast Methyl: First Approval". Drugs. 82 (9): 1011–1016. doi:10.1007/s40265-022-01732-0. PMID 35723803. S2CID 249854654.

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