Carotegrast methyl

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]

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.

[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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