Synonyms: HCA2969
Compound class:
Synthetic organic
Comment: Carotegrast (HCA2969) is the active metabolite of carotegrast methyl [1,4]. It acts as an antagonist of α4 integrin-mediated transmigration of leukocytes to sites of inflammation. The chemical structure of carotegrast is claimed as example 108 in EA Pharma patent US20110065918A1 which claims phenylalanine derivatives as α4 integrin antagonists for use as clinical therapeutics [2].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Fukase H, Kajioka T, Oikawa I, Ikeda N, Furuie H. (2020)
AJM300, a novel oral antagonist of α4-integrin, sustains an increase in circulating lymphocytes: A randomised controlled trial in healthy male subjects. Br J Clin Pharmacol, 86 (3): 591-600. [PMID:31658381] |
2. Makino S, Okuzumi T, Yoshimura T, Satake Y, Suzuki N, Izawa H, Sagi K, Chiba A, Nakanishi E, Murata M et al.. (2011)
New phenylalanine derivatives. Patent number: US20110065918A1. Assignee: EA Pharma Co Ltd. Priority date: 18/08/2000. Publication date: 17/03/2011. |
3. Shukla T, Sands BE. (2019)
Novel Non-biologic Targets for Inflammatory Bowel Disease. Curr Gastroenterol Rep, 21 (5): 22. [PMID:31016396] |
4. Sugiura T, Kageyama S, Andou A, Miyazawa T, Ejima C, Nakayama A, Dohi T, Eda H. (2013)
Oral treatment with a novel small molecule alpha 4 integrin antagonist, AJM300, prevents the development of experimental colitis in mice. J Crohns Colitis, 7 (11): e533-42. [PMID:23623333] |
5. Vetter M, Neurath MF. (2017)
Emerging oral targeted therapies in inflammatory bowel diseases: opportunities and challenges. Therap Adv Gastroenterol, 10 (10): 773-790. [PMID:29051788] |
6. White JR, Phillips F, Monaghan T, Fateen W, Samuel S, Ghosh S, Moran GW. (2018)
Review article: novel oral-targeted therapies in inflammatory bowel disease. Aliment Pharmacol Ther, 47 (12): 1610-1622. [PMID:29672874] |