linaclotide   Click here for help

GtoPdb Ligand ID: 5017

Synonyms: Constella® | Linzess® | MM-416775
Approved drug
linaclotide is an approved drug (FDA and EMA (2012))
Comment: Linaclotide represents a first-in-class, oral guanylate cyclase 2C activator [2]. It is a synthetic analogue of pathological heat-stable bacterial enterotoxins, and retains the same intrachain disulfide bond structure essential for biological activity.
Marketed formulations contain linaclotide acetate (PubChem CID 16158207). See also plecanatide, the second approved GC-C activator.
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References
1. Bharucha AE, Waldman SA. (2010)
Taking a lesson from microbial diarrheagenesis in the management of chronic constipation.
Gastroenterology, 138 (3): 813-7. [PMID:20114092]
2. Busby RW, Bryant AP, Bartolini WP, Cordero EA, Hannig G, Kessler MM, Mahajan-Miklos S, Pierce CM, Solinga RM, Sun LJ et al.. (2010)
Linaclotide, through activation of guanylate cyclase C, acts locally in the gastrointestinal tract to elicit enhanced intestinal secretion and transit.
Eur. J. Pharmacol., 649 (1-3): 328-35. [PMID:20863829]
3. Harris LA, Crowell MD. (2007)
Linaclotide, a new direction in the treatment of irritable bowel syndrome and chronic constipation.
Curr. Opin. Mol. Ther., 9 (4): 403-10. [PMID:17694454]
4. Shailubhai K. (2002)
Therapeutic applications of guanylate cyclase-C receptor agonists.
Curr Opin Drug Discov Devel, 5 (2): 261-8. [PMID:11926132]