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.
Click here for help
IUPHAR Pharmacology Education Project (PEP) logo

View more information in the IUPHAR Pharmacology Education Project: linactolide

No information available.
Summary of Clinical Use Click here for help
Used to treat chronic constipation and irritable bowel syndrome (IBS) where constipation is the main symptom (IBS-C).
Mechanism Of Action and Pharmacodynamic Effects Click here for help
Linaclotide mimics the action of heat-stable enterotoxins in the gut which would cause diarrhea via activation of the enzyme guanylate cyclase 2C (GUCY2C) [1]. Linaclotide activation of guanylate cyclase 2C in the luminal aspect of intestinal epithelium causes increased cGMP levels and this causes activation of the cystic fibrosis transmembrane conductance regulator (CFTR), which controls chloride ion efflux from enterocytes lining the GI tract. The result is a net efflux of water into the intestinal lumen which softens stools and stimulates bowel movements [2,4].
External links Click here for help