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Linaclotide


Mechanism of action:

Linaclotide is a guanylate cyclase-C agonist. Linaclotide binds to guanylate cyclase-C located on the brush border of epithelial cells in the small intestine and colon, promoting intracellular cyclic guanosine monophosphate (cGMP) production. cGMP activates the cystic fibrosis transmembrane conductance regulator chloride channel, increasing secretion of chloride and bicarbonate ions. Water then follows into the intestinal lumen, softening the stool and increasing intestinal content volume.

Reference(s):

Busby RW et al. (2013). Pharmacologic properties, metabolism, and disposition of linaclotide, a novel therapeutic peptide approved for the treatment of irritable bowel syndrome with constipation and chronic idiopathic constipation. J Pharmacol Exp Ther.

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