linaclotide

Linaclotide is a synthetic 14-amino acid peptide and a selective agonist of guanylate cyclase C (GC-C) receptors located on the luminal surface of intestinal epithelial cells. It is minimally absorbed after oral administration and acts locally in the gastrointestinal tract. Activation of GC-C increases intracellular and extracellular cyclic guanosine monophosphate (cGMP), which stimulates secretion of chloride and bicarbonate into the intestinal lumen via activation of cystic fibrosis transmembrane conductance regulator (CFTR) ion channels. This leads to increased intestinal fluid secretion, accelerated transit, and relief from constipation symptoms. Linaclotide also reduces visceral pain by decreasing activity in pain-sensing nerves through elevated extracellular cGMP levels. It is primarily indicated for adults with irritable bowel syndrome with constipation (IBS-C), chronic idiopathic constipation (CIC), and functional constipation[1][2][4][5][6][7].

Brand names

LinzessConstella令泽舒

Other names

利那洛肽