Linaclotide

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Scientific Name: Linaclotide
Brand Name: Constella, Linzess
Company Owner: Not Available
Mechanism Of Action Linaclotide is an agonist of guanylate cyclase-C (GC-C) . Once linaclotide and its active metabolite binds to GC-C, it has local effect on the luminal surface of the intestinal epithelium. Activation of GC-C by linaclotide results in the intra- and extracellular increase of cyclic guanosine monophosphate concentrations (cGMP) . This elevation of cGMP levels stimulates the secretion of chloride and bicarbonate into the intestinal lumen via activation of cystic fibrosis transmembrane conductance regulator (CFTR) ion channel. Ultimately, linaclotide helps patients with IBS (especially with constipation) as GI transit is accelerated and the release of intestinal fluid is increased. In animal models, a decrease in visceral pain after administration of linaclotide may be observed. A decrease in the activity of pain-sensing nerves occurs as a result of an increase in extracellular cGMP.
Description of the Drug: Linaclotide is a guanylate cyclase-C agonist used to treat constipation associated with irritable bowel syndrome or that is idiopathic in nature.
Protein Data Bank: Not Available
Source: DrugBank Online – DrugBank.com. Retrieved 2023-01-23 from https://go.drugbank.com/drugs/DB08890