Product Description

Linaclotide is a guanylate cyclase-C receptor agonist (GCCA) with visceral analgesia and endocrine activity. Both linaclotide and its active metabolites can bind to the guanylate cyclase-C (GC-C) RECEPTOR ON THE LUMEN SURFACE OF THE SMALL INTESTINAL EPITHELIUM. In animal models, by activating GC-C, linaclotide can reduce visceral pain and increase the speed of gastrointestinal transit, while in humans, the drug can also increase the speed of colonic transit. The result of GC-C activation is an increase in intracellular and extracellular cGMP (cyclic guanylate) concentrations. Extracellular cGMP can reduce the activity of pain nerve fibers and may reduce visceral pain in model animals. Intracellular cGMP can increase the secretion of chloride and bicarbonate in the small intestinal lumen by activating CFTR (cystic fibrosis transmembrane conductance modulator), ultimately leading to increased secretion of small intestinal fluid and increased intestinal transport.