NCIt definition : An agonist of intestinal guanylate cyclase type C (GC-C) which is almost structurally
identical to human uroguanylin, with laxative and anti-nociceptive activities. Upon
oral administration, plecanatide binds to and activates GC-C receptors located on
endothelial cells on the luminal surface of the intestinal epithelium. This increases
the concentration of intracellular cyclic guanosine monophosphate (cGMP). cGMP activates
the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel and stimulates
the secretion of chloride and bicarbonate into the intestinal lumen. This also promotes
sodium excretion into the lumen and osmosis. The increased intestinal fluid secretion
accelerates gastrointestinal transit of intestinal contents, improves bowel movement,
softens stool, and relieves constipation. In addition, plecanatide exerts its anti-nociceptive
effects by increasing the concentration of extracellular cGMP which inhibits the activity
of pain-sensitive nerves, decreases muscle contractions and may relieve intestinal
pain.;