Ligand id: 9069

Name: plecanatide

Structure and Physico-chemical Properties

2D Structure
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Summary of Clinical Use
Plecanatide was evaluated in several Phase 3 clinical trials in patients with chronic idiopathic constipation or IBS-C. Click here to link to's list of Phase 3 plecanatide trials. In January 2017 plecanatide was FDA approved for the treatment of chronic idiopathic constipation (CIC) in adults. In January 2018, the FDA expanded approval to include treatment of patients with irritable bowel syndrome, constipation subtype (IBS-C).
Mechanism Of Action and Pharmacodynamic Effects
Aginist-induced activation of GC-C receptors stimulates intracellular production of cyclic guanosine monophosphate (cGMP). This leads to downstream activation of the cystic fibrosis transmembrane conductance regulator (CFTR), the apical ion channel responsible for efflux of chloride ions from enterocytes lining the GI tract. The net result is efflux of water into the intestinal lumen, thus ameliorating constipation and improving intestinal transit.