Plecanatide (SP-304) is a synthetic, 16-amino acid peptide with 2 disulfide bonds that is a secondin-class
guanylate cyclase-C (GC-C) receptor agonist. Plecanatide (brand name Trulance) was approved in January 2017 by the FDA for the treatment of chronic idiopathic constipation (CIC). Plecanatide stimulates intestinal fluid secretions in the gastrointestinal tract to support regular bowel function. Plecanatide, taken orally once daily, works locally in the upper GI tract to stimulate secretion of intestinal fluid and support regular bowel function. Plecanatide is structurally related to human uroguanylin, and similar to uroguanylin, plecanatide functions as a
guanylate cyclase-C (GC-C) agonist. Both plecanatide and its active metabolite bind to GC-C and act locally
on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both
intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation of
intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through
activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in
increased intestinal fluid and accelerated transit. In animal models, plecanatide has been shown to increase
fluid secretion into the gastrointestinal (GI) tract, accelerate intestinal transit, and cause changes in stool
consistency.
CNS Activity
Originator
Approval Year
PubMed
Title | Date | PubMed |
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Safety and tolerability of plecanatide in patients with chronic idiopathic constipation: long-term evidence from an open-label study. | 2018 Apr |
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Efficacy and safety of plecanatide in treating constipation predominant irritable bowel syndrome. | 2018 Feb |
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Efficacy and Tolerability of Guanylate Cyclase-C Agonists for Irritable Bowel Syndrome with Constipation and Chronic Idiopathic Constipation: A Systematic Review and Meta-Analysis. | 2018 Mar |
Patents
Sample Use Guides
The recommended adult dosage of TRULANCE (Plecanatide ) is 3 mg taken orally once daily.
Route of Administration:
Oral
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ACTIVE MOIETY
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