Treatment of chronic idiopathic constipation: plecanatide

The US FDA has approved its new drug TRULANCE (plecanatide) for the treatment of chronic idiopathic constipation (CIC). This is the first new drug approved by the US FDA in 2017.

TRULANCE is the first new drug to mimic the function of urinary guanosine protein in vivo. Urinary guanosine is a naturally existing endogenous gastrointestinal protein peptide, which can stimulate fluid secretion and change the consistency of feces by affecting the normal intestinal function exenatide impurities

Plecanatide is an oral polypeptide composed of 16 amino acids, which is designed to mimic human gastrointestinal peptide, urinoguanosine. At the same time, Pucanatide is a guanylate cyclase - C agonist, which can stimulate intestinal secretion and accelerate defecation in clinical practice.

CAS No.: 467426-54-6

Molecular formula: C65H104N18O26S4

Molecular weight: 1681.88

Appearance White powder

Purity (HPLC) ≥ 95.0%

Single impurity ≤ 2.0%

Acetate content 5.0% ～ 12.0%

Moisture content ≤ 10.0%

Peptide content ≥ 80.0%

Packaging and transportation:

Low temperature and vacuum packaging, accurate to milligram as required.

Storage method: freeze dry at - 20 ℃ and keep away from light

Action mechanism

plecanatide is structurally related to human urinary guanosine, and similar to urinary guanosine, Plecanatide functions as a guanylate cyclase C (GC-C) agonist. Both Plecanatide and its active metabolite bind to GC-C and locally act on the luminal surface of intestinal epithelium. Activation of GC-C leads to the increase of cGMP concentration in both intracellular and extracellular cells. The increase of cGMP in cells stimulates chloride and bicarbonate to be secreted into the small intestinal cavity, mainly through the activation of cystic fibrosis transmembrane conduction regulator (CFTR) ion channels, leading to the increase and acceleration of small intestinal fluid. In animal models, the plecanatide method b shows that it increases the secretion of liquid into the gastrointestinal (GI) tract, accelerates the passage of small intestine, and causes changes in stool viscosity.

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