Plecanatide

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Cat Number

API467426546

CAS Number

467426-54-6

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Product Detail Description Scientific Support Customer Q&A

CAS Number

467426-54-6

Storage

Store at -20℃

Molecular Formula

C65H104N18O26S4

Molecular Weight

1681.89

Boiling Point

2120.0±65.0 ℃ at 760 mmHg

Relative Density

1.5±0.1

Standard

GMP

Qualification

USDMF

General Description

Plecanatide is a cyclic polypeptide composed of 16 amino acids, similar to uridine peptide. Plecanatide is an orally effective Guanylate cyclase-C (GC-C) receptor agonist that can stimulate intestinal secretion of intestinal fluid and accelerate defecation.

Mechanism of Action

Plecanatide and its active metabolites bind to the GC-C enzyme and act locally on the luminal surface of intestinal epithelial cells. The activation of the GC-C enzyme leads to an increase in the concentrations of cyclic guanosine monophosphate (cGMP) both inside and outside the cells, stimulating the secretion of chloride and bicarbonate into the intestinal lumen, thereby increasing the intestinal fluid and accelerating its passage. This ultimately achieves the goal of softening feces, promoting defecation, and alleviating the symptoms of chronic idiopathic constipation.

Application

Plecanatide regulates the acidic and alkaline ions in the gastrointestinal tract, induces the transport of fluids into the gastrointestinal tract, and increases the peristalsis of the gastrointestinal tract. Plecanatide was approved by the FDA for market release in 2017 and is used to treat adults with:
• Chronic Idiopathic Constipation (CIC)
• Irritable Bowel Syndrome with Constipation

Irritable Bowel Syndrome (IBS) and Functional Bowel Disorders (FBDs) are multi-mechanism-driven disorders of the brain-gut axis, requiring multi-targeting and individualized treatment strategies. Most traditional treatments are symptomatic, such as antidiarrhea drugs, laxatives, antispasmodics, and antidepressants, and are limited in their efficacy and generally target only one symptom.
Emerging treatment strategies on the market include regulation of the intestinal microenvironment, regulation of intestinal secretory function, regulation of intestinal motility, regulation of visceral sensitivity and pain, anti-inflammatory and immune regulation. Among them, Plecanatide, as a GC-C agonist, can activate the CFTR chloride ion channel, promoting the secretion of chloride ions and water into the intestinal lumen, and is used for CIC and IBS-C. Clinical studies have shown that Plecanatide has the advantages of definite efficacy, good compliance and safety.

Fig. 1 Mechanism of action of drugs (e.g., Plecanatide) for treating IBS-C and CIC. (Simrén M.; et al. 2018)

References

Simrén M, et al, New treatments and therapeutic targets for IBS and other functional bowel disorders. Nature Reviews Gastroenterology & Hepatology, 2018, 15(10): 589-605.