Products
Plecanatide was approved in the United States in 2017 in film-coated tablet form (Trulance). Plecanatide is not currently approved in many countries.
Structure and properties
Plecanatide (C65H104N18O26S4, Mr = 1681.9 g/mol) is a 16 amino acid peptide derived from uroguanylin. It contains two disulfide bridges. Plecanatide exists as an amorphous white powder that is soluble in water. Structure: Asn-Asp-Glu-Cys-Glu-Leu-Cys-Val-Asn-Val-Ala-Cys-Thr-Gly-Cys-Leu.
Effects
Plecanatide has laxative properties. The effects are due to binding to guanylate cyclase-C (GC-C) on the surface of the intestinal epithelium. Activation of GC-C increases the intracellular and extracellular concentration of cGMP. This increases the secretion of chloride and bicarbonate into the intestinal lumen by activating the CFTR ion channel. More fluid enters the intestine and intestinal motility is stimulated. Plecanatide acts primarily locally and is poorly absorbed.
Indications
For the treatment of chronic idiopathic constipation.
Dosage
According to the SmPC. Tablets are taken once daily, regardless of meals.
Contraindications
For complete precautions, see the drug label.
Adverse effects
The most common possible adverse effect is diarrhea.
