Linaclotide
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Linaclotide is a guanylate cyclase-C agonist used to treat different types of constipation, such as irritable bowel syndrome-related constipation, idiopathic constipation, and functional constipation.
Linaclotide is a guanylate cyclase-C agonist used to treat different types of constipation, such as irritable bowel syndrome-related constipation, idiopathic constipation, and functional constipation.
Linaclotide is a potent, highly selective agonist of guanylate cyclase-C (GC-C), a soluble and single-membrane-spanning enzyme on the luminal surface of intestinal epithelial cells. GC-C regulates chloride secretion. Linaclotide has a dual mode of action. Firstly, linaclotide and its active metabolite bind to transmembrane GC-C. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevated intracellular cGMP activates the cGMP-dependent protein kinase II (PKG-II), which phosphorylates and activates the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel expressed on the apical surface of intestinal epithelial cells. CFTR activation promotes the secretion of chloride and bicarbonate ions and inhibits sodium absorption, resulting in increased intestinal fluid and accelerated GI transit. Secondly, linaclotide exerts anti-nociceptive effects by reducing visceral hypersensitivity. Increased levels of extracellular cGMP in submucosa inhibit colonic nociceptors, relieving intestinal pain.
Linaclotide is indicated for the treatment of irritable bowel syndrome with constipation in adults. This indication is approved in the US, Canada, and Europe. In the US and Canada, it is also indicated for the treatment of chronic idiopathic constipation in adults. In the US, it is also indicated for the treatment of functional constipation in pediatric patients 6 to 17 years of age.
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每项发明一条，涵盖美国、欧洲、PCT 与中国的同族专利。
