Linaclotide is a synthetic 14-amino acid cyclic peptide and first-in-class guanylate cyclase-C (G-CC) agonist. Linaclotide is structurally related to human guanylin and uroguanylin, paracrine peptide hormones that are endogenous activators of GC-C. It is also a homolog of a heat-stable enterotoxin derived from Escherichia coli, the first natural ligand that activates GC-C.
Linaclotide is used for the treatment of various types of constipation, including irritable bowel syndrome with constipation. Linaclotide was first approved by the FDA on August 30, 2012. It gained EMA and Health Canada approval on November 26, 2012 and December 3, 2013, respectively. Linaclotide works to improve the symptoms of constipation and gastrointestinal symptoms of conditions involving constipation.
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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