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Linaclotide

CAT#
10-101-161
Synonyms/Alias
Linaclotide; Linzess; UNII-N0TXR0XR5X
CAS No.
851199-59-2
Sequence
H–Cys1–Cys–Glu–Tyr–Cys–Cys–Asn–Pro–Ala–Cys–Thr–Gly–Cys–Tyr–OH
(Disulfide bridge: 1-6; 2-10; 5-13)
M.W/Mr.
1526.74
Molecular Formula
C₅₉H₇₉N₁₅O₂₁S₆
Source
Synthetic
Application
Linaclotide  is apeptide agonist of guanylate cyclase 2C. It was approved by the FDA in August 2012 for the treatment in adults of constipation-predominant irritable bowel syndrome (IBS-C) and chronic idiopathic constipation (CIC).
Description
Linaclotide is a 14-amino acid peptide indicated for the treatment of adults with CC and IBS-C; agonist of guanylate cyclase C
Areas of Interest
Constipation-predominant irritable bowel syndrome (IBS-C) and chronic idiopathic constipation (CIC)
Storage
-20°C

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Linaclotide is a synthetic, fourteen amino acid peptide and agonist of intestinal guanylate cyclase type C (GC-C), which is structurally related to the guanylin peptide family, with secretagogue, analgesic and laxative activities. Upon oral administration, linaclotide binds to and activates GC-C receptors located on the luminal surface of the intestinal epithelium. This increases the concentration of intracellular cyclic guanosine monophosphate (cGMP), which is derived from guanosine triphosphate (GTP). cGMP activates the cystic fibrosis transmembrane conductance regulator (CFTR) and stimulates the secretion of chloride and bicarbonate into the intestinal lumen. This promotes sodium excretion into the lumen and results in increased intestinal fluid secretion. This ultimately accelerates GI transit of intestinal contents, improves bowel movement and relieves constipation. Increased extracellular cGMP levels may also exert an antinociceptive effect, through an as of yet not fully elucidated mechanism, that may involve modulation of nociceptors found on colonic afferent pain fibers. Linaclotide is minimally absorbed from the GI tract.

Chronic constipation and irritable bowel syndrome (IBS) are functional gastrointestinal disorders that significantly affect patients’ quality of life. Chronic constipation and IBS are prevalent-12% of the US population meet the diagnostic criteria for IBS, and 15% meet the criteria for chronic constipation- and these conditions negatively impact the healthcare system from an economic perspective. Despite attempts at dietary modification, exercise, or use of over-the-counter medications, many patients have persistent symptoms. Alternative treatment options are limited. This article describes linaclotide (Linzess, Ironwood Pharmaceuticals/Forest Pharmaceuticals), a new, first-in-class medication for the treatment of chronic constipation and constipation-predominant IBS.

Lacy, B. E., Levenick, J. M., & Crowell, M. D. (2012). Linaclotide: a novel therapy for chronic constipation and constipation-predominant irritable bowel syndrome. Gastroenterology & hepatology, 8(10), 653.

Linaclotide is the first member of a novel class of drugs to be extensively evaluated for the treatment of chronic constipation (CC) and irritable bowel syndrome with constipation (IBS-C).

Corsetti, M., & Tack, J. (2013). Linaclotide: A new drug for the treatment of chronic constipation and irritable bowel syndrome with constipation. United European gastroenterology journal, 1(1), 7-20.

Linaclotide is a first-in-class, 14-amino acid peptide of the guanylin peptide family and acts as a selective agonist at the guanylate cyclase-C (GC-C) receptor on the luminal surface of intestinal enterocytes. The endogenous ligands of GC-C (guanylin peptide hormones guanylin and uroguanylin) bind to the receptor to promote intestinal secretions in response to a meal. Activation of GC-C by guanylin peptides, including linaclotide, results in increased levels of cyclic guanosine monophosphate (cGMP), a second messenger that plays a critical role in the regulation and secretion of intestinal fluid.

Thomas, R. H., & Allmond, K. (2013). Linaclotide (Linzess) for irritable bowel syndrome with constipation and for chronic idiopathic constipation. Pharmacy and Therapeutics, 38(3), 154.

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