Linaclotide
approvedAlso known as: Linzess, Constella
Linaclotide is a 14-amino acid synthetic peptide that acts as a potent agonist of guanylate cyclase-C (GC-C), a receptor expressed on the luminal surface of intestinal epithelial cells. Upon binding, it increases intracellular cyclic guanosine monophosphate (cGMP) levels, which activates the cystic fibrosis transmembrane conductance regulator (CFTR) and promotes chloride and bicarbonate secretion into the intestinal lumen. This ionic flux drives water secretion, accelerating gastrointestinal transit and softening stool. Additionally, elevated cGMP may reduce visceral hypersensitivity by modulating nociceptive signaling, contributing to its analgesic effects in irritable bowel syndrome with constipation (IBS-C). Key research findings from clinical trials demonstrate that linaclotide significantly improves spontaneous bowel movement frequency, stool consistency, and abdominal pain compared to placebo in patients with IBS-C and chronic idiopathic constipation (CIC). A meta-analysis of phase 3 trials confirmed its efficacy, with a number needed to treat of approximately 6 for IBS-C responders. Common adverse effects include diarrhea (up to 20% incidence), which is dose-dependent and often transient. Long-term safety data support sustained efficacy without tachyphylaxis over 12–18 months. Clinically, linaclotide is approved by the FDA and EMA for adults with IBS-C and CIC, typically dosed at 290 µg (IBS-C) or 145 µg (CIC) once daily. It is contraindicated in pediatric patients under 6 years and should be avoided in those with mechanical gastrointestinal obstruction. Its peptide structure limits systemic absorption, confining activity to the gut lumen and reducing off-target effects. For research purposes only — not medical advice.
Key data
C59H79N15O21S6Research & studies
Treatment begins with lifestyle and dietary changes, then progresses to specialized tests or symptom-based classification.; Newer drugs include osmotic laxatives, secretagogues, bile acid transporter inhibitors, probiotics, prokinetics, and Kampo medicines.; Linaclotide is a small peptide agonist of guanylate cyclase C receptors, used for chronic constipation and irritable bowel syndrome.; Linaclotide is not linked to serum enzyme elevations or clinically apparent liver injury.
Irritable bowel syndrome is a common functional bowel disorder with significant daily life and economic impacts.; Symptoms include abdominal pain, bloating, distention, and altered bowel movements (diarrhea, constipation, or mixed).; The disease affects 5%-10% of healthy individuals and typically follows a relapsing-remitting course.; Aetiopathogenesis and pathophysiological mechanisms remain unknown.
Frequently asked questions
What is Linaclotide?
Linaclotide is a 14-amino acid synthetic peptide that acts as a potent agonist of guanylate cyclase-C (GC-C), a receptor expressed on the luminal surface of intestinal epithelial cells. Upon binding, it increases intracellular cyclic guanosine monophosphate (cGMP) levels, which activates the cystic fibrosis transmembra
How does Linaclotide work?
Guanylate cyclase-C agonist 14-aa peptide that increases intestinal fluid secretion and transit; approved for IBS-C and chronic constipation.
What is the research status of Linaclotide?
Linaclotide is currently classified as approved, with 459 research references on record. This is for research purposes only and is not medical advice.
What is the molecular weight of Linaclotide?
Linaclotide has a molecular weight of approximately 1526.8 g/mol (formula C59H79N15O21S6).
Related peptides
GLP-2 receptor agonist that promotes intestinal mucosal growth and absorption; approved for short bowel syndrome.
Uroguanylin-analog GC-C agonist that promotes pH-dependent intestinal fluid secretion; approved for chronic idiopathic constipation and IBS-C.
Tight-junction-regulating octapeptide that reduces intestinal permeability ('leaky gut'); trialed as an adjunct for celiac disease.
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