Tissue-repair, gut & immune-signalling peptides
Linaclotide
Also known as guanylate cyclase-C agonist
A 14-amino-acid gut-acting peptide that activates guanylate cyclase-C on intestinal cells — one of the few oral peptide drugs.
In 60 seconds
Approved in the US and other markets for chronic idiopathic constipation and constipation-predominant IBS in adults, and for functional constipation in children aged 6–17. In the paediatric phase 3 trial the most frequent treatment-related adverse event was diarrhoea (4% versus 1% on placebo).
- A phase 3 randomised placebo-controlled trial in 328 children aged 6–17 found linaclotide efficacious and well tolerated for functional constipation.
- Reviews guanylate cyclase-C agonists as peripherally acting treatments for chronic visceral pain.
- A systematic review and meta-analysis compared lubiprostone, linaclotide and elobixibat for chronic constipation.
Mechanism
Linaclotide activates guanylate cyclase-C on the luminal surface of intestinal epithelium, raising cyclic GMP. That increases chloride and bicarbonate secretion into the gut and, in research models, reduces visceral pain signalling.
Research status
Approved in the US and other markets for chronic idiopathic constipation and constipation-predominant IBS in adults, and for functional constipation in children aged 6–17.
Key studies
A phase 3 randomised placebo-controlled trial in 328 children aged 6–17 found linaclotide efficacious and well tolerated for functional constipation.
Efficacy and safety of linaclotide in treating functional constipation in paediatric patients: a randomised, double-blind, placebo-controlled, multicentre, phase 3 trial — Lancet Gastroenterol Hepatol, 2024 · PMID 38211604
Reviews guanylate cyclase-C agonists as peripherally acting treatments for chronic visceral pain.
Guanylate cyclase-C agonists as peripherally acting treatments of chronic visceral pain — Trends Pharmacol Sci, 2022 · PMID 34865885
A systematic review and meta-analysis compared lubiprostone, linaclotide and elobixibat for chronic constipation.
Comparative profiles of lubiprostone, linaclotide, and elobixibat for chronic constipation: a systematic literature review with meta-analysis and number needed to treat/harm — BMC Gastroenterol, 2024 · PMID 38166671
An early review of linaclotide as a guanylate cyclase-C agonist for constipation-associated gut disorders.
Linaclotide, a synthetic guanylate cyclase C agonist, for the treatment of functional gastrointestinal disorders associated with constipation — Expert Rev Gastroenterol Hepatol, 2011 · PMID 21651347
Safety signals in the literature
In the paediatric phase 3 trial the most frequent treatment-related adverse event was diarrhoea (4% versus 1% on placebo).
Legal status (South Africa)
Not registered as a medicine for human use in South Africa (unless stated otherwise); research use only.
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Comparisons
Questions
What is Linaclotide?
A 14-amino-acid gut-acting peptide that activates guanylate cyclase-C on intestinal cells — one of the few oral peptide drugs. Linaclotide activates guanylate cyclase-C on the luminal surface of intestinal epithelium, raising cyclic GMP. That increases chloride and bicarbonate secretion into the gut and, in research models, reduces visceral pain signalling.
What is the research status of Linaclotide?
Approved in the US and other markets for chronic idiopathic constipation and constipation-predominant IBS in adults, and for functional constipation in children aged 6–17.
What safety signals are reported for Linaclotide?
In the paediatric phase 3 trial the most frequent treatment-related adverse event was diarrhoea (4% versus 1% on placebo).
Does Living Water Labs stock Linaclotide?
Not at present. Linaclotide is profiled here for reference, with citations to the published literature. You can ask to be notified if we add it. Not registered as a medicine for human use in South Africa (unless stated otherwise); research use only.
More in Repair & immune
Research reference only. This page summarises published literature; it is not medical advice and contains no guidance on human use. Products supplied by Living Water Labs are for laboratory research only.
