Linaclotide
Hormonal and Signaling
ABOUT
Linaclotide is a 14-amino-acid guanylate-cyclase-C agonist with approved gastrointestinal indications. It acts mainly on the luminal surface of the intestinal epithelium and has negligible systemic availability at labelled oral doses.
EVIDENCE OVERVIEW
Supported by controlled human trials
WHAT THIS MEANS
Established. Review the research and limitations before relying on this record.
IDENTITY
HALF-LIFE
HOW IT IS THOUGHT TO WORK
Linaclotide and its active metabolite activate GC-C on the intestinal luminal surface, increasing cyclic GMP and promoting chloride and bicarbonate secretion through CFTR. This increases intestinal fluid and transit.
PHARMACOKINETICS
The cited label reports minimal absorption and negligible systemic availability after oral administration. It is converted in the gut to an active metabolite and then proteolytically degraded to smaller peptides and amino acids, so standard plasma half-life parameters cannot be calculated.
REVIEW
PUBLISHED PAIR RECORDS
with Plecanatide
Overlapping guanylate-cyclase-C activityLinaclotide and plecanatide are both locally acting guanylate-cyclase-C agonists for constipation-related indications. Their labels identify diarrhoea as an important adverse effect, while Peppy did not identify a direct combination study. The shared target and effect make this a sensible review flag, not proof of a specific combined outcome.
Reviewed 8 Oct 2026HUMAN EVIDENCE
U.S. labelling supports use for irritable bowel syndrome with constipation and chronic idiopathic constipation in specified populations. It is not evidence for systemic peptide effects, because measurable systemic exposure is negligible at the labelled doses.
REPORTED EFFECTS
Diarrhoea is a central labelled adverse effect. The label carries a boxed warning for risk of serious dehydration in patients younger than two years and lists mechanical gastrointestinal obstruction as a contraindication.
RESEARCH LIMITATIONS
This is a source-backed medicine and safety summary, not a recommendation or a protocol. Product labels, approvals, contraindications, interactions and availability differ by jurisdiction; check the current official product information and consult a qualified clinician.
CURATED SOURCES · 1
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