--- title: "Linaclotide" canonical_url: https://peptidelibrary.app/library/linaclotide description: "Orally administered 14-amino-acid peptide approved for irritable bowel syndrome with constipation and for chronic idiopathic constipation. It acts locally in the gut lumen and is minimally absorbed systemically." updated: 2026-11-07 publisher: Peptide Library notice: "Research and educational use only. Not medical advice." --- # Linaclotide Linaclotide is an FDA-approved guanylate cyclase-C agonist. Linaclotide is a heat-stable enterotoxin analog that binds guanylate cyclase-C on the luminal surface of intestinal epithelium, raising intracellular and extracellular cyclic GMP. The resulting activation of the cystic fibrosis transmembrane conductance regulator increases chloride and bicarbonate secretion, accelerating transit. Orally administered 14-amino-acid peptide approved for irritable bowel syndrome with constipation and for chronic idiopathic constipation. It acts locally in the gut lumen and is minimally absorbed systemically. ## Classification - Type: FDA-approved guanylate cyclase-C agonist - Mechanism class: Guanylate Cyclase-C Agonist - Development stage: Approved product - Regulatory class: FDA-approved medicine ## Mechanism Linaclotide is a heat-stable enterotoxin analog that binds guanylate cyclase-C on the luminal surface of intestinal epithelium, raising intracellular and extracellular cyclic GMP. The resulting activation of the cystic fibrosis transmembrane conductance regulator increases chloride and bicarbonate secretion, accelerating transit. Extracellular cyclic GMP has additionally been reported to reduce activity of pain-sensing afferent nerves in preclinical models. ## Properties - Molecular formula: C59H79N15O21S6 - Molecular weight: 1,526.8 g/mol - CAS number: 851199-59-2 - Studied routes: Oral ## Evidence - Evidence level: FDA Approved - Highest documented: Regulatory review (FDA label) - Human trials: 0 - Controlled human trials: 0 - Preclinical sources: 0 Each step shows whether the sources Peptide Library has reviewed include that kind of research. Counts are reviewed sources, not every study ever published. Reviews and programme summaries that describe human use are shown as "reported", not as trials, and registered trials without published results are listed but not counted. A higher step means research has progressed further; it does not mean a compound works better or is safer. Compounds whose evidence has not been reviewed yet show "Not reviewed" instead of a guess. ### Studies 1. LINZESS (linaclotide) capsules — FDA prescribing information, DailyMed. Regulatory label (FDA), human. Population: Adults; children aged 7 years and older. Treatment of IBS with constipation [Source](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=09beda19-56d6-4a56-afdc-9a77b70b2ef3) 2. LINZESS (linaclotide) capsules — FDA prescribing information, DailyMed. Regulatory label (FDA), human. Population: Adults with chronic idiopathic constipation. Treatment of chronic idiopathic constipation [Source](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=09beda19-56d6-4a56-afdc-9a77b70b2ef3) 3. LINZESS (linaclotide) capsules — FDA prescribing information, DailyMed. Regulatory label (FDA), human. Population: Children aged 2 years and older with functional constipation. Treatment of functional constipation [Source](https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=09beda19-56d6-4a56-afdc-9a77b70b2ef3) ## Safety Human safety basis: FDA prescribing information ## Regulatory status Linaclotide is an FDA-approved product for specific labelled indications. Approval does not extend to the research contexts described on this page, and approved products are prescription medicines. - FDA status: Approved - Availability: Prescription-Only ## Frequently asked questions ### What is Linaclotide? Orally administered 14-amino-acid peptide approved for irritable bowel syndrome with constipation and for chronic idiopathic constipation. It acts locally in the gut lumen and is minimally absorbed systemically. ### How does Linaclotide work? Linaclotide is a heat-stable enterotoxin analog that binds guanylate cyclase-C on the luminal surface of intestinal epithelium, raising intracellular and extracellular cyclic GMP. The resulting activation of the cystic fibrosis transmembrane conductance regulator increases chloride and bicarbonate secretion, accelerating transit. ### Is Linaclotide FDA approved? Yes. Linaclotide is approved by the FDA, and approved products are prescription medicines. Approval is always for specific indications studied in clinical trials, so an approved status does not mean the compound is approved for every use it is discussed for. Research-chemical material sold under the same name is not the approved product. ### What peptides are similar to Linaclotide? Compounds most often compared with Linaclotide include Teduglutide, Plecanatide, Larazotide and Secretin. They are grouped by shared mechanism or research area rather than by equivalence, and their regulatory status and evidence base differ. ## References - [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](https://pubmed.ncbi.nlm.nih.gov/38211604/) - [Efficacy and safety of linaclotide in treatment-resistant chronic constipation: A multicenter, open-label study — Neurogastroenterol Motil, 2024](https://pubmed.ncbi.nlm.nih.gov/39370607/) - [Efficacy of drugs in chronic idiopathic constipation: a systematic review and network meta-analysis — Lancet Gastroenterol Hepatol, 2019](https://pubmed.ncbi.nlm.nih.gov/31474542/) - [Linaclotide, 2012](https://pubmed.ncbi.nlm.nih.gov/31643353/) - [Linaclotide, 2006](https://pubmed.ncbi.nlm.nih.gov/29999932/)