Linaclotide

FDA-approved guanylate cyclase-C agonistEstablished

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.

Calculate Dose

For research use only.

Key Facts

CAS: 851199-59-2
Molecular Weight (MW): 1526.8 g/mol
Half-life: —
FDA status: Approved
Evidence level: FDA Approved
Human dose established: Yes
Administration Route: Oral
Frequency: Once daily, on an empty stomach at least 30 minutes before a meal
Last updated: Nov 7, 2026
Reviewed: Nov 7, 2026

Research summary

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.

Research evidence

Regulatory review (FDA label)3 reviewed sources
Controlled human trialsNone in reviewed sources
Early or uncontrolled human studiesNone in reviewed sources
Lab & animal studiesNone in reviewed sources

How it works

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.

Peptide Library's Linaclotide profile summarises 5 cited studies listed in the Science section, the compound's regulatory status, and research-protocol parameters reported for it. It is a research reference, not medical advice.

Linaclotide dosage evidence

Linaclotide has FDA-approved human dosages. Linzess for adults with IBS with constipation is 290 mcg by mouth once daily; for adult chronic idiopathic constipation it is 145 mcg once daily, or 72 mcg based on presentation or tolerability. For children it is 145 mcg once daily for IBS with constipation from age 7, and 72 mcg once daily for functional constipation from age 2.

FDA Approved

Dosage evidence summary for Linaclotide
Human dosing established	Yes
Studied dose range	72–290 mcg once daily, by indication and age
Route	Oral
Frequency	Once daily, on an empty stomach at least 30 minutes before a meal
Duration studied	Continuous
Evidence level	FDA Approved
Last reviewed	2026-11-07

Research-reported dosing

Doses as studied, one row per regimen. Different trials used different regimens; they are listed separately rather than averaged.

Research-reported dosing for Linaclotide, one row per studied regimen
Study / context	Population	Dose	Route	Frequency	Duration	Outcome studied	Source
FDA label — Linzess, IBS with constipationFDA-approved label · FDA prescribing information	Adults; children aged 7 years and older	290 mcg (adults); 145 mcg (children 7 and older)	Oral	Once daily	—	Treatment of IBS with constipation	LINZESS (linaclotide) capsules — FDA prescribing information, DailyMed
FDA label — Linzess, chronic idiopathic constipationFDA-approved label · FDA prescribing information	Adults with chronic idiopathic constipation	145 mcg, or 72 mcg based on presentation or tolerability	Oral	Once daily	—	Treatment of chronic idiopathic constipation	LINZESS (linaclotide) capsules — FDA prescribing information, DailyMed
FDA label — Linzess, functional constipation in childrenFDA-approved label · FDA prescribing information	Children aged 2 years and older with functional constipation	72 mcg	Oral	Once daily	—	Treatment of functional constipation	LINZESS (linaclotide) capsules — FDA prescribing information, DailyMed

Where sources disagree

Linzess carries a boxed warning about serious dehydration in children: it is contraindicated under 2 years of age after deaths from dehydration in neonatal mice.
Doses depend on the condition and age; 290 mcg applies only to adults with IBS with constipation.

Linaclotide dosage in published studies and labels →

Sequence & molecular data

Sequence and molecular data for Linaclotide
Molecular formula	C59H79N15O21S6
Molecular weight	1526.8 g/mol
CAS number	851199-59-2
PubChem CID	16158208
FDA UNII	N0TXR0XR5X
ChEMBL	CHEMBL3301675
DrugBank	DB08890

Identifiers link to the public PubChem, FDA Substance Registration (UNII), ChEMBL and DrugBank records for the same entity.

Science

Mechanism of Action

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.

Studies

Research statistics

347 PubMed publications · 30.6% human clinical research · 53 registered trials

Counts of published research through 2026-11-01, not evidence that it works. Publications by year, study types and trials · How publications are counted

Regulatory & research 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.

Regulatory and research status for Linaclotide
FDA status	Approved
Research status	Approved product (see FDA status)
Availability	Prescription-Only
WADA (sport)	Unknown / Not Listed
Library classification	FDA-Approved

How FDA approval, compounding and research-only status differ

Benefits

—

Linaclotide side effects

No side effects listed yet for this entry.

Storage & stability

This compound is not supplied as a powder to be mixed, so the freeze-dried powder and reconstitution handling described for research peptides does not apply. Storage conditions are product-specific: follow the label or packaging of the product itself.

Linaclotide: frequently asked questions

What is Linaclotide?

How does Linaclotide work?

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
External reference
Efficacy and safety of linaclotide in treatment-resistant chronic constipation: A multicenter, open-label study — Neurogastroenterol Motil, 2024
External reference
Efficacy of drugs in chronic idiopathic constipation: a systematic review and network meta-analysis — Lancet Gastroenterol Hepatol, 2019
External reference
Linaclotide, 2012
External reference
Linaclotide, 2006
External reference

Related research, comparisons & guides

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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Nov 7, 2026 · Version 2

This Linaclotide profile is compiled from published literature (5 cited studies linked above), public regulatory records and chemical registries. It describes what research reports; it is not medical advice, and nothing here is a dosing recommendation for humans. Peptide Library does not sell peptides. Editorial policy · How profiles are compiled · Report an error

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