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.
For research use only.
Key Facts
- CAS
- 851199-59-2
- Molecular Weight (MW)
- 1526.8 g/mol
- Half-life
- —
- FDA status
- Approved
- Administration Route
- oral
- Frequency
- —
- Last updated
- Aug 30, 2026
- Reviewed
- Aug 30, 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.
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.
Protocol
- Dosage Range
- —
- Frequency
- —
- Cycle
- —
- Administration Route
- oral
- Reconstitution Guide
- —
Not yet checked against primary sources
These figures are compiled from earlier reference material. They have not been verified against FDA labelling, registered trials or published literature, no citation is attached to them, and none of them is a recommended dose. Linaclotide is queued for dosage evidence review.
Compare reported doses across the whole librarySequence & molecular data
| 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
- Efficacy and safety of linaclotide in treating functional constipation in paediatric patients: a randomised, double-blind, placebo-controlled, multicentre, phase 3 trial
- Efficacy and safety of linaclotide in treatment-resistant chronic constipation: A multicenter, open-label study
- Efficacy of drugs in chronic idiopathic constipation: a systematic review and network meta-analysis
- Linaclotide
- Linaclotide
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.
| FDA status | Approved |
|---|---|
| Research status | Approved product (see FDA status) |
| Availability | Prescription-Only |
| WADA (sport) | Unknown / Not Listed |
| Library classification | FDA-Approved |
Benefits
—
Potential Side Effects
No side effects listed yet for this entry.
Storage & stability
Lyophilized (freeze-dried) peptide powder is far more stable than the reconstituted solution. Keep sealed vials cold, dry and away from light; long-term storage is typically frozen, with short-term refrigeration for vials in use.
Once reconstituted in bacteriostatic water, keep the solution refrigerated, avoid repeated freeze–thaw cycles and agitation, and label the vial with the reconstitution date and concentration. Discard any solution that turns cloudy or shows particulates.
Degradation rates differ by sequence: peptides containing methionine, cysteine, asparagine or glutamine are more prone to oxidation and deamidation, so shelf life after reconstitution is compound-specific rather than universal.
Read the full guide: how to store peptides before and after reconstitution →
Source: Manning MC, Chou DK, Murphy BM, Payne RW, Katayama DS. Stability of protein pharmaceuticals: an update. Pharm Res. 2010;27(4):544–575. (PMID 20143256). General guidance for research handling; not product-specific instructions.
Linaclotide: 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, 2024External reference
- Efficacy and safety of linaclotide in treatment-resistant chronic constipation: A multicenter, open-label study — Neurogastroenterol Motil, 2024External reference
- Efficacy of drugs in chronic idiopathic constipation: a systematic review and network meta-analysis — Lancet Gastroenterol Hepatol, 2019External reference
- Linaclotide, 2012External reference
- Linaclotide, 2006External reference
Related research, comparisons & guides
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Compiled by Peptide Library Editorial · Reviewed Aug 30, 2026 · Updated Aug 30, 2026 · Version 1
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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