Page data last changed: . Chemistry registry snapshot: . Registry refreshes and identity assessments are separate from scientific content review.
A disulfide-rich tetradecapeptide that acts locally in the gut lumen.
Also known as: Linzess · Constella
Part of the Metabolic & GLP-1 peptides cluster
Overview
Linaclotide is a synthetic 14-amino-acid peptide that activates guanylate cyclase-C on the intestinal lining, raising cyclic GMP and driving chloride, bicarbonate and water secretion into the lumen. It is an approved therapeutic for irritable bowel syndrome with constipation and chronic constipation. Content here is educational only.
Source & context
Biological / chemical source: Synthetic tetradecapeptide
Primary research or clinical context: Approved for irritable bowel syndrome with constipation and chronic constipation
Locally acting design
Three disulfide bonds lock linaclotide into a rigid, protease-resistant fold, and it is essentially not absorbed. Acting only within the gut lumen minimizes systemic exposure, a deliberate feature of its design as a minimally absorbed peptide agonist.
Secretory mechanism
Elevated cyclic GMP activates the CFTR chloride channel, pulling fluid into the intestine to soften stool and speed transit, while also modulating visceral pain signaling. Linaclotide is a leading example of the guanylate cyclase-C agonist class studied for functional bowel disorders.
Sequence
One-letter sequence commonly cited for Linaclotide (educational; isoforms and modifications may differ):
CCEYCCNPACTGCY
Residues plotted ~100° apart around an α-helix — clustering of one color reveals an amphipathic face.
Structure & chemistry
Molecular identity & reference confidence
Source-supported reference
Reference values are taken from the cited molecular record or curated profile. A database match is not independent laboratory verification; modifications, counter-ions, and formulations can change the measured mass.
- Molecular form
- Linaclotide (source record; form not independently established)
- Species
- Not established by this molecular identity audit
- Termini (N / C)
- Not specified / Not specified
Average reference mass
Reference policy updated: 2026-10-05
- IUPHAR/BPS source snapshot · 2026-10-01
- PubChem molecular record · 2026-10-01
- Molecular formula
- C59H79N15O21S6
- Average reference mass
- ≈ 1,526.8
- Status
- Approved medicine in at least one jurisdiction (IUPHAR record)
Disulphide bond formation between cysteine residues at positions 1 and 6, 2 and 10, and 5 and 13
- PubChem CID: 16158208
- IUPHAR ligand: 5017
- DrugBank: DB08890
- CAS RN: 851199-59-2
- UNII: N0TXR0XR5X
Chemistry values: PubChem, IUPHAR/BPS Guide to Pharmacology · fetched 2026-10-01.
Clinical development snapshot
ClinicalTrials.gov lists 60 registered studies with “Linaclotide” as an intervention (snapshot 2026-10-01). A registry footprint is not evidence of efficacy or approval.
| NCT | Title | Phase | Status | Updated |
|---|---|---|---|---|
| NCT07780344 | MRI Parameters as Biomarkers in Cystic Fibrosis (FEMPTO) | Not applicable | not yet recruiting | 2026-08-21 |
| NCT05796388 | A Study of Virtual Reality and Linaclotide for IBS-C | Not applicable | recruiting | 2026-07-29 |
| NCT03796884 | Linaclotide in Treating Patients With Stages 0-3 Colorectal Cancer | Phase 2 | active not recruiting | 2026-07-22 |
| NCT05652205 | A Study to Assess Adverse Events and Change in Symptoms With Linaclotide Versus Placebo in Pediatric Subjects, | Phase 3 | completed | 2026-05-14 |
| NCT07569419 | Proof of Principle Study for an Efficacy Trial of Linaclotide for Cystic Fibrosis | Early phase 1 | recruiting | 2026-05-06 |
| NCT05107219 | GCC Agonist Signal in the Small Intestine | Phase 1 | completed | 2026-04-07 |
Linaclotide — reconstitution calculator
Enter how much peptide is in the vial and how much diluent (e.g. bacteriostatic water) is added. The tool returns the resulting solution concentration — and, for any amount you type, the volume it corresponds to. This is educational arithmetic, not a dosing recommendation.
Reference form: Linaclotide (source record; form not independently established)Average reference mass: 1,526.8 Da
Enter an amount to see the volume it corresponds to.
Educational concentration mathematics only. This tool does not recommend a dose, amount, or protocol, and nothing here is medical advice. Many peptides are not authorized by Health Canada for human use — see our reconstitution and bacteriostatic-water guides for context.
FAQ about Linaclotide
What is Linaclotide?+
Linaclotide is a synthetic 14-amino-acid peptide that activates guanylate cyclase-C on the intestinal lining, raising cyclic GMP and driving chloride, bicarbonate and water secretion into the lumen. It is an approved therapeutic for irritable bowel syndrome with constipation and chronic constipation. Content here is educational only.
What Canadian product status is recorded for Linaclotide?+
Canadian product status for Linaclotide has not been verified in this profile. No verified record here does not mean no authorization exists. Status depends on the product, formulation and use; consult Health Canada's product records.
What is the typical length of Linaclotide?+
Linaclotide is commonly described as approximately 14 amino acids (Guanylate cyclase-C agonist).
Related peptides
References & further reading
- 1.Di Lorenzo et al. (2024). 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
- 2.Rao et al. (2024). 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
- 3.Yang et al. (2023). Bowel preparation efficacy and safety of compound polyethylene glycol electrolyte powder combined with linaclotide for colonoscopy: A randomized controlled trial. JGH Open
- 4.Di Lorenzo et al. (2024). Randomized controlled trial of linaclotide in children aged 6-17 years with functional constipation. J Pediatr Gastroenterol Nutr
- 5.Yoshihara et al. (2024). Efficacy and safety of linaclotide in treatment-resistant chronic constipation: A multicenter, open-label study. Neurogastroenterol Motil
- 6.Góngora-Benítez et al. (2013). Constella™(EU)-Linzess™(USA): the last milestone in the long journey of the peptide linaclotide and its implications for the future of peptide drugs. Future Med Chem
- 7.PubChem — compound summary for Linaclotide (CID 16158208)
- 8.Wikipedia — Linaclotide