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Home/Compounds/Linaclotide
OtherFDA approvedRx required

Linaclotide

Also known as: Linzess · Constella
Brands: Linzess · Constella

14-amino-acid peptide guanylate cyclase-C agonist approved for chronic idiopathic constipation, IBS-C, and pediatric functional constipation.

A
Grade A
Multiple human RCTs
Human studies29
PubMed citations29
Routeoral
Regulatory (US)FDA approved · Rx
Last verified2 days ago

Mechanism of action

Agonist of guanylate cyclase-C on the intestinal luminal surface. Increases cGMP, activates CFTR, and drives fluid secretion into the lumen.

Evidence summary

29
Human studies
29
PubMed citations
25
Clinical trials
A
Evidence grade

Evidence summary in progress. See the citations section below for the underlying research papers.

Dosing protocols

Educational information only. Consult a licensed provider before using any peptide.
Administration routes
oral

Side effects & safety

From the FDA label
Source
abdominal painconstipationdehydrationdiarrheadyspepsiagastroesophageal reflux diseaseheadachenausearashurticariavomiting

Terms pulled directly from the referenced source. We don't fabricate frequencies — when a label doesn't publish a percentage, we don't either.

Interactions

No documented drug interactions on file.

Regulatory status

United States
FDA approved

FDA approved for CIC, IBS-C in adults, and functional constipation in pediatric patients (Linzess). Contraindicated under age 2.

Compounding
Not permitted

Not available via 503A/503B compounding pharmacies.

Regulatory data last verified 4/19/2026

Clinical trials

NCT05107219Pilot Study of GCC Agonists to Identify a Cyclic-GMP Signal in Duodenal Tissue of VolunteersCompleted · Phase 1 · Barrett Esophagus · n=43NCT03119584Efficacy of Linaclotide in Type II Diabetics With Chronic Constipation: A Randomized, Double-Blind, Placebo-Controlled, Cross-Over TrialActive Not Recruiting · Phase 4 · Chronic Constipation · n=23NCT03796884Phase II Randomized, Placebo-Controlled Trial of Linaclotide to Demonstrate Bioactivity in Patients With Sporadic Colorectal Adenomas and With Colorectal CancerActive Not Recruiting · Phase 2 · Colorectal Adenoma · n=230NCT07431957"Efficacy and Safety of Linaclotide in Chronic Constipation : A Randomized, Double-Blind, Placebo-Controlled, Parallel-Group Study"Not Yet Recruiting · Phase 4 · Chronic Idiopathic Constipation · n=90NCT06692673Use of Linaclotide as a Single Agent Colonoscopy Bowel Preparation Regimen; A Pilot TrialRecruiting · Phase 1 · Patients Scheduled for Colonoscopy · n=10NCT05796388A Pilot Study to Evaluate the Efficacy and Safety of Virtual Reality in Combination With Linaclotide for the Treatment of Adults With IBS and Constipation PredominanceRecruiting · N/A · Irritable Bowel Syndrome With Constipation · n=65NCT04166058A Phase 3, Open-label, Long-term Safety Study of Oral Linaclotide Administered to Pediatric Participants With Functional Constipation (FC) or Irritable Bowel Syndrome With Constipation (IBS-C)Completed · Phase 3 · Irritable Bowel Syndrome With Constipation · n=381NCT05760313A Phase 2 Dose Finding Study Evaluating the Safety and Efficacy of Linaclotide in Pediatric Subjects 6 Months to Less Than 2 Years of Age With Functional Constipation (FC).Completed · Phase 2 · Functional Constipation · n=19NCT05652205A Phase 3, Multicenter, Randomized, Double-blind, Parallel-group, Safety and Efficacy Study of Linaclotide Versus Placebo in Pediatric Subjects, Ages 2 to 5 Years, With Functional Constipation (FC) With a 24-week Open-label Treatment ExtensionCompleted · Phase 3 · Functional Constipation (FC) · n=123NCT06989268A RANDOMISED, PLACEBO-CONTROLLED, CROSSOVER STUDY TO EVALUATE THE EFFECT OF LINACLOTIDE ON COLONIC MOTILITY ASSESSED WITH INTRALUMINAL COLONIC MANOMETRY IN HEALTHY SUBJECTSCompleted · Phase 4 · Chronic Constipation · n=10NCT06748638Clinical Study on the Application of Lactulose Combined with Linaclotide in Bowel Preparation for ColonoscopyEnrolling By Invitation · Phase 4 · Lactulose · n=444NCT06091735A Single-center, Single-blind, Randomized Controlled Clinical Study of Bowel Preparation Before ColonoscopyCompleted · N/A · Bowel Preparation · n=444

Showing 12 of 25 indexed studies. View all on ClinicalTrials.gov →

Citations

PMID 37952945Hojo M, Shibuya T et al. · Management of Chronic Constipation: A Comprehensive Review.Internal medicine (Tokyo, Japan) (2025)HumanPMID 41404536Eid AM, Vázquez-Vélez GE et al. · Update on the Treatment of Autonomic Disorders.Current treatment options in neurology (2025)HumanPMID 40079184Cheng L, Wang Q et al. · Efficacy of Linaclotide in Functional Dyspepsia and Constipation-Predominant Irritable Bowel Syndrome Overlap: A Randomized Trial.Journal of gastroenterology and hepatology (2025)HumanPMID 38925548Kilgore A, Khlevner J · Functional Constipation: Pathophysiology, evaluation, and management.Alimentary pharmacology & therapeutics (2024)HumanPMID 39109752de Cates AN, Harmer CJ et al. · Association between a selective 5-HT4 receptor agonist and incidence of major depressive disorder: emulated target trial.The British journal of psychiatry : the journal of mental science (2024)HumanPMID 38166671Rao SS, Manabe N et al. · Comparative profiles of lubiprostone, linaclotide, and elobixibat for chronic constipation: a systematic literature review with meta-analysis and number needed to treat/harm.BMC gastroenterology (2024)HumanPMID 38211604Di Lorenzo C, Khlevner J et al. · Efficacy and safety of linaclotide in treating functional constipation in paediatric patients: a randomised, double-blind, placebo-controlled, multicentre, phase 3 trial.The lancet. Gastroenterology & hepatology (2024)HumanPMID 38504394Di Lorenzo C, Nurko S et al. · Safety and efficacy of linaclotide in children aged 7-17 years with irritable bowel syndrome with constipation.Journal of pediatric gastroenterology and nutrition (2024)HumanPMID 39370607Yoshihara T, Kessoku T et al. · Efficacy and safety of linaclotide in treatment-resistant chronic constipation: A multicenter, open-label study.Neurogastroenterology and motility (2024)HumanPMID 38533633Di Lorenzo C, Nurko S et al. · Randomized controlled trial of linaclotide in children aged 6-17 years with functional constipation.Journal of pediatric gastroenterology and nutrition (2024)HumanPMID 37204227Chang L, Chey WD et al. · American Gastroenterological Association-American College of Gastroenterology Clinical Practice Guideline: Pharmacological Management of Chronic Idiopathic Constipation.The American journal of gastroenterology (2023)HumanPMID 37211380Chang L, Chey WD et al. · American Gastroenterological Association-American College of Gastroenterology Clinical Practice Guideline: Pharmacological Management of Chronic Idiopathic Constipation.Gastroenterology (2023)HumanPMID 37417257Cho YS, Lee YJ et al. · 2022 Seoul Consensus on Clinical Practice Guidelines for Functional Constipation.Journal of neurogastroenterology and motility (2023)HumanPMID 34238582Sebastián Domingo JJ · Irritable bowel syndrome.Medicina clinica (2022)HumanPMID 33751780Corsetti M, Landes S et al. · Bisacodyl: A review of pharmacology and clinical evidence to guide use in clinical practice in patients with constipation.Neurogastroenterology and motility (2022)HumanPMID 35738724Chang L, Sultan S et al. · AGA Clinical Practice Guideline on the Pharmacological Management of Irritable Bowel Syndrome With Constipation.Gastroenterology (2022)HumanPMID 33213776Lucak S, Lunsford TN et al. · Evaluation and Treatment of Constipation in the Geriatric Population.Clinics in geriatric medicine (2021)HumanPMID 31756783Serra J, Pohl D et al. · European society of neurogastroenterology and motility guidelines on functional constipation in adults.Neurogastroenterology and motility (2021)HumanPMID 34388141Shah ED, Staller K et al. · Evaluating the Impact of Cost on the Treatment Algorithm for Chronic Idiopathic Constipation: Cost-Effectiveness Analysis.The American journal of gastroenterology (2021)HumanPMID 34463082Bonetto S, Fagoonee S et al. · Recent advances in the treatment of irritable bowel syndrome.Polish archives of internal medicine (2021)Human

Showing 20 of 29 papers. View all on PubMed →