Peptide Association

Insights

NewsBlog
Start free intake

DisclosurePeptide Association LLC is a for-profit company. We receive compensation from the clinical providers listed on this site. We are not an accrediting body, a licensing board, or a government-affiliated organization. See exactly how we make money.

All peptides

Gastrointestinal · FDA Approved

Linaclotide (Linzess)

FDA-approved

How to ask your doctor
Written by Peptide Association Editorial TeamLast reviewed Editorial policy

01 · Overview

A synthetic 14-amino acid peptide structurally related to the heat-stable enterotoxin of Escherichia coli and the endogenous peptide guanylin. Linaclotide is a minimally absorbed agonist of guanylate cyclase-C (GC-C) on the intestinal lining (PMID 21830967).

GC-C activation raises cGMP, stimulating chloride and bicarbonate secretion and speeding intestinal transit. In mouse studies, cGMP released from the gut lining inhibited colonic pain-sensing nerves, suggesting a direct visceral analgesic mechanism (PMID 23958540).

02 · Research summary & key findings

FDA-approved in 2012 for IBS-C and chronic idiopathic constipation (CIC). Two 12-week phase 3 trials in chronic constipation showed significantly more responders on linaclotide than placebo and improvements in bowel and abdominal symptoms (Lembo et al., NEJM, 2011) (PMID 21830967). In a phase 3 IBS-C trial, 33.6% of patients on linaclotide vs. 21.0% on placebo met the FDA combined pain-and-bowel endpoint (PMID 22986440). Animal studies and a post hoc analysis of a 26-week IBS-C trial support pain reduction through extracellular cGMP acting on nociceptors (PMID 23958540). Diarrhea is the most common side effect and led to discontinuation in about 4% to 6% of patients (PMID 21830967) (PMID 22986440).

03 · Regulatory status

Linaclotide (Linzess) has received FDA approval and is available for clinical use under appropriate medical supervision. Consult a qualified healthcare provider for prescribing information.

Linaclotide (Linzess) is an FDA-approved medicine prescribed for the conditions on its label. It is not part of our intake, so we do not propose protocols for it. If you think it may be relevant to you, talk to your own doctor. How to ask your doctor.

04 · Administration routes

  • Oral

References

  1. [1]Two randomized trials of linaclotide for chronic constipation N Engl J Med, 2011. PMID 21830967
  2. [2]A 12-week, randomized, controlled trial with a 4-week randomized withdrawal period to evaluate the efficacy and safety of linaclotide in irritable bowel syndrome with constipation Am J Gastroenterol, 2012. PMID 22986440
  3. [3]Linaclotide inhibits colonic nociceptors and relieves abdominal pain via guanylate cyclase-C and extracellular cyclic guanosine 3',5'-monophosphate Gastroenterology, 2013. PMID 23958540

Primary literature

Related peptides in Gastrointestinal

Disclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol. See our editorial policy for how this content is produced and reviewed. Clinicians: join the network.