Linaclotide

FDA approved

Linaclotide (Linzess) is a 14-amino acid guanylate cyclase-C agonist approved by the FDA in 2012 for irritable bowel syndrome with constipation (IBS-C) and chronic idiopathic constipation. It acts locally in the gut and is minimally absorbed.

At a glance

Where it acts: Digestive & weight
Regulatory status: FDA approvedApproved by the U.S. FDA for at least one medical use.

Mechanism of Action

Linaclotide binds guanylate cyclase-C on the luminal surface of intestinal cells, raising cyclic GMP. This drives chloride and bicarbonate secretion into the gut via the CFTR channel, increasing intestinal fluid and speeding transit. Extracellular cGMP is also thought to reduce the activity of pain-sensing nerves in the colon.

Typical Dosage (Research)

Prescription-only medicine. Dosing is set by a physician according to the FDA-approved label and the condition being treated.

Side Effects & Risks

Diarrhea is the most common side effect, followed by abdominal pain, bloating and flatulence.

Contraindicated in children under 2 because of the risk of serious dehydration, and in known or suspected mechanical bowel obstruction. Severe diarrhea can occur and may require stopping treatment.

Who Uses Linaclotide

Adults with IBS-C or chronic idiopathic constipation; children 6-17 with functional constipation.