Last reviewed 2026-04-20 · How we verify

Linzess (LINACLOTIDE)

Linzess works by activating the heat-stable enterotoxin receptor to increase fluid secretion in the intestines.

Linzess (Linaclotide) is a small molecule guanylate cyclase-C agonist developed by Forest Labs LLC and currently owned by Abbvie. It targets the heat-stable enterotoxin receptor to treat chronic idiopathic constipation and irritable bowel syndrome with constipation. Linzess was FDA-approved in 2012 and has two generic manufacturers. The commercial status of Linzess is not explicitly stated, but it is likely to be off-patent. Key safety considerations include potential gastrointestinal side effects.

At a glance

Mechanism of action

Linaclotide is structurally related to human guanylin and uroguanylin and functions as guanylate cyclase-C (GC-C) agonist. Both linaclotide and its active metabolite bind to GC-C and act locally on the luminal surface of the intestinal epithelium. Activation of GC-C results in an increase in both intracellular and extracellular concentrations of cyclic guanosine monophosphate (cGMP). Elevation in intracellular cGMP stimulates secretion of chloride and bicarbonate into the intestinal lumen, mainly through activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased intestinal fluid and accelerated transit. In animal models, linaclotide has been shown to both accelerate GI transit and reduce intestinal pain. In an animal model of visceral pain, linaclotide reduced abdominal muscle contraction and decreased the activity of pain-sensing nerves by increasing extracellular cGMP.

Approved indications

• Chronic idiopathic constipation
• Irritable bowel syndrome
• Irritable bowel syndrome characterized by constipation

Boxed warnings

• WARNING: RISK OF SERIOUS DEHYDRATION IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE LINZESS is contraindicated in patients less than 2 years of age; in nonclinical studies in neonatal mice, administration of a single, clinically relevant adult oral dose of linaclotide caused deaths due to dehydration [see Contraindications ( 4 ), Warnings and Precautions ( 5.1 ), Use in Specific Populations ( 8.4 )]. WARNING: RISK OF SERIOUS DEHYDRATION IN PEDIATRIC PATIENTS LESS THAN 2 YEARS OF AGE See full prescribing information for complete boxed warning. LINZESS is contraindicated in patients less than 2 years of age; in neonatal mice, linaclotide caused deaths due to dehydration. ( 4 , 5.1 , 8.4 )

Common side effects

• Diarrhea
• Abdominal pain
• Flatulence
• Abdominal distension
• Viral Gastroenteritis
• Headache
• Diarrhea
• Abdominal pain
• Flatulence
• Abdominal distension
• Upper respiratory tract infection
• Sinusitis

Key clinical trials

• "Efficacy and Safety of Linaclotide in Chronic Constipation" (PHASE4)
• Linaclotide for Colonoscopy Bowel Prep (PHASE1,PHASE2)
• A Study of Virtual Reality and Linaclotide for IBS-C (NA)
• Long-term Safety of Linaclotide in Pediatric Participants With FC or IBS-C (PHASE3)
• A Study to Assess Adverse Events and Change in Disease Activity in Pediatric Participants (Age 6 Months to <2 Years) With Functional Constipation Who Are Treated With Linaclotide (PHASE2)
• GCC Agonist Signal in the Small Intestine (PHASE1)
• Linaclotide in Treating Patients With Stages 0-3 Colorectal Cancer (PHASE2)
• A Study to Assess Adverse Events and Change in Symptoms With Linaclotide Versus Placebo in Pediatric Subjects, Ages 2 to 5 Years, With Functional Constipation (PHASE3)

Patents

Primary sources

Every claim on this page is sourced from regulatory or scientific primary sources. See our editorial policy for full methodology.

Competitive intelligence

For the full competitive landscape — auto-detected comparators, recent regulatory actions across the set, upcoming PDUFA, patent timeline, sponsor landscape:

• Linzess CI brief — competitive landscape report
• Linzess updates RSS · CI watch RSS
• AbbVie portfolio CI