Plecanatide (1 brand name, 1 dosage form, 1 route)
Available dosage forms: TABLET.
Routes of administration: ORAL.
Brand Names
- TRULANCE
Boxed Warning
TRULANCE is contraindicated in patients less than 6 years of age; in nonclinical studies in young juvenile mice, administration of a single oral dose of plecanatide caused deaths due to dehydration [see Contraindications (4), Use in Specific Populations (8.4)] . Avoid use of TRULANCE in patients 6 years to less than 18 years of age [see Warnings and Precautions (5.1), Use in Specific Populations (8.4)] . The safety and effectiveness of TRULANCE have not been established in patients less than 18 years of age [see Use in Specific Populations (8.4)] .
Indications and Usage
TRULANCE is indicated in adults for the treatment of: chronic idiopathic constipation (CIC). irritable bowel syndrome with constipation (IBS-C).
Contraindications
TRULANCE is contraindicated in: Patients less than 6 years of age due to the risk of serious dehydration [see Warnings and Precautions (5.1), Use in Specific Populations (8.4)] . Patients with known or suspected mechanical gastrointestinal obstruction.
Mechanism of Action
Plecanatide is a structural analog of human uroguanylin, and similarly to uroguanylin, plecanatide functions as a guanylate cyclase-C (GC-C) agonist. Both plecanatide 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 of extracellular cGMP has been associated with a decrease in the activity of pain-sensing nerves in animal models of visceral pain. Elevation of 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, plecanatide has been shown to increase fluid secretion into the gastrointestinal (GI) tract, accelerate intestinal transit, and cause changes in stool consistency. In an animal model of visceral pain, plecanatide reduced abdominal muscle contractions, a measure of intestinal pain.