Linaclotide

Indications:

• Treatment of irritable bowel syndrome with constipation (IBS-C) in adults.
• Treatment of chronic idiopathic constipation (CIC) in adults.

Mechanism of Action: Linaclotide and its active metabolite bind to and activate the guanylate cyclase-C (GC-C) receptor on the luminal surface of the intestinal epithelium. This activation leads to increased concentrations of cyclic guanosine monophosphate (cGMP), which subsequently leads to the activation of the cystic fibrosis transmembrane conductance regulator (CFTR) ion channel, resulting in increased chloride and bicarbonate secretion into the intestine. This increased fluid secretion helps soften stool and facilitate bowel movements.

Pharmacokinetics:

• Absorption: Minimally absorbed from the gastrointestinal tract.
• Distribution: N/A due to minimal systemic absorption.
• Metabolism: Degraded within the gastrointestinal tract to its active metabolite.
• Excretion: Excreted primarily in the feces.

Form: Linaclotide API is typically available as a white to off-white powder.