Mechanism of Action

Mechanism of Action of GOOFICE®4,18,19,30

Elobixibat inhibits the IBAT expressed on the epithelial cells at the terminal ileum to inhibit bile acid reabsorption, thereby increasing the amount of bile acids flowing into the lumen of the large intestine. Since bile acids induce secretion of fluid into the large intestinal lumen and promotes gastrointestinal motility, elobixibat exerts its therapeutic effect on constipation through dual actions, i.e., secretion of fluid and promotion of large intestinal motility.

Illustrated diagram showing the dual mechanism of action of GOOFICE® (elobixibat) in treating chronic constipation. On the left, elobixibat inhibits the ileal bile acid transporter (IBAT) located on epithelial cells in the terminal ileum, preventing reabsorption of bile acids into the bloodstream. This increases bile acid flow into the large intestine. On the right, two downstream effects are depicted: (1) Fluid secretion—bile acids activate TGR5 receptors, which stimulate CFTR channels, leading to chloride ion (Cl⁻) secretion and subsequent movement of sodium (Na⁺) and water (H₂O) into the intestinal lumen via paracellular pathways. (2) Enhanced motility—bile acids also activate TGR5 receptors on enterochromaffin cells, triggering serotonin (5-HT) release. This stimulates intrinsic primary afferent neurons (IPANs) in the enteric plexus, promoting acetylcholine (ACh)-mediated muscle contraction and nitric oxide (NO)-mediated relaxation, resulting in coordinated peristalsis. These actions together improve bowel movement frequency and consistency.

CFTR: Cystic fibrosis transmembrane conductance regulator, TGR5: Transmembrane G protein-coupled receptor, AC: Adenylate cyclase, ATP: Adenosine triphosphate, cAMP: cyclic adenosine monophosphate, PKA: Protein kinase A, 5-HT: Serotonin, IPAN: Intrinsic primary afferent neuron (It is thought to be the sensory nerve that is localized in the enteric plexus and detects mechanical and chemical stimuli to the gastrointestinal tract.), ACh: Acetylcholine, NO: Nitric oxide

Editorial review: Professor Noriaki Manabe, Endoscopy and Ultrasound Center, Kawasaki Medical University

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