Elobixibat

Summary

Elobixibat is a minimally absorbed, locally acting ileal bile acid transporter inhibitor approved in Japan for the treatment of chronic idiopathic constipation. By blocking bile acid reabsorption in the terminal ileum, it accelerates colonic transit and increases fluid secretion into the colon.

Mechanism of Action

Inhibits the apical sodium-dependent bile acid transporter (ASBT/SLC10A2) in the terminal ileum, reducing reabsorption of bile acids and increasing their delivery to the colon, which stimulates colonic motility and secretion via TGR5 and FXR pathways.

Routes of Administration

Goals & Uses

• Relief of chronic idiopathic constipationGastroenterologyHigh
• Treatment of constipation-predominant IBS (IBS-C)GastroenterologyModerate
• Improvement of stool consistencyGastroenterologyHigh
• Reduction of LDL cholesterolCardiovascular/MetabolicLow

Contraindications

• Bowel obstructionGastrointestinalHigh
• PregnancyPopulationModeratePotential fetal risk or insufficient safety data
• Hypersensitivity to elobixibatAllergyHigh
• Severe inflammatory bowel disease (acute phase)GastrointestinalHigh

Adverse Effects

• NauseaGastrointestinalUncommonFeeling of sickness or urge to vomit
• Elevated liver enzymes (transaminases)HepaticRare
• FlatulenceGastrointestinalCommonExcess gas in the digestive tract
• Abdominal pain/crampingGastrointestinalCommon
• DiarrheaGastrointestinalCommonLoose or frequent stools

Drug Interactions

• Lipid-lowering agents (statins)Low
• Bile acid sequestrants (e.g., cholestyramine)Moderate
• Oral medications with narrow therapeutic indexModerate

Population Constraints

• Nursing mothersReproductiveRelative
• Pediatric patientsAgeRelative
• Elderly patients (≥75 years)AgeRelative
• Patients with severe hepatic impairmentHepaticRelative
• Pregnant womenReproductiveRelative

Regulatory Status

• European UnionUnapprovedNot approved by EMA; development in Europe did not progress to approval.
• United StatesUnapprovedPhase II/III trials were conducted; not submitted for or received FDA approval as of knowledge cutoff.
• United KingdomUnapprovedNot approved by MHRA.

Approved in Japan (2018) by PMDA under the brand name Goofice for chronic idiopathic constipation. Not approved by the FDA or EMA as of the knowledge cutoff; clinical trials in Western markets were conducted but regulatory approval was not pursued in those jurisdictions.

Evidence & Sources

No sources recorded yet.