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Expert Opin Investig Drugs. 2013 Feb;22(2):277-84. doi: 10.1517/13543784.2013.753056. Epub 2012 Dec 8.

Elobixibat for the treatment of constipation.

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College of Medicine, Clinical Enteric Neuroscience Translational and Epidemiological Research, Mayo Clinic, Charlton 8-110, 200 First St. S.W., Rochester, MN 55905, USA.



Elobixibat (formerly A3309) is a first-in-class ileal bile acid transporter (IBAT) inhibitor for treatment of chronic idiopathic constipation (CIC; syn functional constipation). CIC affects up to 25% of the general population; and up to a half are unsatisfied with current therapies. There is an unmet need for safe and effective drugs to treat CIC.


The authors present: i) an overview of Phase II clinical trials of elobixibat in CIC, based on peer-reviewed literature and congress presentations and ii) an evaluation of the efficacy and mechanism of action of elobixibat in the treatment of CIC.


Elobixibat provides a novel approach to treat chronic constipation via IBAT inhibition with enhanced delivery of bile acids to the colon. Pharmacodynamic studies show that it accelerates colonic transit, increases stool frequency, loosens stool consistency and relieves constipation-related symptoms in CIC patients. These beneficial effects are maintained for a minimum of 8 consecutive weeks of treatment. With minimal absorption and low systemic bioavailability, elobixibat is generally well tolerated and may offer the added benefit of improving serum lipid profiles through bile acid depletion.

[Indexed for MEDLINE]

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