Elobixibat

Elobixibat is an inhibitor of the sodium/bile acid and sulfated solute cotransporter (ASBT), also known as the ileal bile acid transporter (IBAT; IC₅₀s = 0.53, 0.13, and 5.8 nM for the human, mouse, and canine transporters, respectively).¹ It is selective for ASBT over the hepatic sodium/bile acid cotransporter (IC₅₀ = 240 nM). Elobixibat induces mild giant migrating contractions in the colon and increases the number of defecations in conscious dogs two hours after administration of 3, 10, or 30 mg/kg doses, as well as increases the number of defecations after ten hours at 30 mg/kg.² Oral administration of elobixibat (1.2 mg/kg per day) reduces methionine- and choline-deficient diet-induced increases in serum bile acid levels and hepatic inflammation, fibrosis, and cytokine gene expression in a mouse model of non-alcoholic steatohepatitis (NASH).³ Formulations containing elobixibat have been used in the treatment of chronic constipation.

WARNING This product is not for human or veterinary use.

1. Gillberg, P.-G., Dahlström, M., Starke, I., et al. The IBAT inhibition by A3309 - a potential mechanism for the treatment of constipation. Gastroenterol. 138(5 suppl. 1), S-224 (2010).

2. Taniguchi, S., Yano, T., Imaizumi, M., et al. Elobixibat, an ileal bile acid transporter inhibitor, induces giant migrating contractions during natural defecation in conscious dogs. Neurogastroenterol. Motil. 30(12), e13448 (2018).

3. Yamauchi, R., Takedatsu, H., Yokoyama, K., et al. Elobixibat, an ileal bile acid transporter inhibitor, ameliorates non-alcoholic steatohepatitis in mice. Hepatol. Int. 15(2), 392-404 (2021).