Elobixibat

Elobixibat (A 3309; AZD 7806) is an orally effective Apical Sodium-Dependent Bile (IBAT) inhibitor, with an IC₅₀ value of 0.53 nM (human IBAT ), 0.13 nM (mouse IBAT), 5.8 nM (canine IBAT). Elobixibat lowers LDL cholesterol, increases serum GLP-1, promotes colon motility, and has the potential to treat metabolic syndrome. Elobixibat can be used to study constipation, dyslipidemia, non-alcoholic hepatitis, and liver tumors^[1][2][3]. IC50 & Target:IC50: 0.53±0.17 nM (human IBAT), 0.13±0.03 nM (mouse IBAT), 5.8±1.6 nM (canine IBAT)^[1]. In Vivo:Elobixibat (0.27 mg/kg/day for 20 weeks, p.o.) inhibits tumor growth in the mouse model of fatty liver disease by inhibiting bile acid reabsorption and reducing total and primary bile acid levels in serum and liver^[2].
Elobixibat (5 days a week for 4 weeks, 0.2, 0.6, or 1.2 mg/kg/day, gavage) improves NASH-related histopathology, reduces cytokine (TNF-α, IL-6, and TGF-β) expression, and normalizes gut microbiome composition in nonsteatohepatitis (NASH) mouse models^[3].