Odevixibat (A4250) is an effective, selective and orally active ileal bile acid transporter inhibitor. Odevixibat has the potential for the treatment of primary biliary cirrhosis. Odevixibat reduces cholestatic liver and bile duct injury in mice model.

Odevixibat 明显降低胆汁流动性和胆汁BA排出量，与bsep转录降低相关，同时诱导Ntcp和Cyp7a1的表达。Odevixibat（饲料中0.01% (w/w)；4周）改善硬化性胆管炎，在Mdr2-/-小鼠中显著降低血清丙氨酸氨基转移酶、碱性磷酸酶和BAs水平，减少肝脏中促炎症和促纤维化基因的表达，以及胆管增殖[1]。