Abstract—

Inhibition of the apical sodium-dependent bile acid transporter (ASBT, also known as IBAT, the ileal bile acid transporter, SLC10A2) leads to impairments in the enterohepatic circulation of bile acids and their excretion with fecal masses. This is accompanied by cholesterol utilization for synthesis of new bile acids. ASBT inhibitors are promising drugs for the treatment of such diseases as non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, type 2 diabetes mellitus, necrotic enterocolitis, chronic constipation, and atherosclerosis. To date the most known chemically synthesized inhibitors are: A3309, SHP626, A4250, 264W94, GSK2330672, SC-435. All of them are at different stages of clinical trials, which confirm high efficacy and good tolerance of these inhibitors. Current trends in this field also include directed chemical synthesis of ASBT inhibitors, as well as their search among substances of plant origin.

中文翻译：

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根尖钠依赖性胆汁酸转运蛋白（ASBT）的抑制剂是有前途的药物。

摘要—

抑制根尖钠依赖性胆汁酸转运蛋白（ASBT，也称为IBAT，回肠胆汁酸转运蛋白，SLC10A2）会导致胆汁酸的肠肝循环受损，并随粪便团块排泄。这伴随着胆固醇的利用来合成新的胆汁酸。ASBT抑制剂是治疗非酒精性脂肪肝，非酒精性脂肪性肝炎，2型糖尿病，坏死性小肠结肠炎，慢性便秘和动脉粥样硬化等疾病的有前途的药物。迄今为止，最已知的化学合成抑制剂是：A3309，SHP626，A4250、264W94，GSK2330672，SC-435。它们都处于临床试验的不同阶段，这证实了这些抑制剂的高功效和良好的耐受性。