The inhibitors of the apical sodium-dependent bile acid transporter (ASBT) as promising drugs

Saveleva E.E.1 , Tyutrina E.S.1, Nakanishi T.2, Tamai I.3, Salmina A.B.1

1. Prof. V.F. Voino-Yasenetsky Krasnoyarsk State Medical University, Krasnoyarsk, Russia
2. Faculty of Pharmacy, Takasaki University of Health and Welfare, Gunma, Japan
3. School of Pharmaceutical Sciences, Institute of Medical, Pharmaceutical and Health Sciences, Kanazawa University, Ishikawa, Japan
Section: Review
DOI: 10.18097/PBMC20206603185      PubMed Id: 32588824
Year: 2020  Volume: 66  Issue: 3  Pages: 185-195
Inhibition of the apical sodium-dependent bile acid transporter (ASBT, also known as IBAT — ileal bile acid transporter, SLC10A2) leads to disruption of 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, 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 the 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.
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Keywords: ASBT, A3309, SHP626, A4250, 264W94, GSK2330672

Saveleva, E. E., Tyutrina, E. S., Nakanishi, T., Tamai, I., Salmina, A. B. (2020). The inhibitors of the apical sodium-dependent bile acid transporter (ASBT) as promising drugs. Biomeditsinskaya Khimiya, 66(3), 185-195.
This paper is also available as the English translation: 10.1134/S1990750821010078
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