Glucose and lipid effects of the ileal apical sodium-dependent bile acid transporter inhibitor GSK2330672: double-blind randomized trials with type 2 diabetes subjects taking metformin

2016 ◽  
Vol 18 (7) ◽  
pp. 654-662 ◽  
Author(s):  
D. J. Nunez ◽  
X. Yao ◽  
J. Lin ◽  
A. Walker ◽  
P. Zuo ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Bile Acid ◽  
Randomized Trials ◽  
Double Blind ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Acid Transporter

Discovery of a Highly Potent, Nonabsorbable Apical Sodium-Dependent Bile Acid Transporter Inhibitor (GSK2330672) for Treatment of Type 2 Diabetes

2013 ◽  
Vol 56 (12) ◽  
pp. 5094-5114 ◽  
Author(s):  
Yulin Wu ◽  
Christopher J. Aquino ◽  
David J. Cowan ◽  
Don L. Anderson ◽  
Jeff L. Ambroso ◽  
...  
Keyword(s):  
Type 2 Diabetes ◽  
Bile Acid ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Acid Transporter

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

2020 ◽  
Vol 66 (3) ◽  
pp. 185-195
Author(s):  
E.E. Saveleva ◽  
E.S. Tyutrina ◽  
T. Nakanishi ◽  
I. Tamai ◽  
A.B. Salmina
Keyword(s):  
Bile Acid ◽  
Bile Acids ◽  
Enterohepatic Circulation ◽  
Alcoholic Fatty Liver ◽  
Good Tolerance ◽  
Current Trends ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Acid Transporter

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.

Induction of sodium-dependent bile acid transporter messenger RNA, protein, and activity in rat ileum by cholic acid

1997 ◽  
Vol 113 (5) ◽  
pp. 1599-1608 ◽  
Author(s):  
RT Stravitz ◽  
AJ Sanyal ◽  
WM Pandak ◽  
ZR Vlahcevic ◽  
JW Beets ◽  
...  
Keyword(s):  
Bile Acid ◽  
Cholic Acid ◽  
Messenger Rna ◽  
Rat Ileum ◽  
Sodium Dependent ◽  
Bile Acid Transporter ◽  
Acid Transporter
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