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SB756050 is a selective small molecule agonist of the bile acid receptor TGR5 (also known as GPBAR1). It was developed primarily for the potential treatment of type 2 diabetes mellitus by modulating glucose metabolism through activation of TGR5, which influences insulin secretion and glucose disposal. The drug exhibits nonlinear pharmacokinetics with less than dose-proportional increases in plasma exposure above 100 mg and shows variable pharmacodynamic effects on glucose levels depending on dose. It has been studied in phase 1 and phase 2 clinical trials but development for type 2 diabetes was discontinued. SB756050 was originally developed by GlaxoSmithKline.
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