RDX8940

RDX8940 is a minimally absorbed, orally administered small molecule agonist of the G-protein-coupled bile acid receptor-1 (GPBAR1), also known as Takeda G protein-coupled receptor 5 (TGR5). It is designed to selectively activate TGR5 in the intestine, leading to increased secretion of incretin hormones such as glucagon-like peptide-1 (GLP-1), GLP-2, and peptide YY from intestinal L cells. This mechanism aims to improve insulin sensitivity and reduce hepatic steatosis without causing systemic side effects commonly associated with other TGR5 agonists, such as inhibition of gallbladder emptying. Preclinical studies have shown that RDX8940 improves liver steatosis and insulin sensitivity in mouse models of nonalcoholic fatty liver disease (NAFLD) and mild insulin resistance. The drug has been developed by Ardelyx for potential use in metabolic diseases including NAFLD, nonalcoholic steatohepatitis (NASH), and type 2 diabetes[1][2][3].

Other names

TGR5 agonistTGR-5 agonistTGR 5 agonist