glycine-beta-muricholic acid

Glycine-beta-muricholic acid is a glycine conjugate of beta-muricholic acid, classified as a synthetic or semi-synthetic bile acid derivative designed for oral administration. It is a potent, selective, and gut-restricted antagonist of the farnesoid X receptor (FXR), a nuclear receptor critical for bile acid homeostasis and metabolic regulation. Glycine-beta-MCA reduces intestinal FXR signaling, thereby altering bile acid composition, lowering total bile acid pool hydrophobicity, promoting fecal excretion of hydrophobic bile acids, and reducing levels of ceramides that contribute to hepatic stress. It has shown efficacy in preclinical studies for the treatment of cholestasis, nonalcoholic steatohepatitis (NASH), obesity, and fatty liver disease by reducing inflammation, portal fibrosis, and hepatic lipid accumulation, with minimal intestinal or hepatic toxicity. Glycine-beta-MCA is resistant to bacterial hydrolysis in the gut and acts mainly locally in the intestine, resulting in low systemic exposure.

Other names

glycine-beta-muricholic acidGlycine-β-Muricholic Acidglyco-beta-muricholic acidN-[(3α,5β,6β,7β)-3,6,7-trihydroxy-24-oxocholan-24-yl]glycineGlyco-β-muricholic acidbeta-Glycomuricholic acidGly-beta-MCA