Drug intelligence / Profile preview

ursodeoxycholic acid + rifaximin

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Ursodeoxycholic acid + rifaximin is a combination therapy consisting of two small molecule drugs. Ursodeoxycholic acid (UDCA) is a hydrophilic bile acid used primarily to improve bile flow and reduce liver enzyme levels in cholestatic liver diseases, such as primary biliary cholangitis. It acts by reducing the cytotoxicity of endogenous bile acids and promoting choleresis. Rifaximin is a non-absorbable antibiotic that targets gut bacteria, modulating the intestinal microbiome and reducing bacterial translocation and endotoxin production; it is used for hepatic encephalopathy, irritable bowel syndrome, and has been investigated for nonalcoholic steatohepatitis (NASH) and other liver-related conditions[2]. The combination aims to leverage complementary mechanisms—enhancing hepatobiliary detoxification pathways (via UDCA) while modulating gut-liver axis inflammation (via rifaximin). Clinical studies suggest this combination can stimulate bile acid synthesis, conjugation, elimination, and may benefit patients with certain chronic liver diseases[1][6].

Other names
熊去氧胆酸 + 利福昔明
02

Targets

GPBAR1ABCB11 (Bile salt export pump)CYP3A4 (Cytochrome P450 3A4)rpoB (DNA-directed RNA polymerase subunit beta)PXR (Pregnane X receptor)

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