Berberine Ursodeoxycholate

Mechanism of Action

Berberine ursodeoxycholate is an orally delivered potentially first-in-class gut-liver anti-inflammatory metabolic modulator being developed for the treatment of metabolic and liver diseases.

Our lead compound, berberine ursodeoxycholate, is a new molecular entity with dual mechanisms of action – AMP kinase activation and NLRP3 inflammasome inhibition. These two key mechanistic pathways have been associated with improvements in glucose metabolism, insulin resistance, lipid metabolism, hepatic inflammation, and gut microbiome potentially providing a comprehensive treatment platform for the multifaceted nature of complex metabolic and liver diseases.

These effects have potential application in a range of liver and cardiometabolic diseases.

AMP Kinase activation and NLRP3 inflammasome inhibition

Inflammation
Steatosis
Fibrosis

Cholestasis
Cholangitis

Body Weight
Inflammation

Atherogenic Lipids
Oxidative Stress

Glucose Clearance

Harmful Microbiota
Beneficial Microbiota

Insulin Resistance
Glycemic Control

Clinical Trials of Berberine Ursodeoxycholate

Clinical trials in patients with T2DM, MASH, SHTG and PSC have been completed or are ongoing, evaluating the effects of berberine ursodeoxycholate on liver fat content, markers of liver fibrosis, markers of liver inflammation and injury, as well as metabolic changes such as reductions in elevated lipids (LDL-C and triglycerides), improvements in HbA1c and fasting glucose and weight loss. An obesity clinical program is in the planning stages.