Technology/ Title:DBPR211: A Peripheral CB1 Antagonist
An IND Approved First-in-Class Drug Candidate for T2DM

Cannabinoid receptor 1 (CB1) is expressed in several peripheral tissues related to metabolic control in addition to its abundancy in the central nervous system. Activation of peripheral CB1 induces lipogenesis, gluconeogenesis and pancreatic β-cell death. In contrast, blockade of CB1 leads to inhibition of lipogenesis and increase of adiponectin expression, glucose uptake, and protection of β-cell survival. In-depth analysis of clinical data from Rimonabant, a centrally acting CB1 antagonist, has revealed that CB1 inhibition confined to the body’s periphery has direct beneficial effects on human cardiometabolic risk factors such as insulin resistance. Besides, both clinical and preclinical studies support CB1 antagonists in treating non-alcoholic fatty liver disease (NAFLD) including non-alcoholic steatohepatitis (NASH). These data imply that targeting at peripheral CB1 is a therapeutic strategy for treating metabolic disorders such as type 2 diabetes (T2D), obesity and non-alcoholic fatty liver disease without causing the undesired psychological side effects resulting from central CB1 inhibition.

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