DBPR211, a novel small-molecule anti-type 2 diabetes drug candidate, was approved for Phase I clinical study by the US Food and Drug Administration (FDA)

Institute of Biotechnology and Pharmaceutical Research (IBPR) received US FDA Investigational New Drug Application (IND) Approval for DBPR211 on May 20, 2016, for initiation of phase I clinical trial for the treatment of type 2 diabetes (T2D). DBPR211 is the first “First-in-Class” drug candidate developed by IBPR successfully approved by US FDA under the support of National Research Program of Biopharmaceuticals and National Health Research Institutes (NHRI).

Cannabinoid receptor type 1 (CB1) is a G protein-coupled receptor expressed centrally to control appetite and peripherally to regulate lipid and glucose metabolism. Blockade of peripheral CB1 receptors improves insulin resistance and protects pancreatic b cell survival with additional benefit in weight loss and reduction of hepatic steatosis. Therefore, targeting peripheral CB1 receptor is a potential therapeutic strategy in treating T2D without inducing the untoward psychological adverse effects.

DBPR211 is a potent and selective peripheral CB1 antagonist possessing an extremely low brain to plasma ratio. It significantly improves insulin resistance in diabetic models, and induces weight loss and decreases hepatic steatosis as well as insulin resistance in obese model. This drug candidate is well protected by various global patent applications. IBPR/NHRI will seek for industrial partner to further develop DBPR211, and clinical trials will be conducted after technical transfer in the near future.

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