Empagliflozin (BI 107730) is a Selective SGLT-2 Inhibitor for Type 2 Diabetes Research

Diabetes has a major impact on the global human population. Generally, blood glucose control is the major method of diabetes treatment. Previous studies indicated that targeting sodium glucose co-transporter-2 (SGLT-2) to induce renal glucose excretion is a novel and promising approach to treating type 2 diabetes.

SGLT-2 is responsible for the reabsorption of the bulk of filtered glucose from the kidney. But, excess glucose is excreted in the urine when the threshold for glucose excretion is reached. So, we can inhibit SGLT-2 to lower the threshold for glucose excretion. And then induce glucose excretion at lower plasma glucose concentrations. Today we will introduce a potent, selective SGLT-2 Inhibitor — Empagliflozin.

 

Empagliflozin (BI 107730) is a selective SGLT-2 inhibitor for type 2 diabetes research.

On the one hand, empagliflozin can increase urinary glucose excretion in a dose-dependent manner and reduce the levels of blood glucose. On the other hand, after multiple doses (5 weeks), empagliflozin reduces the levels of fasting blood glucose by 26 and 39% with 1 and 3 mg/kg empagliflozin, respectively. After 5 weeks, empagliflozin (1 and 3 mg/kg) reduces the levels of HbA1c (from a baseline of 7.9%) by 0.3 and 1.1%, respectively. Therefore, multiple daily doses of empagliflozin can reduce blood glucose and HbA1c levels, and improve glucose tolerance in ZDF rats. Empagliflozin has a good capacity to improve glycaemic control.

In sum, Empagliflozin is a selective inhibitor of SGLT-2. It can be used for the research of type 2 diabetic diseases.

Reference:

[1] Thomas L, Grempler R, Eckhardt M, et al. Diabetes Obes Metab. 2012;14(1):94-96.