Dapagliflozin

Dapagliflozin (rINN/USAN) is an experimental drug being studied by Bristol-Myers Squibb in partnership with AstraZeneca as a potential treatment for type 1 and 2 diabetes. Although dapagliflozin's method of action would operate on either type of diabetes or other conditions resulting in hyperglycemia, the current clinical trials specifically exclude participants with Type 1 diabetes.

In July 2011 an FDA committee recommended against approval until more data was available.

Method of action
Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine.

Selectivity
The IC50 for SGLT2 is less than one thousandth of the IC50 for SGLT1 (1.1 versus 1390 nmol/l), so that the drug does not interfere with the intestinal glucose absorption.