Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.

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Journal of medicinal chemistry (2008-02-12)
Wei Meng, Bruce A Ellsworth, Alexandra A Nirschl, Peggy J McCann, Manorama Patel, Ravindar N Girotra, Gang Wu, Philip M Sher, Eamonn P Morrison, Scott A Biller, Robert Zahler, Prashant P Deshpande, Annie Pullockaran, Deborah L Hagan, Nathan Morgan, Joseph R Taylor, Mary T Obermeier, William G Humphreys, Ashish Khanna, Lorell Discenza, James G Robertson, Aiying Wang, Songping Han, John R Wetterau, Evan B Janovitz, Oliver P Flint, Jean M Whaley, William N Washburn


The C-aryl glucoside 6 (dapagliflozin) was identified as a potent and selective hSGLT2 inhibitor which reduced blood glucose levels in a dose-dependent manner by as much as 55% in hyperglycemic streptozotocin (STZ) rats. These findings, combined with a favorable ADME profile, have prompted clinical evaluation of dapagliflozin for the treatment of type 2 diabetes.