Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes

Meng, Wei; Ellsworth, Bruce A.; Nirschl, Alexandra A.; McCann, Peggy J.; Patel, Manorama M.; Girotra, Ravindar N.; Wu, Gang; Sher, Philip M.; Morrison, Eamonn P.; Biller, Scott A.; Zahler, Robert; Deshpande, Prashant P.; Pullockaran, Annie; Hagan, Deborah; Morgan, Nathan; Taylor, Joseph R.; Obermeier, Mary T.; Humphreys, W. Griffith; Khanna, Ashish K.; Discenza, Lorell; Robertson, James G.; Aiying, Wang; Han, Song‐Ping; Wetterau, John R.; Janovitz, Evan B.; Flint, Oliver; Whaley, Jean M.; Washburn, William N.

doi:10.1021/jm701272q

articleJournal of Medicinal ChemistryFeb 9, 2008GREEN OA

Discovery of Dapagliflozin: A Potent, Selective Renal Sodium-Dependent Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes

WMWei Meng BABruce A. Ellsworth AAAlexandra A. Nirschl PJPeggy J. McCann MMManorama M. Patel

Bristol-Myers Squibb (United States)

PubMed

Indexed incrossrefdatacitepubmed

Abstract

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.

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Topics & keywords

Topics

Keywords

Dapagliflozin
Chemistry
Type 2 diabetes
Cotransporter
Renal glucose reabsorption
Diabetes mellitus
Pharmacology
Sodium

UN Sustainable Development Goals

Good health and well-being

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