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

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

  • J Med Chem. 2008 Mar 13;51(5):1145-9. doi: 10.1021/jm701272q.
Wei Meng 1,  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
Affiliations

Affiliation

  • 1 Drug Safety Evaluation and Development, Bristol -Myers Squibb Company, Princeton, New Jersey 08543, USA. [email protected]
PMID: 18260618 DOI: 10.1021/jm701272q
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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