title: Discovery of dapagliflozin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes.
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.
authors.affiliation: Drug Safety Evaluation and Development, Bristol -Myers Squibb Company, Princeton, New Jersey 08543, USA. wei.meng@bms.com
authors.forename: Wei
authors.initials: W
authors.lastname: Meng
authors.forename: Bruce A
authors.initials: BA
authors.lastname: Ellsworth
authors.forename: Alexandra A
authors.initials: AA
authors.lastname: Nirschl
authors.forename: Peggy J
authors.initials: PJ
authors.lastname: McCann
authors.forename: Manorama
authors.initials: M
authors.lastname: Patel
authors.forename: Ravindar N
authors.initials: RN
authors.lastname: Girotra
authors.forename: Gang
authors.initials: G
authors.lastname: Wu
authors.forename: Philip M
authors.initials: PM
authors.lastname: Sher
authors.forename: Eamonn P
authors.initials: EP
authors.lastname: Morrison
authors.forename: Scott A
authors.initials: SA
authors.lastname: Biller
authors.forename: Robert
authors.initials: R
authors.lastname: Zahler
authors.forename: Prashant P
authors.initials: PP
authors.lastname: Deshpande
authors.forename: Annie
authors.initials: A
authors.lastname: Pullockaran
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Hagan
authors.forename: Nathan
authors.initials: N
authors.lastname: Morgan
authors.forename: Joseph R
authors.initials: JR
authors.lastname: Taylor
authors.forename: Mary T
authors.initials: MT
authors.lastname: Obermeier
authors.forename: William G
authors.initials: WG
authors.lastname: Humphreys
authors.forename: Ashish
authors.initials: A
authors.lastname: Khanna
authors.forename: Lorell
authors.initials: L
authors.lastname: Discenza
authors.forename: James G
authors.initials: JG
authors.lastname: Robertson
authors.forename: Aiying
authors.initials: A
authors.lastname: Wang
authors.forename: Songping
authors.initials: S
authors.lastname: Han
authors.forename: John R
authors.initials: JR
authors.lastname: Wetterau
authors.forename: Evan B
authors.initials: EB
authors.lastname: Janovitz
authors.forename: Oliver P
authors.initials: OP
authors.lastname: Flint
authors.forename: Jean M
authors.initials: JM
authors.lastname: Whaley
authors.forename: William N
authors.initials: WN
authors.lastname: Washburn
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001559:Benzhydryl Compounds; D001786:Blood Glucose / Q000378:metabolism; D003921:Diabetes Mellitus, Experimental / Q000188:drug therapy; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D005960:Glucosides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D007004:Hypoglycemic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007668:Kidney / Q000378:metabolism*; D051381:Rats; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; D013237:Stereoisomerism
chemical_list: D001559:Benzhydryl Compounds; D001786:Blood Glucose; D005960:Glucosides; D007004:Hypoglycemic Agents; C089180:SLC5A2 protein, human; D051297:Sodium-Glucose Transporter 2; D000077203:Sodium-Glucose Transporter 2 Inhibitors; C529054:dapagliflozin