Sodium-glucose cotransport inhibition with dapagliflozin in type 2 diabetes

Diabetes Care

Volumn 32, Issue 4, 2009, Pages 650-657

  List, James F ^a   Woo, Vincent ^b   Morales, Enrique ^c   Tang, Weihua ^a   Fiedorek, Fred T ^a  

^a BRISTOL MYERS SQUIBB   (United States)

^b UNIVERSITY OF MANITOBA   (Canada)

^c Centro de Investigatión Cardiometabólica   (Mexico)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIDIABETIC AGENT; DAPAGLIFLOZIN; GLUCOSE; HEMOGLOBIN A1C; MAGNESIUM; METFORMIN; PHOSPHATE; PLACEBO; UNCLASSIFIED DRUG; URIC ACID;

ADULT; AGED; ARTICLE; BLOOD PRESSURE; CLINICAL EVALUATION; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CYSTITIS; DIARRHEA; DOUBLE BLIND PROCEDURE; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG SAFETY; DRUG WITHDRAWAL; FEMALE; GENITAL TRACT INFECTION; GLUCOSE BLOOD LEVEL; GLUCOSE TRANSPORT; GLUCOSE URINE LEVEL; GLUCOSURIA; HEMATOCRIT; HUMAN; HYPERGLYCEMIA; HYPOGLYCEMIA; HYPOTENSION; KIDNEY FUNCTION; LABORATORY TEST; MAGNESIUM BLOOD LEVEL; MAJOR CLINICAL STUDY; MALE; MONOTHERAPY; MULTICENTER STUDY; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS; PHOSPHATE BLOOD LEVEL; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; TREATMENT DURATION; URIC ACID BLOOD LEVEL; URINARY EXCRETION; URINARY TRACT INFECTION; URINE VOLUME; WEIGHT REDUCTION;

ADOLESCENT; ADULT; AGED; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; DIURETICS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; GLUCOSIDES; GLYCOSURIA; HEMOGLOBIN A, GLYCOSYLATED; HUMANS; HYPERGLYCEMIA; HYPOGLYCEMIC AGENTS; MALE; METFORMIN; MIDDLE AGED; PLACEBOS; SODIUM-GLUCOSE TRANSPORT PROTEINS; WEIGHT LOSS; YOUNG ADULT;

EID: 65349196064     PISSN: 01495992     EISSN: 19355548     Source Type: Journal    
DOI: 10.2337/dc08-1863     Document Type: Article

References (25)

1. Kles KA, Vinik AI: Pathophysiology and treatment of diabetic peripheral neuropathy: the case for diabetic neurovascular function as an essential component. Curr Diabetes Rev 2:131-145, 2006
2. Nazimek-Siewniak B, Moczulski D, Grz-eszczak W: Risk of macrovascular and mi-crovascular complications in type 2 diabetes: results of longitudinal study design. J Diabetes Complications 16:271-276, 2002
3. Rahman S, Rahman T, Ismail AA, Rashid AR: Diabetes-associated macrovasculopa-thy: pathophysiology and pathogenesis. Diabetes Obes Metab 9:767-780, 2007
4. Holman RR, Paul SK, Bethel MA, Matthews DR, Neil HAW: 10-year follow-up of intensive glucose control in type 2 diabetes. N Engl J Med 359:1577-1589, 2008
5. Andrews WJ, Vasquez B, Nagulesparan M, Klimes I, FoleyJ, Unger R, Reaven GM: Insulin therapy in obese, non-insulin-de-pendent diabetes induces improvements in insulin action and secretion that are maintained for two weeks after insulin withdrawal. Diabetes 33:634-642, 1984
6. Prentki M, Nolan CJ: Islet β3 cell failure in type 2 diabetes. J Clin Invest 116:1802-1812, 2006
7. Blonde L: State of diabetes care in the United States. Am J Manage Care 13 (Suppl. 2):S36-S40, 2007
8. Han S, Hagan DL, Taylor JR, Xin L, Meng W, Biller SA, Wetterau JR, Washburn WN, Whaley JM: Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes 57:1723-1729, 2008
9. Meng W, Ellsworth BA, Nirschl AA, Mc-Cann PJ, Patel M, Girotra RN, Wu G, Sher PM, Morrison EP, Biller SA, Zahler R, Deshpande PP, Pullockaran A, Hagan DL, Morgan N, Taylor JR, Obermeier MT, Humphreys WG, Khanna A, Discensa L, Robertson JG, Wang A, Han S, Wetterau JR, Janovitz EB, Flint OP, Whaley JM, Washburn WN: Discovery of dapagliflo-zin: a potent, selective renal sodium-dependent glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes. J Med Chem 51:1145-1149, 2008
10. Santer R, Kinner M, Lassen CL, Schnep-penheim R, Eggert P, Bald M, Brodehl J, Daschner, Ehrich JH, Kemper M, Li Volti S, Neuhaus T, Skovby F, Swift PG, Schaub J, Klaerke D: Molecular analysis of the SGLT2 gene in patients with renal glu-cosuria. J Am Soc Nephrol 14:2873-2882, 2003
11. Wright EM, Hirayama BA, Loo DF: Active sugar transport in health and disease. J Intern Med 261:32-43, 2007
12. +/glucose cotransporter SGLT2: delineation of the major renal reabsorptive mechanism for D-glucose. J Clin Invest 93: 397-404, 1994
13. Hediger MA, Rhoads DB: Molecular physiology of sodium-glucose cotransporters. Physiol Rev 74:993-1026, 1994
14. Rossetti L, Smith D, Shulman GI, Papach-ristou D, DeFronzo RA: Correction of hy-perglycemia with phlorizin normalizes tissue sensitivity to insulin in diabetic rats. JClin Invest 79:1510-1515, 1987
15. Kahn BB, Shulman GI, DeFronzo RA, Cushman SW, Rossetti L: Normalization of blood glucose in diabetic rats with phlorizin treatment reverses insulin-resistant glucose transport in adipose cells without restoring glucose transporter gene expression. JClin Invest 87:561-570, 1991
16. Komoroski BJ, Brenner E, Li L, Vachhara-jani N, Kornhauser D: Dapagliflozin (BMS-512148), a selective SGLT2 inhibitor, inhibits glucose reabsorption and reduces fasting glucose in patients with type 2 diabetes. Presented at the 43rd annual meeting of the European Association for the Study of Diabetes; 17-21 September 2007; Amsterdam, The Netherlands, 2007, abstract 0763
17. +/D- glucose cotransport defects leading to renal glycosuria, congenital selective intestinal malabsorption of glucose, galactose. In The Metabolic Basis of Inherited Disease, 7th ed. Scriver CR, Beaudet AL, Sly WS, Valle D, Eds. New York, McGraw-Hill, 1994, p. 3563-3580
18. van den Heuvel LP, Assink K, Willemsen M, Monnens L: Autosomal recessive renal glucosuria attributable to a mutation in the sodium glucose cotransporter (SGLT2). Hum Genet 111:544-547, 2002
19. Levey AS, Bosch JP, Lewis JB, Greene T, Rogers N, Roth D: A more accurate method to estimate glomerular filtration rate from serum creatinine: a new prediction equation, the Modification of Diet in Renal Disease Study Group. Ann Intern Med 130:461-470, 1999
20. Farber SJ, Berger EY, Earle DP: Effect of diabetes and insulin of the maximum capacity of the renal tubules to reabsorb glucose. JClin Invest 30:125-129, 1951
21. AmericanDiabetes Association: Executive summary: standards of medical care in di-abetes-2008. Diabetes Care31 (Suppl. 1): S5-S11, 2008
22. Bradford BJ, Allen MS: Phlorizin induces lipolysis and alters meal patterns in both early- and late-lactation dairy cows. J Dairy Sci 90:1810-1815, 2007
23. DevenneyJ, HarveyS, RooneyS, Godonis H, Washburn W, WhaleyJ, Taylor S, Pel-leymounter M: The effect of dapagliflozin, a highly selective SGLT2 inhibitor, on body weight in diet-induced obese rats. Presented at The Obesity Society Annual Scientific Meeting 2007; New Orleans, LA, 2007, Abstract 0384
24. Amori RE, Lau J, Pittas AG: Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis. JAMA 2989:194-206, 2007
25. Ribera MC, Pascual R, Orozco D, Perez Barba C, Pedrera V, Gil V: Incidence and risk factors associated with urinary tract infections in diabetic patients with and without asymptomatic bacteriuria. Eur J Clin Microbiol Infect Dis 25:389-393, 2006