Dapagliflozin: Where does it fit in the treatment of type 2 diabetes?

Expert Opinion on Pharmacotherapy

Volumn 10, Issue 15, 2009, Pages 2527-2535

  Woo, Vincent C ^a  

^a UNIVERSITY OF MANITOBA   (Canada)

Author keywords

Antihyperglycemic agents; Dapagliflozin; Sodium glucose co transporter 2 inhibitor; Type 2 diabetes

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; DAPAGLIFLOZIN; HYPERGLYCEMIC AGENT; INSULIN; METFORMIN; ORAL ANTIDIABETIC AGENT; PHLORIZIN; PLACEBO; PROTEIN INHIBITOR; SODIUM GLUCOSE COTRANSPORTER 2; SODIUM GLUCOSE COTRANSPORTER 2 INHIBITOR; SULFONYLUREA; UNCLASSIFIED DRUG;

ABSENCE OF SIDE EFFECTS; AREA UNDER THE CURVE; CLINICAL TRIAL; DIARRHEA; DIET THERAPY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG DOSE TITRATION; DRUG EFFICACY; DRUG EXCRETION; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG MECHANISM; DRUG SAFETY; DRUG SELECTIVITY; GENITAL TRACT INFECTION; GLUCOSURIA; HUMAN; HYPERGLYCEMIA; HYPOGLYCEMIA; INDUCED HYPOTENSION; LIFESTYLE MODIFICATION; NAUSEA; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PHYSICIAN; QT INTERVAL; QT PROLONGATION; REVIEW; SIDE EFFECT; SINGLE DRUG DOSE; TREATMENT DURATION; TREATMENT OUTCOME; URINARY TRACT INFECTION;

ANIMALS; CLINICAL TRIALS AS TOPIC; DIABETES MELLITUS, TYPE 2; DRUG DELIVERY SYSTEMS; GLUCOSIDES; HUMANS; HYPOGLYCEMIC AGENTS; LIFE STYLE; SODIUM-GLUCOSE TRANSPORT PROTEINS; SODIUM-GLUCOSE TRANSPORTER 2;

EID: 70349392502     PISSN: 14656566     EISSN: None     Source Type: Journal    
DOI: 10.1517/14656560903222281     Document Type: Review

References (43)

1. International Diabetes Federation. Diabetes prevalence. Available from: http://www.idf.org/diabetes-prevalence. [Accessed 16 May 2009]
2. Klein R, Klein BEK. Vision disorders in diabetes. In: 2nd edition. Diabetes in America. Bethesda, MD: National Diabetes Data Group, National Institutes of Health, National Institute of Diabetes and Digestive and Kidney Diseases; 1995. p. 293-338
3. Warram JH, Gearin G, Laffel L, et al. Effect of duration of type I diabetes on the prevalence of stages of diabetic nephropathy defined by urinary albumin/creatinine ratio. J Am Soc Nephrol 1996;7:930-937 (Pubitemid 27465988)
4. Reenders K, de Nobel E, van den Hoogen HJ, et al. Diabetes and its long-term complications in general practice: a survey in a well-defined population. Fam Pract 1993;10:169-172
5. Lee WL, Cheung AM, Cape D, et al. Impact of diabetes on coronary artery disease in women and men: a meta-analysis of prospective studies. Diabetes Care 2000;23:962-968
6. Booth GL, Kapral MK, Fung K, et al. Relation between age and cardiovascular disease in men and women with diabetes compared with non-diabetic people: a population-based retrospective cohort study. Lancet 2006;368:29-36
7. The Diabetes Control and Complications Trial Research Group. The effect of intensive treatment of diabetes on the development and progression of long-term complications in insulin-dependent diabetes mellitus. N Engl J Med 1993;329:977-986
8. Ohkubo Y, Kishikawa H, Araki E, et al. Intensive insulin therapy prevents the progression of diabetic microvascular complications in Japanese patients with non-insulin-dependent diabetes mellitus: a randomized prospective 6-year study. Diabetes Res Clin Pract 1995;28:103-117
9. UK Prospective Diabetes Study (UKPDS) Group. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). Lancet 1998;352:837-853
10. Nathan DM, Cleary PA, Backlund JY, et al. Intensive diabetes treatment and cardiovascular disease in patients with type 1 diabetes. N Eng J Med 2005;353:2643-2653 (Pubitemid 41817713)
11. Holman RR, Rahman T, Ismail AA, et al. 10-year follow-up of intensive glucose control in type 2 diabetes. N Engl J Med 2008;359:1577-1589
12. Ray KR, Seshasai SRK, Sivakumaran R, et al. Effect of intensive control of glucose on cardiovascular outcomes and death inpatients with diabetes mellitus: a meta-analysis of randomized controlled trials. Lancet 2009;373:1765-1772
13. Harris M. Health care and health status and outcomes for patients with type 2 diabetes. Diabetes Care 2000;23:754-758 (Pubitemid 30414188)
14. Silverman M. Structure and function of hexose transporters. Annu Rev Biochem 1991;60:757-794
15. Wright EM. Renal Na(+) - glucose cotransporters. Am J Physiol Renal Physiol 2001;280(1):F10-8
16. Thomson AB, Wild G. Adaptation of intestinal nutrient transport in health and disease. Dig Dis Sci 1997;42(3);453-88 (Pubitemid 27148329)
17. Santer R, Kinner M, Lassen CL, et al. Molecular analysis of the SGLT2 gene in patients with renal glucosuria. J Am Soc Nephrol 2003;14:2873-2882 (Pubitemid 37305650)
18. Wright EM, Hirayama BA, Loo DF. Active sugar transport in health and disease. J Intern Med 2007;261(1):32-43 (Pubitemid 46046470)
19. Kanai Y, Lee WS, You G, et al. The human kidney low affinity Na+/glucose cotransporter SGLT2. Delineation of the major renal reabsorptive mechanism for D-glucose. J Clin Invest 1994;93(1):397-404 (Pubitemid 24983192)
20. Hediger MA, Rhoads DB. Molecular physiology of sodium-glucose cotransporters. Physiol Rev 1994;74(4):993-1026
21. Francis J, Zhang J, Farhi A, et al. A novel SGLT2 mutation in a patient with autosomal recessive renal glucosuria. Nephrol Dial Transplant 2004;19:2394-2396
22. Scholl-Burgi S, Santer R, Ehrich JH. Long-term outcome of renal glucosuria type O: the original patient and his natural history. Nephrol Dial Transplant 2004;19:2394-2396 (Pubitemid 39214139)
23. Oemar BS, Byrd DJ, Brohehl J. Complete absence of tubular glucose reabsorption: a new type of renal glucosuria (type 0). Clin Nephrol 1987;27:156-160
24. Desjeux J-F, Turk E, Wright E. Congenital selective Na/D-glucose cotransport defects leading to renal glucosuria, congenital selective intestinal malabsorption of glucose, galactose. In: Scriver CR, Beaudet al, Sly WS, Valle D, editors, The metabolic basis of inherited disease. 7th edition. New York, McGraw-Hill; 1994. p. 3563-3580
25. van den Heuvel LP, Assink K, Willemsen M, et al. Autosomal recessive renal glucosuria attributable to a mutation in the sodium glucose cotransporter (SGLT2). Hum Genet 2002;111:544-547
26. Calado J, et al. Familial renal glucosuria: SLC5A2 mutation analysis and evidence of salt-wasting. Kidney Int 2006;69:852-855
27. Ehrenkranz JRL, Lewis NG, Kahn CR. Phlorizin: a review. Diabetes Metab Res Rev 2005;21:31-38
28. Keller DM, Lotspeich WD. Effect of phlorizin on the osmotic behaviour of mitochondria in isotonic sucrose. J Biol Chem 1959;234:991-994
29. Alvarado FC, Crane RK. Phlorizin as a competitive inhibitor of the active transport of sugars by hamster small intestine in vitro. Biochim Biophys Acta 1962;56:170-172
30. Idris I, Donnelly R. Sodium-glucose co-transporter-2 inhibitors: an emerging new class of oral antidiabetic drug. Diabetes Obes Metab 2009;11:79-88
31. Han S, Hagan DL, Taylor JR, et al. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes 2008;57:1723-1729
32. Komoroski B, Vachharajani N, Feng Y, et al. Dapagliflozin, a novel, selective SGLT2 inhibitor, improved glycemic control over 2 weeks in patients with type 2 diabetes mellitus. Clin Pharmacol 2009;85(5):513-519
33. Devenny J, Harvey S, Roony S, et al. The effect of dapagliflozin (BMS-512148), a selective SGLT2 inhibitor, on body weight in diet-induced obese rats. North American Association for the Study of Obesity Annual Meeting 2007;15(suppl 9):A121
34. Meng W, Ellsworth BA, Nirschl AA, et al. 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;51:1145-1149
35. Li L, Komoroski B, Boulton D, et al. Safety, Pharmacokinetics, and pharmacodynamics of dapagliflozin (BMS-512148), a selective SGLT2 inhibitor, in an ascending, placebo-controlled, single-dose study in healthy adult participants. June 5 - 9, 2009, New Orleans USA EASD meeting, #0764 2007
36. List J, Woo VC, Morales E, et al. Sodium-glucose co-transport inhibition with dapagliflozin in type2 diabetes mellitus. Diabetes Care 2009;32:650-657
37. Wilding PH, Norwood P, et al. Dapagliflozin Pilot Study in Insulin-Resistant T2DM Patients. American Diabetes Association Annual Meeting June 5-9, 2009, New Orleans USA, 482P
38. Carlson GF, Tou CKP, Darjkh S, et al. Dapagliflozin was not observed to prolong the QTc in a thorough QT/QTc Study. American Diabetes Association Annual Meeting June 5-9, 2009, New Orleans USA, 483P
39. Kahn SE, Haffner SM, Heise MA, et al. Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med 2006;355:2427-2443
40. Nathan DM, Buse JB, Davidson MB, et al. Medical management of hyperglycemia in type 2 diabetes: a consensus algorithm for the initiation and adjustment of therapy. Diabetes Care 2008;31:1-11
41. Pharmacologic management of type 2 diabetes. Can J Diabetes 2008;32(suppl 1):S53-61
42. Woo V. Important differences: Canadian Diabetes Association 2008 clinical practice guidelines and the consensus statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetologia 2009;52:552-553
43. Home PD, Pocock SJ, Beck-Nielsen, et al. Rosiglitazone evaluated for cardiovascular outcomes in oral agent combination therapy for type2 diabetes (RECORD): a multicentre, randomised, open-label trial. Lancet 2009:273(9681);2125-2135