Sodium-glucose co-transporter 2 inhibition-a novel strategy for: Glucose control in type 2 diabetes

US Endocrinology

Volumn 6, Issue 1, 2010, Pages 42-47

  Norton, Luke ^a   DeFronzo, Ralph A ^a   Abdul Ghani, Muhammad A ^a  

^a UNIVERSITY OF TEXAS HEALTH SCIENCE CENTER AT SAN ANTONIO   (United States)

Author keywords

Kidney; Sodium glucose co transport; Sodium glucose co transporter 2 (SGLT2) inhibition; Type 2 diabetes

Indexed keywords

EID: 84857201839     PISSN: 17583918     EISSN: 17583926     Source Type: Journal    
DOI: 10.17925/use.2010.06.1.42     Document Type: Article

References (49)

1. Schalkwijk CG, Stehouwer CD, Vascular complications in diabetes mellitus: the role of endothelial dysfunction, Clin Sci (Lond), 2005;109:143-59
2. He Z, King GL, Microvascular complications of diabetes, Endocrinol Metab Clin North Am, 2004;33:215-38
3. 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: 977-86
4. 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;352:837-53
5. DeFronzo RA, Banting Lecture: From the triumvirate to the ominous octet: a new paradigm for the treatment of type 2 diabetes mellitus, Diabetes, 2009;58:773-95
6. Rossetti L, Giaccari A, DeFronzo RA, Glucose toxicity, Diabetes Care, 1990;13:610-30
7. The American Diabetes Association, Standards of medical care in diabetes-2007, Diabetes Care, 2007;30(Suppl. 1): S4-41.
8. Qaseem A, Vijan S, Snow V, et al., Clinical Efficacy Assessment Subcommittee of the American College of Physicians, Glycemic control and type 2 diabetes mellitus: the optimal hemoglobin A1c targets. A guidance statement from the American College of Physicians, Ann Int Med, 2007;147:417-22.
9. Rodbard HW, Davidson JA, Garber AJ, et al., AACE/ACE Consensus Statement. Statement by an American Association of Clinical Endocrinologists/American College of Endocrinology Consensus Panel on Type 2 Diabetes Mellitus: an algorithm for glycemic control, Endocr Pract, 2009;15:540-59.
10. Nathan DM, Buse JB, Davidson MB, et al., Management of hyperglycaemia in type 2 diabetes mellitus: a consensus algorithm for the initiation and adjustment of therapy: Update regarding the thiazolidinediones, Diabetologia, 2008;51:8-11.
11. Valtin H, Tubular reabsorption. In: Renal Function, Boston: Little, Brown and Company, 1983.
12. Gribble FM, Williams L, Simpson AK, Reimann F, A novel glucose-sensing mechanism contributing to glucagon-like peptide-1 secretion from the GLUTag cell line, Diabetes, 2003;52:1147-54
13. von Mering J, Ueber kunstlichen diabetes, Centralbl Med Wiss, 1886;22:531
14. Vick HD, Deidrich DF, Re-evaluation of renal tubular glucose transport inhibition by phlorizin analogs, Am J Physiol, 1973;224:552-7
15. Chassis H, Jolliffe N, Smith H, The action of phlorizin on the excretion of glucose, xylose, sucrose, creatinine, and urea by man, J Clin Invest, 1933;12:1083-9
16. Ehrenkranz JR, Lewis NG, Kahn CR, Roth J, Phlorizin: a review, Diabetes Metab Res Rev, 2005;21:31-8
17. Bhanot S, Murray SF, Booten SL, et al., ISIS 388626, an SGLT2 antisense drug, causes robust and sustained glucosuria in multiple species and is safe and well-tolerated, Diabetes, 2009;58(Suppl. 1):A328.
18. Kahn BB, 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, J Clin Invest, 1999;87: 561-70
19. Rossetti L, Smith D, Shulman GI, Papachristou D, DeFronzo RA, Correction of hyperglycemia with phlorizin normalizes tissue sensitivity to insulin in diabetic rats, J Clin Invest, 1987;79:1510-5
20. Rossetti L, Shulman GI, Zawalich W, DeFronzo RA, Effect of chronic hyperglycemia on in vivo insulin secretion in partially pancreatectomized rats, J Clin Invest, 1987;80:1037-44
21. Oku A, Ueta K, Nawano M, et al., Antidiabetic effect of T-1095, an inhibitor of Na(+)-glucose cotransporter, in neonatally streptozotocin-treated rats, Eur J Pharmacol, 2000;391:183-92.
22. Katsuno K, Fujimori Y, Takemura Y, et al., Sergliflozin, a novel selective inhibitor of low-affinity sodium glucose cotransporter (SGLT2), validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level, J Pharmacol Exp Ther, 2007;320:323-30.
23. Han S, Hagan DL, Taylor JR, et al., Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats, Diabetes, 2008;57:1723-9.
24. Santer R, Kinner M, Lassen CL, et al., Molecular analysis of the SGLT2 gene in patients with renal glucosuria, J Am Soc Nephrol, 2003;14:2873-82.
25. Bailey CJ, Gross JL, Pieter A, Bastien A, List JF, Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with metformin; a randomized, double-blind, placebo-controlled trail, Lancet, 2010;375:2223-33
26. Ferrannini E, Ramos SJ, Tang W, et al., Dapagliflozin monotherapy in T2DM patients with inadequate glycemic control by diet and exercise: a randomized, double-blind, placebo-controlled, multicenter phase III trial, (Late-Breaking Abstract) International Diabetes Federation World Congress, Montreal, Canada, November, 2009.
27. 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 Ther, 2009;85:513.
28. Obermeier M, Yao M, Khanna A, et al., In vitro characterization and pharmacokinetics of dapagliflozin (BMS-512148), a potent sodium-glucose cotransporter type II inhibitor, in animals and humans, Amer Soc Pharm Exp Ther, 2010;38:405-14.
29. List J, Woo V, Morales E, et al., Sodium-glucose cotransport inhibition with dapagliflozin in type 2 diabetes, Diabetes Care, 2009;32:650-7.
30. Wilding JPH, Norwood P, Tjoen C, et al., A study of dapagliflozin in patients with type 2 diabetes receiving high doses of insulin plus insulin sensitizers. Applicability of a novel insulin-independent treatment, Diabetes Care, 2009;32:1656-62.
31. Zhang L, Feng Y, List J, et al., Dapagliflozin treatment in patients with different stages of type 2 diabetes mellitus: effects on glycaemic control and body weight, Diab Obesity Metab, 2010;12:510-6.
32. Hussey E, Clark R, Amin D, et al., Early clinical studies to assess safety, tolerability, pharmacokinetics and pharmacodynamics of single dose of sergliflozin, a novel inhibitor of renal glucose reabsorption in healthy volunteers and subjects with type 2 diabetes mellitus, Diabetes, 2007;56(Suppl. 1):A189.
33. Hussey E, Dobbins R, Stolz R, et al., A double-blind randomized repeat dose study to assess safety, tolerability, pharmacokineticks and pharmacodynamics of three times daily dosing of sergliflozin, a novel inhibitor of renal glucose reabsorption in healthy overweight and obese subjects, Diabetes, 2007;56(Suppl. 1):A491.
34. Rosensotck J, Arbit D, Usiskin K, et al., Canagliflozin an inhibitor of sodium glucose co-transporter 2 (SGLT2), improves glycemic control and lowers body weight in subjects with type 2 diabetes (T2D) on metformin, Diabetes, 2010;59(Suppl. 1):A21.
35. Polidori D, Zhao Y, Sha S, Canovatchel W, Canagliflozin treatment improves beta cell function in subject with type 2 diabetes, Diabetes, 2010;59(Suppl. 1):A176.
36. Schwartz S, Morrow L, Hompesch M, et al., Canagliflozine improves glycemic control in subjects with type 2 diabetes (T2D) not optimally controlled on stable doses of insulin, Diabetes, 2010;59(Suppl. 1):564P.
37. Koiwai K, Seman L, Yamamura N, et al., Safety, tolerability, pharmacokinetics and pharmacodynamics of single doses of BI 10773, a sodium-glucose co-transporter inhibitor (SGLT2), in Japanese healthy volunteers, Diabetes, 2010;59(Suppl. 1):2175PO.
38. Kashiwagi A, Utsuno A, Kazuta K, et al., ASP1941, a novel, selective SGLT2 inhibitor, was effective and safe in Japanese healthy volunteers and patients with type 2 diabetes mellitus, Diabetes, 2010;59(Suppl. 1):A21.
39. Freiman J, Ruff DA, Frazier KS, et al., LX4211, a dual SGLT2/SGLT1 inhibtor, shows rapid and significant improvements in glycemic control over 28 days in patients with type 2 diabetes (T2DM), Diabetes, 2010;59(Suppl. 1), late breaking abstract.
40. Fujimori Y, Katsuno K, Nakashima I, et al., Remogliflozin etabonate, in a novel category of selective low-affinity sodium glucose cotransporter (SGLT2) inhibitors, exhibits antidiabetic efficacy in rodent models, J Pharmacol Exp Ther, 2008;327:268-76.
41. Dobbins RL, Kapur A, Kapitza C, et al., Remogliflozin etabonate, a selective inhibitor of the sodium-glucose transporter 2 (SGLT2) reduces serum glucose in type 2 diabetes mellitus (T2DM) patients, Diabetes, 2009;58 (Suppl. 1):A573.
42. Vallon V, Richter K, Blantz RC, et al., Glomerular hyperfiltration in experimental diabetes mellitus: potential role of tubular reabsorption, J Am Soc Nephrol, 1999;10:2569-76.
43. Thomson SC, Vallon V, Blantz RC, Kidney function in early diabetes: the tubular hypothesis of glomerular filtration, Am J Physiol, 2004;286:F8-18
44. Noonan WT, Shapiro VM, Banks RO, Renal glucose reabsorption during hypertonic glucose infusion in female streptozotocin-induced diabetic rats, Life Sci, 2001;68:2967-77
45. Dominguez JH, Camp K, Maianu L, et al., Molecular adaptations of GLUT1 and GLUT2 in renal proximal tubules of diabetic rats, Am J Physiol, 1994;266:F283-90.
46. Nelson RG, Bennett PH, Beck GJ, et al., Development and progression of renal disease in Pima Indians with non-insulin-dependent diabetes mellitus. Diabetic Renal Disease Study Group, N Engl J Med, 1996;335:1636-42.
47. Tuttle KR, Bruton JL, Perusek MC, et al., Effect of strict glycemic control on renal hemodynamic response to amino acids and renal enlargement in insulin-dependent diabetes mellitus, N Engl J Med, 1991;324:1626-32.
48. Arakawa K, Ishihara T, Oku A, et al., Improved diabetic syndrome in C57BL/KsJ-db/db mice by oral administration of the Na(+)-glucose cotransporter inhibitor T-1095, Br J Pharmacol, 2001;132:578-86.
49. Bickel M, Brummerhop H, Frick W, et al., Effects of AVE2268, a substituted glycopyranoside, on urinary glucose excretion and blood glucose in mice and rats, Arzneimittelforschung, 2008;58:574-80.