Lowering plasma glucose concentration by inhibiting renal sodium-glucose cotransport

Journal of Internal Medicine

Volumn 276, Issue 4, 2014, Pages 352-363

  Abdul Ghani, M A ^a   Defronzo, R A ^a  

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

Author keywords

Kidney; SGLT2 inhibition; Sodium glucose cotransport; Type 2 diabetes

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; ANTIDIABETIC AGENT; CANAGLIFLOZIN; DAPAGLIFLOZIN; DAPAGLIFLOZIN PLUS METFORMIN; EMPAGLIFLOZIN; GLIPIZIDE; GLUCOSE; HEMOGLOBIN A1C; HIGH DENSITY LIPOPROTEIN CHOLESTEROL; INSULIN; IPRAGLIFLOZIN; LOW DENSITY LIPOPROTEIN CHOLESTEROL; METFORMIN; PF 04791729; PHLORIZIN; PIOGLITAZONE; SODIUM GLUCOSE COTRANSPORTER 2; SODIUM GLUCOSE COTRANSPORTER 2 INHIBITOR; SOTAGLIFLOZIN; SULFONYLUREA; TS 071; UNCLASSIFIED DRUG; GLUCOSE BLOOD LEVEL; GLYCOSYLATED HEMOGLOBIN;

DIET RESTRICTION; DRUG SAFETY; GLUCOSE BLOOD LEVEL; GLUCOSE TRANSPORT; GLUCOSURIA; HUMAN; HYPOGLYCEMIA; INSULIN DEPENDENT DIABETES MELLITUS; INSULIN RELEASE; INSULIN RESISTANCE; JUXTAGLOMERULAR APPARATUS; KIDNEY FUNCTION; KIDNEY PROXIMAL TUBULE; KIDNEY TUBULE ABSORPTION; NON INSULIN DEPENDENT DIABETES MELLITUS; ORAL GLUCOSE TOLERANCE TEST; PANCREAS ISLET BETA CELL; PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL (TOPIC); REVIEW; SIDE EFFECT; SODIUM ABSORPTION; TREATMENT DURATION; WEIGHT GAIN; ANIMAL; ANTAGONISTS AND INHIBITORS; BLOOD; DIABETES MELLITUS, TYPE 1; DIABETES MELLITUS, TYPE 2; DRUG EFFECTS; KIDNEY; METABOLISM;

ANIMALS; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 1; DIABETES MELLITUS, TYPE 2; GLUCOSE; GLYCOSURIA; HEMOGLOBIN A, GLYCOSYLATED; HUMANS; HYPOGLYCEMIC AGENTS; KIDNEY; SODIUM-GLUCOSE TRANSPORTER 2;

EID: 84914173984     PISSN: 09546820     EISSN: 13652796     Source Type: Journal    
DOI: 10.1111/joim.12244     Document Type: Review

References (62)

1. Rossetti L, Giaccari A, DeFronzo RA. Glucose toxicity. Diabetes Care 1990; 13: 610-30.
2. Abdul-Ghani MA, Norton L, DeFronzo RA. Efficacy and Safety of SGLT2 inhibitors in the treatment of type 2 diabetes mellitus. Curr Diab Rep 2012; 12: 230-8.
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. Standards of medical care in diabetes-2007. Diabetes Care 2007; 30(Suppl 1): S4-41.
7. Hoerger TJ, Segel JE, Gregg EW, Saaddine JB. Is glycemic control improving in U.S. adults? Diabetes Care 2008; 31: 81-6.
8. Abdul-Ghani MA, Norton L, DeFronzo RA. Role of sodium-glucose cotransporter 2 (SGLT 2) inhibitors in the treatment of type 2 diabetes. Endocr Rev 2011; 32: 515-31.
9. Wright EM, Loo DD, Hirayama BA. Biology of human sodium glucose transporters. Physiol Rev 2011; 91: 733-94.
10. Abdul-Ghani MA, Norton L, DeFronzo RA. Efficacy and safety of SGLT2 inhibitors in the treatment of type 2 diabetes mellitus. Curr Diab Rep 2012; 12: 230-8.
11. Farber SJ, Berger EY, Earle DP. Effect of diabetes and insulin of the maximum capacity of the renal tubules to reabsorb glucose. J Clin Invest 1951; 30: 125-9.
12. Kamran M, Peterson RG, Dominguez JH. Overexpression of GLUT2 gene in renal proximal tubules of diabetic Zucker rats. J Am Soc Nephrol 1997; 8: 943-8.
13. Thomson SC, Rieg T, Miracle C et al. Acute and chronic effects of SGLT2 blockade on glomerular and tubular function in the early diabetic rat. Am J Physiol Regul Integr Comp Physiol 2012; 302: R75-83.
14. Ferrannini E, Solini A. SGLT2 inhibition in diabetes mellitus: rationale and clinical prospects. Nat Rev Endocrinol 2012; 8: 495-502.
15. Hasan FM, Alsahli M, Gerich JE. SGLT2 inhibitors in the treatment of type 2 diabetes. Diabetes Res Clin Pract 2014. [Epub ahead of print].
16. Komoroski B, Vachharajani N, Feng Y, Li L, Kornhauser D, Pfister M. Dapagliflozin, a novel, selective SGLT2 inhibitor, improved glycemic control over 2 weeks in patients with type 2 diabetes mellitus. Clin Pharmacol Ther 2009; 85: 513-19.
17. 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. Drug Metab Dispos 2010; 38: 405-14.
18. List JF, Woo V, Morales E, Tang W, Fiedorek FT. Sodium-glucose cotransport inhibition with dapagliflozin in type 2 diabetes. Diabetes Care 2009; 32: 650-7.
19. Bristol Myers-Squibb; AstraZeneca. U.S. Food and Drug Administration Endocrinologic & Metabolic Advisory Committee Background Document: Dapagliflozin, BMS-512148, NDA 202293. Princeton, NJ: Bristol-Myers Squibb. Accessed at www.fda.gov/AdvisoryCommittees/CommitteesMeetingMaterials/Drugs/EndocrinologicandMetabolicDrugsAdvisoryCommittee/ucm262993.htm. 2011.
20. Ferrannini E, Ramos SJ, Salsali A, Tang W, List JF. Dapagliflozin monotherapy in type 2 diabetic patients with inadequate glycemic control by diet and exercise: a randomized, double-blind, placebo-controlled, phase 3 trial. Diabetes Care 2010; 33: 2217-24.
21. Ji L, Ma J, Li H et al. Dapagliflozin as monotherapy in drug-naive Asian patients with type 2 diabetes mellitus: a randomized, blinded, prospective phase III study. Clin Ther 2014; 36: 84-100.
22. Wilding JP, Norwood P, T'Joen C, Bastien A, List JF, Fiedorek FT. 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.
23. Wilding JP, Woo V, Soler NG et al. Long-term efficacy of dapagliflozin in patients with type 2 diabetes mellitus receiving high doses of insulin: a randomized trial. Ann Intern Med 2012; 156: 405-15.
24. Zhang L, Feng Y, List J, Kasichayanula S, Pfister M. Dapagliflozin treatment in patients with different stages of type 2 diabetes mellitus: effects on glycaemic control and body weight. Diabetes Obes Metab 2010; 12: 510-16.
25. Nauck MA, Del Prato S, Meier JJ et al. Dapagliflozin versus glipizide as add-on therapy in patients with type 2 diabetes who have inadequate glycemic control with metformin: a randomized, 52-week, double-blind, active-controlled noninferiority trial. Diabetes Care 2011; 34: 2015-22.
26. Baily CJ, Gross JI, Yadav M, Iqbal N, Mansfield TA, List JF. Dapagliflozin add-on to metformin in type 2 diabetes inadequately controlled with metformin: a randomized, double-blind, placebo-controlled 102-week trial. BMC Med 2013; 11: 43-52.
27. Del Prato S, Nauck M, Rohwedder K, Theuerkauf A, Langkilde AM, Parikh S. Long term efficacy and safety of add-on dapagliflozin vs add-on glipizide in patients with type 2 diabetes mellitus inadequately controlled with metformin: 2 year results. Diabetologia 2011; 54(Suppl 1): A852.
28. Sha S, Devineni D, Ghosh A et al. Canagliflozin, a novel inhibitor of sodium glucose co-transporter 2, dose dependently reduces calculated renal threshold for glucose excretion and increases urinary glucose excretion in healthy subjects. Diabetes Obes Metab 2011; 13: 669-72.
29. Inagaki N, Kondo K, Iwasaki T et al. Efficacy and safety of canagliflozin in Japanese patients with type 2 diabetes: a randomized, double-blind, placebo-controlled, 12-week study. Diab Obes Metab 2013; 15: 1136-45.
30. Stenlöf K, Cefalu WT, Kim KA et al. Long-term efficacy and safety of canagliflozin monotherapy in patients with type 2 diabetes inadequately controlled with diet and exercise: findings from the 52-week CANTATA-M study. Curr Med Res Opin 2014; 30: 163-75.
31. Rosenstock J, Aggarwal N, Polidori D et al. Dose-ranging effects of canagliflozin, a sodium-glucose cotransporter 2 inhibitor, as add-on to metformin in subjects with type 2 diabetes. Diabetes Care 2012; 35: 1232-8.
32. Lavalle-González FJ, Januszewicz A, Davidson J et al. Efficacy and safety of canagliflozin compared with placebo and sitagliptin in patients with type 2 diabetes on background metformin monotherapy: a randomised trial. Diabetologia 2013; 56: 2582-92.
33. Cefalu WT, Leiter LA, Yoon KH et al. Efficacy and safety of canagliflozin versus glimepiride in patients with type 2 diabetes inadequately controlled with metformin (CANTATA-SU): 52 week results from a randomised, double-blind, phase 3 non-inferiority trial. Lancet 2013; 382: 941-50.
34. Schernthaner G, Gross JL, Rosenstock J et al. Canagliflozin compared with sitagliptin for patients with type 2 diabetes who do not have adequate glycemic control with metformin plus sulfonylurea: a 52-week randomized trial. Diabetes Care 2013; 36: 2508-15.
35. Devineni D, Morrow L, Hompesch M et al. Canagliflozin improves glycaemic control over 28 days in subjects with type 2 diabetes not optimally controlled on insulin. Diabetes Obes Metab 2012; 14: 539-45.
36. Polidori D, Mari A, Ferrannini E. Canagliflozin, a sodium glucose co-transporter 2 inhibitor, improves model-based indices of beta cell function in patients with type 2 diabetes. Diabetologia 2014; 57: 891-901.
37. Grempler R, Thomas L, Eckhardt M et al. Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab 2012; 14: 83-90.
38. Koiwai K, Seman L, Yamamura N et al. Safety, tolerability, pharmacokinetics and pharmacodynamics of single doses of empagliflozin, a sodium-glucose co-transporter inhibitor (SGLT2). Japanese healthy volunteers. Drug Metab Pharmacokinet 2013; 28: 213-19.
39. Heise T, Seewaldt-Becker E, Macha S et al. Safety, tolerability, pharmacokinetics and pharmacodynamics following 4 weeks' treatment with empagliflozin once daily in patients with type 2 diabetes. Diabetes Obes Metab 2013; 15: 613-21.
40. Rosenstock J, Seman LJ, Jelaska A et al. Efficacy and safety of empagliflozin, a sodium glucose cotransporter 2 (SGLT2) inhibitor as add-on to metformin in type 2 diabetes with mild hyperglycemia. Diabetes Obes Metab 2013; 15: 1154-60.
41. Roden M, Weng J, Eilbracht J et al. Empagliflozin monotherapy with sitagliptin as an active comparator in patients with type 2 diabetes: a randomised, double-blind, placebo-controlled, phase 3 trial. Lancet Diabetes Endocrinol 2013; 1: 208-19.
42. Häring HU, Merker L, Seewaldt-Becker E et al. Empagliflozin as add-on to metformin in patients with type 2 diabetes: a 24-week, randomized, double-blind, placebo-controlled trial. Diabetes Care 2014; 37: 1650-9.
43. Häring HU, Merker L, Seewaldt-Becker E et al. Empagliflozin As Add-on to Metformin Plus Sulfonylurea in Patients With Type 2 Diabetes: A 24-week, randomized, double-blind, placebo-controlled trial. Diabetes Care 2013; 36: 3396-404.
44. Kovacs CS, Seshiah V, Swallow R et al. Empagliflozin improves glycaemic and weight control as add-on therapy to pioglitazone or pioglitazone plus metformin in patients with type 2 diabetes: a 24-week, randomized, placebo-controlled trial. Diabetes Obes Metab 2013; 16: 147-58. [Epub ahead of print].
45. Perkins BA, Cherney DZ, Partridge H et al. Sodium-glucose cotransporter 2 inhibition and glycemic control in type 1 diabetes: results of an 8-week open-label proof-of-concept trial. Diabetes Care 2014; 37: 1480-3.
46. Kohan DE, Fioretto P, Tang W, List JF. Long-term study of patients with type 2 diabetes and moderate renal impairment shows that dapagliflozin reduces weight and blood pressure but does not improve glycemic control. Kidney Int 2014; 85: 962-71.
47. Yale JF, Bakris G, Cariou B et al. Efficacy and safety of canagliflozin in subjects with type 2 diabetes and chronic kidney disease. Diabetes Obes Metab 2013; 15: 463-73.
48. 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.
49. DeFronzo RA, Hompesch M, Kasichayanula S et al. Characterization of renal glucose reabsorption in response to dapagliflozin in healthy subjects and subjects with type 2 diabetes. Diabetes Care 2013; 36: 3169-76.
50. Abdul-Ghani MA, DeFronzo RA, Norton L. Novel hypothesis to explain why SGLT2 inhibitors inhibit only 30-50% of filtered glucose load in humans. Diabetes 2013; 62: 3324-8.
51. Vallon V, Richter K, Blantz RC, Thomson S, Osswald H. Glomerular hyperfiltration in experimental diabetes mellitus: potential role of tubular reabsorption. J Am Soc Nephrol 1999; 10: 2569-76.
52. Thomson SC, Vallon V, Blantz RC. Kidney function in early diabetes: the tubular hypothesis of glomerular filtration. Am J Physiol Renal Physiol 2004; 286: F8-15.
53. 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.
54. Dominguez JH, Camp K, Maianu L, Feister H, Garvey WT. Molecular adaptations of GLUT1 and GLUT2 in renal proximal tubules of diabetic rats. Am J Physiol 1994; 266: F283-90.
55. 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.
56. Tuttle KR, Bruton JL, Perusek MC, Lancaster JL, Kopp DT, DeFronzo RA. 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.
57. 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.
58. Knapp S. Diabetes and infection: is there a link?-A mini-review. Gerontology 2013; 59: 99-104.
59. Parikh S, Johnsson K, Ptaszynska A, Schmitz B, Sugg J, List JF. Characterization of urinary tract infection in the setting of pharmacologically induced glucosuria. Diabetologia 2011; 54(Suppl): A841.
60. Nigro SC, Riche DM, Pheng M, Baker WL. Canagliflozin, a Novel SGLT2 Inhibitor for Treatment of Type 2 Diabetes. Ann Pharmacother 2013; 47: 1301-11.
61. Neal B, Perkovic V, de Zeeuw D et al. Rationale, design, and baseline characteristics of the Canagliflozin Cardiovascular Assessment Study (CANVAS)-a randomized placebo-controlled trial. Am Heart J 2013; 166: 217-223.
62. Ridderstråle M, Svaerd R, Zeller C et al. Rationale, design and baseline characteristics of a 4-year (208-week) phase III trial of empagliflozin, an SGLT2 inhibitor, versus glimepiride as add-on to metformin in patients with type 2 diabetes mellitus with insufficient glycemic control. Cardiovasc Diabetol 2013; 12: 129-138.