Ipragliflozin, a sodium-glucose cotransporter 2 inhibitor, in the treatment of type 2 diabetes

Expert Opinion on Drug Metabolism and Toxicology

Volumn 11, Issue 4, 2015, Pages 613-623

  Hedrington, Maka S ^a   Davis, Stephen N ^a  

^a UNIVERSITY OF MARYLAND SCHOOL OF MEDICINE   (United States)

Author keywords

Diabetes; Glucose; Ipragliflozin; Sodium glucose cotransporter 2 inhibitors

Indexed keywords

IPRAGLIFLOZIN; METFORMIN; PIOGLITAZONE; SULFONYLUREA; ANTIDIABETIC AGENT; GLUCOSIDE; GLYCOSYLATED HEMOGLOBIN; SODIUM GLUCOSE COTRANSPORTER 2; THIOPHENE DERIVATIVE;

AREA UNDER THE CURVE; ARTICLE; DRUG CLEARANCE; DRUG EFFICACY; DRUG LEGISLATION; DRUG METABOLISM; DRUG SAFETY; DRUG TOLERABILITY; ELIMINATION HALF-LIFE; GLUCOSE BLOOD LEVEL; GLUCOSE URINE LEVEL; GLUCOSURIA; HUMAN; HYPOGLYCEMIA; INSULIN SENSITIVITY; JAPAN; KIDNEY PROXIMAL TUBULE; MAXIMUM PLASMA CONCENTRATION; MONOTHERAPY; MULTICENTER STUDY (TOPIC); NON INSULIN DEPENDENT DIABETES MELLITUS; PHASE 2 CLINICAL TRIAL (TOPIC); PHASE 3 CLINICAL TRIAL (TOPIC); RANDOMIZED CONTROLLED TRIAL (TOPIC); TIME TO MAXIMUM PLASMA CONCENTRATION; WEIGHT REDUCTION; ANTAGONISTS AND INHIBITORS; CHEMICALLY INDUCED; DIABETES MELLITUS, TYPE 2; DRUG EFFECTS; DRUG INTERACTION; METABOLISM; PATHOPHYSIOLOGY;

DIABETES MELLITUS, TYPE 2; DRUG INTERACTIONS; GLUCOSIDES; HEMOGLOBIN A, GLYCOSYLATED; HUMANS; HYPOGLYCEMIA; HYPOGLYCEMIC AGENTS; SODIUM-GLUCOSE TRANSPORTER 2; THIOPHENES; WEIGHT LOSS;

EID: 84924799557     PISSN: 17425255     EISSN: 17447607     Source Type: Journal    
DOI: 10.1517/17425255.2015.1009893     Document Type: Article

References (53)

1. American Diabetes Association. Standards of medical care in diabetes - 2014. Diabetes Care 2014;37(Suppl 1):S14-80
2. Defronzo RA. From the triumvirate to the ominous octet: a new paradigm for the treatment of type 2 diabetes mellitus. Diabetes 2009;58(4):773-95
3. Bennett WL, Maruthur NM, Singh S, et al. Comparative effectiveness and safety of medications for type 2 diabetes: an update including new drugs and 2-drug combinations. Ann Intern Med 2011;154(9):602-13; Review. Erratum in: Ann Intern Med. 2011 Jul 5;155 (1):67-8
4. Cryer PE. Hypoglycaemia: the limiting factor in the glycaemic management of Type I and Type II diabetes. Diabetologia 2002;45(7):937-48
5. Zammitt NN, Frier BM. Hypoglycemia in type 2 diabetes: pathophysiology, frequency, and effects of different treatment modalities. Diabetes Care 2005;28(12):2948-61
6. Barendse S, Singh H, Frier BM, Speight J. The impact of hypoglycaemia on quality of life and related patientreported outcomes in Type 2 diabetes: a narrative review. Diabet Med 2012;29(3):293-302
7. Phillips P. Type 2 Diabetes - failure, blame and guilt in the adoption of insulin therapy. Rev Diabet Stud 2005;2(1):35-9
8. Pi-Sunyer FX. The obesity epidemic: pathophysiology and consequences of obesity. Obes Res 2002;10(Suppl 2):97S-104S
9. Bray GA. Medical consequences of obesity. J Clin Endocrinol Metab 2004;89(6):2583-9; Review
10. Wright EM, Hirayama BA, Loo DF. Active sugar transport in health and disease. J Intern Med 2007;261(1):32-43
11. Wright EM, Loo DD, Hirayama BA. Biology of human sodium glucose transporters. Physiol Rev 2011;91(2):733-94
12. 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
13. Bailey CJ. Renal glucose reabsorption inhibitors to treat diabetes. Trends Pharmacol Sci 2011;32(2):63-71
14. Rahmoune H, Thompson PW, Ward JM, et al. Glucose transporters in human renal proximal tubular cells isolated from the urine of patients with non-insulin-dependent diabetes. Diabetes 2005;54(12):3427-34
15. Mogensen CE. Maximum tubular reabsorption capacity for glucose and renal hemodynamcis during rapid hypertonic glucose infusion in normal and diabetic subjects. Scand J Clin Lab Invest 1971;28(1):101-9
16. Gerich JE. Role of the kidney in normal glucose homeostasis and in the hyperglycaemia of diabetes mellitus: therapeutic implications. Diabet Med 2010;27(2):136-42
17. Nauck MA. Update on developments with SGLT2 inhibitors in the management of type 2 diabetes. Drug Des Devel Ther 2014;8:1335-80
18. Jabbour SA, Goldstein BJ. Sodium glucose co-transporter 2 inhibitors: blocking renal tubular reabsorption of glucose to improve glycaemic control in patients with diabetes. Int J Clin Pract 2008;62(8):1279-84
19. Liu JJ, Lee T, DeFronzo RA. Why Do SGLT2 inhibitors inhibit only 30-50% of renal glucose reabsorption in humans?. Diabetes 2012;61(9):2199-204
20. U.S. Food and Drug Administration. FDA approves Farxiga to treat type 2 diabetes. January 2014. Available from: http://www.fda. gov/NewsEvents/Newsroom/PressAnnouncements/ucm380829.htm
21. Bristol-Myers Squibb. U.S. FDA Approves Farxiga- (Dapagliflozin) Tablets for the treatment of adult patients with type 2 diabetes. January 2014. Available from: http://news.bms. com/press-release/rd-news/us-fdaapproves-farxiga-dapagliflozin-tabletstreatment-Adult-patients-type-2
22. U.S. Food and Drug Administration. FDA approves Invokana to treat type 2 diabetes. March 2013. Available from: http://www.fda. gov/NewsEvents/Newsroom/PressAnnouncements/ucm345848.htm
23. U.S. Food and Drug Administration. FDA approves Jardiance to treat type 2 diabetes. August 2014. Available from: http://www.fda. gov/newsevents/newsroom/pressannouncements/ucm407637.htm
24. Tahara A, Kurosaki E, Yokono M, et al. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol 2012;385(4):423-36
25. Veltkamp SA, Kadokura T, Krauwinkel WJ, Smulders RA. Effect of Ipragliflozin (ASP1941), a novel selective sodium-dependent glucose co-transporter 2 inhibitor, on urinary glucose excretion in healthy subjects. Clin Drug Investig 2011;31(12):839-51
26. Kadokura T, Akiyama N, Kashiwagi A, et al. Pharmacokinetic and pharmacodynamic study of ipragliflozin in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, placebo-controlled study. Diabetes Res Clin Pract 2014;106(1):50-6
27. Imamura M, Nakanishi K, Suzuki T, et al. Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. Bioorg Med Chem 2012;20(10):3263-79
28. Zhang W, Krauwinkel WJ, Keirns J, et al. The effect of moderate hepatic impairment on the pharmacokinetics of ipragliflozin, a novel sodium glucose co-transporter 2 (SGLT2) inhibitor. Clin Drug Investig 2013;33(7):489-96
29. Kadokura T, Saito M, Utsuno A, et al. Ipragliflozin (ASP1941), a selective sodium-dependent glucose cotransporter 2 inhibitor, safely stimulates urinary glucose excretion without inducing hypoglycemia in healthy Japanese subjects. Diabetol Int 2011;2:172-82
30. Schwartz SL, Akinlade B, Klasen S, et al. Safety, pharmacokinetic, and pharmacodynamic profiles of ipragliflozin (ASP1941), a novel and selective inhibitor of sodium-dependent glucose co-transporter 2, in patients with type 2 diabetes mellitus. Diabetes Technol Ther 2011;13(12):1219-27
31. Smulders RA, Zhang W, Veltkamp SA, et al. No pharmacokinetic interaction between ipragliflozin and sitagliptin, pioglitazone, or glimepiride in healthy subjects. Diabetes Obes Metab 2012;14(10):937-43
32. Scheen AJ. Drug-drug interactions with sodium-glucose cotransporters type 2 (SGLT2) inhibitors, new oral glucoselowering agents for the management of type 2 diabetes mellitus. Clin Pharmacokinet 2014;53(4):295-304; Review
33. Fonseca VA, Ferrannini E, Wilding JP, et al. Active- and placebo-controlled dose-finding study to assess the efficacy, safety, and tolerability of multiple doses of ipragliflozin in patients with type 2 diabetes mellitus. J Diabetes Complications 2013;27(3):268-73
34. Kashiwagi A, Kazuta K, Takinami Y, et al. Ipragliflozin improves glycemic control in Japanese patients with type 2 diabetes mellitus: the BRIGHTEN study. Diabetol Int 2014;5:2190-1678
35. Kashiwagi A, Kazuta K, Yoshida S, Nagase I. Randomized, placebocontrolled, double-blind glycemic control trial of novel sodium-dependent glucose cotransporter 2 inhibitor ipragliflozin in Japanese patients with type 2 diabetes mellitus. J Diabetes Investig 2014;5:382-91
36. Kashiwagi A, Takahashi H, Ishikawa H, et al. A randomized, double blind, placebo-controlled study on long-term efficacy and safety of ipragliflozin treatment in patients with type 2 diabetes mellitus and renal impairment: results of the LANTERN study (Long-term ASP1941 Safety Evaluation in T2DM Patients with Renal Impairment. Diabetes Obes Metab 2015;17(2):152-60
37. Kadokura T, Ishikawa H, Nakajo I, et al. The effect of renal impairment on the pharmacokinetics and urinary glucose excretion of the SGLT2 inhibitor ipragliflozin (ASP1941) in Japanese type 2 diabetes mellitus patients. Diabetologia 2011;54:S847
38. Kashiwagi A, Shiga T, Akiyama N, et al. Efficacy and safety of ipragliflozin as an add-on to pioglitazone in Japanese patients with inadequately controlled type 2 diabetes: a randomized, doubleblind, placebo-controlled study (the SPOTLIGHT study). Diabetol Int 2014;5:2190-1686
39. Kashiwagi A, Kazuta K, Goto K, et al. Ipragliflozin in combination with metformin for the treatment of Japanese patients with type 2 diabetes: ILLUMINATE, a randomized, doubleblind, placebo-controlled study. Diabetes Obes Metab 2014. doi: 10.1111/dom.12331
40. Wilding JP, Ferrannini E, Fonseca VA, et al. Efficacy and safety of ipragliflozin in patients with type 2 diabetes inadequately controlled on metformin: a dose-finding study. Diabetes Obes Metab 2013;15(5):403-9
41. Kashiwagi A, Akiyama N, Shiga T, et al. Efficacy and safety of ipragliflozin as an add-on to a sulfonylurea in Japanese patients with inadequately controlled type 2 diabetes: results of the randomized, placebo-controlled, doubleblind, phase III EMIT study. Diabetol Int 2014;5:2190-1678
42. Zhang W, Smulders R, Abeyratne A, et al. Ipragliflozin does not prolong QTc interval in healthy male and female subjects: a phase I study. Clin Ther 2013;35(8):1150-1161.e3
43. Astellas Pharma. Research and development pipeline. November 2012. Available from: www.astellas.com/en/ir/library/pdf/2q2013-rdén.pdf [Last accessed 12 November 2014]
44. Approval of Suglat- tablets, a selective SGLT2 inhibitor for treatment of type 2 diabetes, in Japan. Astellas Pharma, Tokyo Japan: 2014 news releases, 17 January 2014. Available from: www.astellas.com/en/corporate/news/detail/approval-of-suglat-tablets-A-s. html [Last accessed 12 November 2014]
45. Scheen AJ. Pharmacodynamics, efficacy and safety of sodium-glucose cotransporter type 2 (SGLT2) inhibitors for the treatment of type 2 diabetes mellitus. Drugs 2015;75(1):33-59
46. Poole RM, Dungo RT. Ipragliflozin: first global approval. Drugs 2014;74(5):611-17
47. Nyirjesy P, Zhao Y, Ways K, Usiskin K. Evaluation of vulvovaginal symptoms and Candida colonization in women with type 2 diabetes mellitus treated with canagliflozin, a sodium glucose cotransporter 2 inhibitor. Curr Med Res Opin 2012;28(7):1173-8
48. Bailey CJ, Gross JL, Pieters A, et al. Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with metformin: a randomised, double-blind, placebocontrolled trial. Lancet 2010;375(9733):2223-33
49. Rosenstock J, Aggarwal N, Polidori D, et al. Canagliflozin DIA 2001 Study Group. 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(6):1232-8
50. Scheen AJ. Evaluating SGLT2 inhibitors for type 2 diabetes: pharmacokinetic and toxicological considerations. Expert Opin Drug Metab Toxicol 2014;10(5):647-63
51. Stenlöf K, Cefalu WT, Kim KA, et al. Efficacy and safety of canagliflozin monotherapy in subjects with type 2 diabetes mellitus inadequately controlled with diet and exercise. Diabetes Obes Metab 2013;15(4):372-82
52. Kadowaki T, Haneda M, Inagaki N, et al. Empagliflozin monotherapy in Japanese patients with type 2 diabetes mellitus: a randomized, 12-week, doubleblind, placebo-controlled, phase II trial. Adv Ther 2014;31(6):621-38
53. Bailey CJ, Morales Villegas EC, Woo V, et al. Efficacy and safety of dapagliflozin monotherapy in people with Type 2 diabetes: a randomized doubleblind placebo-controlled 102-week trial. Diabet Med 2014. [Epub ahead of print]