Pharmacotherapy of type 2 diabetes: An update

Metabolism: Clinical and Experimental

Volumn 78, Issue , 2018, Pages 13-42

  Upadhyay, Jagriti ^a,b   Polyzos, Stergios A ^c   Perakakis, Nikolaos ^b,d   Thakkar, Bindiya ^a   Paschou, Stavroula A ^b   Katsiki, Niki ^e   Underwood, Patricia ^a   Park, Kyung Hee ^f   Seufert, Jochen ^d   Kang, Eun Seok ^g   Sternthal, Elliot ^a   Karagiannis, Asterios ^c   Mantzoros, Christos S ^a,b  

^a VETERANS AFFAIRS MEDICAL CENTER   (United States)

^b HARVARD MEDICAL SCHOOL   (United States)

^c ARISTOTLE UNIVERSITY OF THESSALONIKI   (Greece)

^d UNIVERSITY OF FREIBURG   (Germany)

^e ARISTOTLE UNIVERSITY MEDICAL SCHOOL   (Greece)

^f Hallym University   (South Korea)

^g Yonsei University College of Medicine   (South Korea)

Author keywords

Algorithm; Goals pharmacotherapy; Personalized therapy; Type 2 diabetes

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; ALPHA GLUCOSIDASE INHIBITOR; AMYLIN DERIVATIVE; ANTIDIABETIC AGENT; BIGUANIDE DERIVATIVE; BROMOCRIPTINE; DIPEPTIDYL PEPTIDASE IV INHIBITOR; GLUCAGON LIKE PEPTIDE 1 RECEPTOR AGONIST; INCRETIN; INSULIN DEGLUDEC; INSULIN DERIVATIVE; LIRAGLUTIDE; MEGLITINIDE; MITIGLINIDE; NATEGLINIDE; PROTEIN TYROSINE PHOSPHATASE; RANOLAZINE; REPAGLINIDE; SALSALATE; SODIUM GLUCOSE COTRANSPORTER 2 INHIBITOR; SULFONYLUREA DERIVATIVE;

ADVERSE EVENT; DIABETIC PATIENT; DRUG DOSE REGIMEN; DRUG EFFICACY; DRUG MECHANISM; DRUG SAFETY; DRUG THERAPY; GLYCEMIC CONTROL; HEALTH CARE COST; HUMAN; NON INSULIN DEPENDENT DIABETES MELLITUS; OUTCOME ASSESSMENT; PHARMACODYNAMICS; PRIORITY JOURNAL; REVIEW; ANIMAL; DRUG EFFECTS; GLUCOSE BLOOD LEVEL;

ANIMALS; BLOOD GLUCOSE; DIABETES MELLITUS, TYPE 2; HUMANS; HYPOGLYCEMIC AGENTS;

EID: 85039561524     PISSN: 00260495     EISSN: 15328600     Source Type: Journal    
DOI: 10.1016/j.metabol.2017.08.010     Document Type: Review

References (358)

1. Cho, N.H., Q&A: five questions on the 2015 IDF Diabetes Atlas. Diabetes Res Clin Pract 115 (2016), 157–159 [Epub 2016/06/01].
2. Economic costs of diabetes in the U.S. in 2012. Diabetes Care, 36(4), 2013, 1033–1046 [Epub 2013/03/08].
3. Guillausseau, P.J., Meas, T., Virally, M., Laloi-Michelin, M., Medeau, V., Kevorkian, J.P., Abnormalities in insulin secretion in type 2 diabetes mellitus. Diabete Metab 34:Suppl. 2 (2008), S43–8 [Epub 2008/07/22].
4. U.K. prospective diabetes study 16. Overview of 6 years' therapy of type II diabetes: a progressive disease. U.K. Prospective Diabetes Study Group. Diabetes, 44(11), 1995, 1249–1258 [Epub 1995/11/01].
5. Wild, S., Roglic, G., Green, A., Sicree, R., King, H., Global prevalence of diabetes: estimates for the year 2000 and projections for 2030. Diabetes Care 27:5 (2004), 1047–1053 [Epub 2004/04/28].
6. Zimmet, P., Alberti, K.G., Magliano, D.J., Bennett, P.H., Diabetes mellitus statistics on prevalence and mortality: facts and fallacies. Nat Rev Endocrinol 12:10 (2016), 616–622 [Epub 2016/07/09].
7. The effect of intensive treatment of diabetes on the development and progression of long-term complications in insulin-dependent diabetes mellitus. The Diabetes Control and Complications Trial Research Groups. N Engl J Med, 329(14), 1993, 977–986 [Epub 1993/09/30].
8. Ohkubo, Y., Kishikawa, H., Araki, E., Miyata, T., Isami, S., Motoyoshi, S., 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 28:2 (1995), 103–117 [Epub 1995/05/01].
9. Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complications in patients with type 2 diabetes (UKPDS 33). UK Prospective Diabetes Study (UKPDS) Group. Lancet, 352(9131), 1998, 837–853 [Epub 1998/09/22].
10. Stratton, I.M., Adler, A.I., Neil, H.A., Matthews, D.R., Manley, S.E., Cull, C.A., et al. Association of glycaemia with macrovascular and microvascular complications of type 2 diabetes (UKPDS 35): prospective observational study. BMJ 321:7258 (2000), 405–412 [Epub 2000/08/11].
11. Gerstein, H.C., Miller, M.E., Byington, R.P., Goff, D.C. Jr., Bigger, J.T., Buse, J.B., et al. Effects of intensive glucose lowering in type 2 diabetes. N Engl J Med 358:24 (2008), 2545–2559 [Epub 2008/06/10].
12. Patel, A., MacMahon, S., Chalmers, J., Neal, B., Billot, L., Woodward, M., et al. Intensive blood glucose control and vascular outcomes in patients with type 2 diabetes. N Engl J Med 358:24 (2008), 2560–2572 [Epub 2008/06/10].
13. Inzucchi, S.E., Bergenstal, R.M., Buse, J.B., Diamant, M., Ferrannini, E., Nauck, M., et al. Management of hyperglycemia in type 2 diabetes, 2015: a patient-centered approach: update to a position statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care 38:1 (2015), 140–149 [Epub 2014/12/30].
14. Garvey, W.T., Mechanick, J.I., Brett, E.M., Garber, A.J., Hurley, D.L., Jastreboff, A.M., et al. American Association of Clinical Endocrinologists and American College of Endocrinology comprehensive clinical practice guidelines for medical care of patients with obesity. Endocr Pract 22:Suppl. 3 (2016), 1–203 [Epub 2016/05/25].
15. Bailey, C.J., Biguanides and NIDDM. Diabetes Care 15:6 (1992), 755–772 [Epub 1992/06/01].
16. Goodarzi, M.O., Bryer-Ash, M., Metformin revisited: re-evaluation of its properties and role in the pharmacopoeia of modern antidiabetic agents. Diabetes Obes Metab 7:6 (2005), 654–665 [Epub 2005/10/13].
17. Bailey, C.J., Turner, R.C., Metformin. N Engl J Med 334:9 (1996), 574–579 [Epub 1996/02/29].
18. Mannucci, E., Ognibene, A., Cremasco, F., Bardini, G., Mencucci, A., Pierazzuoli, E., et al. Effect of metformin on glucagon-like peptide 1 (GLP-1) and leptin levels in obese nondiabetic subjects. Diabetes Care 24:3 (2001), 489–494 [Epub 2001/04/06].
19. Lindsay, J.R., Duffy, N.A., McKillop, A.M., Ardill, J., O'Harte, F.P., Flatt, P.R., et al. Inhibition of dipeptidyl peptidase IV activity by oral metformin in type 2 diabetes. Diabet Med 22:5 (2005), 654–657 [Epub 2005/04/22].
20. Cuthbertson, J., Patterson, S., O'Harte, F.P., Bell, P.M., Investigation of the effect of oral metformin on dipeptidylpeptidase-4 (DPP-4) activity in type 2 diabetes. Diabet Med 26:6 (2009), 649–654 [Epub 2009/06/23].
21. Buse, J.B., DeFronzo, R.A., Rosenstock, J., Kim, T., Burns, C., Skare, S., et al. The primary glucose-lowering effect of metformin resides in the gut, not the circulation: results from short-term pharmacokinetic and 12-week dose-ranging studies. Diabetes Care 39:2 (2016), 198–205 [Epub 2015/08/20].
22. Ceriello, A., Johns, D., Widel, M., Eckland, D.J., Gilmore, K.J., Tan, M.H., Comparison of effect of pioglitazone with metformin or sulfonylurea (monotherapy and combination therapy) on postload glycemia and composite insulin sensitivity index during an oral glucose tolerance test in patients with type 2 diabetes. Diabetes Care 28:2 (2005), 266–272 [Epub 2005/01/29].
23. Kahn, S.E., Haffner, S.M., Heise, M.A., Herman, W.H., Holman, R.R., Jones, N.P., et al. Glycemic durability of rosiglitazone, metformin, or glyburide monotherapy. N Engl J Med 355:23 (2006), 2427–2443 [Epub 2006/12/06].
24. Dornan, T.L., Heller, S.R., Peck, G.M., Tattersall, R.B., Double-blind evaluation of efficacy and tolerability of metformin in NIDDM. Diabetes Care 14:4 (1991), 342–344 [Epub 1991/04/01].
25. Standl, E., Schnell, O., McGuire, D.K., Heart failure considerations of antihyperglycemic medications for type 2 diabetes. Circ Res 118:11 (2016), 1830–1843 [Epub 2016/05/28].
26. Eurich, D.T., Weir, D.L., Majumdar, S.R., Tsuyuki, R.T., Johnson, J.A., Tjosvold, L., et al. Comparative safety and effectiveness of metformin in patients with diabetes mellitus and heart failure: systematic review of observational studies involving 34,000 patients. Circ Heart Fail 6:3 (2013), 395–402 [Epub 2013/03/20].
27. Nathan, D.M., Buse, J.B., Davidson, M.B., Ferrannini, E., Holman, R.R., Sherwin, R., et al. Medical management of hyperglycemia in type 2 diabetes: a consensus algorithm for the initiation and adjustment of therapy: a consensus statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care 32:1 (2009), 193–203 [Epub 2008/10/24].
28. Knowler, W.C., Barrett-Connor, E., Fowler, S.E., Hamman, R.F., Lachin, J.M., Walker, E.A., et al. Reduction in the incidence of type 2 diabetes with lifestyle intervention or metformin. N Engl J Med 346:6 (2002), 393–403 [Epub 2002/02/08].
29. Effect of intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). UK Prospective Diabetes Study (UKPDS) Group. Lancet, 352(9131), 1998, 854–865 [Epub 1998/09/22].
30. Kooy, A., de Jager, J., Lehert, P., Bets, D., Wulffele, M.G., Donker, A.J., et al. Long-term effects of metformin on metabolism and microvascular and macrovascular disease in patients with type 2 diabetes mellitus. Arch Intern Med 169:6 (2009), 616–625 [Epub 2009/03/25].
31. Evans, J.M., Donnelly, L.A., Emslie-Smith, A.M., Alessi, D.R., Morris, A.D., Metformin and reduced risk of cancer in diabetic patients. BMJ 330:7503 (2005), 1304–1305 [Epub 2005/04/26].
32. Bowker, S.L., Majumdar, S.R., Veugelers, P., Johnson, J.A., Increased cancer-related mortality for patients with type 2 diabetes who use sulfonylureas or insulin. Diabetes Care 29:2 (2006), 254–258 [Epub 2006/01/31].
33. Thakkar, B., Aronis, K.N., Vamvini, M.T., Shields, K., Mantzoros, C.S., Metformin and sulfonylureas in relation to cancer risk in type II diabetes patients: a meta-analysis using primary data of published studies. Metabolism 62:7 (2013), 922–934 [Epub 2013/02/20].
34. Zakikhani, M., Dowling, R., Fantus, I.G., Sonenberg, N., Pollak, M., Metformin is an AMP kinase-dependent growth inhibitor for breast cancer cells. Cancer Res 66:21 (2006), 10269–10273 [Epub 2006/10/26].
35. Proks, P., Reimann, F., Green, N., Gribble, F., Ashcroft, F., Sulfonylurea stimulation of insulin secretion. Diabetes 51:Suppl. 3 (2002), S368–76 [Epub 2002/12/12].
36. Ashcroft, F.M., Rorsman, P., Electrophysiology of the pancreatic beta-cell. Prog Biophys Mol Biol 54:2 (1989), 87–143 [Epub 1989/01/01].
37. Bryan, J., Crane, A., Vila-Carriles, W.H., Babenko, A.P., Aguilar-Bryan, L., Insulin secretagogues, sulfonylurea receptors and K(ATP) channels. Curr Pharm Des 11:21 (2005), 2699–2716 [Epub 2005/08/17].
38. Shorr, R.I., Ray, W.A., Daugherty, J.R., Griffin, M.R., Individual sulfonylureas and serious hypoglycemia in older people. J Am Geriatr Soc 44:7 (1996), 751–755 [Epub 1996/07/01].
39. Gangji, A.S., Cukierman, T., Gerstein, H.C., Goldsmith, C.H., Clase, C.M., A systematic review and meta-analysis of hypoglycemia and cardiovascular events: a comparison of glyburide with other secretagogues and with insulin. Diabetes Care 30:2 (2007), 389–394 [Epub 2007/01/30].
40. Holstein, A., Plaschke, A., Egberts, E.H., Lower incidence of severe hypoglycaemia in patients with type 2 diabetes treated with glimepiride versus glibenclamide. Diabetes Metab Res Rev 17:6 (2001), 467–473 [Epub 2002/01/05].
41. Inzucchi, S.E., Bergenstal, R.M., Buse, J.B., Diamant, M., Ferrannini, E., Nauck, M., et al. Management of hyperglycaemia in type 2 diabetes: a patient-centered approach. Position statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD). Diabetologia 55:6 (2012), 1577–1596 [Epub 2012/04/25].
42. DeFronzo, R.A., Goodman, A.M., Efficacy of metformin in patients with non-insulin-dependent diabetes mellitus. The Multicenter Metformin Study Group. N Engl J Med 333:9 (1995), 541–549 [Epub 1995/08/31].
43. Sherifali, D., Nerenberg, K., Pullenayegum, E., Cheng, J.E., Gerstein, H.C., The effect of oral antidiabetic agents on A1C levels: a systematic review and meta-analysis. Diabetes Care 33:8 (2010), 1859–1864 [Epub 2010/05/21].
44. Gerstein, H.C., Yusuf, S., Bosch, J., Pogue, J., Sheridan, P., Dinccag, N., et al. Effect of rosiglitazone on the frequency of diabetes in patients with impaired glucose tolerance or impaired fasting glucose: a randomised controlled trial. Lancet 368:9541 (2006), 1096–1105 [Epub 2006/09/26].
45. Basit, A., Riaz, M., Fawwad, A., Glimepiride: evidence-based facts, trends, and observations (GIFTS). [corrected]. Vasc Health Risk Manag 8 (2012), 463–472 [Epub 2012/10/03].
46. Klarenbach, S., Cameron, C., Singh, S., Ur, E., Cost-effectiveness of second-line antihyperglycemic therapy in patients with type 2 diabetes mellitus inadequately controlled on metformin. CMAJ 183:16 (2011), E1213–20 Epub 2011/10/05.
47. Jiang, Y.F., Chen, X.Y., Ding, T., Wang, X.F., Zhu, Z.N., Su, S.W., Comparative efficacy and safety of OADs in management of GDM: network meta-analysis of randomized controlled trials. J Clin Endocrinol Metab 100:5 (2015), 2071–2080 [Epub 2015/03/25].
48. Ye, Y., Perez-Polo, J.R., Aguilar, D., Birnbaum, Y., The potential effects of anti-diabetic medications on myocardial ischemia-reperfusion injury. Basic Res Cardiol 106:6 (2011), 925–952 [Epub 2011/09/06].
49. Mocanu, M.M., Maddock, H.L., Baxter, G.F., Lawrence, C.L., Standen, N.B., Yellon, D.M., Glimepiride, a novel sulfonylurea, does not abolish myocardial protection afforded by either ischemic preconditioning or diazoxide. Circulation 103:25 (2001), 3111–3116 [Epub 2001/06/27].
50. Lee, T.M., Chou, T.F., Impairment of myocardial protection in type 2 diabetic patients. J Clin Endocrinol Metab 88:2 (2003), 531–537 [Epub 2003/02/08].
51. Flynn, D.M., Smith, A.H., Treadway, J.L., Levy, C.B., Soeller, W.C., Boettner, W.A., et al. The sulfonylurea glipizide does not inhibit ischemic preconditioning in anesthetized rabbits. Cardiovasc Drugs Ther 19:5 (2005), 337–346 [Epub 2005/12/31].
52. Buse, J.B., Tan, M.H., Prince, M.J., Erickson, P.P., The effects of oral anti-hyperglycaemic medications on serum lipid profiles in patients with type 2 diabetes. Diabetes Obes Metab 6:2 (2004), 133–156 [Epub 2004/01/30].
53. Charbonnel, B.H., Matthews, D.R., Schernthaner, G., Hanefeld, M., Brunetti, P., A long-term comparison of pioglitazone and gliclazide in patients with type 2 diabetes mellitus: a randomized, double-blind, parallel-group comparison trial. Diabet Med 22:4 (2005), 399–405 [Epub 2005/03/25].
54. Bennett, W.L., Maruthur, N.M., Singh, S., Segal, J.B., Wilson, L.M., Chatterjee, R., et al. Comparative effectiveness and safety of medications for type 2 diabetes: an update including new drugs and 2-drug combinations. Ann Intern Med 154:9 (2011), 602–613 [Epub 2011/03/16].
55. Belcher, G., Lambert, C., Goh, K.L., Edwards, G., Valbuena, M., Cardiovascular effects of treatment of type 2 diabetes with pioglitazone, metformin and gliclazide. Int J Clin Pract 58:9 (2004), 833–837 [Epub 2004/11/09].
56. St John Sutton, M., Rendell, M., Dandona, P., Dole, J.F., Murphy, K., Patwardhan, R., et al. A comparison of the effects of rosiglitazone and glyburide on cardiovascular function and glycemic control in patients with type 2 diabetes. Diabetes Care 25:11 (2002), 2058–2064 [Epub 2002/10/29].
57. Meinert, C.L., Knatterud, G.L., Prout, T.E., Klimt, C.R., A study of the effects of hypoglycemic agents on vascular complications in patients with adult-onset diabetes. II. Mortality results. Diabetes 19 (1970), 789–830 [Suppl, Epub 1970/01/01].
58. Seltzer, H.S., A summary of criticisms of the findings and conclusions of the University Group Diabetes Program (UGDP). Diabetes 21:9 (1972), 976–979 [Epub 1972/09/01].
59. Duckworth, W., Abraira, C., Moritz, T., Reda, D., Emanuele, N., Reaven, P.D., et al. Glucose control and vascular complications in veterans with type 2 diabetes. N Engl J Med 360:2 (2009), 129–139 [Epub 2008/12/19].
60. Home, P.D., Pocock, S.J., Beck-Nielsen, H., Gomis, R., Hanefeld, M., Jones, N.P., et al. Rosiglitazone evaluated for cardiovascular outcomes—an interim analysis. N Engl J Med 357:1 (2007), 28–38 [Epub 2007/06/07].
61. Fuhlendorff, J., Rorsman, P., Kofod, H., Brand, C.L., Rolin, B., MacKay, P., et al. Stimulation of insulin release by repaglinide and glibenclamide involves both common and distinct processes. Diabetes 47:3 (1998), 345–351 [Epub 1998/03/31].
62. Hu, S., Wang, S., Fanelli, B., Bell, P.A., Dunning, B.E., Geisse, S., et al. Pancreatic beta-cell K(ATP) channel activity and membrane-binding studies with nateglinide: a comparison with sulfonylureas and repaglinide. J Pharmacol Exp Ther 293:2 (2000), 444–452 [Epub 2000/04/25].
63. McKillop, A.M., Duffy, N.A., Lindsay, J.R., Green, B.D., Patterson, S., O'Harte, F.P., et al. Insulinotropic actions of nateglinide in type 2 diabetic patients and effects on dipeptidyl peptidase-IV activity and glucose-dependent insulinotropic polypeptide degradation. Eur J Endocrinol 161:6 (2009), 877–885 [Epub 2009/09/17].
64. Stephens, J.W., Bodvarsdottir, T.B., Wareham, K., Prior, S.L., Bracken, R.M., Lowe, G.D., et al. Effects of short-term therapy with glibenclamide and repaglinide on incretin hormones and oxidative damage associated with postprandial hyperglycaemia in people with type 2 diabetes mellitus. Diabetes Res Clin Pract 94:2 (2011), 199–206 [Epub 2011/08/13].
65. Damsbo, P., Clauson, P., Marbury, T.C., Windfeld, K., A double-blind randomized comparison of meal-related glycemic control by repaglinide and glyburide in well-controlled type 2 diabetic patients. Diabetes Care 22:5 (1999), 789–794 [Epub 1999/05/20].
66. Gerich, J., Raskin, P., Jean-Louis, L., Purkayastha, D., Baron, M.A., PRESERVE-beta: two-year efficacy and safety of initial combination therapy with nateglinide or glyburide plus metformin. Diabetes Care 28:9 (2005), 2093–2099 [Epub 2005/08/27].
67. Nathan, D.M., Buse, J.B., Davidson, M.B., Heine, R.J., Holman, R.R., Sherwin, R., et al. Management of hyperglycemia in type 2 diabetes: a consensus algorithm for the initiation and adjustment of therapy: a consensus statement from the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care 29:8 (2006), 1963–1972 [Epub 2006/07/29].
68. Raskin, P., Klaff, L., McGill, J., South, S.A., Hollander, P., Khutoryansky, N., et al. Efficacy and safety of combination therapy: repaglinide plus metformin versus nateglinide plus metformin. Diabetes Care 26:7 (2003), 2063–2068 [Epub 2003/07/02].
69. Goldberg, R.B., Einhorn, D., Lucas, C.P., Rendell, M.S., Damsbo, P., Huang, W.C., et al. A randomized placebo-controlled trial of repaglinide in the treatment of type 2 diabetes. Diabetes Care 21:11 (1998), 1897–1903 [Epub 1998/11/05].
70. Moses, R., Slobodniuk, R., Boyages, S., Colagiuri, S., Kidson, W., Carter, J., et al. Effect of repaglinide addition to metformin monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 22:1 (1999), 119–124 [Epub 1999/05/20].
71. Schramm, T.K., Gislason, G.H., Vaag, A., Rasmussen, J.N., Folke, F., Hansen, M.L., et al. Mortality and cardiovascular risk associated with different insulin secretagogues compared with metformin in type 2 diabetes, with or without a previous myocardial infarction: a nationwide study. Eur Heart J 32:15 (2011), 1900–1908 [Epub 2011/04/08].
72. Ceriello, A., Davidson, J., Hanefeld, M., Leiter, L., Monnier, L., Owens, D., et al. Postprandial hyperglycaemia and cardiovascular complications of diabetes: an update. Nutr Metab Cardiovasc Dis 16:7 (2006), 453–456 [Epub 2006/08/29].
73. Esposito, K., Giugliano, D., Nappo, F., Marfella, R., Regression of carotid atherosclerosis by control of postprandial hyperglycemia in type 2 diabetes mellitus. Circulation 110:2 (2004), 214–219 [Epub 2004/06/16].
74. Inzucchi, S.E., Oral antihyperglycemic therapy for type 2 diabetes: scientific review. JAMA 287:3 (2002), 360–372 [Epub 2002/01/16].
75. Holman, R.R., Haffner, S.M., McMurray, J.J., Bethel, M.A., Holzhauer, B., Hua, T.A., et al. Effect of nateglinide on the incidence of diabetes and cardiovascular events. N Engl J Med 362:16 (2010), 1463–1476 [Epub 2010/03/17].
76. Desai, N.R., Shrank, W.H., Fischer, M.A., Avorn, J., Liberman, J.N., Schneeweiss, S., et al. Patterns of medication initiation in newly diagnosed diabetes mellitus: quality and cost implications. Am J Med 125:3 (2012), 302–307.e1 [Epub 2012/02/22].
77. Abdelmoneim, A.S., Hasenbank, S.E., Seubert, J.M., Brocks, D.R., Light, P.E., Simpson, S.H., Variations in tissue selectivity amongst insulin secretagogues: a systematic review. Diabetes Obes Metab 14:2 (2012), 130–138 [Epub 2011/09/20].
78. Hanefeld, M., Cagatay, M., Petrowitsch, T., Neuser, D., Petzinna, D., Rupp, M., Acarbose reduces the risk for myocardial infarction in type 2 diabetic patients: meta-analysis of seven long-term studies. Eur Heart J 25:1 (2004), 10–16 [Epub 2003/12/20].
79. Yamagishi, S., Matsui, T., Ueda, S., Fukami, K., Okuda, S., Clinical utility of acarbose, an alpha-glucosidase inhibitor in cardiometabolic disorders. Curr Drug Metab 10:2 (2009), 159–163 [Epub 2009/03/12].
80. van de Laar, F.A., Lucassen, P.L., Akkermans, R.P., van de Lisdonk, E.H., Rutten, G.E., van Weel, C., Alpha-glucosidase inhibitors for patients with type 2 diabetes: results from a Cochrane systematic review and meta-analysis. Diabetes Care 28:1 (2005), 154–163 [Epub 2004/12/24].
81. Chiasson, J.L., Josse, R.G., Gomis, R., Hanefeld, M., Karasik, A., Laakso, M., Acarbose treatment and the risk of cardiovascular disease and hypertension in patients with impaired glucose tolerance: the STOP-NIDDM trial. JAMA 290:4 (2003), 486–494 [Epub 2003/07/24].
82. Hanefeld, M., Chiasson, J.L., Koehler, C., Henkel, E., Schaper, F., Temelkova-Kurktschiev, T., Acarbose slows progression of intima-media thickness of the carotid arteries in subjects with impaired glucose tolerance. Stroke 35:5 (2004), 1073–1078 [Epub 2004/04/10].
83. Cavalot, F., Petrelli, A., Traversa, M., Bonomo, K., Fiora, E., Conti, M., et al. Postprandial blood glucose is a stronger predictor of cardiovascular events than fasting blood glucose in type 2 diabetes mellitus, particularly in women: lessons from the San Luigi Gonzaga Diabetes Study. J Clin Endocrinol Metab 91:3 (2006), 813–819 [Epub 2005/12/15].
84. Shimabukuro, M., Tanaka, A., Sata, M., Dai, K., Shibata, Y., Inoue, Y., et al. alpha-Glucosidase inhibitor miglitol attenuates glucose fluctuation, heart rate variability and sympathetic activity in patients with type 2 diabetes and acute coronary syndrome: a multicenter randomized controlled (MACS) study. Cardiovasc Diabetol, 16(1), 2017, 86 [Epub 2017/07/08].
85. Dabhi, A.S., Bhatt, N.R., Shah, M.J., Voglibose: an alpha glucosidase inhibitor. J Clin Diagn Res 7:12 (2013), 3023–3027 [Epub 2014/02/20].
86. Vichayanrat, A., Ploybutr, S., Tunlakit, M., Watanakejorn, P., Efficacy and safety of voglibose in comparison with acarbose in type 2 diabetic patients. Diabetes Res Clin Pract 55:2 (2002), 99–103 [Epub 2002/02/14].
87. Sugihara, H., Nagao, M., Harada, T., Nakajima, Y., Tanimura-Inagaki, K., Okajima, F., et al. Comparison of three alpha-glucosidase inhibitors for glycemic control and bodyweight reduction in Japanese patients with obese type 2 diabetes. J Diabetes Investig 5:2 (2014), 206–212 [Epub 2014/05/21].
88. Lalloyer, F., Staels, B., Fibrates, glitazones, and peroxisome proliferator-activated receptors. Arterioscler Thromb Vasc Biol 30:5 (2010), 894–899 [Epub 2010/04/16].
89. Yki-Jarvinen, H., Thiazolidinediones. N Engl J Med 351:11 (2004), 1106–1118 [Epub 2004/09/10].
90. Saltiel, A.R., Olefsky, J.M., Thiazolidinediones in the treatment of insulin resistance and type II diabetes. Diabetes 45:12 (1996), 1661–1669 [Epub 1996/12/01].
91. Nyenwe, E.A., Jerkins, T.W., Umpierrez, G.E., Kitabchi, A.E., Management of type 2 diabetes: evolving strategies for the treatment of patients with type 2 diabetes. Metabolism 60:1 (2011), 1–23 [Epub 2010/12/08].
92. Einhorn, D., Rendell, M., Rosenzweig, J., Egan, J.W., Mathisen, A.L., Schneider, R.L., Pioglitazone hydrochloride in combination with metformin in the treatment of type 2 diabetes mellitus: a randomized, placebo-controlled study. The Pioglitazone 027 Study Group. Clin Ther 22:12 (2000), 1395–1409 [Epub 2001/02/24].
93. Schernthaner, G., Matthews, D.R., Charbonnel, B., Hanefeld, M., Brunetti, P., Efficacy and safety of pioglitazone versus metformin in patients with type 2 diabetes mellitus: a double-blind, randomized trial. J Clin Endocrinol Metab 89:12 (2004), 6068–6076 [Epub 2004/12/08].
94. Scherbaum, W.A., Goke, B., Metabolic efficacy and safety of once-daily pioglitazone monotherapy in patients with type 2 diabetes: a double-blind, placebo-controlled study. Horm Metab Res 34:10 (2002), 589–595 [Epub 2002/11/20].
95. Herz, M., Johns, D., Reviriego, J., Grossman, L.D., Godin, C., Duran, S., et al. A randomized, double-blind, placebo-controlled, clinical trial of the effects of pioglitazone on glycemic control and dyslipidemia in oral antihyperglycemic medication-naive patients with type 2 diabetes mellitus. Clin Ther 25:4 (2003), 1074–1095 [Epub 2003/06/18].
96. Aronoff, S., Rosenblatt, S., Braithwaite, S., Egan, J.W., Mathisen, A.L., Schneider, R.L., Pioglitazone hydrochloride monotherapy improves glycemic control in the treatment of patients with type 2 diabetes: a 6-month randomized placebo-controlled dose-response study. The Pioglitazone 001 Study Group. Diabetes Care 23:11 (2000), 1605–1611 [Epub 2000/11/25].
97. Tan, M., Johns, D., Gonzalez Galvez, G., Antunez, O., Fabian, G., Flores-Lozano, F., et al. Effects of pioglitazone and glimepiride on glycemic control and insulin sensitivity in Mexican patients with type 2 diabetes mellitus: a multicenter, randomized, double-blind, parallel-group trial. Clin Ther 26:5 (2004), 680–693 [Epub 2004/06/29].
98. Petrie, J.R., Adler, A., Vella, S., What to add in with metformin in type 2 diabetes?. QJM 104:3 (2011), 185–192 [Epub 2010/12/16].
99. Goldberg, R.B., Kendall, D.M., Deeg, M.A., Buse, J.B., Zagar, A.J., Pinaire, J.A., et al. A comparison of lipid and glycemic effects of pioglitazone and rosiglitazone in patients with type 2 diabetes and dyslipidemia. Diabetes Care 28:7 (2005), 1547–1554 [Epub 2005/06/29].
100. Chiquette, E., Ramirez, G., Defronzo, R., A meta-analysis comparing the effect of thiazolidinediones on cardiovascular risk factors. Arch Intern Med 164:19 (2004), 2097–2104 [Epub 2004/10/27].
101. Dormandy, J.A., Charbonnel, B., Eckland, D.J., Erdmann, E., Massi-Benedetti, M., Moules, I.K., et al. Secondary prevention of macrovascular events in patients with type 2 diabetes in the PROactive Study (PROspective pioglitAzone Clinical Trial In macroVascular Events): a randomised controlled trial. Lancet 366:9493 (2005), 1279–1289 [Epub 2005/10/11].
102. Qayyum, R., Schulman, P., Cardiovascular effects of the thiazolidinediones. Diabetes Metab Res Rev 22:2 (2006), 88–97 [Epub 2005/09/27].
103. Sarafidis, P.A., Bakris, G.L., Protection of the kidney by thiazolidinediones: an assessment from bench to bedside. Kidney Int 70:7 (2006), 1223–1233 [Epub 2006/08/03].
104. Pfutzner, A., Hohberg, C., Lubben, G., Pahler, S., Pfutzner, A.H., Kann, P., et al. Pioneer study: PPARgamma activation results in overall improvement of clinical and metabolic markers associated with insulin resistance independent of long-term glucose control. Horm Metab Res 37:8 (2005), 510–515 [Epub 2005/09/03].
105. Neuschwander-Tetri, B.A., Brunt, E.M., Wehmeier, K.R., Oliver, D., Bacon, B.R., Improved nonalcoholic steatohepatitis after 48 weeks of treatment with the PPAR-gamma ligand rosiglitazone. Hepatology 38:4 (2003), 1008–1017 [Epub 2003/09/27].
106. Belfort, R., Harrison, S.A., Brown, K., Darland, C., Finch, J., Hardies, J., et al. A placebo-controlled trial of pioglitazone in subjects with nonalcoholic steatohepatitis. N Engl J Med 355:22 (2006), 2297–2307 [Epub 2006/12/01].
107. Polyzos, S.A., Mantzoros, C.S., Adiponectin as a target for the treatment of nonalcoholic steatohepatitis with thiazolidinediones: a systematic review. Metabolism 65:9 (2016), 1297–1306 [Epub 2016/08/11].
108. Athyros, V.G., Alexandrides, T.K., Bilianou, H., Cholongitas, E., Doumas, M., Ganotakis, E.S., et al. The use of statins alone, or in combination with pioglitazone and other drugs, for the treatment of non-alcoholic fatty liver disease/non-alcoholic steatohepatitis and related cardiovascular risk. An Expert Panel Statement. Metabolism 71 (2017), 17–32 [Epub 2017/05/20].
109. Gerstein, H.C., Ratner, R.E., Cannon, C.P., Serruys, P.W., Garcia-Garcia, H.M., van Es, G.A., et al. Effect of rosiglitazone on progression of coronary atherosclerosis in patients with type 2 diabetes mellitus and coronary artery disease: the assessment on the prevention of progression by rosiglitazone on atherosclerosis in diabetes patients with cardiovascular history trial. Circulation 121:10 (2010), 1176–1187 [Epub 2010/03/03].
110. Riche, D.M., Valderrama, R., Henyan, N.N., Thiazolidinediones and risk of repeat target vessel revascularization following percutaneous coronary intervention: a meta-analysis. Diabetes Care 30:2 (2007), 384–388 [Epub 2007/01/30].
111. Bolen, S., Feldman, L., Vassy, J., Wilson, L., Yeh, H.C., Marinopoulos, S., et al. Systematic review: comparative effectiveness and safety of oral medications for type 2 diabetes mellitus. Ann Intern Med 147:6 (2007), 386–399 [Epub 2007/07/20].
112. Smith, S.R., De Jonge, L., Volaufova, J., Li, Y., Xie, H., Bray, G.A., Effect of pioglitazone on body composition and energy expenditure: a randomized controlled trial. Metabolism 54:1 (2005), 24–32 [Epub 2004/11/25].
113. Rasouli, N., Raue, U., Miles, L.M., Lu, T., Di Gregorio, G.B., Elbein, S.C., et al. Pioglitazone improves insulin sensitivity through reduction in muscle lipid and redistribution of lipid into adipose tissue. Am J Phys Endocrinol Metab 288:5 (2005), E930–4 [Epub 2005/01/06].
114. Scheen, A.J., Combined thiazolidinedione-insulin therapy: should we be concerned about safety?. Drug Saf 27:12 (2004), 841–856 [Epub 2004/09/16].
115. Erdmann, E., Charbonnel, B., Wilcox, R.G., Skene, A.M., Massi-Benedetti, M., Yates, J., et al. Pioglitazone use and heart failure in patients with type 2 diabetes and preexisting cardiovascular disease: data from the PROactive study (PROactive 08). Diabetes Care 30:11 (2007), 2773–2778 [Epub 2007/08/02].
116. Idris, I., Warren, G., Donnelly, R., Association between thiazolidinedione treatment and risk of macular edema among patients with type 2 diabetes. Arch Intern Med 172:13 (2012), 1005–1011 [Epub 2012/06/13].
117. Dormandy, J., Bhattacharya, M., van Troostenburg de Bruyn, A.R., Safety and tolerability of pioglitazone in high-risk patients with type 2 diabetes: an overview of data from PROactive. Drug Saf 32:3 (2009), 187–202 [Epub 2009/04/03].
118. Kahn, S.E., Zinman, B., Lachin, J.M., Haffner, S.M., Herman, W.H., Holman, R.R., et al. Rosiglitazone-associated fractures in type 2 diabetes: an analysis from A Diabetes Outcome Progression Trial (ADOPT). Diabetes Care 31:5 (2008), 845–851 [Epub 2008/01/29].
119. Colmers, I.N., Bowker, S.L., Majumdar, S.R., Johnson, J.A., Use of thiazolidinediones and the risk of bladder cancer among people with type 2 diabetes: a meta-analysis. CMAJ 184:12 (2012), E675–83 [Epub 2012/07/05].
120. Lewis, J.D., Habel, L.A., Quesenberry, C.P., Strom, B.L., Peng, T., Hedderson, M.M., et al. Pioglitazone use and risk of bladder cancer and other common cancers in persons with diabetes. JAMA 314:3 (2015), 265–277 [Epub 2015/07/22].
121. Erdmann, E., Dormandy, J.A., Charbonnel, B., Massi-Benedetti, M., Moules, I.K., Skene, A.M., The effect of pioglitazone on recurrent myocardial infarction in 2,445 patients with type 2 diabetes and previous myocardial infarction: results from the PROactive (PROactive 05) Study. J Am Coll Cardiol 49:17 (2007), 1772–1780 [Epub 2007/05/01].
122. Kernan, W.N., Viscoli, C.M., Furie, K.L., Young, L.H., Inzucchi, S.E., Gorman, M., et al. Pioglitazone after ischemic stroke or transient ischemic attack. N Engl J Med 374:14 (2016), 1321–1331 [Epub 2016/02/18].
123. McGuire, D.K., Inzucchi, S.E., New drugs for the treatment of diabetes mellitus: part I: thiazolidinediones and their evolving cardiovascular implications. Circulation 117:3 (2008), 440–449 [Epub 2008/01/24].
124. Marx, N., Wohrle, J., Nusser, T., Walcher, D., Rinker, A., Hombach, V., et al. Pioglitazone reduces neointima volume after coronary stent implantation: a randomized, placebo-controlled, double-blind trial in nondiabetic patients. Circulation 112:18 (2005), 2792–2798 [Epub 2005/10/26].
125. Nishio, K., Sakurai, M., Kusuyama, T., Shigemitsu, M., Fukui, T., Kawamura, K., et al. A randomized comparison of pioglitazone to inhibit restenosis after coronary stenting in patients with type 2 diabetes. Diabetes Care 29:1 (2006), 101–106 [Epub 2005/12/24].
126. Takagi, T., Yamamuro, A., Tamita, K., Yamabe, K., Katayama, M., Mizoguchi, S., et al. Pioglitazone reduces neointimal tissue proliferation after coronary stent implantation in patients with type 2 diabetes mellitus: an intravascular ultrasound scanning study. Am Heart J, 146(2), 2003, E5 [Epub 2003/08/02].
127. Mannucci, E., Monami, M., Lamanna, C., Gensini, G.F., Marchionni, N., Pioglitazone and cardiovascular risk. A comprehensive meta-analysis of randomized clinical trials. Diabetes Obes Metab 10:12 (2008), 1221–1238 [Epub 2008/05/29].
128. Lincoff, A.M., Wolski, K., Nicholls, S.J., Nissen, S.E., Pioglitazone and risk of cardiovascular events in patients with type 2 diabetes mellitus: a meta-analysis of randomized trials. JAMA 298:10 (2007), 1180–1188 [Epub 2007/09/13].
129. Nissen, S.E., Wolski, K., Effect of rosiglitazone on the risk of myocardial infarction and death from cardiovascular causes. N Engl J Med 356:24 (2007), 2457–2471 [Epub 2007/05/23].
130. Singh, S., Loke, Y.K., Furberg, C.D., Long-term risk of cardiovascular events with rosiglitazone: a meta-analysis. JAMA 298:10 (2007), 1189–1195 [Epub 2007/09/13].
131. Bloomgarden, Z.T., Glycemic control in diabetes: a tale of three studies. Diabetes Care 31:9 (2008), 1913–1919 [Epub 2008/08/30].
132. Nissen, S.E., Wolski, K., Rosiglitazone revisited: an updated meta-analysis of risk for myocardial infarction and cardiovascular mortality. Arch Intern Med 170:14 (2010), 1191–1201 [Epub 2010/07/27].
133. Mahaffey, K.W., Hafley, G., Dickerson, S., Burns, S., Tourt-Uhlig, S., White, J., et al. Results of a reevaluation of cardiovascular outcomes in the RECORD trial. Am Heart J 166:2 (2013), 240–249.e1 [Epub 2013/07/31].
134. Li, Y., Xu, W., Liao, Z., Yao, B., Chen, X., Huang, Z., et al. Induction of long-term glycemic control in newly diagnosed type 2 diabetic patients is associated with improvement of beta-cell function. Diabetes Care 27:11 (2004), 2597–2602 [Epub 2004/10/27].
135. Devries, J.H., Nattrass, M., Pieber, T.R., Refining basal insulin therapy: what have we learned in the age of analogues?. Diabetes Metab Res Rev 23:6 (2007), 441–454 [Epub 2007/08/02].
136. Pettus, J., Santos Cavaiola, T., Tamborlane, W.V., Edelman, S., The past, present, and future of basal insulins. Diabetes Metab Res Rev 32:6 (2016), 478–496 [Epub 2015/10/29].
137. Riddle, M.C., Rosenstock, J., Gerich, J., The treat-to-target trial: randomized addition of glargine or human NPH insulin to oral therapy of type 2 diabetic patients. Diabetes Care 26:11 (2003), 3080–3086 [Epub 2003/10/28].
138. Anderson, J.E., An evolutionary perspective on basal insulin in diabetes treatment: innovations in insulin: insulin glargine U-300. J Fam Pract 65:10 Suppl. (2016), S23–S28 [Epub 2016/11/16].
139. Janka, H.U., Plewe, G., Riddle, M.C., Kliebe-Frisch, C., Schweitzer, M.A., Yki-Jarvinen, H., Comparison of basal insulin added to oral agents versus twice-daily premixed insulin as initial insulin therapy for type 2 diabetes. Diabetes Care 28:2 (2005), 254–259 [Epub 2005/01/29].
140. Monami, M., Marchionni, N., Mannucci, E., Long-acting insulin analogues versus NPH human insulin in type 2 diabetes: a meta-analysis. Diabetes Res Clin Pract 81:2 (2008), 184–189 [Epub 2008/05/23].
141. Vague, P., Selam, J.L., Skeie, S., De Leeuw, I., Elte, J.W., Haahr, H., et al. Insulin detemir is associated with more predictable glycemic control and reduced risk of hypoglycemia than NPH insulin in patients with type 1 diabetes on a basal-bolus regimen with premeal insulin aspart. Diabetes Care 26:3 (2003), 590–596 [Epub 2003/03/01].
142. Nakamura, T., Sakaguchi, K., So, A., Nakajima, S., Takabe, M., Komada, H., et al. Effects of insulin degludec and insulin glargine on day-to-day fasting plasma glucose variability in individuals with type 1 diabetes: a multicentre, randomised, crossover study. Diabetologia 58:9 (2015), 2013–2019 [Epub 2015/06/06].
143. Haahr, H., Heise, T., A review of the pharmacological properties of insulin degludec and their clinical relevance. Clin Pharmacokinet 53:9 (2014), 787–800 [Epub 2014/09/03].
144. Heise, T., Hermanski, L., Nosek, L., Feldman, A., Rasmussen, S., Haahr, H., Insulin degludec: four times lower pharmacodynamic variability than insulin glargine under steady-state conditions in type 1 diabetes. Diabetes Obes Metab 14:9 (2012), 859–864 [Epub 2012/05/19].
145. Rodbard, H.W., Gough, S., Lane, W., Korsholm, L., Bretler, D.M., Handelsman, Y., Reduced risk of hypoglycemia with insulin degludec versus insulin glargine in patients with type 2 diabetes requiring high doses of Basal insulin: a meta-analysis of 5 randomized begin trials. Endocr Pract 20:4 (2014), 285–292 [Epub 2013/11/20].
146. Weinstein, D., Simon, M., Yehezkel, E., Laron, Z., Werner, H., Insulin analogues display IGF-I-like mitogenic and anti-apoptotic activities in cultured cancer cells. Diabetes Metab Res Rev 25:1 (2009), 41–49 [Epub 2009/01/16].
147. Hemkens, L.G., Grouven, U., Bender, R., Gunster, C., Gutschmidt, S., Selke, G.W., et al. Risk of malignancies in patients with diabetes treated with human insulin or insulin analogues: a cohort study. Diabetologia 52:9 (2009), 1732–1744 [Epub 2009/07/01].
148. Jonasson, J.M., Ljung, R., Talback, M., Haglund, B., Gudbjornsdottir, S., Steineck, G., Insulin glargine use and short-term incidence of malignancies-a population-based follow-up study in Sweden. Diabetologia 52:9 (2009), 1745–1754 [Epub 2009/07/10].
149. Colhoun, H.M., Use of insulin glargine and cancer incidence in Scotland: a study from the Scottish Diabetes Research Network Epidemiology Group. Diabetologia 52:9 (2009), 1755–1765 [Epub 2009/07/16].
150. Currie, C.J., Poole, C.D., Gale, E.A., The influence of glucose-lowering therapies on cancer risk in type 2 diabetes. Diabetologia 52:9 (2009), 1766–1777 [Epub 2009/07/03].
151. Rosenstock, J., Fonseca, V., McGill, J.B., Riddle, M., Halle, J.P., Hramiak, I., et al. Similar risk of malignancy with insulin glargine and neutral protamine Hagedorn (NPH) insulin in patients with type 2 diabetes: findings from a 5 year randomised, open-label study. Diabetologia 52:9 (2009), 1971–1973 [Epub 2009/07/18].
152. Bordeleau, L., Yakubovich, N., Dagenais, G.R., Rosenstock, J., Probstfield, J., Chang Yu, P., et al. The association of basal insulin glargine and/or n-3 fatty acids with incident cancers in patients with dysglycemia. Diabetes Care 37:5 (2014), 1360–1366 [Epub 2014/02/28].
153. Hirsch, I.B., Insulin analogues. N Engl J Med 352:2 (2005), 174–183 [Epub 2005/01/14].
154. Rosenstock, J., Lorber, D.L., Gnudi, L., Howard, C.P., Bilheimer, D.W., Chang, P.C., et al. Prandial inhaled insulin plus basal insulin glargine versus twice daily biaspart insulin for type 2 diabetes: a multicentre randomised trial. Lancet 375:9733 (2010), 2244–2253 [Epub 2010/07/09].
155. Holman, R.R., Farmer, A.J., Davies, M.J., Levy, J.C., Darbyshire, J.L., Keenan, J.F., et al. Three-year efficacy of complex insulin regimens in type 2 diabetes. N Engl J Med 361:18 (2009), 1736–1747 [Epub 2009/10/24].
156. Kruger, D.F., Gatcomb, P.M., Owen, S.K., Clinical implications of amylin and amylin deficiency. Diabetes Educ 25:3 (1999), 389–397 [quiz 98; Epub 1999/10/26].
157. Young, A., Inhibition of gastric emptying. Adv Pharmacol 52 (2005), 99–121 [Epub 2006/02/24].
158. Chapman, I., Parker, B., Doran, S., Feinle-Bisset, C., Wishart, J., Strobel, S., et al. Effect of pramlintide on satiety and food intake in obese subjects and subjects with type 2 diabetes. Diabetologia 48:5 (2005), 838–848 [Epub 2005/04/22].
159. Smith, S.R., Blundell, J.E., Burns, C., Ellero, C., Schroeder, B.E., Kesty, N.C., et al. Pramlintide treatment reduces 24-h caloric intake and meal sizes and improves control of eating in obese subjects: a 6-wk translational research study. Am J Phys Endocrinol Metab 293:2 (2007), E620–7 [Epub 2007/05/17].
160. Edelman, S., Garg, S., Frias, J., Maggs, D., Wang, Y., Zhang, B., et al. A double-blind, placebo-controlled trial assessing pramlintide treatment in the setting of intensive insulin therapy in type 1 diabetes. Diabetes Care 29:10 (2006), 2189–2195 [Epub 2006/09/28].
161. Riddle, M., Pencek, R., Charenkavanich, S., Lutz, K., Wilhelm, K., Porter, L., Randomized comparison of pramlintide or mealtime insulin added to basal insulin treatment for patients with type 2 diabetes. Diabetes Care 32:9 (2009), 1577–1582 [Epub 2009/06/09].
162. Standards of medical care in diabetes—2013. Diabetes Care, 36(Suppl. 1), 2013, S11–S66 [Epub 2013/01/04].
163. Hollander, P., Ratner, R., Fineman, M., Strobel, S., Shen, L., Maggs, D., et al. Addition of pramlintide to insulin therapy lowers HbA1c in conjunction with weight loss in patients with type 2 diabetes approaching glycaemic targets. Diabetes Obes Metab 5:6 (2003), 408–414 [Epub 2003/11/18].
164. Riddle, M., Frias, J., Zhang, B., Maier, H., Brown, C., Lutz, K., et al. Pramlintide improved glycemic control and reduced weight in patients with type 2 diabetes using basal insulin. Diabetes Care 30:11 (2007), 2794–2799 [Epub 2007/08/19].
165. Ratner, R.E., Want, L.L., Fineman, M.S., Velte, M.J., Ruggles, J.A., Gottlieb, A., et al. Adjunctive therapy with the amylin analogue pramlintide leads to a combined improvement in glycemic and weight control in insulin-treated subjects with type 2 diabetes. Diabetes Technol Ther 4:1 (2002), 51–61 [Epub 2002/05/23].
166. Karl, D., Philis-Tsimikas, A., Darsow, T., Lorenzi, G., Kellmeyer, T., Lutz, K., et al. Pramlintide as an adjunct to insulin in patients with type 2 diabetes in a clinical practice setting reduced A1C, postprandial glucose excursions, and weight. Diabetes Technol Ther 9:2 (2007), 191–199 [Epub 2007/04/12].
167. Maggs, D., Shen, L., Strobel, S., Brown, D., Kolterman, O., Weyer, C., Effect of pramlintide on A1C and body weight in insulin-treated African Americans and Hispanics with type 2 diabetes: a pooled post hoc analysis. Metabolism 52:12 (2003), 1638–1642 [Epub 2003/12/12].
168. Hollander, P., Maggs, D.G., Ruggles, J.A., Fineman, M., Shen, L., Kolterman, O.G., et al. Effect of pramlintide on weight in overweight and obese insulin-treated type 2 diabetes patients. Obes Res 12:4 (2004), 661–668 [Epub 2004/04/20].
169. Thompson, R.G., Pearson, L., Schoenfeld, S.L., Kolterman, O.G., Pramlintide, a synthetic analog of human amylin, improves the metabolic profile of patients with type 2 diabetes using insulin. The Pramlintide in Type 2 Diabetes Group. Diabetes Care 21:6 (1998), 987–993 [Epub 1998/06/06].
170. Ratner, R.E., Dickey, R., Fineman, M., Maggs, D.G., Shen, L., Strobel, S.A., et al. Amylin replacement with pramlintide as an adjunct to insulin therapy improves long-term glycaemic and weight control in type 1 diabetes mellitus: a 1-year, randomized controlled trial. Diabet Med 21:11 (2004), 1204–1212 [Epub 2004/10/23].
171. Elrick, H., Stimmler, L., Hlad, C.J. Jr., Arai, Y., Plasma insulin response to oral and intravenous glucose administration. J Clin Endocrinol Metab 24 (1964), 1076–1082 [Epub 1964/10/01].
172. Kreymann, B., Williams, G., Ghatei, M.A., Bloom, S.R., Glucagon-like peptide-1 7-36: a physiological incretin in man. Lancet 2:8571 (1987), 1300–1304 [Epub 1987/12/05].
173. Vilsboll, T., Holst, J.J., Incretins, insulin secretion and type 2 diabetes mellitus. Diabetologia 47:3 (2004), 357–366 [Epub 2004/02/18].
174. Deacon, C.F., What do we know about the secretion and degradation of incretin hormones?. Regul Pept 128:2 (2005), 117–124 [Epub 2005/03/23].
175. Fehmann, H.C., Goke, R., Goke, B., Cell and molecular biology of the incretin hormones glucagon-like peptide-I and glucose-dependent insulin releasing polypeptide. Endocr Rev 16:3 (1995), 390–410 [Epub 1995/06/01].
176. Drucker, D.J., Nauck, M.A., The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 368:9548 (2006), 1696–1705 [Epub 2006/11/14].
177. Holst, J.J., Glucagon-like peptide 1 (GLP-1): an intestinal hormone, signalling nutritional abundance, with an unusual therapeutic potential. Trends Endocrinol Metab 10:6 (1999), 229–235 [Epub 1999/07/17].
178. Herrmann, C., Goke, R., Richter, G., Fehmann, H.C., Arnold, R., Goke, B., Glucagon-like peptide-1 and glucose-dependent insulin-releasing polypeptide plasma levels in response to nutrients. Digestion 56:2 (1995), 117–126 [Epub 1995/01/01].
179. Burcelin, R., Cani, P.D., Knauf, C., Glucagon-like peptide-1 and energy homeostasis. J Nutr 137:11 Suppl. (2007), 2534s–2538s [Epub 2007/10/24].
180. Flint, A., Raben, A., Astrup, A., Holst, J.J., Glucagon-like peptide 1 promotes satiety and suppresses energy intake in humans. J Clin Invest 101:3 (1998), 515–520 [Epub 1998/03/21].
181. Verdich, C., Toubro, S., Buemann, B., Lysgard Madsen, J., Juul Holst, J., Astrup, A., The role of postprandial releases of insulin and incretin hormones in meal-induced satiety—effect of obesity and weight reduction. Int J Obes Relat Metab Disord 25:8 (2001), 1206–1214 [Epub 2001/07/31].
182. Naslund, E., Barkeling, B., King, N., Gutniak, M., Blundell, J.E., Holst, J.J., et al. Energy intake and appetite are suppressed by glucagon-like peptide-1 (GLP-1) in obese men. Int J Obes Relat Metab Disord 23:3 (1999), 304–311 [Epub 1999/04/08].
183. Zander, M., Madsbad, S., Madsen, J.L., Holst, J.J., Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and beta-cell function in type 2 diabetes: a parallel-group study. Lancet 359:9309 (2002), 824–830 [Epub 2002/03/19].
184. Nauck, M., Stockmann, F., Ebert, R., Creutzfeldt, W., Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia 29:1 (1986), 46–52 [Epub 1986/01/01].
185. Nauck, M.A., Heimesaat, M.M., Orskov, C., Holst, J.J., Ebert, R., Creutzfeldt, W., Preserved incretin activity of glucagon-like peptide 1 [7-36 amide] but not of synthetic human gastric inhibitory polypeptide in patients with type-2 diabetes mellitus. J Clin Invest 91:1 (1993), 301–307 [Epub 1993/01/01].
186. Nauck, M.A., Sauerwald, A., Ritzel, R., Holst, J.J., Schmiegel, W., Influence of glucagon-like peptide 1 on fasting glycemia in type 2 diabetic patients treated with insulin after sulfonylurea secondary failure. Diabetes Care 21:11 (1998), 1925–1931 [Epub 1998/11/05].
187. Rachman, J., Barrow, B.A., Levy, J.C., Turner, R.C., Near-normalisation of diurnal glucose concentrations by continuous administration of glucagon-like peptide-1 (GLP-1) in subjects with NIDDM. Diabetologia 40:2 (1997), 205–211 [Epub 1997/02/01].
188. Hare, K.J., Vilsboll, T., Asmar, M., Deacon, C.F., Knop, F.K., Holst, J.J., The glucagonostatic and insulinotropic effects of glucagon-like peptide 1 contribute equally to its glucose-lowering action. Diabetes 59:7 (2010), 1765–1770 [Epub 2010/02/13].
189. Salehi, M., Aulinger, B., Prigeon, R.L., D'Alessio, D.A., Effect of endogenous GLP-1 on insulin secretion in type 2 diabetes. Diabetes 59:6 (2010), 1330–1337 [Epub 2010/03/11].
190. Nauck, M.A., Kleine, N., Orskov, C., Holst, J.J., Willms, B., Creutzfeldt, W., Normalization of fasting hyperglycaemia by exogenous glucagon-like peptide 1 (7-36 amide) in type 2 (non-insulin-dependent) diabetic patients. Diabetologia 36:8 (1993), 741–744 [Epub 1993/08/01].
191. Flint, A., Raben, A., Ersboll, A.K., Holst, J.J., Astrup, A., The effect of physiological levels of glucagon-like peptide-1 on appetite, gastric emptying, energy and substrate metabolism in obesity. Int J Obes Relat Metab Disord 25:6 (2001), 781–792 [Epub 2001/07/06].
192. Verdich, C., Flint, A., Gutzwiller, J.P., Naslund, E., Beglinger, C., Hellstrom, P.M., et al. A meta-analysis of the effect of glucagon-like peptide-1 (7-36) amide on ad libitum energy intake in humans. J Clin Endocrinol Metab 86:9 (2001), 4382–4389 [Epub 2001/09/11].
193. Gutzwiller, J.P., Goke, B., Drewe, J., Hildebrand, P., Ketterer, S., Handschin, D., et al. Glucagon-like peptide-1: a potent regulator of food intake in humans. Gut 44:1 (1999), 81–86 [Epub 1998/12/24].
194. Gutzwiller, J.P., Drewe, J., Goke, B., Schmidt, H., Rohrer, B., Lareida, J., et al. Glucagon-like peptide-1 promotes satiety and reduces food intake in patients with diabetes mellitus type 2. Am J Phys 276:5 Pt 2 (1999), R1541–4 [Epub 1999/05/08].
195. Nikolaidis, L.A., Mankad, S., Sokos, G.G., Miske, G., Shah, A., Elahi, D., et al. Effects of glucagon-like peptide-1 in patients with acute myocardial infarction and left ventricular dysfunction after successful reperfusion. Circulation 109:8 (2004), 962–965 [Epub 2004/02/26].
196. Merchenthaler, I., Lane, M., Shughrue, P., Distribution of pre-pro-glucagon and glucagon-like peptide-1 receptor messenger RNAs in the rat central nervous system. J Comp Neurol 403:2 (1999), 261–280 [Epub 1999/01/14].
197. Turton, M.D., O'Shea, D., Gunn, I., Beak, S.A., Edwards, C.M., Meeran, K., et al. A role for glucagon-like peptide-1 in the central regulation of feeding. Nature 379:6560 (1996), 69–72 [Epub 1996/01/04].
198. Alvarez, E., Martinez, M.D., Roncero, I., Chowen, J.A., Garcia-Cuartero, B., Gispert, J.D., et al. The expression of GLP-1 receptor mRNA and protein allows the effect of GLP-1 on glucose metabolism in the human hypothalamus and brainstem. J Neurochem 92:4 (2005), 798–806 [Epub 2005/02/03].
199. Schlogl, H., Kabisch, S., Horstmann, A., Lohmann, G., Muller, K., Lepsien, J., et al. Exenatide-induced reduction in energy intake is associated with increase in hypothalamic connectivity. Diabetes Care 36:7 (2013), 1933–1940 [Epub 2013/03/07].
200. Farr, O.M., Sofopoulos, M., Tsoukas, M.A., Dincer, F., Thakkar, B., Sahin-Efe, A., et al. GLP-1 receptors exist in the parietal cortex, hypothalamus and medulla of human brains and the GLP-1 analogue liraglutide alters brain activity related to highly desirable food cues in individuals with diabetes: a crossover, randomised, placebo-controlled trial. Diabetologia 59:5 (2016), 954–965 [Epub 2016/02/03].
201. Farr, O.M., Tsoukas, M.A., Triantafyllou, G., Dincer, F., Filippaios, A., Ko, B.J., et al. Short-term administration of the GLP-1 analog liraglutide decreases circulating leptin and increases GIP levels and these changes are associated with alterations in CNS responses to food cues: a randomized, placebo-controlled, crossover study. Metabolism 65:7 (2016), 945–953 [Epub 2016/06/11].
202. Carbone, L.J., Angus, P.W., Yeomans, N.D., Incretin-based therapies for the treatment of non-alcoholic fatty liver disease: a systematic review and meta-analysis. J Gastroenterol Hepatol 31:1 (2016), 23–31 [Epub 2015/06/26].
203. Lambeir, A.M., Durinx, C., Scharpe, S., De Meester, I., Dipeptidyl-peptidase IV from bench to bedside: an update on structural properties, functions, and clinical aspects of the enzyme DPP IV. Crit Rev Clin Lab Sci 40:3 (2003), 209–294 [Epub 2003/08/02].
204. Havale, S.H., Pal, M., Medicinal chemistry approaches to the inhibition of dipeptidyl peptidase-4 for the treatment of type 2 diabetes. Bioorg Med Chem 17:5 (2009), 1783–1802 [Epub 2009/02/17].
205. Green, B.D., Flatt, P.R., Bailey, C.J., Dipeptidyl peptidase IV (DPP IV) inhibitors: a newly emerging drug class for the treatment of type 2 diabetes. Diab Vasc Dis Res 3:3 (2006), 159–165 [Epub 2006/12/13].
206. Hildebrandt, M., Reutter, W., Arck, P., Rose, M., Klapp, B.F., A guardian angel: the involvement of dipeptidyl peptidase IV in psychoneuroendocrine function, nutrition and immune defence. Clin Sci (Lond) 99:2 (2000), 93–104 [Epub 2000/08/05].
207. Bergmann, A., Bohuon, C., Decrease of serum dipeptidylpeptidase activity in severe sepsis patients: relationship to procalcitonin. Clin Chim Acta 321:1–2 (2002), 123–126 [Epub 2002/05/29].
208. Drucker, D.J., Enhancing incretin action for the treatment of type 2 diabetes. Diabetes Care 26:10 (2003), 2929–2940 [Epub 2003/09/30].
209. Charbonnel, B., Karasik, A., Liu, J., Wu, M., Meininger, G., Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes inadequately controlled with metformin alone. Diabetes Care 29:12 (2006), 2638–2643 [Epub 2006/11/30].
210. Brown, N.J., Byiers, S., Carr, D., Maldonado, M., Warner, B.A., Dipeptidyl peptidase-IV inhibitor use associated with increased risk of ACE inhibitor-associated angioedema. Hypertension 54:3 (2009), 516–523 [Epub 2009/07/08].
211. Amori, R.E., Lau, J., Pittas, A.G., Efficacy and safety of incretin therapy in type 2 diabetes: systematic review and meta-analysis. JAMA 298:2 (2007), 194–206 [Epub 2007/07/12].
212. Williams-Herman, D., Engel, S.S., Round, E., Johnson, J., Golm, G.T., Guo, H., et al. Safety and tolerability of sitagliptin in clinical studies: a pooled analysis of data from 10,246 patients with type 2 diabetes. BMC Endocr Disord, 10, 2010, 7 [Epub 2010/04/24].
213. Goossen, K., Graber, S., Longer term safety of dipeptidyl peptidase-4 inhibitors in patients with type 2 diabetes mellitus: systematic review and meta-analysis. Diabetes Obes Metab 14:12 (2012), 1061–1072 [Epub 2012/04/24].
214. Scott, R., Wu, M., Sanchez, M., Stein, P., Efficacy and tolerability of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy over 12 weeks in patients with type 2 diabetes. Int J Clin Pract 61:1 (2007), 171–180 [Epub 2006/12/13].
215. Rosenstock, J., Brazg, R., Andryuk, P.J., Lu, K., Stein, P., Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin added to ongoing pioglitazone therapy in patients with type 2 diabetes: a 24-week, multicenter, randomized, double-blind, placebo-controlled, parallel-group study. Clin Ther 28:10 (2006), 1556–1568 [Epub 2006/12/13].
216. Raz, I., Hanefeld, M., Xu, L., Caria, C., Williams-Herman, D., Khatami, H., Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus. Diabetologia 49:11 (2006), 2564–2571 [Epub 2006/09/27].
217. DeFronzo, R.A., Hissa, M.N., Garber, A.J., Luiz Gross, J., Yuyan Duan, R., Ravichandran, S., et al. The efficacy and safety of saxagliptin when added to metformin therapy in patients with inadequately controlled type 2 diabetes with metformin alone. Diabetes Care 32:9 (2009), 1649–1655 [Epub 2009/05/30].
218. Chacra, A.R., Tan, G.H., Apanovitch, A., Ravichandran, S., List, J., Chen, R., Saxagliptin added to a submaximal dose of sulphonylurea improves glycaemic control compared with uptitration of sulphonylurea in patients with type 2 diabetes: a randomised controlled trial. Int J Clin Pract 63:9 (2009), 1395–1406 [Epub 2009/07/21].
219. Scirica, B.M., Bhatt, D.L., Braunwald, E., Steg, P.G., Davidson, J., Hirshberg, B., et al. Saxagliptin and cardiovascular outcomes in patients with type 2 diabetes mellitus. N Engl J Med 369:14 (2013), 1317–1326 [Epub 2013/09/03].
220. White, W.B., Cannon, C.P., Heller, S.R., Nissen, S.E., Bergenstal, R.M., Bakris, G.L., et al. Alogliptin after acute coronary syndrome in patients with type 2 diabetes. N Engl J Med 369:14 (2013), 1327–1335 [Epub 2013/09/03].
221. Scirica, B.M., Braunwald, E., Raz, I., Cavender, M.A., Morrow, D.A., Jarolim, P., et al. Heart failure, saxagliptin, and diabetes mellitus: observations from the SAVOR-TIMI 53 randomized trial. Circulation 130:18 (2014), 1579–1588 [Epub 2014/09/06].
222. Williams-Herman, D., Round, E., Swern, A.S., Musser, B., Davies, M.J., Stein, P.P., et al. Safety and tolerability of sitagliptin in patients with type 2 diabetes: a pooled analysis. BMC Endocr Disord, 8, 2008, 14 [Epub 2008/10/29].
223. Van Raalte, D.H., van Genugten, R.E., Eliasson, B., Moller-Goede, D.L., Mari, A., Tura, A., et al. The effect of alogliptin and pioglitazone combination therapy on various aspects of beta-cell function in patients with recent-onset type 2 diabetes. Eur J Endocrinol 170:4 (2014), 565–574 [Epub 2014/01/15].
224. Aschner, P., Kipnes, M.S., Lunceford, J.K., Sanchez, M., Mickel, C., Williams-Herman, D.E., Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 29:12 (2006), 2632–2637 [Epub 2006/11/30].
225. Seino, Y., Fujita, T., Hiroi, S., Hirayama, M., Kaku, K., Efficacy and safety of alogliptin in Japanese patients with type 2 diabetes mellitus: a randomized, double-blind, dose-ranging comparison with placebo, followed by a long-term extension study. Curr Med Res Opin 27:9 (2011), 1781–1792 [Epub 2011/08/03].
226. Del Prato, S., Barnett, A.H., Huisman, H., Neubacher, D., Woerle, H.J., Dugi, K.A., Effect of linagliptin monotherapy on glycaemic control and markers of beta-cell function in patients with inadequately controlled type 2 diabetes: a randomized controlled trial. Diabetes Obes Metab 13:3 (2011), 258–267 [Epub 2011/01/06].
227. de la Tour, D., Halvorsen, T., Demeterco, C., Tyrberg, B., Itkin-Ansari, P., Loy, M., et al. Beta-cell differentiation from a human pancreatic cell line in vitro and in vivo. Mol Endocrinol 15:3 (2001), 476–483 [Epub 2001/02/27].
228. Del Prato, S., Camisasca, R., Wilson, C., Fleck, P., Durability of the efficacy and safety of alogliptin compared with glipizide in type 2 diabetes mellitus: a 2-year study. Diabetes Obes Metab 16:12 (2014), 1239–1246 [Epub 2014/08/19].
229. Mistry, G.C., Maes, A.L., Lasseter, K.C., Davies, M.J., Gottesdiener, K.M., Wagner, J.A., et al. Effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on blood pressure in nondiabetic patients with mild to moderate hypertension. J Clin Pharmacol 48:5 (2008), 592–598 [Epub 2008/03/21].
230. White, W.B., Bakris, G.L., Bergenstal, R.M., Cannon, C.P., Cushman, W.C., Fleck, P., et al. EXamination of cArdiovascular outcoMes with alogliptIN versus standard of carE in patients with type 2 diabetes mellitus and acute coronary syndrome (EXAMINE): a cardiovascular safety study of the dipeptidyl peptidase 4 inhibitor alogliptin in patients with type 2 diabetes with acute coronary syndrome. Am Heart J 162:4 (2011), 620–626.e1 [Epub 2011/10/11].
231. Zannad, F., Cannon, C.P., Cushman, W.C., Bakris, G.L., Menon, V., Perez, A.T., et al. Heart failure and mortality outcomes in patients with type 2 diabetes taking alogliptin versus placebo in EXAMINE: a multicentre, randomised, double-blind trial. Lancet 385:9982 (2015), 2067–2076 [Epub 2015/03/15].
232. Green, J.B., Bethel, M.A., Armstrong, P.W., Buse, J.B., Engel, S.S., Garg, J., et al. Effect of sitagliptin on cardiovascular outcomes in type 2 diabetes. N Engl J Med 373:3 (2015), 232–242 [Epub 2015/06/09].
233. Ahren, B., Mathieu, C., Bader, G., Schweizer, A., Foley, J.E., Efficacy of vildagliptin versus sulfonylureas as add-on therapy to metformin: comparison of results from randomised controlled and observational studies. Diabetologia 57:7 (2014), 1304–1307 [Epub 2014/04/01].
234. Seck, T., Nauck, M., Sheng, D., Sunga, S., Davies, M.J., Stein, P.P., et al. Safety and efficacy of treatment with sitagliptin or glipizide in patients with type 2 diabetes inadequately controlled on metformin: a 2-year study. Int J Clin Pract 64:5 (2010), 562–576 [Epub 2010/05/12].
235. Gallwitz, B., Rosenstock, J., Rauch, T., Bhattacharya, S., Patel, S., von Eynatten, M., et al. 2-year efficacy and safety of linagliptin compared with glimepiride in patients with type 2 diabetes inadequately controlled on metformin: a randomised, double-blind, non-inferiority trial. Lancet 380:9840 (2012), 475–483 [Epub 2012/07/04].
236. Ferrannini, E., Fonseca, V., Zinman, B., Matthews, D., Ahren, B., Byiers, S., et al. Fifty-two-week efficacy and safety of vildagliptin vs. glimepiride in patients with type 2 diabetes mellitus inadequately controlled on metformin monotherapy. Diabetes Obes Metab 11:2 (2009), 157–166 [Epub 2009/01/08].
237. Inagaki, N., Onouchi, H., Sano, H., Funao, N., Kuroda, S., Kaku, K., SYR-472, a novel once-weekly dipeptidyl peptidase-4 (DPP-4) inhibitor, in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet Diabetes Endocrinol 2:2 (2014), 125–132 [Epub 2014/03/14].
238. Fineman, M.S., Cirincione, B.B., Maggs, D., Diamant, M., GLP-1 based therapies: differential effects on fasting and postprandial glucose. Diabetes Obes Metab 14:8 (2012), 675–688 [Epub 2012/01/12].
239. Raufman, J.P., Singh, L., Singh, G., Eng, J., Truncated glucagon-like peptide-1 interacts with exendin receptors on dispersed acini from guinea pig pancreas. Identification of a mammalian analogue of the reptilian peptide exendin-4. J Biol Chem 267:30 (1992), 21432–21437 [Epub 1992/10/25].
240. Young, A.A., Gedulin, B.R., Bhavsar, S., Bodkin, N., Jodka, C., Hansen, B., et al. Glucose-lowering and insulin-sensitizing actions of exendin-4: studies in obese diabetic (ob/ob, db/db) mice, diabetic fatty Zucker rats, and diabetic rhesus monkeys (Macaca mulatta). Diabetes 48:5 (1999), 1026–1034 [Epub 1999/05/20].
241. Fineman, M., Flanagan, S., Taylor, K., Aisporna, M., Shen, L.Z., Mace, K.F., et al. Pharmacokinetics and pharmacodynamics of exenatide extended-release after single and multiple dosing. Clin Pharmacokinet 50:1 (2011), 65–74 [Epub 2010/12/15].
242. Standards of medical care in diabetes-2017: summary of revisions. Diabetes Care, 40(Suppl. 1), 2017, S4–S5 [Epub 2016/12/17].
243. Moretto, T.J., Milton, D.R., Ridge, T.D., Macconell, L.A., Okerson, T., Wolka, A.M., et al. Efficacy and tolerability of exenatide monotherapy over 24 weeks in antidiabetic drug-naive patients with type 2 diabetes: a randomized, double-blind, placebo-controlled, parallel-group study. Clin Ther 30:8 (2008), 1448–1460 [Epub 2008/09/23].
244. Buse, J.B., Bergenstal, R.M., Glass, L.C., Heilmann, C.R., Lewis, M.S., Kwan, A.Y., et al. Use of twice-daily exenatide in Basal insulin-treated patients with type 2 diabetes: a randomized, controlled trial. Ann Intern Med 154:2 (2011), 103–112 [Epub 2010/12/09].
245. DeFronzo, R.A., Ratner, R.E., Han, J., Kim, D.D., Fineman, M.S., Baron, A.D., Effects of exenatide (exendin-4) on glycemic control and weight over 30 weeks in metformin-treated patients with type 2 diabetes. Diabetes Care 28:5 (2005), 1092–1100 [Epub 2005/04/28].
246. Buse, J.B., Henry, R.R., Han, J., Kim, D.D., Fineman, M.S., Baron, A.D., Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes. Diabetes Care 27:11 (2004), 2628–2635 [Epub 2004/10/27].
247. Kendall, D.M., Riddle, M.C., Rosenstock, J., Zhuang, D., Kim, D.D., Fineman, M.S., et al. Effects of exenatide (exendin-4) on glycemic control over 30 weeks in patients with type 2 diabetes treated with metformin and a sulfonylurea. Diabetes Care 28:5 (2005), 1083–1091 [Epub 2005/04/28].
248. Buse, J.B., Rosenstock, J., Sesti, G., Schmidt, W.E., Montanya, E., Brett, J.H., et al. Liraglutide once a day versus exenatide twice a day for type 2 diabetes: a 26-week randomised, parallel-group, multinational, open-label trial (LEAD-6). Lancet 374:9683 (2009), 39–47 [Epub 2009/06/12].
249. Jones, M.R., Hall, O.M., Kaye, A.M., Kaye, A.D., Drug-induced acute pancreatitis: a review. Ochsner J 15:1 (2015), 45–51 [Epub 2015/04/02].
250. Faillie, J.L., Babai, S., Crepin, S., Bres, V., Laroche, M.L., Le Louet, H., et al. Pancreatitis associated with the use of GLP-1 analogs and DPP-4 inhibitors: a case/non-case study from the French Pharmacovigilance Database. Acta Diabetol 51:3 (2014), 491–497 [Epub 2013/12/20].
251. Egan, A.G., Blind, E., Dunder, K., de Graeff, P.A., Hummer, B.T., Bourcier, T., et al. Pancreatic safety of incretin-based drugs—FDA and EMA assessment. N Engl J Med 370:9 (2014), 794–797 [Epub 2014/02/28].
252. Filippatos, T.D., Panagiotopoulou, T.V., Elisaf, M.S., Adverse effects of GLP-1 receptor agonists. Rev Diabet Stud 11:3–4 (2014), 202–230 [Epub 2015/07/16].
253. Esposito, K., Mosca, C., Brancario, C., Chiodini, P., Ceriello, A., Giugliano, D., GLP-1 receptor agonists and HBA1c target of < 7% in type 2 diabetes: meta-analysis of randomized controlled trials. Curr Med Res Opin 27:8 (2011), 1519–1528 [Epub 2011/06/15].
254. Drucker, D.J., Buse, J.B., Taylor, K., Kendall, D.M., Trautmann, M., Zhuang, D., et al. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study. Lancet 372:9645 (2008), 1240–1250 [Epub 2008/09/11].
255. Kim, D., MacConell, L., Zhuang, D., Kothare, P.A., Trautmann, M., Fineman, M., et al. Effects of once-weekly dosing of a long-acting release formulation of exenatide on glucose control and body weight in subjects with type 2 diabetes. Diabetes Care 30:6 (2007), 1487–1493 [Epub 2007/03/14].
256. Zinman, B., Hoogwerf, B.J., Duran Garcia, S., Milton, D.R., Giaconia, J.M., Kim, D.D., et al. The effect of adding exenatide to a thiazolidinedione in suboptimally controlled type 2 diabetes: a randomized trial. Ann Intern Med 146:7 (2007), 477–485 [Epub 2007/04/04].
257. Buse, J.B., Klonoff, D.C., Nielsen, L.L., Guan, X., Bowlus, C.L., Holcombe, J.H., et al. Metabolic effects of two years of exenatide treatment on diabetes, obesity, and hepatic biomarkers in patients with type 2 diabetes: an interim analysis of data from the open-label, uncontrolled extension of three double-blind, placebo-controlled trials. Clin Ther 29:1 (2007), 139–153 [Epub 2007/03/24].
258. Klonoff, D.C., Buse, J.B., Nielsen, L.L., Guan, X., Bowlus, C.L., Holcombe, J.H., et al. Exenatide effects on diabetes, obesity, cardiovascular risk factors and hepatic biomarkers in patients with type 2 diabetes treated for at least 3 years. Curr Med Res Opin 24:1 (2008), 275–286 [Epub 2007/12/07].
259. Sarkar, G., Alattar, M., Brown, R.J., Quon, M.J., Harlan, D.M., Rother, K.I., Exenatide treatment for 6 months improves insulin sensitivity in adults with type 1 diabetes. Diabetes Care 37:3 (2014), 666–670 [Epub 2013/11/07].
260. Bunck, M.C., Diamant, M., Corner, A., Eliasson, B., Malloy, J.L., Shaginian, R.M., et al. One-year treatment with exenatide improves beta-cell function, compared with insulin glargine, in metformin-treated type 2 diabetic patients: a randomized, controlled trial. Diabetes Care 32:5 (2009), 762–768 [Epub 2009/02/07].
261. Heine, R.J., Van Gaal, L.F., Johns, D., Mihm, M.J., Widel, M.H., Brodows, R.G., Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial. Ann Intern Med 143:8 (2005), 559–569 [Epub 2005/10/19].
262. Barnett, A.H., Burger, J., Johns, D., Brodows, R., Kendall, D.M., Roberts, A., et al. Tolerability and efficacy of exenatide and titrated insulin glargine in adult patients with type 2 diabetes previously uncontrolled with metformin or a sulfonylurea: a multinational, randomized, open-label, two-period, crossover noninferiority trial. Clin Ther 29:11 (2007), 2333–2348 [Epub 2007/12/26].
263. Nauck, M.A., Duran, S., Kim, D., Johns, D., Northrup, J., Festa, A., et al. A comparison of twice-daily exenatide and biphasic insulin aspart in patients with type 2 diabetes who were suboptimally controlled with sulfonylurea and metformin: a non-inferiority study. Diabetologia 50:2 (2007), 259–267 [Epub 2006/12/13].
264. Blonde, L., Klein, E.J., Han, J., Zhang, B., Mac, S.M., Poon, T.H., et al. Interim analysis of the effects of exenatide treatment on A1C, weight and cardiovascular risk factors over 82 weeks in 314 overweight patients with type 2 diabetes. Diabetes Obes Metab 8:4 (2006), 436–447 [Epub 2006/06/17].
265. Bergenstal, R., Lewin, A., Bailey, T., Chang, D., Gylvin, T., Roberts, V., Efficacy and safety of biphasic insulin aspart 70/30 versus exenatide in subjects with type 2 diabetes failing to achieve glycemic control with metformin and a sulfonylurea. Curr Med Res Opin 25:1 (2009), 65–75 [Epub 2009/02/13].
266. DeFronzo, R.A., Okerson, T., Viswanathan, P., Guan, X., Holcombe, J.H., MacConell, L., Effects of exenatide versus sitagliptin on postprandial glucose, insulin and glucagon secretion, gastric emptying, and caloric intake: a randomized, cross-over study. Curr Med Res Opin 24:10 (2008), 2943–2952 [Epub 2008/09/13].
267. Frias, J.P., Guja, C., Hardy, E., Ahmed, A., Dong, F., Ohman, P., et al. Exenatide once weekly plus dapagliflozin once daily versus exenatide or dapagliflozin alone in patients with type 2 diabetes inadequately controlled with metformin monotherapy (DURATION-8): a 28 week, multicentre, double-blind, phase 3, randomised controlled trial. Lancet Diabetes Endocrinol 4:12 (2016), 1004–1016 [Epub 2016/09/22].
268. Agerso, H., Jensen, L.B., Elbrond, B., Rolan, P., Zdravkovic, M., The pharmacokinetics, pharmacodynamics, safety and tolerability of NN2211, a new long-acting GLP-1 derivative, in healthy men. Diabetologia 45:2 (2002), 195–202 [Epub 2002/04/06].
269. Juhl, C.B., Hollingdal, M., Sturis, J., Jakobsen, G., Agerso, H., Veldhuis, J., et al. Bedtime administration of NN2211, a long-acting GLP-1 derivative, substantially reduces fasting and postprandial glycemia in type 2 diabetes. Diabetes 51:2 (2002), 424–429 [Epub 2002/01/29].
270. Vilsboll, T., Brock, B., Perrild, H., Levin, K., Lervang, H.H., Kolendorf, K., et al. Liraglutide, a once-daily human GLP-1 analogue, improves pancreatic B-cell function and arginine-stimulated insulin secretion during hyperglycaemia in patients with type 2 diabetes mellitus. Diabet Med 25:2 (2008), 152–156 [Epub 2008/01/19].
271. Bjerre Knudsen, L., Madsen, L.W., Andersen, S., Almholt, K., de Boer, A.S., Drucker, D.J., et al. Glucagon-like Peptide-1 receptor agonists activate rodent thyroid C-cells causing calcitonin release and C-cell proliferation. Endocrinology 151:4 (2010), 1473–1486 [Epub 2010/03/06].
272. Buse, J.B., Sesti, G., Schmidt, W.E., Montanya, E., Chang, C.T., Xu, Y., et al. Switching to once-daily liraglutide from twice-daily exenatide further improves glycemic control in patients with type 2 diabetes using oral agents. Diabetes Care 33:6 (2010), 1300–1303 [Epub 2010/03/25].
273. Marre, M., Shaw, J., Brandle, M., Bebakar, W.M., Kamaruddin, N.A., Strand, J., et al. Liraglutide, a once-daily human GLP-1 analogue, added to a sulphonylurea over 26 weeks produces greater improvements in glycaemic and weight control compared with adding rosiglitazone or placebo in subjects with type 2 diabetes (LEAD-1 SU). Diabet Med 26:3 (2009), 268–278 [Epub 2009/03/26].
274. Nauck, M., Frid, A., Hermansen, K., Shah, N.S., Tankova, T., Mitha, I.H., et al. Efficacy and safety comparison of liraglutide, glimepiride, and placebo, all in combination with metformin, in type 2 diabetes: the LEAD (liraglutide effect and action in diabetes)-2 study. Diabetes Care 32:1 (2009), 84–90 [Epub 2008/10/22].
275. Vilsboll, T., Zdravkovic, M., Le-Thi, T., Krarup, T., Schmitz, O., Courreges, J.P., et al. Liraglutide, a long-acting human glucagon-like peptide-1 analog, given as monotherapy significantly improves glycemic control and lowers body weight without risk of hypoglycemia in patients with type 2 diabetes. Diabetes Care 30:6 (2007), 1608–1610 [Epub 2007/03/21].
276. Garber, A., Henry, R., Ratner, R., Garcia-Hernandez, P.A., Rodriguez-Pattzi, H., Olvera-Alvarez, I., et al. Liraglutide versus glimepiride monotherapy for type 2 diabetes (LEAD-3 Mono): a randomised, 52-week, phase III, double-blind, parallel-treatment trial. Lancet 373:9662 (2009), 473–481 [Epub 2008/09/30].
277. Zinman, B., Gerich, J., Buse, J.B., Lewin, A., Schwartz, S., Raskin, P., et al. Efficacy and safety of the human glucagon-like peptide-1 analog liraglutide in combination with metformin and thiazolidinedione in patients with type 2 diabetes (LEAD-4 Met + TZD). Diabetes Care 32:7 (2009), 1224–1230 [Epub 2009/03/18].
278. Russell-Jones, D., Vaag, A., Schmitz, O., Sethi, B.K., Lalic, N., Antic, S., et al. Liraglutide vs insulin glargine and placebo in combination with metformin and sulfonylurea therapy in type 2 diabetes mellitus (LEAD-5 met + SU): a randomised controlled trial. Diabetologia 52:10 (2009), 2046–2055 [Epub 2009/08/19].
279. Buse, J.B., Drucker, D.J., Taylor, K.L., Kim, T., Walsh, B., Hu, H., et al. DURATION-1: exenatide once weekly produces sustained glycemic control and weight loss over 52 weeks. Diabetes Care 33:6 (2010), 1255–1261 [Epub 2010/03/11].
280. Funch, D., Gydesen, H., Tornoe, K., Major-Pedersen, A., Chan, K.A., A prospective, claims-based assessment of the risk of pancreatitis and pancreatic cancer with liraglutide compared to other antidiabetic drugs. Diabetes Obes Metab 16:3 (2014), 273–275 [Epub 2013/11/10].
281. Pratley, R.E., Nauck, M., Bailey, T., Montanya, E., Cuddihy, R., Filetti, S., et al. Liraglutide versus sitagliptin for patients with type 2 diabetes who did not have adequate glycaemic control with metformin: a 26-week, randomised, parallel-group, open-label trial. Lancet 375:9724 (2010), 1447–1456 [Epub 2010/04/27].
282. Gutzwiller, J.P., Tschopp, S., Bock, A., Zehnder, C.E., Huber, A.R., Kreyenbuehl, M., et al. Glucagon-like peptide 1 induces natriuresis in healthy subjects and in insulin-resistant obese men. J Clin Endocrinol Metab 89:6 (2004), 3055–3061 [Epub 2004/06/08].
283. Pi-Sunyer, X., Astrup, A., Fujioka, K., Greenway, F., Halpern, A., Krempf, M., et al. A randomized, controlled trial of 3.0 mg of liraglutide in weight management. N Engl J Med 373:1 (2015), 11–22 [Epub 2015/07/03].
284. Nauck, M.A., Petrie, J.R., Sesti, G., Mannucci, E., Courreges, J.P., Lindegaard, M.L., et al. A phase 2, randomized, dose-finding study of the novel once-weekly human GLP-1 analog, semaglutide, compared with placebo and open-label liraglutide in patients with type 2 diabetes. Diabetes Care 39:2 (2016), 231–241 [Epub 2015/09/12].
285. Giorgino, F., Benroubi, M., Sun, J.H., Zimmermann, A.G., Pechtner, V., Efficacy and safety of once-weekly dulaglutide versus insulin glargine in patients with type 2 diabetes on metformin and glimepiride (AWARD-2). Diabetes Care 38:12 (2015), 2241–2249 [Epub 2015/06/20].
286. Blonde, L., Jendle, J., Gross, J., Woo, V., Jiang, H., Fahrbach, J.L., et al. Once-weekly dulaglutide versus bedtime insulin glargine, both in combination with prandial insulin lispro, in patients with type 2 diabetes (AWARD-4): a randomised, open-label, phase 3, non-inferiority study. Lancet 385:9982 (2015), 2057–2066 [Epub 2015/05/27].
287. Karagiannis, T., Liakos, A., Bekiari, E., Athanasiadou, E., Paschos, P., Vasilakou, D., et al. Efficacy and safety of once-weekly glucagon-like peptide 1 receptor agonists for the management of type 2 diabetes: a systematic review and meta-analysis of randomized controlled trials. Diabetes Obes Metab 17:11 (2015), 1065–1074 [Epub 2015/09/24].
288. Werner, U., Haschke, G., Herling, A.W., Kramer, W., Pharmacological profile of lixisenatide: a new GLP-1 receptor agonist for the treatment of type 2 diabetes. Regul Pept 164:2–3 (2010), 58–64 [Epub 2010/06/24].
289. Pfeffer, M.A., Claggett, B., Diaz, R., Dickstein, K., Gerstein, H.C., Kober, L.V., et al. Lixisenatide in patients with type 2 diabetes and acute coronary syndrome. N Engl J Med 373:23 (2015), 2247–2257 [Epub 2015/12/03].
290. Eng, C., Kramer, C.K., Zinman, B., Retnakaran, R., Glucagon-like peptide-1 receptor agonist and basal insulin combination treatment for the management of type 2 diabetes: a systematic review and meta-analysis. Lancet 384:9961 (2014), 2228–2234 [Epub 2014/09/16].
291. Diamant, M., Nauck, M.A., Shaginian, R., Malone, J.K., Cleall, S., Reaney, M., et al. Glucagon-like peptide 1 receptor agonist or bolus insulin with optimized basal insulin in type 2 diabetes. Diabetes Care 37:10 (2014), 2763–2773 [Epub 2014/07/12].
292. Marso, S.P., Daniels, G.H., Brown-Frandsen, K., Kristensen, P., Mann, J.F., Nauck, M.A., et al. Liraglutide and cardiovascular outcomes in type 2 diabetes. N Engl J Med 375:4 (2016), 311–322 [Epub 2016/06/14].
293. Robinson, L.E., Holt, T.A., Rees, K., Randeva, H.S., O'Hare, J.P., Effects of exenatide and liraglutide on heart rate, blood pressure and body weight: systematic review and meta-analysis. BMJ Open, 3(1), 2013 [Epub 2013/01/29].
294. Rutten, G.E., Tack, C.J., Pieber, T.R., Comlekci, A., Orsted, D.D., Baeres, F.M., et al. LEADER 7: cardiovascular risk profiles of US and European participants in the LEADER diabetes trial differ. Diabetol Metab Syndr, 8, 2016, 37 [Epub 2016/06/09].
295. Kumarathurai, P., Anholm, C., Nielsen, O.W., Kristiansen, O.P., Molvig, J., Madsbad, S., et al. Effects of the glucagon-like peptide-1 receptor agonist liraglutide on systolic function in patients with coronary artery disease and type 2 diabetes: a randomized double-blind placebo-controlled crossover study. Cardiovasc Diabetol, 15(1), 2016, 105 [Epub 2016/07/28].
296. Holman, R.R., Bethel, M.A., George, J., Sourij, H., Doran, Z., Keenan, J., et al. Rationale and design of the EXenatide Study of Cardiovascular Event Lowering (EXSCEL) trial. Am Heart J 174 (2016), 103–110 [Epub 2016/03/21].
297. Roos, S.T., Timmers, L., Biesbroek, P.S., Nijveldt, R., Kamp, O., van Rossum, A.C., et al. No benefit of additional treatment with exenatide in patients with an acute myocardial infarction. Int J Cardiol 220 (2016), 809–814 [Epub 2016/07/11].
298. Gamble, J.M., Thomas, J.M., Twells, L.K., Midodzi, W.K., Majumdar, S.R., Comparative effectiveness of incretin-based therapies and the risk of death and cardiovascular events in 38,233 metformin monotherapy users. Medicine, 95(26), 2016, e3995 [Epub 2016/07/02].
299. Wang, T., Wang, F., Zhou, J., Tang, H., Giovenale, S., Adverse effects of incretin-based therapies on major cardiovascular and arrhythmia events: meta-analysis of randomized trials. Diabetes Metab Res Rev 32:8 (2016), 843–857.
300. Marso, S.P., Bain, S.C., Consoli, A., Eliaschewitz, F.G., Jodar, E., Leiter, L.A., et al. Semaglutide and cardiovascular outcomes in patients with type 2 diabetes. N Engl J Med 375:19 (2016), 1834–1844 [Epub 2016/09/17].
301. Marso, S.P., Bain, S.C., Consoli, A., Eliaschewitz, F.G., Jodar, E., Leiter, L.A., et al. Semaglutide and cardiovascular outcomes in patients with type 2 diabetes. N Engl J Med 375:19 (2016), 1834–1844.
302. Gerich, J.E., Role of the kidney in normal glucose homeostasis and in the hyperglycaemia of diabetes mellitus: therapeutic implications. Diabet Med 27:2 (2010), 136–142 [Epub 2010/06/16].
303. Ferrannini, E., Solini, A., SGLT2 inhibition in diabetes mellitus: rationale and clinical prospects. Nat Rev Endocrinol 8:8 (2012), 495–502 [Epub 2012/02/09].
304. Hediger, M.A., Rhoads, D.B., Molecular physiology of sodium-glucose cotransporters. Physiol Rev 74:4 (1994), 993–1026 [Epub 1994/10/01].
305. Wright, E.M., Loo, D.D., Hirayama, B.A., Biology of human sodium glucose transporters. Physiol Rev 91:2 (2011), 733–794 [Epub 2011/04/30].
306. Rahmoune, H., Thompson, P.W., Ward, J.M., Smith, C.D., Hong, G., Brown, J., Glucose transporters in human renal proximal tubular cells isolated from the urine of patients with non-insulin-dependent diabetes. Diabetes 54:12 (2005), 3427–3434 [Epub 2005/11/25].
307. Mogensen, C.E., Maximum tubular reabsorption capacity for glucose and renal hemodynamcis during rapid hypertonic glucose infusion in normal and diabetic subjects. Scand J Clin Lab Invest 28:1 (1971), 101–109 [Epub 1971/09/01].
308. DeFronzo, R.A., Davidson, J.A., Del Prato, S., The role of the kidneys in glucose homeostasis: a new path towards normalizing glycaemia. Diabetes Obes Metab 14:1 (2012), 5–14 [Epub 2011/10/01].
309. Ohgaki, R., Wei, L., Yamada, K., Hara, T., Kuriyama, C., Okuda, S., et al. Interaction of the sodium/glucose cotransporter (SGLT) 2 inhibitor canagliflozin with SGLT1 and SGLT2. J Pharmacol Exp Ther 358:1 (2016), 94–102 [Epub 2016/05/18].
310. Katsiki, N., Mikhailidis, D.P., Theodorakis, M.J., Sodium-glucose cotransporter 2 inhibitors (SGLT2i): their role in cardiometabolic risk management. Curr Pharm Des 23:10 (2017), 1522–1532.
311. Handelsman, Y., Henry, R.R., Bloomgarden, Z.T., Dagogo-Jack, S., DeFronzo, R.A., Einhorn, D., et al. American Association of Clinical Endocrinologists and American College of Endocrinology Position Statement on the Association of Sglt-2 Inhibitors and Diabetic Ketoacidosis. Endocr Pract 22:6 (2016), 753–762 [Epub 2016/04/16].
312. Deol, H., Lekkakou, L., Viswanath, A.K., Pappachan, J.M., Combination therapy with GLP-1 analogues and SGLT-2 inhibitors in the management of diabesity: the real world experience. Endocrine 55:1 (2017), 173–178 [Epub 2016/10/04].
313. Stenlof, K., Cefalu, W.T., Kim, K.A., Alba, M., Usiskin, K., Tong, C., et al. Efficacy and safety of canagliflozin monotherapy in subjects with type 2 diabetes mellitus inadequately controlled with diet and exercise. Diabetes Obes Metab 15:4 (2013), 372–382 [Epub 2013/01/03].
314. Rosenstock, J., Aggarwal, N., Polidori, D., Zhao, Y., Arbit, D., Usiskin, K., 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 35:6 (2012), 1232–1238 [Epub 2012/04/12].
315. Wilding, J.P., Charpentier, G., Hollander, P., Gonzalez-Galvez, G., Mathieu, C., Vercruysse, F., et al. Efficacy and safety of canagliflozin in patients with type 2 diabetes mellitus inadequately controlled with metformin and sulphonylurea: a randomised trial. Int J Clin Pract 67:12 (2013), 1267–1282 [Epub 2013/10/15].
316. Cefalu, W.T., Leiter, L.A., Yoon, K.H., Arias, P., Niskanen, L., Xie, J., 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 382:9896 (2013), 941–950 [Epub 2013/07/16].
317. Schernthaner, G., Gross, J.L., Rosenstock, J., Guarisco, M., Fu, M., Yee, 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 36:9 (2013), 2508–2515 [Epub 2013/04/09].
318. Yale, J.F., Bakris, G., Cariou, B., Yue, D., David-Neto, E., Xi, L., et al. Efficacy and safety of canagliflozin in subjects with type 2 diabetes and chronic kidney disease. Diabetes Obes Metab 15:5 (2013), 463–473 [Epub 2013/03/08].
319. Lavalle-Gonzalez, F.J., Januszewicz, A., Davidson, J., Tong, C., Qiu, R., Canovatchel, W., 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 56:12 (2013), 2582–2592 [Epub 2013/09/13].
320. Devineni, D., Morrow, L., Hompesch, M., Skee, D., Vandebosch, A., Murphy, J., et al. Canagliflozin improves glycaemic control over 28 days in subjects with type 2 diabetes not optimally controlled on insulin. Diabetes Obes Metab 14:6 (2012), 539–545 [Epub 2012/01/10].
321. Watts, N.B., Bilezikian, J.P., Usiskin, K., Edwards, R., Desai, M., Law, G., et al. Effects of canagliflozin on fracture risk in patients with type 2 diabetes mellitus. J Clin Endocrinol Metab 101:1 (2016), 157–166 [Epub 2015/11/19].
322. Blevins, T.C., Farooki, A., Bone effects of canagliflozin, a sodium glucose co-transporter 2 inhibitor, in patients with type 2 diabetes mellitus. Postgrad Med 129:1 (2017), 159–168 [Epub 2016/11/30].
323. Mannucci, E., Monami, M., Bone fractures with sodium-glucose co-transporter-2 inhibitors: how real is the risk?. Drug Saf 40:2 (2017), 115–119 [Epub 2016/11/09].
324. Alba, M., Xie, J., Fung, A., Desai, M., The effects of canagliflozin, a sodium glucose co-transporter 2 inhibitor, on mineral metabolism and bone in patients with type 2 diabetes mellitus. Curr Med Res Opin 32:8 (2016), 1375–1385 [Epub 2016/04/06].
325. Ljunggren, O., Bolinder, J., Johansson, L., Wilding, J., Langkilde, A.M., Sjostrom, C.D., et al. Dapagliflozin has no effect on markers of bone formation and resorption or bone mineral density in patients with inadequately controlled type 2 diabetes mellitus on metformin. Diabetes Obes Metab 14:11 (2012), 990–999 [Epub 2012/06/02].
326. Davies, M.J., Merton, K., Vijapurkar, U., Yee, J., Qiu, R., Efficacy and safety of canagliflozin in patients with type 2 diabetes based on history of cardiovascular disease or cardiovascular risk factors: a post hoc analysis of pooled data. Cardiovasc Diabetol, 16(1), 2017, 40 [Epub 2017/03/23].
327. Messana, J.A., Schwartz, S.S., Townsend, R.R., An evidence-based practice-oriented review focusing on canagliflozin in the management of type 2 diabetes. Vasc Health Risk Manag 13 (2017), 43–54 [Epub 2017/03/04].
328. Davies, M.J., Merton, K.W., Vijapurkar, U., Balis, D.A., Desai, M., Canagliflozin improves risk factors of metabolic syndrome in patients with type 2 diabetes mellitus and metabolic syndrome. Diabetes Metab Syndr Obes 10 (2017), 47–55 [Epub 2017/02/12].
329. Lee, S., Update on SGLT2 inhibitors-new data released at the American Diabetes Association. Crit Pathw Cardiol 16:3 (2017), 93–95 [Epub 2017/07/26].
330. Zhang, M., Zhang, L., Wu, B., Song, H., An, Z., Li, S., Dapagliflozin treatment for type 2 diabetes: a systematic review and meta-analysis of randomized controlled trials. Diabetes Metab Res Rev 30:3 (2014), 204–221 [Epub 2013/10/12].
331. Sun, Y.N., Zhou, Y., Chen, X., Che, W.S., Leung, S.W., The efficacy of dapagliflozin combined with hypoglycaemic drugs in treating type 2 diabetes mellitus: meta-analysis of randomised controlled trials. BMJ Open, 4(4), 2014, e004619 [Epub 2014/04/09].
332. Leiter, L.A., Cefalu, W.T., de Bruin, T.W., Xu, J., Parikh, S., Johnsson, E., et al. Long-term maintenance of efficacy of dapagliflozin in patients with type 2 diabetes mellitus and cardiovascular disease. Diabetes Obes Metab 18:8 (2016), 766–774 [Epub 2016/03/25].
333. Weber, M.A., Mansfield, T.A., Cain, V.A., Iqbal, N., Parikh, S., Ptaszynska, A., Blood pressure and glycaemic effects of dapagliflozin versus placebo in patients with type 2 diabetes on combination antihypertensive therapy: a randomised, double-blind, placebo-controlled, phase 3 study. Lancet Diabetes Endocrinol 4:3 (2016), 211–220 [Epub 2015/12/02].
334. Liakos, A., Karagiannis, T., Athanasiadou, E., Sarigianni, M., Mainou, M., Papatheodorou, K., et al. Efficacy and safety of empagliflozin for type 2 diabetes: a systematic review and meta-analysis. Diabetes Obes Metab 16:10 (2014), 984–993 [Epub 2014/04/29].
335. Haring, H.U., Merker, L., Seewaldt-Becker, E., Weimer, M., Meinicke, T., Broedl, U.C., 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 37:6 (2014), 1650–1659 [Epub 2014/04/12].
336. Chino, Y., Samukawa, Y., Sakai, S., Nakai, Y., Yamaguchi, J., Nakanishi, T., et al. SGLT2 inhibitor lowers serum uric acid through alteration of uric acid transport activity in renal tubule by increased glycosuria. Biopharm Drug Dispos 35:7 (2014), 391–404 [Epub 2014/07/22].
337. Fioretto, P., Zambon, A., Rossato, M., Busetto, L., Vettor, R., SGLT2 inhibitors and the diabetic kidney. Diabetes Care 39:Suppl. 2 (2016), S165–71 [Epub 2016/07/22].
338. Zinman, B., Wanner, C., Lachin, J.M., Fitchett, D., Bluhmki, E., Hantel, S., et al. Empagliflozin, cardiovascular outcomes, and mortality in type 2 diabetes. N Engl J Med 373:22 (2015), 2117–2128 [Epub 2015/09/18].
339. Chamberlain, J.J., Herman, W.H., Leal, S., Rhinehart, A.S., Shubrook, J.H., Skolnik, N., et al. Pharmacologic therapy for type 2 diabetes: synopsis of the 2017 American Diabetes Association Standards of Medical Care in Diabetes. Ann Intern Med 166:8 (2017), 572–578.
340. Salsali, A., Kim, G., Woerle, H.J., Broedl, U.C., Hantel, S., Cardiovascular safety of empagliflozin in patients with type 2 diabetes: a meta-analysis of data from randomized placebo-controlled trials. Diabetes Obes Metab 18:10 (2016), 1034–1040 [Epub 2016/07/05].
341. Wu, J.H., Foote, C., Blomster, J., Toyama, T., Perkovic, V., Sundstrom, J., et al. Effects of sodium-glucose cotransporter-2 inhibitors on cardiovascular events, death, and major safety outcomes in adults with type 2 diabetes: a systematic review and meta-analysis. Lancet Diabetes Endocrinol 4:5 (2016), 411–419 [Epub 2016/03/25].
342. Sonesson, C., Johansson, P.A., Johnsson, E., Gause-Nilsson, I., Cardiovascular effects of dapagliflozin in patients with type 2 diabetes and different risk categories: a meta-analysis. Cardiovasc Diabetol, 15, 2016, 37 [Epub 2016/02/21].
343. Wanner, C., Inzucchi, S.E., Lachin, J.M., Fitchett, D., von Eynatten, M., Mattheus, M., et al. Empagliflozin and progression of kidney disease in type 2 diabetes. N Engl J Med 375:4 (2016), 323–334 [Epub 2016/06/15].
344. Kashiwagi, A., Maegawa, H., Metabolic and hemodynamic effects of sodium-dependent glucose co-transporter 2 inhibitors on cardio-renal protection in the treatment of patients with type 2 diabetes mellitus. J Diabetes Investig 8:4 (2017), 416–427.
345. Abdul-Ghani, M., Del Prato, S., Chilton, R., DeFronzo, R.A., SGLT2 inhibitors and cardiovascular risk: lessons learned from the EMPA-REG OUTCOME study. Diabetes Care 39:5 (2016), 717–725 [Epub 2016/05/22].
346. Kosiborod, M., Cavender, M.A., Fu, A.Z., Wilding, J.P., Khunti, K., Holl, R.W., et al. Lower risk of heart failure and death in patients initiated on SGLT-2 inhibitors versus other glucose-lowering drugs: the CVD-REAL study. Circulation 136:3 (2017), 249–259.
347. Inzucchi, S.E., Zinman, B., Wanner, C., Ferrari, R., Fitchett, D., Hantel, S., et al. SGLT-2 inhibitors and cardiovascular risk: proposed pathways and review of ongoing outcome trials. Diab Vasc Dis Res 12:2 (2015), 90–100 [Epub 2015/01/16].
348. Scranton, R.E., Gaziano, J.M., Rutty, D., Ezrokhi, M., Cincotta, A., A randomized, double-blind, placebo-controlled trial to assess safety and tolerability during treatment of type 2 diabetes with usual diabetes therapy and either Cycloset or placebo. BMC Endocr Disord, 7, 2007, 3 [Epub 2007/06/27].
349. Morrow, D.A., Scirica, B.M., Chaitman, B.R., McGuire, D.K., Murphy, S.A., Karwatowska-Prokopczuk, E., et al. Evaluation of the glycometabolic effects of ranolazine in patients with and without diabetes mellitus in the MERLIN-TIMI 36 randomized controlled trial. Circulation 119:15 (2009), 2032–2039 [Epub 2009/04/08].
350. Fleischman, A., Shoelson, S.E., Bernier, R., Goldfine, A.B., Salsalate improves glycemia and inflammatory parameters in obese young adults. Diabetes Care 31:2 (2008), 289–294 [Epub 2007/10/26].
351. Higgins, L.S., Mantzoros, C.S., The development of INT131 as a selective PPARgamma modulator: approach to a safer insulin sensitizer. PPAR Res, 2008, 2008, 936906 [Epub 2008/09/05].
352. Johnson, T.O., Ermolieff, J., Jirousek, M.R., Protein tyrosine phosphatase 1B inhibitors for diabetes. Nat Rev Drug Discov 1:9 (2002), 696–709 [Epub 2002/09/05].
353. Muchmore, D.B., Vaughn, D.E., Accelerating and improving the consistency of rapid-acting analog insulin absorption and action for both subcutaneous injection and continuous subcutaneous infusion using recombinant human hyaluronidase. J Diabetes Sci Technol 6:4 (2012), 764–772 [Epub 2012/08/28].
354. Pozzilli, P., Leslie, R.D., Chan, J., De Fronzo, R., Monnier, L., Raz, I., et al. The A1C and ABCD of glycaemia management in type 2 diabetes: a physician's personalized approach. Diabetes Metab Res Rev 26:4 (2010), 239–244 [Epub 2010/05/27].
355. Paschou, S.A., Leslie, R.D., Personalizing guidelines for diabetes management: twilight or dawn of the expert?. BMC Med, 11, 2013, 161 [Epub 2013/07/12].
356. McFarland, M.S., Knight, T.N., Brown, A., Thomas, J., The continuation of oral medications with the initiation of insulin therapy in type 2 diabetes: a review of the evidence. South Med J 103:1 (2010), 58–65 [Epub 2009/12/10].
357. Holman, R.R., Paul, S.K., Bethel, M.A., Matthews, D.R., Neil, H.A., 10-year follow-up of intensive glucose control in type 2 diabetes. N Engl J Med 359:15 (2008), 1577–1589 [Epub 2008/09/12].
358. Cheung, N.W., Conn, J.J., d'Emden, M.C., Gunton, J.E., Jenkins, A.J., Ross, G.P., et al. Position statement of the Australian Diabetes Society: individualisation of glycated haemoglobin targets for adults with diabetes mellitus. Med J Aust 191:6 (2009), 339–344 [Epub 2009/09/23].