Incretin-based therapies for obesity treatment

Metabolism: Clinical and Experimental

Volumn 64, Issue 9, 2015, Pages 967-981

  De Mello, Aline Haas ^a   Prá, Morgana ^a   Cardoso, Larissa Colonetti ^a   De Bona Schraiber, Rosiane ^a   Rezin, Gislaine Tezza ^a,b  

^a UNIVERSITY OF SOUTHERN SANTA CATARINA   (Brazil)

^b HOSPITAL NOSSA SENHORA DA CONCEIÇÃO   (Brazil)

Author keywords

DPP 4; GLP 1; Incretin; Obesity; Treatment

Indexed keywords

ALOGLIPTIN; ANTIDIABETIC AGENT; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; EXENDIN 4; GLIBENCLAMIDE; GLIMEPIRIDE; GLIPIZIDE; GLUCAGON LIKE PEPTIDE 1; GLUCAGON LIKE PEPTIDE 1 RECEPTOR AGONIST; INCRETIN; INSULIN ASPART; INSULIN GLARGINE; LINAGLIPTIN; LIRAGLUTIDE; LIXISENATIDE; METFORMIN; PIOGLITAZONE; SAXAGLIPTIN; SITAGLIPTIN; VILDAGLIPTIN; ANTIOBESITY AGENT; GASTRIC INHIBITORY POLYPEPTIDE RECEPTOR; HORMONE RECEPTOR;

ARTICLE; BODY WEIGHT; GLUCOSE BLOOD LEVEL; GLUCOSE HOMEOSTASIS; HEART PROTECTION; HUMAN; NON INSULIN DEPENDENT DIABETES MELLITUS; OBESITY; PRIORITY JOURNAL; STOMACH EMPTYING; WEIGHT REDUCTION; AGONISTS; ANIMAL; ANTAGONISTS AND INHIBITORS; PATHOPHYSIOLOGY; PHYSIOLOGY;

ANIMALS; ANTI-OBESITY AGENTS; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; GLUCAGON-LIKE PEPTIDE 1; HUMANS; INCRETINS; OBESITY; RECEPTORS, GASTROINTESTINAL HORMONE;

EID: 84939565602     PISSN: 00260495     EISSN: 15328600     Source Type: Journal    
DOI: 10.1016/j.metabol.2015.05.012     Document Type: Review

References (136)

1. World Health Organization (WHO) Obesity and overweight - fact sheet N°311. 2013 Retrieved April 20, 2014, from: http://www.who.int/mediacentre/factsheets/fs311/en/
2. World Obesity Federation About obesity Retrieved April 20, 2014, from: http://www.worldobesity.org/aboutobesity/ 2012
3. S.F. Kirk, T.L. Penney, T.L. McHugh, and A.M. Sharma Effective weight management practice: a review of the lifestyle intervention evidence Int J Obes (Lond) 36 2012 178 185 10.1038/ijo.2011
4. S.L. Thomas, J. Hyde, A. Karunaratne, R. Kausman, and P.A. Komesaroff "They all work...when you stick to them": a qualitative investigation of dieting, weight loss, and physical exercise, in obese individuals Nutr J 7 2008 34 10.1186/1475-2891-7-34
5. Associação Brasileira para o Estudo da Obesidade e da Síndrome Metabólica (ABESO) Atualização das Diretrizes para o Tratamento Farmacológico da Obesidade e do Sobrepeso: Posicionamento Oficial da ABESO/ SBEM - 2010 Retrieved July 25, 2014, from: http://www.abeso.org.br/pdf/ diretrizes2010.pdf
6. W. Coutinho The first decade of sibutramine and orlistat: a reappraisal of their expanding roles in the treatment of obesity and associated conditions Arq Bras Endocrinol Metabol 53 2009 262 270
7. A.M. Faria, M.C. Mancini, M.E. Melo, C. Cercato, and A. Halpern Progressos recentes e novas perspectivas em farmacoterapia da obesidade Arq Bras Endocrinol Metabol 54 2010 516 529
8. B.M. Cheung, T.T. Cheung, and N.R. Samaranayake Safety of antiobesity drugs Ther Adv Drug Saf 4 2013 171 181 10.1177/2042098613489721
9. M. Baretić Targets for medical therapy in obesity Dig Dis 30 2012 168 172 10.1159/000336672
10. S. Manning, A. Pucci, and N. Finer Pharmacotherapy for obesity: novel agents and paradigms Ther Adv Chronic Dis 5 2014 135 148 10.1177/2040622314522848
11. Y. Seino, and D. Yabe Glucose-dependent insulinotropic polypeptide and glucagon-like peptide-1: Incretin actions beyond the pancreas J Diabetes Investig 4 2013 108 130 10.1111/jdi.12065
12. J. Seufert, and B. Gallwitz The extra-pancreatic effects of GLP-1 receptor agonists: a focus on the cardiovascular, gastrointestinal and central nervous systems Diabetes Obes Metab 16 2014 673 688 10.1111/dom.12251
13. J.J. Holst Incretin hormones and the satiation signal Int J Obes (Lond) 37 2013 1161 1168 10.1038/ijo.2012.208
14. S.Y. Ng, and J.P. Wilding Liraglutide in the treatment of obesity Expert Opin Biol Ther 14 2014 1215 1224 10.1517/14712598.2014.925870
15. B. Gallwitz, J. Rosenstock, T. Rauch, S. Bhattacharya, S. Patel, M. von Eynatten, and 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 2012 10.1016/S0140-6736(12)60691-6
16. J.H. Martin, C.F. Deacon, M.D. Gorrell, and J.B. Prins Incretin-based therapies - review of the physiology, pharmacology and emerging clinical experience Intern Med J 41 2011 299 307 10.1111/j.1445-5994.2011.02439.x
17. J.E. Campbell, and D.J. Drucker Pharmacology, physiology, and mechanisms of incretin hormone action Cell Metab 17 2013 819 837 10.1016/j.cmet.2013.04.008
18. B. Gallwitz Extra-pancreatic effects of incretin-based therapies Endocrine 47 2014 360 371 10.1007/s12020-014-0223-0
19. L. van Bloemendaal, J.S. Ten Kulve, S.E. la Fleur, R.G. Ijzerman, and M. Diamant Effects of glucagon-like peptide 1 on appetite and body weight: focus on the CNS J Endocrinol 221 2014 T1 T16 10.1530/JOE-13-0414
20. U.S. Food and Drug Administration (FDA) FDA approves weight-management drug Saxenda Retrieved January 19, 2015, from: http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm427913.htm 2014
21. J.J. Holst The physiology of glucagon-like peptide 1 Physiol Rev 87 2007 1409 1439
22. P.A. Maranhão, E. Bouskela, and L.G.K. Aguiar Lipemia pós-prandial e incretinas na reatividade endotelial Rev HUPE 13 2014 80 86
23. D.J. Drucker The biology of incretin hormones Cell Metab 3 2006 153 165
24. L.L. Baggio, and D.J. Drucker Biology of incretins: GLP-1 and GIP Gastroenterology 132 2007 2131 2157
25. D.J. Drucker, and M.A. Nauck The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes Lancet 368 2006 1696 1705
26. T. Wikarek, J. Chudek, A. Owczarek, and M. Olszanecka-Glinianowicz Effect of dietary macronutrients on postprandial incretin hormone release and satiety in obese and normal-weight women Br J Nutr 111 2014 236 246 10.1017/S0007114513002389
27. P.J. Larsen Mechanisms behind GLP-1 induced weight loss Br J Diabetes Vasc Dis 8 Suppl. 2 2008 S34 S41 10.1177/1474651408100525
28. T. Edholm, M. Degerblad, P. Grybäck, L. Hilsted, J.J. Holst, H. Jacobsson, and et al. Differential incretin effects of GIP and GLP-1 on gastric emptying, appetite, and insulin-glucose homeostasis Neurogastroenterol Motil 22 2010 1191 1200 10.1111/j.1365-2982. 2010.01554.x
29. M. Asmar, W. Tangaa, S. Madsbad, K. Hare, A. Astrup, A. Flint, and et al. On the role of glucose-dependent insulintropic polypeptide in postprandial metabolism in humans Am J Physiol Endocrinol Metab 298 2010 E614 E621 10.1152/ajpendo.00639.2009
30. L. Bouchard, G. Faucher, A. Tchernof, Y. Deshaies, S. Lebel, F.S. Hould, and et al. Comprehensive genetic analysis of the dipeptidyl peptidase-4 gene and cardiovascular disease risk factors in obese individuals Acta Diabetol 46 2009 13 21 10.1007/s00592-008-0049-4
31. V. Turcot, L. Bouchard, G. Faucher, A. Tchernof, Y. Deshaies, L. Pérusse, and et al. DPP4 gene DNA methylation in the omentum is associated with its gene expression and plasma lipid profile in severe obesity Obesity (Silver Spring) 19 2011 388 395 10.1038/oby.2010.198
32. G.S. Panagoulias, and J. Doupis Clinical utility in the treatment of type 2 diabetes with the saxagliptin/metformin fixed combination Patient Prefer Adherence 8 2014 227 236 10.2147/PPA.S34089
33. A. Peters Incretin-based therapies: review of current clinical trial data Am J Med 123 3 Suppl. 2010 S28 S37 10.1016/j.amjmed.2009.12.007
34. N. Mentis, I. Vardarli, L.D. Köthe, J.J. Holst, C.F. Deacon, M. Theodorakis, and et al. GIP does not potentiate the antidiabetic effects of GLP-1 in hyperglycemic patients with type 2 diabetes Diabetes 60 2011 1270 1276 10.2337/db10-1332
35. D. Russell-Jones, and S. Gough Recent advances in incretin-based therapies Clin Endocrinol (Oxf) 77 2012 489 499 10.1111/j.1365-2265.2012.04483.x
36. J. van Can, B. Sloth, C.B. Jensen, A. Flint, E.E. Blaak, and W.H. Saris Effects of the once-daily GLP-1 analog liraglutide on gastric emptying, glycemic parameters, appetite and energy metabolism in obese, non-diabetic adults Int J Obes (Lond) 38 2014 784 793 10.1038/ijo.2013.162
37. A. Astrup, S. Rössner, L. Van Gaal, A. Rissanen, L. Niskanen, M. Al Hakim, and et al. Effects of liraglutide in the treatment of obesity: a randomised, double-blind, placebo-controlled study Lancet 374 2009 1606 1616 10.1016/S0140-6736(09)61375-1
38. J. Rosenstock, L.J. Klaff, S. Schwartz, J. Northrup, J.H. Holcombe, K. Wilhelm, and et al. Effects of exenatide and lifestyle modification on body weight and glucose tolerance in obese subjects with and without pre-diabetes Diabetes Care 33 2010 1173 1175 10.2337/dc09-1203
39. A. Astrup, R. Carraro, N. Finer, A. Harper, M. Kunesova, M.E. Lean, and et al. Safety, tolerability and sustained weight loss over 2 years with the once-daily human GLP-1 analog, liraglutide Int J Obes (Lond) 36 2012 843 854 10.1038/ijo.2011.158
40. D. Russell-Jones, R.M. Cuddihy, M. Hanefeld, A. Kumar, J.G. González, M. Chan, and et al. Efficacy and safety of exenatide once weekly versus metformin, pioglitazone, and sitagliptin used as monotherapy in drug-naive patients with type 2 diabetes (DURATION-4): a 26-week double-blind study Diabetes Care 35 2012 252 258 10.2337/dc11-1107
41. T. Vilsbøll, M. Christensen, A.E. Junker, F.K. Knop, and L.L. Gluud Effects of glucagon-like peptide-1 receptor agonists on weight loss: systematic review and meta-analyses of randomised controlled trials BMJ 344 2012 d7771 10.1136/bmj.d7771
42. J.B. Buse, M. Nauck, T. Forst, W.H. Sheu, S.K. Shenouda, C.R. Heilmann, and et al. Exenatide once weekly versus liraglutide once daily in patients with type 2 diabetes (DURATION-6): a randomised, open-label study Lancet 38 2013 117 124 10.1016/S0140-6736(12)61267-7
43. L.J. Scott Lixisenatide: a review of its use in patients with type 2 diabetes mellitus BioDrugs 27 2013 509 523 10.1007/s40259-013-0057-y
44. J.B. Buse, J. Rosenstock, G. Sesti, W.E. Schmidt, E. Montanya, J.H. Brett, and 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 2009 39 47 10.1016/S0140-6736(09)60659-0
45. M.E. Lean, R. Carraro, N. Finer, H. Hartvig, M.L. Lindegaard, S. Rössner, and et al. Tolerability of nausea and vomiting and associations with weight loss in a randomized trial of liraglutide in obese, non-diabetic adults Int J Obes (Lond) 38 2014 689 697 10.1038/ijo.2013.149
46. K. Niswender, X. Pi-Sunyer, J. Buse, K.H. Jensen, A.D. Toft, D. Russell-Jones, and et al. Weight change with liraglutide and comparator therapies: an analysis of seven phase 3 trials from the liraglutide diabetes development programme Diabetes Obes Metab 15 2013 42 54 10.1111/j.1463-1326.2012.01673.x
47. G.H. Yuan, W.L. Song, Y.Y. Huang, X.H. Guo, and Y. Gao Efficacy and tolerability of exenatide monotherapy in obese patients with newly diagnosed type 2 diabetes: a randomized, 26 weeks metformin-controlled, parallel-group study Chin Med J (Engl) 125 2012 2677 2681
48. J. Jelsing, N. Vrang, G. Hansen, K. Raun, M. Tang-Christensen, and L.B. Knudsen Liraglutide: short-lived effect on gastric emptying - long lasting effects on body weight Diabetes Obes Metab 14 2012 531 538 10.1111/j.1463-1326.2012.01557.x
49. B. Gallwitz Anorexigenic effects of GLP-1 and its analogues Handb Exp Pharmacol 209 2012 185 207 10.1007/978-3-642-24716-3-8
50. K. Hunter, and C. Hölscher Drugs developed to treat diabetes, liraglutide and lixisenatide, cross the blood brain barrier and enhance neurogenesis BMC Neurosci 13 2012 33 10.1186/1471-2202-13-33
51. E.W. Iepsen, S.S. Torekov, and J.J. Holst Therapies for inter-relating diabetes and obesity - GLP-1 and obesity Expert Opin Pharmacother 15 2014 2487 2500 10.1517/14656566.2014.965678
52. European Medicines Agency (EMA) Retrieved December 02, 2014, from: http://www.ema.europa.eu/ema/
53. U.S. Food and Drug Administration (FDA) Retrieved January 19, 2015, from: http://www.fda.gov/Drugs/default.htm
54. V. Gupta Glucagon-like peptide-1 analogues: an overview Ind J Endocrinol Metab 17 2013 413 421 10.4103/2230-8210.111625
55. B. Ahrén Insulin plus incretin: a glucose-lowering strategy for type 2-diabetes World J Diabetes 5 2014 40 51 10.4239/wjd.v5.i1.40
56. D.M. Kendall, M.C. Riddle, J. Rosenstock, D. Zhuang, D.D. Kim, M.S. Fineman, and 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 2005 1083 1091
57. R.J. Heine, L.F. Van Gaal, D. Johns, M.J. Mihm, M.H. Widel, R.G. Brodows, and et al. Exenatide versus insulin glargine in patients with suboptimally controlled type 2 diabetes: a randomized trial Ann Intern Med 143 2005 559 569
58. B. Zinman, B.J. Hoogwerf, S. Durán García, D.R. Milton, J.M. Giaconia, D.D. Kim, and et al. The effect of adding exenatide to a thiazolidinedione in suboptimally controlled type 2 diabetes: a randomized trial Ann Intern Med 146 2007 477 485
59. M.A. Nauck, S. Duran, D. Kim, D. Johns, J. Northrup, A. Festa, and 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 2007 259 267
60. H. Fan, Q. Pan, Y. Xu, and X. Yang Exenatide improves type 2 diabetes concomitant with non-alcoholic fatty liver disease Arq Bras Endocrinol Metabol 57 2013 702 708
61. D.J. Drucker, J.B. Buse, K. Taylor, D.M. Kendall, M. Trautmann, D. Zhuang, and et al. Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study Lancet 372 2008 1240 1250 10.1016/S0140-6736(08)61206-4
62. R.M. Bergenstal, C. Wysham, L. Macconell, J. Malloy, B. Walsh, P. Yan, and et al. Efficacy and safety of exenatide once weekly versus sitagliptin or pioglitazone as an adjunct to metformin for treatment of type 2 diabetes (DURATION-2): a randomised trial Lancet 376 2010 431 439 10.1016/S0140-6736(10)60590-9
63. M. Diamant, L. Van Gaal, S. Stranks, J. Northrup, D. Cao, K. Taylor, and et al. Once weekly exenatide compared with insulin glargine titrated to target in patients with type 2 diabetes (DURATION-3): an open-label randomised trial Lancet 375 2010 2234 2243 10.1016/S0140-6736(10)60406-0
64. T. Blevins, J. Pullman, J. Malloy, P. Yan, K. Taylor, C. Schulteis, and et al. DURATION-5: exenatide once weekly resulted in greater improvements in glycemic control compared with exenatide twice daily in patients with type 2 diabetes J Clin Endocrinol Metab 96 2011 1301 1310 10.1210/jc.2010-2081
65. M. Marre, J. Shaw, M. Brändle, W.M. Bebakar, N.A. Kamaruddin, J. Strand, and 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 2009 268 278 10.1111/j.1464-5491.2009.02666.x
66. M. Nauck, A. Frid, K. Hermansen, N.S. Shah, T. Tankova, I.H. Mitha, and 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 2009 84 90 10.2337/dc08-1355
67. A. Garber, R.R. Henry, R. Ratner, P. Hale, C.T. Chang, and B. Bode Liraglutide, a once-daily human glucagon-like peptide 1 analogue, provides sustained improvements in glycaemic control and weight for 2 years as monotherapy compared with glimepiride in patients with type 2 diabetes Diabetes Obes Metab 13 2011 348 356 10.1111/j.1463-1326.2010.01356.x
68. B. Zinman, J. Gerich, J.B. Buse, A. Lewin, S. Schwartz, P. Raskin, and 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 2009 1224 1230 10.2337/dc08-2124
69. D. Russell-Jones, A. Vaag, O. Schmitz, B.K. Sethi, N. Lalic, S. Antic, and 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 2009 2046 2055 10.1007/s00125-009-1472-y
70. A.J. Scheen Lixisenatide (Lyxumia), a new agonist of glucagon-like peptide-1 receptors with a predominant postprandial action Rev Med Liege 69 2014 102 109
71. L.J. Schmidt, W. Habacher, T. Augustin, E. Krahulec, and T. Semlitsch A systematic review and meta-analysis of the efficacy of lixisenatide in the treatment of patients with type 2 diabetes Diabetes Obes Metab 16 2014 769 779 10.1111/dom.12269
72. M. Pinget, R. Goldenberg, E. Niemoeller, I. Muehlen-Bartmer, H. Guo, and R. Aronson Efficacy and safety of lixisenatide once daily versus placebo in type 2 diabetes insufficiently controlled on pioglitazone (GetGoal-P) Diabetes Obes Metab 15 2013 1000 1007 10.1111/dom.12121
73. M.C. Riddle, R. Aronson, P. Home, M. Marre, E. Niemoeller, P. Miossec, and et al. Adding once-daily lixisenatide for type 2 diabetes inadequately controlled by established basal insulin: a 24-week, randomized, placebo-controlled comparison (GetGoal-L) Diabetes Care 36 2013 2489 2496 10.2337/dc12-2454
74. J. Rosenstock, M. Hanefeld, P. Shamanna, K.W. Min, G. Boka, P. Miossec, and et al. Beneficial effects of once-daily lixisenatide on overall and postprandial glycemic levels without significant excess of hypoglycemia in type 2 diabetes inadequately controlled on a sulfonylurea with or without metformin (GetGoal-S) J Diabetes Complications 28 2014 386 392 10.1016/j.jdiacomp.2014.01.012
75. G.B. Bolli, M. Munteanu, S. Dotsenko, E. Niemoeller, G. Boka, Y. Wu, and et al. Efficacy and safety of lixisenatide once daily vs. placebo in people with type 2 diabetes insufficiently controlled on metformin (GetGoal-F1) Diabet Med 31 2014 176 184 10.1111/dme.12328
76. J. Rosenstock, D. Raccah, L. Korányi, L. Maffei, G. Boka, P. Miossec, and et al. Efficacy and safety of lixisenatide once daily versus exenatide twice daily in type 2 diabetes inadequately controlled on metformin: a 24-week, randomized, open-label, active-controlled study (GetGoal-X) Diabetes Care 36 2013 2945 2951 10.2337/dc12-2709
77. B. Wang, J. Zhong, H. Lin, Z. Zhao, Z. Yan, H. He, and et al. Blood pressure-lowering effects of GLP-1 receptor agonists exenatide and liraglutide: a meta-analysis of clinical trials Diabetes Obes Metab 15 2013 737 749 10.1111/dom.12085
78. M.J. Davies, R. Kela, and K. Khunti Liraglutide - overview of the preclinical and clinical data and its role in the treatment of type 2 diabetes Diabetes Obes Metab 13 2011 207 220 10.1111/j.1463-1326.2010.01330.x
79. A. Stonehouse, B. Walsh, and R. Cuddihy Exenatide once-weekly clinical development: safety and efficacy across a range of background therapies Diabetes Technol Ther 13 2011 1063 1069 10.1089/dia.2011.0076
80. Ö. Erdogdu, L. Eriksson, T. Nyström, Å. Sjöholm, and Q. Zhang Exendin-4 restores glucolipotoxicity-induced gene expression in human coronary artery endothelial cells Biochem Biophys Res Commun 419 2012 790 795 10.1016/j.bbrc.2012.02.106
81. A. Shiraki, J. Oyama, H. Komoda, M. Asaka, A. Komatsu, M. Sakuma, and et al. The glucagon-like peptide 1 analog liraglutide reduces TNF-α-induced oxidative stress and inflammation in endothelial cells Atherosclerosis 221 2012 375 382 10.1016/j.atherosclerosis.2011.12.039
82. C. Irace, S. De Luca, E. Shehaj, C. Carallo, A. Loprete, F. Scavelli, and et al. Exenatide improves endothelial function assessed by flow mediated dilation technique in subjects with type 2 diabetes: results from an observational research Diab Vasc Dis Res 10 2013 72 77 10.1177/1479164112449562
83. M. Rizzo, M. Chandalia, A.M. Patti, V. Di Bartolo, A.A. Rizvi, G. Montalto, and et al. Liraglutide decreases carotid intima-media thickness in patients with type 2 diabetes: 8-month prospective pilot study Cardiovasc Diabetol 13 2014 49 10.1186/1475-2840-13-49
84. S.P. Marso, N.R. Poulter, S.E. Nissen, M.A. Nauck, B. Zinman, G.H. Daniels, and et al. Design of the liraglutide effect and action in diabetes: evaluation of cardiovascular outcome results (LEADER)trial Am Heart J 166 2013 823 830.e5 10.1016/j.ahj.2013.07.012 [.e5]
85. P.L. McClean, N. Irwin, K. Hunter, V.A. Gault, and P.R. Flatt (Pro(3))GIP[mPEG]: novel, long-acting, mPEGylated antagonist of gastric inhibitory polypeptide for obesity-diabetes (diabesity) therapy Br J Pharmacol 155 2008 690 701 10.1038/bjp.2008.317
86. N. Irwin, P.L. McClean, F.P. O'Harte, V.A. Gault, P. Harriott, and P.R. Flatt Early administration of the glucose-dependent insulinotropic polypeptide receptor antagonist (Pro3)GIP prevents the development of diabetes and related metabolic abnormalities associated with genetically inherited obesity in ob/ob mice Diabetologia 50 2007 1532 1540
87. M. Lorenz, A. Evers, and M. Wagner Recent progress and future options in the development of GLP-1 receptor agonists for the treatment of diabesity Bioorg Med Chem Lett 23 2013 4011 4018 10.1016/j.bmcl.2013.05.022
88. M.J. Jespersen, F.K. Knop, and M. Christensen GLP-1 agonists for type 2 diabetes: pharmacokinetic and toxicological considerations Expert Opin Drug Metab Toxicol 9 2013 17 29 10.1517/17425255.2013.731394
89. T. Nakamura, T. Ito, M. Uchida, M. Hijioka, H. Igarashi, T. Oono, and et al. PSCs and GLP-1R: occurrence in normal pancreas, acute/chronic pancreatitis and effect of their activation by a GLP-1R agonist Lab Invest 94 2014 63 78 10.1038/labinvest.2013.133
90. A.E. Butler, M. Campbell-Thompson, T. Gurlo, D.W. Dawson, M. Atkinson, and P.C. Butler Marked expansion of exocrine and endocrine pancreas with incretin therapy in humans with increased exocrine pancreas dysplasia and the potential for glucagon-producing neuroendocrine tumors Diabetes 62 2013 2595 2604 10.2337/db12-1686
91. S. Bonner-Weir, P.A. In't Veld, and G.C. Weir Reanalysis of study of pancreatic effects of incretin therapy: methodological deficiencies Diabetes Obes Metab 16 7 2014 661 666 10.1111/dom.12257
92. N. Irwin, and P.R. Flatt Therapeutic potential for GIP receptor agonists and antagonists Best Pract Res Clin Endocrinol Metab 23 2009 499 512 10.1016/j.beem.2009.03.001
93. J.J. Meier, and M.A. Nauck GIP as a potential therapeutic agent? Horm Metab Res 36 2004 859 866
94. K. Miyawaki, Y. Yamada, N. Ban, Y. Ihara, K. Tsukiyama, H. Zhou, and et al. Inhibition of gastric inhibitory polypeptide signaling prevents obesity Nat Med 8 2002 738 742
95. M.C. Althage, E.L. Ford, S. Wang, P. Tso, K.S. Polonsky, and B.M. Wice Targeted ablation of glucose-dependent insulinotropic polypeptide-producing cells in transgenic mice reduces obesity and insulin resistance induced by a high fat diet J Biol Chem 283 2008 18365 18376 10.1074/jbc.M710466200
96. V.A. Gault, N. Irwin, B.D. Green, J.T. McCluskey, B. Greer, C.J. Bailey, and et al. Chemical ablation of gastric inhibitory polypeptide receptor action by daily (Pro3)GIP administration improves glucose tolerance and ameliorates insulin resistance and abnormalities of islet structure in obesity-related diabetes Diabetes 54 2005 2436 2446
97. B.D. Kerr, N. Irwin, P.R. Flatt, and V.A. Gault Prolonged GIP receptor activation using stable mini-PEGylated GIP improves glucose homeostasis and beta-cell function in age-related glucose intolerance Peptides 30 2009 219 225 10.1016/j.peptides.2008.10.017
98. S.B. Widenmaier, S.J. Kim, G.K. Yang, Reyes T. De Los, C. Nian, A. Asadi, and et al. A GIP receptor agonist exhibits beta-cell anti-apoptotic actions in rat models of diabetes resulting in improved beta-cell function and glycemic control PLoS One 5 2010 e9590 10.1371/journal.pone.0009590
99. C.M. Martin, N. Irwin, P.R. Flatt, and V.A. Gault A novel acylated form of (d-Ala(2))GIP with improved antidiabetic potential, lacking effect on body fat stores Biochim Biophys Acta 2013 1830 3407 3413 10.1016/j.bbagen.2013.03.011
100. K. Tatarkiewicz, D.M. Hargrove, C.M. Jodka, B.R. Gedulin, P.A. Smith, J.A. Hoyt, and et al. A novel long-acting glucose-dependent insulinotropic peptide analogue: enhanced efficacy in normal and diabetic rodents Diabetes Obes Metab 16 2014 75 85 10.1111/dom.12181
101. C.F. Deacon Circulation and degradation of GIP and GLP-1 Horm Metab Res 36 2004 761 765
102. M. Kirby, D.M. Yu, S. O'Connor, and M.D. Gorrell Inhibitor selectivity in the clinical application of dipeptidyl peptidase-4 inhibition Clin Sci (Lond) 118 2009 31 41 10.1042/CS20090047
103. C.F. Deacon, and J.J. Holst Dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes: comparison, efficacy and safety Expert Opin Pharmacother 14 2013 2047 2058 10.1517/14656566.2013.824966
104. D.A. Nadeau Review of liraglutide versus sitagliptin for patients with uncontrolled type 2 diabetes: more effective HbA 1c reduction with subcutaneous GLP-1 receptor agonist versus an oral DPP-4 inhibitor Postgrad Med 122 2010 185 188 10.3810/pgm.2010.09.2215
105. T. Karagiannis, P. Boura, and A. Tsapas Safety of dipeptidyl peptidase 4 inhibitors: a perspective review Ther Adv Drug Saf 5 2014 138 146 10.1177/2042098614523031
106. P. Aschner, M.S. Kipnes, J.K. Lunceford, M. Sanchez, C. Mickel, and D.E. Williams-Herman Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes Diabetes Care 29 2006 2632 2637
107. I. Raz, M. Hanefeld, L. Xu, C. Caria, D. Williams-Herman, and H. Khatami Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus Diabetologia 49 2006 2564 2571
108. R. Pratley, M. Nauck, T. Bailey, E. Montanya, R. Cuddihy, S. Filetti, and et al. One year of liraglutide offers sustained and more effective glycaemic control and weight reduction compared with sitagliptin, both in combination with metformin, in patients with type 2 diabetes: a randomized, parallel-group, open-label trial Int J Clin Pract 65 2011 397 407 10.1111/j.1742-1241.2011.02656.x
109. T. Hibuse, N. Maeda, K. Kishida, T. Kimura, T. Minami, E. Takeshita, and et al. A pilot three-month sitagliptin treatment increases serum adiponectin level in Japanese patients with type 2 diabetes mellitus-a randomized controlled trial START-J study Cardiovasc Diabetol 13 2014 96 10.1186/1475-2840-13-96
110. F.X. Pi-Sunyer, A. Schweizer, D. Mills, and S. Dejager Efficacy and tolerability of vildagliptin monotherapy in drug-naïve patients with type 2 diabetes Diabetes Res Clin Pract 76 2007 132 138
111. A.J. Garber, J.E. Foley, M.A. Banerji, P. Ebeling, S. Gudbjörnsdottir, R.P. Camisasca, and et al. Effects of vildagliptin on glucose control in patients with type 2 diabetes inadequately controlled with a sulphonylurea Diabetes Obes Metab 10 2008 1047 1056 10.1111/j.1463-1326.2008.00859.x
112. G. Bolli, F. Dotta, L. Colin, B. Minic, and M. Goodman Comparison of vildagliptin and pioglitazone in patients with type 2 diabetes inadequately controlled with metformin Diabetes Obes Metab 11 2009 589 595 10.1111/j.1463-1326.2008.01023.x
113. C.O. Mendivil, E. Márquez-Rodríguez, I.D. Angel, G. Paz, C. Rodríguez, J. Almada, and et al. Comparative effectiveness of vildagliptin in combination with other oral anti-diabetes agents in usual-care conditions: the EDGE-Latin America study Curr Med Res Opin 11 2014 1 8 10.1185/03007995.2014.928274
114. G. Derosa, A. Bonaventura, L. Bianchi, D. Romano, E. Fogari, A. D'Angelo, and et al. Comparison of vildagliptin and glimepiride: effects on glycaemic control, fat tolerance and inflammatory markers in people with type 2 diabetes Diabet Med 31 2014 1515 1523 10.1111/dme.12499
115. J. Rosenstock, C. Aguilar-Salinas, E. Klein, S. Nepal, J. List, and R. Chen Effect of saxagliptin monotherapy in treatment-naive patients with type 2 diabetes Curr Med Res Opin 25 2009 2401 2411 10.1185/03007990903178735
116. R.A. DeFronzo, M.N. Hissa, A.J. Garber, J. Luiz Gross, R. Yuyan Duan, S. Ravichandran, and 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 2009 1649 1655 10.2337/dc08-1984
117. B. Göke, B. Gallwitz, J.G. Eriksson, Å. Hellqvist, and I. Gause-Nilsson Saxagliptin vs. glipizide as add-on therapy in patients with type 2 diabetes mellitus inadequately controlled on metformin alone: long-term (52-week) extension of a 52-week randomised controlled trial Int J Clin Pract 67 2013 307 316
118. A.R. Chacra, G.H. Tan, A. Apanovitch, S. Ravichandran, J. List, R. Chen, and et al. 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 2009 1395 1406 10.1111/j.1742-1241.2009.02143.x
119. P. Hollander, J. Li, E. Allen, R. Chen CV181-013 Investigators Saxagliptin added to a thiazolidinedione improves glycemic control in patients with type 2 diabetes and inadequate control on thiazolidinedione alone J Clin Endocrinol Metab 94 2009 4810 4819 10.1210/jc.2009-0550
120. M.R. Taskinen, J. Rosenstock, I. Tamminen, R. Kubiak, S. Patel, K.A. Dugi, and et al. Safety and efficacy of linagliptin as add-on therapy to metformin in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled study Diabetes Obes Metab 13 2011 65 74 10.1111/j.1463-1326.2010.01326.x
121. T. Haak, T. Meinicke, R. Jones, S. Weber, M. von Eynatten, and H.J. Woerle Initial combination of linagliptin and metformin in patients with type 2 diabetes: efficacy and safety in a randomised, double-blind 1-year extension study Int J Clin Pract 67 2013 1283 1293 10.1111/ijcp.12308
122. M. Bajaj, R. Gilman, S. Patel, J. Kempthorne-Rawson, D. Lewis-D'Agostino, and H.J. Woerle Linagliptin improved glycaemic control without weight gain or hypoglycaemia in patients with Type 2 diabetes inadequately controlled by a combination of metformin and pioglitazone: a 24-week randomized, double-blind study Diabet Med 31 2014 1505 1514 10.1111/dme.12495
123. M. Lehrke, N. Marx, S. Patel, T. Seck, S. Crowe, K. Cheng, and et al. Safety and tolerability of linagliptin in patients with type 2 diabetes: a comprehensive pooled analysis of 22 placebo-controlled studies Clin Ther 36 2014 1130 1146 10.1016/j.clinthera.2014.06.008
124. R.A. DeFronzo, P.R. Fleck, C.A. Wilson, Q. Mekki Alogliptin Study 010 Group Efficacy and safety of the dipeptidyl peptidase-4 inhibitor alogliptin in patients with type 2 diabetes and inadequate glycemic control: a randomized, double-blind, placebo-controlled study Diabetes Care 31 2008 2315 2317 10.2337/dc08-1035
125. Y. Seino, S. Hiroi, M. Hirayama, and K. Kaku Efficacy and safety of alogliptin added to sulfonylurea in Japanese patients with type 2 diabetes: a randomized, double-blind, placebo-controlled trial with an open-label, long-term extension study J Diabetes Investig 3 2012 517 525 10.1111/j.2040-1124.2012.00226.x
126. C.I. Jarvis, A. Cabrera, and D. Charron Alogliptin: a new dipeptidyl peptidase-4 inhibitor for type 2 diabetes mellitus Ann Pharmacother 47 2013 1532 1539 10.1177/1060028013504076
127. A.B. Marino, and S.W. Cole Alogliptin: safety, efficacy, and clinical implications J Pharm Pract 2014 10.1177/0897190014522063
128. J. Rosenstock, C. Wilson, and P. Fleck Alogliptin versus glipizide monotherapy in elderly type 2 diabetes mellitus patients with mild hyperglycaemia: a prospective, double-blind, randomized, 1-year study Diabetes Obes Metab 15 2013 906 914 10.1111/dom.12102
129. R.E. Pratley, P. Fleck, and C. Wilson Efficacy and safety of initial combination therapy with alogliptin plus metformin versus either as monotherapy in drug-naïve patients with type 2 diabetes: a randomized, double-blind, 6-month study Diabetes Obes Metab 16 2014 613 621 10.1111/dom.12258
130. A. Berhan, and Y. Berhan Efficacy of alogliptin in type 2 diabetes treatment: a meta-analysis of randomized double-blind controlled studies BMC Endocr Disord 13 2013 9 10.1186/1472-6823-13-9
131. P. Yousefzadeh, and X. Wang The effects of dipeptidyl peptidase-4 inhibitors on cardiovascular disease risks in type 2 diabetes mellitus J Diabetes Res 2013 2013 459821 10.1155/2013/459821
132. S. Ogawa, M. Ishiki, K. Nako, M. Okamura, M. Senda, T. Mori, and et al. Sitagliptin, a dipeptidyl peptidase-4 inhibitor, decreases systolic blood pressure in Japanese hypertensive patients with type 2 diabetes Tohoku J Exp Med 223 2011 133 135
133. N. Gomez, K. Touihri, V. Matheeussen, A. Mendes Da Costa, M. Mahmoudabady, M. Mathieu, and et al. Dipeptidyl peptidase IV inhibition improves cardiorenal function in overpacing-induced heart failure Eur J Heart Fail 14 2012 14 21 10.1093/eurjhf/hfr146
134. K. Nakamura, H. Oe, H. Kihara, K. Shimada, S. Fukuda, K. Watanabe, and et al. DPP-4 inhibitor and alpha-glucosidase inhibitor equally improve endothelial function in patients with type 2 diabetes: EDGE study Cardiovasc Diabetol 13 2014 110 10.1186/s12933-014-0110-2
135. M. Monami, C. Lamanna, C.M. Desideri, and E. Mannucci DPP-4 inhibitors and lipids: systematic review and meta-analysis Adv Ther 29 2012 14 25 10.1007/s12325-011-0088-z
136. E.Y. Choe, Y. Cho, Y. Choi, Y. Yun, H.J. Wang, O. Kwon, and et al. The effect of DPP-4 inhibitors on metabolic parameters in patients with type 2 diabetes Diabetes Metab J 38 2014 211 219 10.4093/dmj.2014.38.3.211