252
Views
4
CrossRef citations to date
0
Altmetric
Review

New treatments for type 2 diabetes mellitus: combined therapy with sitagliptin

, MD, , MD, , MD & , MD PhD
Pages 1495-1507 | Published online: 02 Jun 2008

Bibliography

  • Defronzo RA. Lilly lecture 1987. The triumvirate: beta-cell, muscle, liver. A collusion responsible for NIDDM. Diabetes 1988;37:667-87
  • UKPDS 16. UK prospective diabetes study 16. Overview of 6 years' therapy of type II diabetes: a progressive disease. UK Prospective Diabetes Study Group. Diabetes 1995;44:1249-58
  • UKPDS. Effect of the intensive blood-glucose control with metformin on complications in overweight patients with type 2 diabetes (UKPDS 34). Lancet 1998;352:854-65
  • Ong KL, Cheung BM, Man YB, et al. Treatment and control of diabetes mellitus in the United States National Health and Nutrition Examination Survey, 1999 – 2002. J Cardiometab Syndr 2006;1(5):301-7
  • Nauck M, Stockman M, Beehle K. Reduce incretin effect in type 2 diabetes. Diabetologia 1986;29(1):46-52
  • Stoffers DA, Kieffer TJ, Hussain MA, et al. Insulinotropic glucagon-like peptide 1 agonists stimulate expression of homeodomain protein IDX-1 and increase islet size in mouse pancreas. Diabetes 2000;49:741-8
  • Tourrel C, Bailbe D, Lacorne M, et al. Persistent improvement of type 2 diabetes in the Goto-Kakizaki rat model by expansion of the β-cell mass during the prediabetic period with glucagon-like peptide-1 or exendin-4. Diabetes 2002;51:1443-52
  • Drucker DJ. Enhancing incretin action for the treatment of type 2 diabetes. Diabetes Care 2003;26:2929-40
  • Nauck M, Kleine N, Orshov C, et al. Normalization of fasting hyperglycemia by exogenous glucagon like peptide in type 2 diabetic patients. Diabetologia 1993;36:741-4
  • Mentlein R. Dipeptidyl-peptidase IV (CD26): role in the inactivation of regulatory peptides. Regul Pept 1999;85(1):9-24
  • Herman G, Stevens C, Van Dyck K, et al. Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double blind placebo controlled studies with single oral doses. Clin Pharmacol Ther 2005;78:675-88
  • Drucker DJ. Glucagon-like peptides. Diabetes 1998;47:159-69
  • Jackson RS, Creemers JW, Sadaf Farooqi I, et al. Small-intestinal dysfunction accompanies the complex endocrinopathy of human proprotein convertase 1 deficiency. Clin Invest 2003;112:1550-60
  • Elliott RM, Morgan LM, Tredger JA, et al. Glucagon-like peptide-1 (7 – 36)amide and glucose-dependent insulinotropic polypeptide secretion in response to nutrient ingestion in man: acute post-prandial and 24-h secretion patterns. J Endocrinol 1993;138:159-66
  • Rocca AS, Brubaker Pl. Role of the vagus nerve in mediating proximal nutrient-induced glucagon-like peptide-1 secretion. Endocrinology 1999;140:1687-94
  • Anini Y, Brubaker Pl. Muscarinic receptors control glucagon-like peptide 1 secretion by human endocrine L cells. Endocrinology 2003;144:3244-50
  • Ahren B, Holst JJ. The cephalic insulin response to meal ingestion in humans is dependent on both cholinergic and non cholinergic mechanisms and is important for postprandial glycemia. Diabetes 2001;50:1030-8
  • Toft-Nielsen MB, Madsbad S, Holst JJ. Continuous subcutaneous infusions of glucagon-like peptide 1 lowers plasma glucosa and reduces appetite in type 2 diabetic patients. Diabetes Care 1999;22:1137-43
  • Hansotia T, Baggio LL, Delmeire D, et al. Double incretin receptor knockout (DIRKO) mice reveal an essential role for the enteroinsular axis in transducing the glucoregulatory actions of DPP-IV inhibitors. Diabetes 2004;53:1326-35
  • Holst JJ, Deacon CF. Inhibition of the activity of dipeptidyl-peptidase IV as a treatment for type 2 diabetes. Diabetes 1998;47:1663-70
  • Zhu X, Zhou A, Dey A, et al. Disruption of PC1/3 expression in mice causes dwarfism and multiple neuroendocrine peptide processing defects. Proc Natl Acad Sci USA 2002;99:10293-8
  • Ahren B, Lundin-Olsson M, Jansson PA, et al. The DPP IV inhibitor, LAF237 reduces fasting and postprandial glucose in subjects with type 2 diabetes over a 4 week period by increasing active GLP-1 sustaining insulin and reducing glucagons (abstract). Diabetes 2003;52(Suppl 1):A15
  • Moens K, Heimberg H, Flamez D, et al. Expression and functional activity of glucagon, glucagon-like peptide 1, and glucose-dependent insulinotropic peptide receptors in rat pancreatic islet cells. Diabetes 1996;45:257-61
  • Thorens B, Dériaz N, Bosco D, et al. Protein kinase A dependent phosphorylation of GLUT2 in pancreatic β cells. J Biol Chem 1996;271:8075-81
  • Beguin P, Nagashima K, Nishimura M, et al. PKA-mediated phosphorylation of the human KATP channel: separate roles of Kir6.2 and SUR1 subunit phosphorylation. EMBO J 1999;18:4722-32
  • Leiser M, Fleischer N. cAMP-dependent phosphorylation of the cardiac-type a1 subunit of the voltage-dependent Ca2+ channel in a murine pancreatic β cell line. Diabetes 1996;45:1412-8
  • Kashima Y, Miki T, Shibasaki T, et al. Critical role of cAMP–GEFII–Rim2 complex in incretin-potentiated insulin secretion. J Biol Chem 2001;276:46046-53
  • Ritzel R, Orskov C, Holst JJ, et al. Pharmacokinetic, insulinotropic, and glucagonostatic properties of GLP-1 [7 – 36 amide] after subcutaneous injection in healthy volunteers. Dose–response-relationships. Diabetologia 1995;38:720-5
  • Vilsboll T, Knop FK, Krarup T, et al. The pathophysiology of diabetes involves a defective amplification of the late-phase insulin response to glucose by glucose-dependent insulinotropic poplypeptide – regardless of etiology and phenotype. J Clin Endocrinol Metab 2003;88:4897-903
  • Zander M, Madsbad S, Madsen JL, et al. Effect of 6-week course of glucagon-like peptide 1 on glycaemic control, insulin sensitivity, and β-cell function in type 2 diabetes: a parallel-group study. Lancet 2002;359:824-30
  • Preitner F, Ibberson M, Franklin I, et al. Gluco-incretin control insulin secretion at multiple levels as revealed in mice lacking GLP-1 and GIP receptors. J Clin Invest 2004;113:635-45
  • Farilla L, Bulotta A, Hirshberg B, et al. Glucagon-like peptide 1 inhibits cell apoptosis and improves glucose responsiveness of freshly isolated human islets. Endocrinology 2003;144(12):5149-58
  • Vilsboll T, Krarup T, Deacon CF, et al. Reduced postprandial concentrations of intact biologically active glucagon-like peptide 1 in type 2 diabetic patients. Diabetes 2001;50:609-13
  • Egan JM, Meneilly GS, Elia D. Effects of 1-mo bolus subcutaneous administration of GLP-1 receptor agonist in type 2 diabetes. Am J Physiol Endocrinol Metab 2003;284:E1072-9
  • Buchan MT, Pollak JM, Capella C, et al. Electroinmmunochemical evidence for the K-cell localization of gastric inhibitory poplypeptide (GIP) in man. Histochemistry 1978;56:37-44
  • Tseng CC, Jarboe LA, Landau SB, et al. Glucose-dependent insulinotropic peptide: structure of the precursor and tissue-specific expression in rat. Proc Nat Acad Sci USA 1993;90(5):1992-6
  • Hampton SM, Morgan LM, Tredger JA, et al. Insulin and C-peptide levels after oral and intravenous glucose. Contribution of enteroinsular axis to insulin secretion. Diabetes 1986;35:612-6
  • Murphy MC, Isherwood SG, Sethi S, et al. Postprandial lipid and hormones responses to meals of varying fat contents: modulatory role of lipoprotein lipase? Eur J Clin Nutr 1995; 49:578-88
  • Mentlein R. Cell-surface peptidases. Int Rev Cytol 2004;235:165-213
  • Deacon CF, Holst JJ. Dipeptidyl peptidase IV inhibition as an approach to the treatment and prevention of type 2 diabetes: a historical perspective. Biochem Biophys Res Commun 2002;294:1-4
  • Sudre B, Broqua P, White RH, et al. Chronic inhibition of circulating dipeptidyl peptidase IV by FE 999011 delays the occurrence of diabetes in male Zucker diabetic fatty rats. Diabetes 2002;51:1661-9
  • Wheeler MB, Lu M, Dillon JS, et al. Functional expression of the rat glucagon-like peptide-I receptor, evidence for coupling to both adenylyl cyclase and phospholipase-c. Endocrinology 1993;133:57-62
  • Yip RG, Wolfe MM. GIP biology and fat metabolism. Life Sci 2000;66(2):91-103
  • Fehmann HC, Goke R. Characterization of GIP (1 – 30) and GIP (1 – 42) as stimulators of proinsulin gene transcription. Peptides 1995;16:1149-52
  • Jhala US, Gianluca Canettieri RA, Screaton RN, et al. cAMP promotes pancreatic beta-cells survival via CREB-mediated induction of IRS2. Genes Dev 2003;17:1575-80
  • Pospisilik JA, Martin J, Doty T, et al. Dipeptidyl peptidase IV inhibitor treatment stimulates beta-survival and islet neogenesis in streptozotocin-induced diabetic rats. Diabetes 2003;52:741-50
  • Trumper A, Trumper K, Horsch D. Mechanisms of mitogenic and anti-apoptotic signaling by glucose-dependent insulinotropic polypeptide in β (INS)-cells. J Endocrinol 2002;174:233-45
  • Holst JJ, Gromada J, Nauck MA. The pathogenesis of NIDDM involves a defective expression of the GIP receptor. Diabetologia 1997;40:984-6
  • Elahi D, Meneilly GS, Minaker KL, et al. Regulation of hepatic glucose production by gastric inhibitory poplypeptide in man [abstract]. Can J Physiol Pharmacol 1986;65:18
  • O'Harte FP, Gray AM, Flatt PR. Gastric inhibitory polypeptide and effects of glycation on glucose transport and metabolism in isolated mouse abdominal muscle. J Endocrinol 1998;156:237-43
  • Eckel RH, Fujimoto WY, Brunzell JD. Gastric inhibitory polypeptide enhanced lipoprotein activity in cultured preadipocytes. Diabetes 1979;28:1141-2
  • Oben J, Morgan LM, Fletcher J, et al. Effect of the entro-pancreatic hormones, gastric inhibitory polypeptide and glucagon-like polypeptide (7 – 36 amide), on fatty acid synthesis in explants of rat adipose tissue. J Endocrinol 1991;130:267-72
  • Knapper JM, Puddicombe SM, Morgan LM, et al. Investigations into actions of glucose-dependent insulinotropic polypeptide and glucagon-like peptide 1 (7 – 36) amide on lipoprotein lipase activity in explants of adipose tissue. J Nutr 1995;125:183-8
  • Miyawaki K, Yamada Y, Ban N, et al. Inhibition of gastric inhibitory polypeptide signaling prevents obesity. Nat Med 2002;8:738-42
  • Gault VA, O'Harte FPM, Flatt PR. Glucose-dependent insulinotropic polypeptide (GIP): anti-diabetic and anti-obesity potential? Neuropeptides 2003;37:253-63
  • Sokos GG, Nikolaidis LA, Mankad S, et al. Glucagon-like peptide-1 infusion improves left ventricular ejection fraction and functional status in patients with chronic heart failure. J Cardiac Fail 2006;12:694-9
  • Nikolaidis LA, Mankad S, Sokos GG, et al. Effects of glucagon-like peptide-1 in patients with acute myocardial infarction and left ventricular dysfunction after successful reperfusion. Circulation 2004;109(8):962-5
  • Nystrom T, Gutniak MK, Zhang Q, et al. Effect of glucagon-like peptide-1 on endothelial function in type 2 diabetes patients with stable coronary artery disease. Am J Physiol Endocrinol Metab 2004;287:E1209-15
  • Yu M, Moreno C, Hoagland KM, et al. Antihypertensive effect of glucagon-like peptide 1 in Dahl salt-sensitive rats. J Hypertens 2003;21(6):1125-35
  • Gros R, You X, Baggio L, et al. Cardiac function in mice lacking the glucagon-like peptide-1 receptor. Endocrinology 2003;144:2242-52
  • Ding X, Saxena NK, Lin S, et al. Exendin-4, a glucagon-like protein-1 (GLP-1) receptor agonist, reverses hepatic steatosis in ob/ob mice. Hepatology 2006;43:173-81
  • Yamada C, Yamada Y, Tsukiyama K, et al. The murine glucagon-like peptide-1 receptor is essential for control of bone resorption. Endocrinology 2008;149:574-9
  • Bollag RJ, Zhong Q, Phillips P, et al. Osteoblast-derived cells express functional glucose-dependent insulinotropic peptide receptors. Endocrinology 2000;141:1228-35
  • Zhong Q, Itokawa T, Sridhar S, et al. Effects of glucose-dependent insulinotropic peptide on osteoclast function. Am J Physiol Endocrinol Metab 2007;292:E543-8
  • Gallwitz B. Sitagliptin: profile of a novel DPP-IV inhibitor for the treatment of type 2 diabetes. Drugs Today 2007;43:1-14
  • Aschner P, Kipnes M, Lunceford J, et al. Effect of dipeptidyl peptidase 4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 2006;29:2632-7
  • Raz I, Hanefeld M, Xu L, et al. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus. Diabetologia 2006;49(11):2564-71
  • Green B, Lavery K, Irwin N, et al. Novel glucagon-like peptide-1 (GLP-1) analog (Val8)GLP-1 results in significant improvements of glucose tolerance and pancreatic beta-cell function after 3-week daily administration in obese diabetic (ob/ob) mice. J Pharmacol Exp Ther 2006;318(2):914-21
  • Migoya E, Miller J, Larson P, et al. A randomized, placebo-controlled, double-blind, double-dummy, crossover study to assess the effects of sitagliptin and metformin on post-meal incretin hormone concentrations in healthy adult subjects. Diabetologia 2007;50(Suppl 1):S52
  • Marchetti P, Del Guerra S, Marselli L, et al. Pancreatic islets from type 2 diabetic patients have functional defects and increased apoptosis that are ameliorated by metformin. J Clin Endocrinol Metab 2004;89:5535-41
  • Sinha Roy R, Zhu L, He H, et al. Metformin is a GLP-1 secretagogue, not a dipeptidyl peptidase-4 inhibitor. Diabetologia 2007;50(Suppl 1):S284
  • Charbonnel B, Karasik A, Liu J, et al. 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 2006;29(12):2638-43
  • Karasik A, Wu M, Williams-Herman D, et al. Sitagliptin added to ongoing metformin therapy provides sustained glycemic control over 54 weeks, with a low incidence of hypoglycaemia and weight loss. American Diabetes Association Congress; 2007; P0523
  • Brazg R, Xu L, Dalla Man C, et al. Effect of adding sitagliptin, a dipeptidyl peptidase-4 inhibitor, to metformin on 24-h glycaemic control and b-cell function in patients with type 2 diabetes. Diabetes Obes Metab 2007;9:186-93
  • Hermansen K, Kipnes M, Luo E, et al. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or on glimepiride and metformin. Diabetes Obes Metab 2007;9:733-45
  • Nauck M, Meininger G, Sheng D, et al. Efficacy and safety of the dipeptidyl peptidase 4 inhibitor sitagliptin, compared to the sulfonylurea, glipizide, in patients with type 2 diabetes inadequately controlled on metformine alone: a randomized, double blind, non-inferiority trial. Diabetes Obes Metab 2007;9:194-205
  • Rosenstock J, Brazg R, Andryuk P, et al. Efficacy and safety of the dipeptidyl peptidase-4 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 2006;28(10):1556-68
  • Mistry C, Bergman A, Lu W, et al. Multiple-dose administration of sitagliptin, a dipeptidyl peptidase-4 inhibitor, does not alter the single-dose pharmacokinetics of rosiglitazone in healthy subjects. J Clin Pharmacol 2007;47:159-64
  • Goldstein BJ, Feinglos M, Lunceford J, et al. Effect of initial combination therapy with sitagliptin, a dipeptidyl peptidase-4 inhibitor, and metformin on glycemic control in patients with type 2 diabetes. Diabetes Care 2007;30:1979-87
  • Williams-Herman D, Johnson J, Lunceford J. Initial combination therapy with sitagliptin and metformin provides effective and durable glycemic control over 1 year in patients with type 2 diabetes: a pivotal phase III clinical trial. Diabetologia 2007;50(Suppl 1):S52-3
  • Xu, L, Williams-Herman D. Initial combination therapy with sitagliptin, a selective DPP-4 inhibitor, and metformin leads to marked improvement in -cell function in patients with type 2 diabetes. Diabetologia 2007;50(Suppl 1):365

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.