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Drug Evaluations

Sitagliptin: a review

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Pages 1613-1622 | Published online: 09 Jun 2011

Bibliography

  • Cheung BM, Ong KL, Cherny SS, Diabetes prevalence and therapeutic target achievement in the United States, 1999 to 2006. Am J Med 2009;122:443-53
  • Narayan KM, Boyle JP, Geiss LS, Impact of recent increase in incidence on future diabetes burden: U.S., 2005 – 2050. Diabetes Care 2006;29:2114-16
  • Grouzmann E, Bigliardi P, Appenzeller M, Substance P-induced skin inflammation is not modulated by a single dose of Sitagliptin in human volunteers. Biol Chem 2011;392:217-21
  • Elrick H, Stimmler L, Hlad CJ Jr, Arai Y. Plasma insulin response to oral and intravenous glucose administration. J Clin Endocrinol Metab 1964;24:1076-82
  • Creutzfeldt W. The pre-history of the incretin concept. Regul Pept 2005;128:87-91
  • Creutzfeldt W. The incretin concept today. Diabetologia 1979;16:75-85
  • Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 2006;368:1696-705
  • Rehfeld JF, Stadil F. The effect of gastrin on basal- and glucose-stimulated insulin secretion in man. J Clin Invest 1973;52:1415-26
  • McKennon SA, Campbell RK. The physiology of incretin hormones and the basis for DPP-4 inhibitors. Diabetes Educ 2007;33:55-66
  • Gutzwiller JP, Drewe J, Goke B, Glucagon-like peptide-1 promotes satiety and reduces food intake in patients with diabetes mellitus type 2. Am J Physiol 1999;276:R1541-4
  • Nauck M, Stockmann F, Ebert R, Creutzfeldt W. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia 1986;29:46-52
  • Nauck MA, Kleine N, Orskov C, Normalization of fasting hyperglycaemia by exogenous glucagon-like peptide 1 (7-36 amide) in type 2 (non-insulin-dependent) diabetic patients. Diabetologia 1993;36:741-4
  • Gutniak M, Orskov C, Holst JJ, Antidiabetogenic effect of glucagon-like peptide-1 (7-36)amide in normal subjects and patients with diabetes mellitus. N Engl J Med 1992;326:1316-22
  • Rachman J, Barrow BA, Levy JC, Turner RC. Near-normalisation of diurnal glucose concentrations by continuous administration of glucagon-like peptide-1 (GLP-1) in subjects with NIDDM. Diabetologia 1997;40:205-11
  • Kieffer TJ, McIntosh CH, Pederson RA. Degradation of glucose-dependent insulinotropic polypeptide and truncated glucagon-like peptide 1 in vitro and in vivo by dipeptidyl peptidase IV. Endocrinology 1995;136:3585-96
  • Goke R, Fehmann HC, Linn T, Exendin-4 is a high potency agonist and truncated exendin-(9-39)-amide an antagonist at the glucagon-like peptide 1-(7-36)-amide receptor of insulin-secreting beta-cells. J Biol Chem 1993;268:19650-5
  • Kim D, Wang L, Beconi M, (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)- yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: a potent, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem 2005;48:141-51
  • Lankas GR, Leiting B, Roy RS, Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes 2005;54:2988-94
  • Mentlein R. Dipeptidyl-peptidase IV (CD26) – role in the inactivation of regulatory peptides. Regul Pept 1999;85:9-24
  • Deacon CF, Ahren B, Holst JJ. Inhibitors of dipeptidyl peptidase IV: a novel approach for the prevention and treatment of Type 2 diabetes? Expert Opin Investig Drugs 2004;13:1091-102
  • Herman GA, Stevens C, Van Dyck K, 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
  • Bergman A, Ebel D, Liu F, Absolute bioavailability of sitagliptin, an oral dipeptidyl peptidase-4 inhibitor, in healthy volunteers. Biopharm Drug Dispos 2007;28:315-22
  • Januvia package insert. Available from: http://www.merck.com/product/usa/pi_circulars/j/januvia/januvia_pi.pdf [Last accessed 2 February 2011]
  • Chan JC, Scott R, Arjona Ferreira JC, Safety and efficacy of sitagliptin in patients with type 2 diabetes and chronic renal insufficiency. Diabetes Obes Metab 2008;10:545-55
  • Migoya E, Larson P, Bergman A, Sitagliptin, a dipeptidyl peptidase-4 inhibitor, does not affect the pharmacokinetics of ethinyl estradiol or norethindrone in healthy female subjects. J Clin Pharmacol 2011. [Epub ahead of print]
  • Migoya EM, Stevens CH, Bergman AJ, Effect of moderate hepatic insufficiency on the pharmacokinetics of sitagliptin. Can J Clin Pharmacol 2009;16:e165-70
  • Scheen AJ. Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab 2010;12:648-58
  • Alba M, Sheng D, Guan Y, Sitagliptin 100 mg daily effect on DPP-4 inhibition and compound-specific glycemic improvement. Curr Med Res Opin 2009;25:2507-14
  • Bergman AJ, Stevens C, Zhou Y, Pharmacokinetic and pharmacodynamic properties of multiple oral doses of sitagliptin, a dipeptidyl peptidase-IV inhibitor: a double-blind, randomized, placebo-controlled study in healthy male volunteers. Clin Ther 2006;28:55-72
  • Goldstein BJ, Feinglos MN, Lunceford JK, 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
  • Migoya EM, Bergeron R, Miller JL, Dipeptidyl peptidase-4 inhibitors administered in combination with metformin result in an additive increase in the plasma concentration of active GLP-1. Clin Pharmacol Ther 2010;88:801-8
  • Seck T, Nauck M, Sheng D, 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 2010;64:562-76
  • Pratley RE, Nauck M, Bailey T, 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 2010;375:1447-56
  • DeFronzo RA, Okerson T, Viswanathan P, 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 2008;24:2943-52
  • Bergenstal RM, Wysham C, Macconell L, 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 2010;376:431-9
  • Nauck MA, Vilsboll T, Gallwitz B, Incretin-based therapies: viewpoints on the way to consensus. Diabetes Care 2009;32(Suppl 2):S223-31
  • Fadini GP, Boscaro E, Albiero M, The oral dipeptidyl peptidase-4 inhibitor sitagliptin increases circulating endothelial progenitor cells in patients with type 2 diabetes: possible role of stromal-derived factor-1alpha. Diabetes Care 2010;33:1607-9
  • Wright DH, Herman GA, Maes A, Multiple doses of sitagliptin, a selective DPP-4 inhibitor, do not meaningfully alter pharmacokinetics and pharmacodynamics of warfarin. J Clin Pharmacol 2009;49:1157-67
  • Miller JL, Migoya E, Talaty JE, The effect of MK-0431 on the pharmacokinetics of digoxin after concomitant administration for 10 days in healthy subjects. Clin Pharmacol Ther 2006;79:P24
  • DiGregorio RV, Pasikhova Y. Rhabdomyolysis caused by a potential sitagliptin-lovastatin interaction. Pharmacotherapy 2009;29:352-6
  • Kao DP, Kohrt HE, Kugler J. Renal failure and rhabdomyolysis associated with sitagliptin and simvastatin use. Diabet Med 2008;25:1229-30
  • Boucher BJ. Renal failure and rhabdomyolysis associated with sitagliptin and simvastatin use. But what about the amiodarone? Diabet Med 2009;26:192-3
  • Bergman AJ, Cote J, Maes A, Effect of sitagliptin on the pharmacokinetics of simvastatin. J Clin Pharmacol 2009;49:483-8
  • Krishna R, Bergman A, Larson P, Effect of a single cyclosporine dose on the single-dose pharmacokinetics of sitagliptin (MK-0431), a dipeptidyl peptidase-4 inhibitor, in healthy male subjects. J Clin Pharmacol 2007;47:165-74
  • Chu XY, Bleasby K, Yabut J, Transport of the dipeptidyl peptidase-4 inhibitor sitagliptin by human organic anion transporter 3, organic anion transporting polypeptide 4C1, and multidrug resistance P-glycoprotein. J Pharmacol Exp Ther 2007;321:673-83
  • Engel SS, Williams-Herman DE, Golm GT, Sitagliptin: review of preclinical and clinical data regarding incidence of pancreatitis. Int J Clin Pract 2010;64:984-90
  • Williams-Herman D, Engel SS, Round E, Safety and tolerability of sitagliptin in clinical studies: a pooled analysis of data from 10,246 patients with type 2 diabetes. BMC Endocr Disord 2010;10:7
  • Skalli S, Wion-Barbot N, Baudrant M, Angio-oedema induced by dual dipeptidyl peptidase inhibitor and angiotensin II receptor blocker: a first case report. Diabet Med 2010;27:486-7
  • Mu J, Woods J, Zhou YP, Chronic inhibition of dipeptidyl peptidase-4 with a sitagliptin analog preserves pancreatic beta-cell mass and function in a rodent model of type 2 diabetes. Diabetes 2006;55:1695-704
  • Aschner P, Kipnes MS, Lunceford JK, Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care 2006;29:2632-7
  • Mohan V, Yang W, Son HY, Efficacy and safety of sitagliptin in the treatment of patients with type 2 diabetes in China, India, and Korea. Diabetes Res Clin Pract 2009;83:106-16
  • Charbonnel B, Karasik A, Liu J, 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;29:2638-43
  • Hermansen K, Kipnes M, Luo E, 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
  • Gerstein HC, Miller ME, Byington RP, Effects of intensive glucose lowering in type 2 diabetes. N Engl J Med 2008;358(24):2545-59
  • Hoogwerf BJ, Action to Control Cardiovascular Risk in Diabetes Study Group. Does intensive therapy of type 2 diabetes help or harm? Seeking accord on ACCORD. Cleve Clin J Med 2008;75:729-37
  • 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 2007;61:171-80
  • Hanefeld M, Herman GA, Wu M, Once-daily sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of patients with type 2 diabetes. Curr Med Res Opin 2007;23:1329-39
  • Nonaka K, Kakikawa T, Sato A, Efficacy and safety of sitagliptin monotherapy in Japanese patients with type 2 diabetes. Diabetes Res Clin Pract 2008;79:291-8
  • Rosenstock J, Brazg R, Andryuk PJ, 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 2006;28:1556-68
  • Vilsboll T, Rosenstock J, Yki-Jarvinen H, Efficacy and safety of sitagliptin when added to insulin therapy in patients with type 2 diabetes. Diabetes Obes Metab 2010;12:167-77
  • Aschner P, Katzeff HL, Guo H, Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes. Diabetes Obes Metab 2010;12:252-61
  • Raz I, Hanefeld M, Xu L, Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy in patients with type 2 diabetes mellitus. Diabetologia 2006;49:2564-71
  • Raz I, Chen Y, Wu M, Efficacy and safety of sitagliptin added to ongoing metformin therapy in patients with type 2 diabetes. Curr Med Res Opin 2008;24:537-50
  • Aschner P, Katzeff HL, Guo H, Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes. Diabetes Obes Metab 2010;12:252-61
  • Derosa G, Maffioli P, Salvadeo SA, Effects of sitagliptin or metformin added to pioglitazone monotherapy in poorly controlled type 2 diabetes mellitus patients. Metabolism 2010;59:887-95
  • Mistry GC, Bergman AJ, Zheng W, Sitagliptin, an dipeptidyl peptidase-4 inhibitor, does not alter the pharmacokinetics of the sulphonylurea, glyburide, in healthy subjects. Br J Clin Pharmacol 2008;66:36-42
  • Arechavaleta R, Seck T, Chen Y, Efficacy and safety of treatment with sitagliptin or glimepiride in patients with type 2 diabetes inadequately controlled on metformin monotherapy: a randomized, double-blind, non-inferiority trial. Diabetes Obes Metab 2011;13:160-8
  • Scheen AJ, Charpentier G, Ostgren CJ, Efficacy and safety of saxagliptin in combination with metformin compared with sitagliptin in combination with metformin in adult patients with type 2 diabetes mellitus. Diabetes Metab Res Rev 2010;26:540-9

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