DPP IV inhibitors: Successes, failures and future prospects

Diabetes and Metabolic Syndrome: Clinical Research and Reviews

Volumn 5, Issue 2, 2011, Pages 105-112

  Kshirsagar, Ajay D ^a   Aggarwal, Ashish S ^a   Harle, Uday N ^a   Deshpande, Avinash D ^a  

^a DR D Y PATIL INSTITUTE OF PHARMACEUTICAL SCIENCES AND RESEARCH   (India)

Author keywords

DPP IV inhibitors; Incretin; Insulin; Sitagliptin; Type 2 diabetes

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; ALOGLIPTIN; AMYLOID BETA PROTEIN; AMYLOID PRECURSOR PROTEIN; ANTIDIABETIC AGENT; DDP 728; DIPEPTIDYL PEPTIDASE IV; DIPEPTIDYL PEPTIDASE IV INHIBITOR; FE 999011; GLIMEPIRIDE; GLIMEPIRIDE PLUS METFORMIN; GLIPIZIDE; GLUCAGON LIKE PEPTIDE 1 DERIVATIVE; GLUCOSE; HEMOGLOBIN A1C; INSULIN; LINAGLIPTIN; LIVER ENZYME; METFORMIN; NEUROPEPTIDE Y; PFK 275 055; PIOGLITAZONE; ROSIGLITAZONE; SAXAGLIPTIN; SITAGLIPTIN; SUBSTANCE P; SULFONYLUREA; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALINE PYRROLIDIDE; VILDAGLIPTIN;

ADD ON THERAPY; ALZHEIMER DISEASE; ARTHRALGIA; BLOOD PRESSURE; CARDIOVASCULAR DISEASE; COLORECTAL CANCER; DIABETIC PATIENT; DIARRHEA; DIZZINESS; DRUG DOSE REDUCTION; DRUG EFFICACY; DRUG HYPERSENSITIVITY; DRUG INDICATION; DRUG SAFETY; DRUG TOLERABILITY; DRUG TREATMENT FAILURE; DRUG WITHDRAWAL; EDEMA; FLU LIKE SYNDROME; GASTROINTESTINAL SYMPTOM; GLUCOSE BLOOD LEVEL; GLYCEMIC CONTROL; HEADACHE; HEART INFARCTION; HEART MUSCLE ISCHEMIA; HUMAN; HYPOGLYCEMIA; INFLAMMATION; INSULIN BLOOD LEVEL; MONOTHERAPY; NEUROGENIC INFLAMMATION; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET BETA CELL; PRESCRIPTION; PRIORITY JOURNAL; PROSTATE CANCER; REPERFUSION INJURY; REVIEW; RHINORRHEA; RISK ASSESSMENT; SIDE EFFECT; SKIN CANCER; SORE THROAT; TREATMENT DURATION; TREATMENT RESPONSE; UPPER RESPIRATORY TRACT INFECTION; URINARY TRACT INFECTION; VALIDATION PROCESS; WEIGHT GAIN; WOUND HEALING; WOUND HEALING IMPAIRMENT;

ANIMALS; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; FORECASTING; HUMANS; HYPOGLYCEMIC AGENTS; TREATMENT FAILURE; TREATMENT OUTCOME;

EID: 84861095436     PISSN: 18714021     EISSN: 18780334     Source Type: Journal    
DOI: 10.1016/j.dsx.2012.02.017     Document Type: Review

References (72)

1. The Diabetes Control and Complications Trial Research Group The effect of intensive treatment of diabetes on the development and progression of long-term complications in insulin-dependent diabetes mellitus N Engl J Med 329 1993 977 986
2. UK Prospective Diabetes Study (UKPDS) Group Intensive blood-glucose control with sulphonylureas or insulin compared with conventional treatment and risk of complication in patients with type 2 diabetes (UKPDS 33) Lancet 352 1998 837 853
3. M.M. Engelgau, L.S. Geiss, and J.B. Saaddine The evolving diabetes burden in the United States Ann Intern Med 140 2004 945 950 (Pubitemid 38685285)
4. K. Narayan, J. Boyle, and T. Thompson Lifetime risk for diabetes mellitus in the United States JAMA 290 2003 1884 1890 (Pubitemid 37430605)
5. S. Wild, G. Roglic, and A. Green Global prevalence of diabetes: estimates for the year 2000 and projections for 2030 Diabetes Care 5 2004 1047 1053 (Pubitemid 38579764)
6. O. Pinhas-Hamiel, L. Dolan, and S. Daniels Increased incidence of non-insulin-dependent diabetes mellitus among adolescents J Pediatr 128 1996 608 615 (Pubitemid 26137717)
7. H. Keenan, K.E. Deft'awl, and M. Walsh Are trends in diabetes incidence changing for minority children? Ann Epidemiol 10 2000 459
8. A. Tahrani, C. Bailey, and S. Prato Management of type 2 diabetes: new and future developments in treatment Lancet 378 2011 182 197
9. L.L. Baggio, and D.J. Drucker Biology of incretins: GLP-1 and GIP Gastroenterology 132 2007 2131 2157 (Pubitemid 46711096)
10. M.A. Nauck, M.M. Heimesaat, and C. Orskov 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 9 1993 301 307 (Pubitemid 23037285)
11. K. Vollmer, J.J. Holst, and B. Baller Predictors of incretin concentrations in subjects with normal, impaired, and diabetic glucose tolerance Diabetes 57 2008 678 687
12. M.A. Nauck, E. Bartels, and C. Orskov Additive insulinotropic effects of exogenous synthetic human gastric inhibitory polypeptide and glucagon-like peptide-1-(7-36) amide infused at near-physiological insulinotropic hormone and glucose concentrations J Clin Endocrinol Metab 76 1993 912 917 (Pubitemid 23110837)
13. G. Xu, H. Kaneto, and D.R. Laybutt Downregulation of GLP-1 and GIP receptor expression by hyperglycemia: possible contribution to impaired incretin effects in diabetes Diabetes 56 2007 1551 1558 (Pubitemid 46842610)
14. M.A. Nauck Unraveling the science of incretin biology Am J Med 122 6A 2009 S3 S10
15. C.A. Abbott, E. Baker, and G.R. Sutherland Genomic organization, exact localization, and tissue expression of the human CD26 (dipeptidyl peptidase IV) gene Immunogenetics 40 1994 31 38
16. R. Mentlein Dipeptidyl-peptidase IV (CD26) - role in the inactivation of regulatory peptides Regul Pept 85 1999 9 24 (Pubitemid 29505281)
17. A.M. Lambeir, C. Durinx, and S. Scharpe 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 2003 209 294 (Pubitemid 36775376)
18. 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 (Pubitemid 46048557)
19. G.R. Lankas, B. Leiting, and R.S. Roy Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9 Diabetes 54 2005 2988 2994 (Pubitemid 41401097)
20. A.M. Lambeir, C. Durinx, and S. Sharpe 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 2003 209 294 (Pubitemid 36775376)
21. T. Vilsboll, H. Agerso, and T. Krarup Similar elimination rates of glucagon-like peptide-1 in obese type 2 diabetic patients and healthy subjects J Clin Endocrinol Metab 88 2003 220 224 (Pubitemid 36115169)
22. J.J. Holst, and C.F. Deacon Inhibition of the activity of dipeptidyl-peptidase IV as a treatment for type 2 diabetes Diabetes 47 1998 1663 1670 (Pubitemid 28476238)
23. M.K. Reimer, J.J. Holst, and B. Ahren Long-term inhibition of dipeptidyl peptidase IV improves glucose tolerance and preserves islet function in mice Eur J Endocrinol 146 2002 717 727 (Pubitemid 34552507)
24. B. Ahren, E. Simonsson, and H. Larsson Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4-week study period in type 2 diabetes Diabetes Care 25 2002 869 875 (Pubitemid 41094285)
25. G. Zhao, P.C. Taunk, and D.R. Magnin Diprolyl nitriles as potent dipeptidyl peptidase IV inhibitors Bioorg Med Chem Lett 15 2005 3992 3995 (Pubitemid 41132648)
26. Y. Nishio, H. Kimura, and S. Tosaki Discovery of new chemotype dipeptidyl peptidase IV inhibitors having (R)-3-amino-3-methyl piperidine as a pharmacophore Bioorg Med Chem Lett 20 2010 7246 7249
27. I.L. Lu, S.J. Lee, and H. Tsu Glutamic acid analogues as potent dipeptidyl peptidase IV and 8 inhibitors Bioorg Med Chem Lett 15 2005 3271 3275 (Pubitemid 40799072)
28. D.J. Drucker Therapeutic potential of dipeptidyl peptidase IV inhibitors for the treatment of type 2 diabetes Expert Opin Invest Drugs 12 1 2003 87 100 (Pubitemid 36104645)
29. J.J. Holst, and C.F. Deacon Inhibition of the activity of dipeptidyl-peptidase IV as a treatment for type 2 diabetes Diabetes 47 11 1998 1663 1670 (Pubitemid 28476238)
30. R.P. Pauly, H.U. Demuth, and F. Rosche Improved glucose tolerance in rats treated with the dipeptidyl peptidase IV (CD26) inhibitor Ile-thiazolidide Metab: Clin Exp 48 3 1999 385 389 (Pubitemid 29116004)
31. B. Sudre, P. Broqua, and R.B. White Chronic inhibition of circulating dipeptidyl peptidase IV by FE 999011 delays the occurrence of diabetes in male Zucker diabetic fatty rats Diabetes 51 5 2002 1461 1469 (Pubitemid 34826612)
32. B. Ahren, J.J. Holst, and H. Martensson Improved glucose tolerance and insulin secretion by inhibition of dipeptidyl peptidase IV in mice Eur J Pharmacol 404 1-2 2000 239 245
33. M. Reimer, J. Holst, and B. Ahren Long-term inhibition of DPP-IV improves glucose tolerance and preserves islet function in mice Eur J Endocrinol 146 5 2002 717 727 (Pubitemid 34552507)
34. N. Yasuda, T. Inoue, and T. Nagakura Enhanced secretion of glucagon-like peptide 1 by biguanide compounds Biochem Biophys Res Commun 298 5 2002 779 784 (Pubitemid 35356808)
35. N. Yasuda, T. Inoue, and T. Nagakura Metformin causes reduction of food intake and body weight gain and improvement of glucose intolerance in combination with dipeptidyl peptidase IV inhibitor in Zucker fa/fa rats J Pharmacol Exp Ther 310 2 2004 614 619 (Pubitemid 38988906)
36. S.A. Hinke, J.A. Pospisilik, and H.U. Demuth Dipeptidyl peptidase IV (DPIV/CD26) degradation of glucagon. Characterization of glucagon degradation products and DPIV-resistant analogs J Biol Chem 275 6 2000 3827 3834 (Pubitemid 30094605)
37. B. Ahren, M. Landin-Olsson, and P.A. Jansson Inhibition of dipeptidyl peptidase-4 reduces glycemia, sustains insulin levels and reduces glucagon levels in type 2 diabetes J Clin Endocrinol Metab 89 2004 2078 2084 (Pubitemid 38619835)
38. S. Ristic, S. Byiers, and J. Foley Improved glycaemic control with dipeptidyl peptidase-4 inhibition in patients with type 2 diabetes: vildagliptin (LAF237) dose response Diabetes Obes Metab 7 2005 692 698 (Pubitemid 41601073)
39. F.X. Pi-Sunyer, A. Schweizer, and D. Mills Efficacy and tolerability of vildagliptin monotherapy in drug-naïve patients with type 2 diabetes Diabetes Res Clin Pract 76 2007 132 138 (Pubitemid 46240373)
40. J. Rosenstock, J.E. Foley, and M. Rendell Effects of the dipeptidyl peptidase-IV inhibitor vildagliptin on incretin hormones, islet function, and postprandial glycemia in subjects with impaired glucose tolerance Diabetes Care 31 2008 30 35
41. M. Hanefeld, G.A. Herman, and M. Wu Once-daily sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of patients with type 2 diabetes Curr Med Res Opin 23 2007 1329 1339 (Pubitemid 46998442)
42. R. Scott, L. Wu, and M. Sanchez 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 2007 171 180
43. P. Aschner, M.S. Kipnes, and J.K. Lunceford 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 (Pubitemid 44912190)
44. A. Schweizer, A. Couturier, and J.E. Foley Comparison between vildagliptin and metformin to sustain reductions in HbA1c over 1 year in drug-naïve patients with type 2 diabetes Diabet Med 24 2007 955 961 (Pubitemid 47301637)
45. B. Ahrén, R. Gomis, and E. Standl 12- and 52-week efficacy of the DPP IV inhibitor LAF237 in metformin-treated patients with type 2 diabetes Diabetes Care 27 2004 2874 2880 (Pubitemid 39565052)
46. B. Charbonnel, A. Karasik, and J. Liu 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 2006 2638 2643 (Pubitemid 44912191)
47. A.J. Garber, A. Schweizer, and M.A. Baron Vildagliptin in combination with pioglitazone improves glycaemic control in patients with type 2 diabetes failing thiazolidinedione monotherapy: a randomized, placebo-controlled study Diabetes Obes Metab 9 2007 166 174 (Pubitemid 46206560)
48. J. Rosenstock, R.G. Brazg, and P.J. Andryuk 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 2006 1556 1568 (Pubitemid 44841980)
49. A.J. Garber, J.E. Foley, and M.A. Banerji Effects of vildagliptin on glucose control in patients with type 2 diabetes inadequately controlled with a sulphonylurea Diabetes Obes Metab 10 2008 1047 1056
50. K. Hermansen, M. Kipnes, and E. Luo 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 9 2007 733 745 (Pubitemid 47261855)
51. V. Fonseca, A. chweizer, and D. Albrecht Addition of vildagliptin to insulin improves glycemic control in type 2 diabetes Diabetologia 50 2007 1148 1155 (Pubitemid 46701545)
52. H.W. de Valk DPP IV inhibitors and combined treatment in type 2 diabetes: re-evaluation of clinical success and safety Rev Diabet Stud 4 2007 126 133
53. A.J. Scheen Pharmacokinetics of dipeptidyl peptidase-4 inhibitors Diabetes Obes Metab 12 2010 648 658
54. A.L. Peters Patient and treatment perspectives: revisiting the link between type 2 diabetes, weight gain, and cardiovascular risk Cleve Clin J Med 76 Suppl 5 2009 S20 S27
55. J. White Efficacy and safety of incretin based therapies: clinical trial data J Am Pharm Assoc 49 Suppl 1 2009 S30 S40
56. J.J. Neumiller Differential chemistry, mechanism of action, & pharmacology of GLP-1 receptor agonists & DPP IV inhibitors J Am Pharm Assoc 49 Suppl 1 2009 S16 S29
57. G. Herman, M. Hanefeld, and M. Wu Effect of MK-0431, a dipeptidyl peptidase IV (DPP IV) inhibitor, on glycemic control after 12 weeks in patients with type 2 diabetes 2005 Program and Abstracts of the 65th Scientific Sessions of the American Diabetes Association San Diego, CA [abstract 541-P]
58. V. Fonseca, S. deJager, and D. Albrecht Vildagliptin as add-on to insulin in patients with type 2 diabetes (T2DM) Diabetes 55 Suppl 1 2006 [abstract 467-P]
59. C. Jago American Diabetes Association - 66th scientific sessions 9-13 June 2006, Washington, DC, USA IDrugs 9 2006 538 541 (Pubitemid 44263162)
60. B. Buse, R. Henry, and J. Han Effects of exenatide (exendin-4) on glycemic control over 30 weeks in sulfonylurea-treated patients with type 2 diabetes Diabetes Care 27 2004 2628 2635 (Pubitemid 39441462)
61. A.J. Bergman, J. Cote, and B. Yi Effect of renal insufficiency on the pharmacokinetics of sitagliptin, a dipeptidyl peptidase-4 inhibitor Diabetes Care 30 2007 1862 1864 (Pubitemid 47036366)
62. J. Chan, R. Scott, and J. Ferreira Safety and efficacy of sitagliptin in patients with type 2 diabetes and chronic renal insufficiency Diabetes Obes Metab 10 2008 545 555 (Pubitemid 351850898)
63. D. Williams-Herman, S.S. Engel, and E. Round 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
64. Squibb BM. Onglyza (saxagliptin) 5 mg film coated tablets. Summary of product characteristics. Last date of revision: 09 October 2009. Available from: http://emc. medicines.org.uk/medicine/22315/SPC/Onglyza+5mg+film-coated+tablets [accessed 06.10.09].
65. M.L. Sulda, C.A. Abbott, and M. Hildebrandt DPIV/CD26 and FAP in cancer: a tale of contradictions Adv Exp Med Biol 575 2006 197 206
66. A. Matveyenko, S. Dry, and H.I. Cox Beneficial endocrine but adverse exocrine effects of sitagliptin in the human islet amyloid polypeptide transgenic rat model of type 2 diabetes: interactions with metformin Diabetes 58 2009 1604 1615
67. FDA Januvia Approval Package: medical review. Available from: http://www.fda.gov/cder/foi/nda/2006/021995s000-MedR.pdf [accessed 11.01.09].
68. A. Linke, S. Frank, and M. Mark The DPP IV inhibitor linagliptin (BI 1356) improves wound healing in ob/ob mice Diabetes 58 Suppl 1 2009 A161 [abstract]
69. M.D. Amico, C.D. Filippo, and R. Marfella Long-term inhibition of dipeptidyl peptidase-4 in Alzheimer's prone mice Exp Gerontol 45 2010 202 207
70. B.J. Lamont, and D.J. Drucker Differential antidiabetic efficacy of incretin agonists versus DPP IV inhibition in high fat fed mice Diabetes 57 2008 190 198
71. M.M. Zaruba, H.D. Theiss, M. Vallaster, and U. Mehl Synergy between CD26/DPP IV inhibition and G-CSF improves cardiac function after acute myocardial infarction Cell Stem Cell 4 2009 313 323
72. D.J. Drucker Dipeptidyl peptidase-4 inhibition and the treatment of Type 2 diabetes Diabetes Care 30 2007 1335 1343