Choosing between GLP-1 receptor agonists and DPP-4 inhibitors: A pharmacological perspective

Journal of Nutrition and Metabolism

Volumn 2012, Issue , 2012, Pages

  Brown, Dominique Xavier ^a   Evans, Marc ^a  

^a LLANDOUGH HOSPITAL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

EID: 84873852937     PISSN: 20900724     EISSN: 20900732     Source Type: Journal    
DOI: 10.1155/2012/381713     Document Type: Review

References (71)

1. Reid T., Choosing GLP-1 receptor agonists or DPP-4 inhibitors: weighing the clinical trial evidence. Clinical Diabetes 2012 30 1 3 12 2-s2.0-84855905976 10.2337/diaclin.30.1.3
2. Holst J. J., Vilsbøll T., Deacon C. F., The incretin system and its role in type 2 diabetes mellitus. Molecular and Cellular Endocrinology 2009 297 1-2 127 136 2-s2.0-57649234120 10.1016/j.mce.2008.08.012
3. Knop F. K., Vilsbøll T., Højberg P. V., Larsen S., Madsbad S., Vølund A., Holst J. J., Krarup T., Reduced incretin effect in type 2 diabetes: cause or consequence of the diabetic state? Diabetes 2007 56 8 1951 1959 2-s2.0-34547586659 10.2337/db07-0100 (Pubitemid 47195814)
4. Mcintyre N., Holdsworth C. D., Turner D. S., New interpretation of oral glucose tolerance. The Lancet 1964 284 7349 20 21 2-s2.0-0002294149
5. 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 2006 368 9548 1696 1705 2-s2.0-33846006173 10.1016/S0140-6736(06)69705-5 (Pubitemid 46048557)
6. Nauck M. A., Unraveling the science of incretin biology. European Journal of Internal Medicine 2009 20 supplement 2 S303 S308 2-s2.0-67649518005 10.1016/j.ejim.2009.05.012
7. Perry T., Greig N. H., The glucagon-like peptides: a double-edged therapeutic sword? Trends in Pharmacological Sciences 2003 24 7 377 383 2-s2.0-0041733259 10.1016/S0165-6147(03)00160-3 (Pubitemid 37315530)
8. 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 β -cell function in type 2 diabetes: a parallel-group study. Lancet 2002 359 9309 824 830 2-s2.0-0037045845 10.1016/S0140-6736(02)07952-7 (Pubitemid 34233752)
9. Baggio L. L., Drucker D. J., Biology of incretins: GLP-1 and GIP. Gastroenterology 2007 132 6 2131 2157 2-s2.0-34248223285 10.1053/j.gastro.2007. 03.054 (Pubitemid 46711096)
10. Morales J., The pharmacologic basis for clinical differences among GLP-1 receptor agonists and DPP-4 inhibitors. Postgraduate Medicine 2011 123 6 189 201 2-s2.0-82155192702 10.3810/pgm.2011.11.2508
11. Nathan D. M., 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 2009 32 3 e37 e38 2-s2.0-64749100501 10.2337/dc08-2195
12. Rodbard H. W., Jellinger P. S., Davidson J. A., Einhorn D., Garber A. J., Grunberger G., Handelsman Y., Horton E. S., Lebovitz H., Levy P., Moghissi E. S., Schwartz S. S., Statement by an American association of clinical endocrinologists / American college of endocrinology consensus panel on type 2 diabetes mellitus: an algorithm for glycemic control. Endocrine Practice 2009 15 6 540 559 2-s2.0-75549091263
13. Garber A. J., Long-acting glucagon-like peptide 1 receptor agonists: a review of their efficacy and tolerability. Diabetes Care 2011 34 S279 284 2-s2.0-79959778328
14. EMA, Summary of product characteristics: exenatide. 2012, http://www.ema.europa.eu/docs/en-GB/document-library/EPAR-Product-Information/ human/000698/WC500051845.pdf
15. Augeri D. J., Robl J. A., Betebenner D. A., Magnin D. R., Khanna A., Robertson J. G., Wang A., Simpkins L. M., Taunk P., Huang Q., Han S. P., Abboa-Offei B., Cap M., Xin L., Tao L., Tozzo E., Welzel G. E., Egan D. M., Marcinkeviciene J., Chang S. Y., Biller S. A., Kirby M. S., Parker R. A., Hamann L. G., Discovery and preclinical profile of saxagliptin (BMS-477118): ahighly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. Journal of Medicinal Chemistry 2005 48 15 5025 5037 2-s2.0-22744449063 10.1021/jm050261p (Pubitemid 41033142)
16. Kim D., Wang L., Beconi M., Eiermann G. J., Fisher M. H., He H., Hickey G. J., Kowalchick J. E., Leiting B., Lyons K., Marsilio F., McCann M. E., Patel R. A., Petrov A., Scapin G., Patel S. B., Roy R. S., Wu J. K., Wyvratt M. J., Zhang B. B., Zhu L., Thornberry N. A., Weber A. E., (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. Journal of Medicinal Chemistry 2005 48 1 141 151 2-s2.0-19944427998 10.1021/jm0493156 (Pubitemid 40105255)
17. Villhauer E. B., Brinkman J. A., Naderi G. B., Burkey B. F., Dunning B. E., Prasad K., Mangold B. L., Russell M. E., Hughes T. E., 1-[[(3-Hydroxy-1- adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. Journal of Medicinal Chemistry 2003 46 13 2774 2789 2-s2.0-0037777695 10.1021/jm030091l (Pubitemid 36702545)
18. Jose T., Inzucchi S. E., Cardiovascular effects of the DPP-4 inhibitors. Diabetes and Vascular Disease Research 2012 9 2 109 116 2-s2.0-84861131970 10.1177/1479164111436236
19. EMA, Summary of Product Characteristics: Linagliptin. 2012, http://www.ema.europa.eu/docs/en-GB/document-library/EPAR-Product-Information/ human/002110/WC500115745.pdf
20. Patel C. G., Li L., Girgis S., Kornhauser D. M., Frevert E. U., Boulton D. W., Two-way pharmacokinetic interaction studies between saxagliptin and cytochrome P450 substrates or inhibitors: simvastatin, diltiazem extended-release, and ketoconazole. Clinical Pharmacology: Advances and Applications 2011 3 1 13 25 2-s2.0-81255189032
21. Barnett A. H., Linagliptin: a novel dipeptidyl peptidase 4 inhibitor with a unique place in therapy. Advances in Therapy 2011 28 6 447 459 2-s2.0-79958230306 10.1007/s12325-011-0028-y
22. Buse J. B., Rosenstock J., Sesti G., Schmidt W. E., Montanya E., Brett J. H., Zychma M., Blonde L., 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). The Lancet 2009 374 9683 39 47 2-s2.0-67649666737 10.1016/S0140-6736(09)60659-0
23. Drucker D. J., Buse J. B., Taylor K., Kendall D. M., Trautmann M., Zhuang D., Porter L., Exenatide once weekly versus twice daily for the treatment of type 2 diabetes: a randomised, open-label, non-inferiority study. The Lancet 2008 372 9645 1240 1250 2-s2.0-53249142132 10.1016/S0140-6736(08)61206-4
24. EMA, Summary of product characteristics: BYDUREON. 2012, http://www.ema.europa.eu/docs/en-GB/document-library/EPAR-Product-Information/ human/002020/WC500108241.pdf
25. 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. Current Medical Research and Opinion 2008 24 10 2943 2952 2-s2.0-55549136417 10.1185/03007990802418851
26. Bergenstal R. M., Wysham C., MacConell L., Malloy J., Walsh B., Yan P., Wilhelm K., Malone J., Porter L. E., 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. The Lancet 2010 376 9739 431 439 2-s2.0-77955573674 10.1016/S0140-6736(10)60590-9
27. Pratley R. E., Nauck M., Bailey T., Montanya E., Cuddihy R., Filetti S., Thomsen A. B., Søndergaard R. E., Davies M., 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. The Lancet 2010 375 9724 1447 1456 2-s2.0-77952309372 10.1016/S0140-6736(10)60307-8
28. Ross S. A., Dzida G., Vora J., Khunti K., Kaiser M., Ligthelm R. J., Impact of weight gain on outcomes in type 2 diabetes. Current Medical Research and Opinion 2011 27 7 1431 1438 2-s2.0-79960061889 10.1185/03007995.2011.585396
29. Aroda V. R., Henry R. R., Han J., Huang W., DeYoung M. B., Darsow T., Hoogwerf B. J., Efficacy of GLP-1 receptor agonists and DPP-4 inhibitors: meta-analysis and systematic review. Clinical Therapeutics 2012 34 6 1247 1258.e22 2-s2.0-84863919671 10.1016/j.clinthera.2012.04.013
30. Shyangdan D. S., Royle P. L., Clar C., Sharma P., Waugh N. R., Glucagon-like peptide analogues for type 2 diabetes mellitus: systematic review and meta-analysis. BMC Endocrine Disorders 2010 10, article no. 20 2-s2.0-78649800940 10.1186/1472-6823-10-20
31. Madsbad S., Dipeptidyl peptidase-4 (DPP-4) inhibitors are favourable to Glucagon-Like Peptide-1 (GLP-1) agonists: no. European Journal of Internal Medicine 2012 23 2 132 136 2-s2.0-84859174317 10.1016/j.ejim.2011.11.003
32. Karagiannis T., Paschos P., Paletas K., Matthews D. R., Tsapas A., Dipeptidyl peptidase-4 inhibitors for treatment of type 2 diabetes mellitus in the clinical setting: systematic review and meta-analysis. BMJ 2012 344 e1369 2-s2.0-84859174317 10.1136/bmj.e1369
33. Campbell R. K., Fate of the beta-cell in the pathophysiology of type 2 diabetes. Journal of the American Pharmacists Association 2009 49 supplement 1 S10 15 2-s2.0-76749166241 10.1331/JAPhA.2009.09076
34. Farilla L., Bulotta A., Hirshberg B., Li Calzi S., Khoury N., Noushmehr H., Bertolotto C., Di Mario U., Harlan D. M., Perfetti R., Glucagon-Like Peptide 1 inhibits cell apoptosis and improves glucose responsiveness of freshly isolated human islets. Endocrinology 2003 144 12 5149 5158 2-s2.0-0345374580 10.1210/en.2003-0323 (Pubitemid 37476040)
35. Song W. J., Seshadri M., Ashraf U., Mdluli T., Mondal P., Keil M., Azevedo M., Kirschner L. S., Stratakis C. A., Hussain M. A., Snapin mediates incretin action and augments glucose-dependent insulin secretion. Cell Metabolism 2011 13 3 308 319 2-s2.0-79952126838 10.1016/j.cmet.2011.02.002
36. Cunha D. A., Ladrière L., Ortis F., Igoillo-Esteve M., Gurzov E. N., Lupi R., Marchetti P., Eizirik D. L., Cnop M., Glucagon-like peptide-1 agonists protect pancreatic β -cells from lipotoxic endoplasmic reticulum stress through upregulation of BIP and JunB. Diabetes 2009 58 12 2851 2862 2-s2.0-73249116246 10.2337/db09-0685
37. Duttaroy A., Voelker F., Merriam K., Zhang X., Ren X., Subramanian K., Hughes T. E., Burkey B. F., The DPP-4 inhibitor vildagliptin increases pancreatic beta cell mass in neonatal rats. European Journal of Pharmacology 2011 650 2-3 703 707 2-s2.0-78651101398 10.1016/j.ejphar.2010.10.062
38. Scheen A. J., Dipeptidylpeptidase-4 (DPP-4) inhibitors are favourable to glucagon-like peptide-1 (GLP-1) receptor agonists: yes. European Journal of Internal Medicine 2012 23 2 126 131 2-s2.0-84856440706 10.1016/j.ejim.2011.10. 007
39. Sinha A., Rajan M., Hoerger T., Pogach L., Costs and consequences associated with newer medications for glycemic control in type 2 diabetes. Diabetes Care 2010 33 4 695 700 2-s2.0-77953046644 10.2337/dc09-1488
40. Lage M. J., Fabunmi R., Boye K. S., Misurski D. A., Comparison of costs among patients with type 2 diabetes treated with exenatide or sitagliptin therapy. Advances in Therapy 2009 26 2 217 229 2-s2.0-73449122627 10.1007/s12325-009-0002-0
41. Levey A. S., Coresh J., Balk E., Kausz A. T., Levin A., Steffes M. W., Hogg R. J., Perrone R. D., Lau J., Eknoyan G., Willis K., National kidney foundation practice guidelines for chronic kidney disease: evaluation, classification, and stratification. Annals of Internal Medicine 2003 139 2 137 I47 2-s2.0-1642502319
42. Oulahiane A., Anaddam S., Ouleghzal H., Elhaddad N., Moussaoui S., Yaagoubi N., Boufares F., Belmejdoub G., Diabetes management issues for patients with chronic kidney disease. Nephrologie et Therapeutique 2012 8 3 135 140 2-s2.0-84865372953 10.1016/j.nephro.2011.07.410
43. Neumiller J. J., Clinical pharmacology of incretin therapies for type 2 diabetes mellitus: Implications for treatment. Clinical Therapeutics 2011 33 5 528 576 2-s2.0-79958743689 10.1016/j.clinthera.2011.04.024
44. Simonsen L., Holst J. J., Deacon C. F., Exendin-4, but not glucagon-like peptide-1, is cleared exclusively by glomerular filtration in anaesthetised pigs. Diabetologia 2006 49 4 706 712 2-s2.0-33644819643 10.1007/s00125-005-0128- 9 (Pubitemid 43357544)
45. Linnebjerg H., Kothare P. A., Park S., Mace K., Reddy S., Mitchell M., Lins R., Effect of renal impairment on the pharmacokinetics of exenatide. British Journal of Clinical Pharmacology 2007 64 3 317 327 2-s2.0-34548034895 10.1111/j.1365-2125.2007.02890.x (Pubitemid 47283860)
46. Malm-Erjefält M., Bjørnsdottir I., Vanggaard J., Helleberg H., Larsen U., Oosterhuis B., Van Lier J. J., Zdravkovic M., Olsen A. K., Metabolism and excretion of the once-daily human glucagon-like peptide-1 analog liraglutide in healthy male subjects and its in vitro degradation by dipeptidyl peptidase IV and neutral endopeptidase. Drug Metabolism and Disposition 2010 38 11 1944 1953 2-s2.0-78049365082 10.1124/dmd.110.034066
47. Jacobsen L. V., Hindsberger C., Robson R., Zdravkovic M., Effect of renal impairment on the pharmacokinetics of the GLP-1 analogue liraglutide. British Journal of Clinical Pharmacology 2009 68 6 898 905 2-s2.0-70849096647 10.1111/j.1365-2125.2009.03536.x
48. EMA, Summary of product characteristics: liraglutide. 2012, http://www.ema.europa.eu/docs/en-GB/document-library/EPAR-Product-Information/ human/001026/WC500050017.pdf
49. Bergman A. J., Cote J., Yi B., Marbury T., Swan S. K., Smith W., Gottesdiener K., Wagner J., Herman G. A., Effect of renal insufficiency on the pharmacokinetics of sitagliptin, a dipeptidyl peptidase-4 inhibitor. Diabetes Care 2007 30 7 1862 1864 2-s2.0-34447120048 10.2337/dc06-2545 (Pubitemid 47036366)
50. Migoya E. M., Stevens C. H., Bergman A. J., Luo W. L., Lasseter K. C., Dilzer S. C., Davies M. J., Wagner J. A., Herman G. A., Effect of moderate hepatic insufficiency on the pharmacokinetics of sitagliptin. Canadian Journal of Clinical Pharmacology 2009 16 1 e165 e170 2-s2.0-63049113329
51. Boulton D. W., Li L., Frevert E. U., Tang A., Castaneda L., Vachharajani N. N., Kornhauser D. M., Patel C. G., Influence of renal or hepatic impairment on the pharmacokinetics of saxagliptin. Clinical Pharmacokinetics 2011 50 4 253 265 2-s2.0-79952088990 10.2165/11584350-000000000-00000
52. EEIG, BMS-A, Summary of product characteristics: Saxagliptin. 2012, http://www.medicines.org.uk/emc/medicine/22315/SPC/
53. He Y. L., Sadler B. M., Sabo R., Balez S., Wang Y., Campestrini J., Laurent A., Ligueros-Saylan M., Howard D., The absolute oral bioavailability and population-based pharmacokinetic modelling of a novel dipeptidylpeptidase-IV inhibitor, vildagliptin, in healthy volunteers. Clinical Pharmacokinetics 2007 46 9 787 802 2-s2.0-34548324787 10.2165/00003088-200746090-00006 (Pubitemid 47347450)
54. He H., Tran P., Yin H., Smith H., Batard Y., Wang L., Einolf H., Gu H., Mangold J. B., Fischer V., Howard D., Absorption, metabolism, and excretion of [14C]vildagliptin, a novel dipeptidyl peptidase 4 inhibitor, in humans. Drug Metabolism and Disposition 2009 37 3 536 544 2-s2.0-61449170189 10.1124/dmd.108.023010
55. He Y. L., Sabo R., Campestrini J., Wang Y., Ligueros-Saylan M., Lasseter K. C., Dilzer S. C., Howard D., Dole W. P., The influence of hepatic impairment on the pharmacokinetics of the dipeptidyl peptidase IV (DPP-4) inhibitor vildagliptin. European Journal of Clinical Pharmacology 2007 63 7 677 686 2-s2.0-34250307638 10.1007/s00228-007-0312-6 (Pubitemid 46911348)
56. EMA, Summary of product characteristics: Vildagliptin. 2012, http://www.ema.europa.eu/docs/en-GB/document-library/EPAR-Product-Information/ human/000771/WC500020327.pdf
57. Graefe-Mody U., Friedrich C., Port A., Ring A., Retlich S., Heise T., Halabi A., Woerle H.-J., Effect of renal impairment on the pharmacokinetics of the dipeptidyl peptidase-4 inhibitor linagliptin. Diabetes, Obesity and Metabolism 2011 13 10 939 946 2-s2.0-81855166062 10.1111/j.1463-1326.2011.01458. x
58. Moretto T. J., Milton D. R., Ridge T. D., MacConell L. A., Okerson T., Wolka A. M., Brodows R. G., 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. Clinical Therapeutics 2008 30 8 1448 1460 2-s2.0-51549095571 10.1016/j.clinthera.2008.08. 006
59. Garber A., Henry R., Ratner R., Garcia-Hernandez P. A., Rodriguez-Pattzi H., Olvera-Alvarez I., Hale P. M., Zdravkovic M., Bode B., Liraglutide versus glimepiride monotherapy for type 2 diabetes (LEAD-3 Mono): a randomised, 52-week, phase III, double-blind, parallel-treatment trial. The Lancet 2009 373 9662 473 481 2-s2.0-59449101432 10.1016/S0140-6736(08)61246-5
60. Campbell R. K., Cobble M. E., Reid T. S., Shomali M. E., Safety, tolerability, and nonglycemic effects of incretin-based therapies. Journal of Family Practice 2010 59 9, supplement 9 S20 S27 2-s2.0-77956665223
61. Näslund E., Bogefors J., Skogar S., Grybäck P., Jacobsson H., Holst J. J., Hellström P. M., GLP-1 slows solid gastric emptying and inhibits insulin, glucagon, and PYY release in humans. American Journal of Physiology 1999 277 3 R910 R916 2-s2.0-0032871230 (Pubitemid 29458166)
62. Nauck M. A., Heimesaat M. M., Behle K., Holst J. J., Nauck M. S., Ritzel R., Hüfner M., Schmiegel W. H., Effects of glucagon-like peptide 1 on counterregulatory hormone responses, cognitive functions, and insulin secretion during hyperinsulinemic, stepped hypoglycemic clamp experiments in healthy volunteers. Journal of Clinical Endocrinology and Metabolism 2002 87 3 1239 1246 2-s2.0-0036959991 10.1210/jc.87.3.1239 (Pubitemid 36121094)
63. Nelson P., Poon T., Guan X., Schnabel C., Wintle M., Fineman M., The incretin mimetic exenatide as a monotherapy in patients with type 2 diabetes. Diabetes Technology and Therapeutics 2007 9 4 317 326 2-s2.0-34548321003 10.1089/dia.2006.0024 (Pubitemid 47340082)
64. 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. International Journal of Clinical Practice 2007 61 1 171 180 2-s2.0-33847024333 10.1111/j.1742-1241.2006.01246.x
65. 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 2006 29 12 2632 2637 2-s2.0-33845472504 10.2337/dc06-0703 (Pubitemid 44912190)
66. 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 2006 49 11 2564 2571 2-s2.0-33845489598 10.1007/s00125-006-0416-z
67. EMA, Summary of product characteristics: Sitagliptin. 2012, http://www.ema.europa.eu/docs/en-GB/document-library/EPAR-Product-Information/ human/000722/WC500039054.pdf
68. Noel R. A., Braun D. K., Patterson R. E., Bloomgren G. L., Increased risk of acute pancreatitis and biliary disease observed in patients with type 2 diabetes: a retrospective cohort study. Diabetes Care 2009 32 5 834 838 2-s2.0-65949111736 10.2337/dc08-1755
69. Garg R., Chen W., Pendergrass M., Acute pancreatitis in type 2 diabetes treated with exenatide or sitagliptin: a retrospective observational pharmacy claims analysis. Diabetes Care 2010 33 11 2349 2354 2-s2.0-79951704452 10.2337/dc10-0482
70. Dore D. D., Seeger J. D., Chan K. A., Use of a claims-based active drug safety surveillance system to assess the risk of acute pancreatitis with exenatide or sitagliptin compared to metformin or glyburide. Current Medical Research and Opinion 2009 25 4 1019 1027 2-s2.0-67649304917 10.1185/ 03007990902820519
71. Parks M., Rosebraugh C., Weighing risks and benefits of liraglutide-the FDA's review of a new antidiabetic therapy. New England Journal of Medicine 2010 362 9 774 777 2-s2.0-77649294607 10.1056/NEJMp1001578