Sitagliptyna – czy jest dla niej miejsce w nowoczesnym leczeniu cukrzycy typu 2? Artykuł przeglądowy
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Opublikowane:
cze 30, 2023
Słowa kluczowe:
cukrzyca typu 2, inhibitor DPP-4, sitagliptyna, inkretyny
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Abstrakt
Cukrzyca typu 2 (DM2) stanowi rosnący problem kliniczny, a niedostateczna kontrola metaboliczna choroby u wielu pacjentów skłania do poszukiwania nowych metod terapii. W ostatnich latach wprowadzono nowe leki, których mechanizm działania opiera się na wykorzystaniu osi inktretynowej do optymalizacji leczenia cukrzycy. Wśród leków wykorzystujących potencjał efektu inkretynowego znajdują się inhibitory dipeptydylopeptydazy 4 (DPP-4).
W artykule przedstawiono podstawy koncepcji wykorzystania efektu inkretynowego w terapii cukrzycy, podstawowy profil farkamologiczny sitagliptyny oraz istotne badania kliniczne dotyczące skuteczności i bezpieczeństwa leku. Przegląd ten ma na celu podsumowanie pozycji sitagliptyny jako leku dobrze tolerowanego, względnie skutecznego, bezpiecznego dla pacjentów z umiarkowanymi zaburzeniami funkcji nerek i wątroby, jak również leku o niskim ryzyku wywołania hipoglikemii.
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Jak cytować
KosińskiM. (2023). Sitagliptyna – czy jest dla niej miejsce w nowoczesnym leczeniu cukrzycy typu 2? . Medycyna Faktów , 16(2(59), 219-224. https://doi.org/10.24292/01.MF.0223.14
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Bibliografia
1. McIntyre N, Holdsworth CD, Turner DS. Intestinal factors in the control of insulin secretion. J Clin Endocrinol Metab. 1965; 25(10): 1317-24. http://doi.org/10.1210/jcem-25-10-1317.
2. Perley MJ, Kipnis DM. Plasma insulin responses to oral and intravenous glucose: studies in normal and diabetic sujbjects. J Clin Invest. 1967; 46(12): 1954-62. http://doi.org/10.1172/JCI105685.
3. Schmidt WE, Siegel EG, Creutzfeldt W. Glucagon-like peptide-1 but not glucagon-like peptide-2 stimulates insulin release from isolated rat pancreatic islets. Diabetologia. 1985; 28(9): 704-7. http://doi.org/10.1007/BF00291980.
4. Ahrén B. Gut peptides and type 2 diabetes mellitus treatment. Curr Diab Rep. 2003; 3(5): 365-72. http://doi.org/10.1007/s11892-003-0079-9.
5. Ehses JA, Casilla VR, Doty T et al. Glucose-dependent insulinotropic polypeptide promotes beta-(INS-1) cell survival via cyclic adenosine monophosphate-mediated caspase-3 inhibition and regulation of p38 mitogen-activated protein kinase. Endocrinology. 2003; 144(10): 4433-45. http://doi.org/10.1210/en.2002-0068.
6. Drucker DJ. Biological actions and therapeutic potential of the glucagon-like peptides. Gastroenterology. 2002; 122(2): 531-44. http://doi.org/10.1053/gast.2002.31068.
7. 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. http://doi.org/10.1210/en.2003-0323.
8. Vilsbøll T, Holst JJ. Incretins, insulin secretion and Type 2 diabetes mellitus. Diabetologia. 2004; 47(3): 357-66. http://doi.org/10.1007/s00125-004-1342-6.
9.Nauck MA, Heimesaat MM, Orskov C et al. 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. 1993; 91(1): 301-7. http://doi.org/10.1172/JCI116186.
10. Vilsbøll 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(3): 609-13. http://doi.org/10.2337/diabetes.50.3.609.
11. Lankas GR, Leiting B, Roy RS et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes. 2005; 54(10): 2988-94. http://doi.org/10.2337/diabetes.54.10.2988.
12. Kim D, Wang L, Beconi M et al. (2R)-4-oxo-4-3-(trifluoromethyl)-5,6-dihydro1,2,4triazolo4,3-apyrazin-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(1): 141-51. http://doi.org/10.1021/jm0493156.
13. Herman GA, Stein PP, Thornberry NA et al. Dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes: focus on sitagliptin. Clin Pharmacol Ther. 2007; 81(5): 761-7. http://doi.org/10.1038/sj.clpt.6100167.
14. Palalau AI, Tahrani AA, Piya MK et al. DPP-4 inhibitors in clinical practice. Postgrad Med. 2009; 121(6): 70-100. http://doi.org/10.3810/pgm.2009.11.2079.
15. 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(9548): 1696-705. http://doi.org/10.1016/S0140-6736(06)69705-5.
16.Hanefeld M, Herman GA, Wu M et al. Once-daily sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of patients with type 2 diabetes. Curr Med Res Opin. 2007; 23(6): 1329-39. http://doi.org/10.1185/030079907X188152.
17. Goldstein BJ, Feinglos MN, Lunceford JK 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(8): 1979-87. http://doi.org/10.2337/dc07-0627.
18.Migoya EM, Bergeron R, Miller JL et al. 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(6): 801-8. http://doi.org/10.1038/clpt.2010.184.
19.Mohan V, Yang W, Son H-Y et al. 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(1): 106-16. http://doi.org/10.1016/j.diabres.2008.10.009.
20. 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. http://doi.org/10.1007/s00125-006-0416-z.
21. 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. http://doi.org/10.2337/dc06-0706.
22.Bergenstal RM, Wysham C, MacConell L 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. 2010; 376(9739): 431-9. http://doi.org/10.1016/S0140-6736(10)60590-9.
23. 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(5): 733-45. http://doi.org/10.1111/j.1463-1326.2007.00744.x.
24. Rosenstock J, Brazg R, Andryuk PJ et al. 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(10): 1556-68. http://doi.org/10.1016/j.clinthera.2006.10.007.
25. Vilsbøll T, Rosenstock J, Yki-Järvinen H et al. Efficacy and safety of sitagliptin when added to insulin therapy in patients with type 2 diabetes. Diabetes Obes Metab. 2010; 12(2): 167-77. http://doi.org/10.1111/j.1463-1326.2009.01173.x.
26. Seck T, Nauck M, Sheng D et al. 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(5): 562-76. http://doi.org/10.1111/j.1742-1241.2010.02353.x.
27. Aschner P, Katzeff HL, Guo H et al. Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes. Diabetes Obes Metab. 2010; 12(3): 252-61. http://doi.org/10.1111/j.1463-1326.2009.01187.x.
28.Arechavaleta R, Seck T, Chen Y et al. 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(2): 160-8. http://doi.org/10.1111/j.1463-1326.2010.01334.x.
29. Scheen AJ, Charpentier G, Ostgren CJ et al. 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(7): 540-9. http://doi.org/10.1002/dmrr.1114.
30. Pratley RE, Nauck M, Bailey T et al. 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(9724): 1447-56. http://doi.org/10.1016/S0140-6736(10)60307-8.
31. DeFronzo RA, Okerson T, Viswanathan P et al. 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(10): 2943-52. http://doi.org/10.1185/03007990802418851.
32. Green JB, Bethel MA, Armstrong PW et al. Effect of Sitagliptin on Cardiovascular Outcomes in Type 2 Diabetes. N Engl J Med. 2015; 373(3): 232-42. http://doi.org/10.1056/NEJMoa1501352.
33. Nauck M, Stöckmann F, Ebert R et al. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia. 1986; 29(1): 46-52.
2. Perley MJ, Kipnis DM. Plasma insulin responses to oral and intravenous glucose: studies in normal and diabetic sujbjects. J Clin Invest. 1967; 46(12): 1954-62. http://doi.org/10.1172/JCI105685.
3. Schmidt WE, Siegel EG, Creutzfeldt W. Glucagon-like peptide-1 but not glucagon-like peptide-2 stimulates insulin release from isolated rat pancreatic islets. Diabetologia. 1985; 28(9): 704-7. http://doi.org/10.1007/BF00291980.
4. Ahrén B. Gut peptides and type 2 diabetes mellitus treatment. Curr Diab Rep. 2003; 3(5): 365-72. http://doi.org/10.1007/s11892-003-0079-9.
5. Ehses JA, Casilla VR, Doty T et al. Glucose-dependent insulinotropic polypeptide promotes beta-(INS-1) cell survival via cyclic adenosine monophosphate-mediated caspase-3 inhibition and regulation of p38 mitogen-activated protein kinase. Endocrinology. 2003; 144(10): 4433-45. http://doi.org/10.1210/en.2002-0068.
6. Drucker DJ. Biological actions and therapeutic potential of the glucagon-like peptides. Gastroenterology. 2002; 122(2): 531-44. http://doi.org/10.1053/gast.2002.31068.
7. 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. http://doi.org/10.1210/en.2003-0323.
8. Vilsbøll T, Holst JJ. Incretins, insulin secretion and Type 2 diabetes mellitus. Diabetologia. 2004; 47(3): 357-66. http://doi.org/10.1007/s00125-004-1342-6.
9.Nauck MA, Heimesaat MM, Orskov C et al. 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. 1993; 91(1): 301-7. http://doi.org/10.1172/JCI116186.
10. Vilsbøll 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(3): 609-13. http://doi.org/10.2337/diabetes.50.3.609.
11. Lankas GR, Leiting B, Roy RS et al. Dipeptidyl peptidase IV inhibition for the treatment of type 2 diabetes: potential importance of selectivity over dipeptidyl peptidases 8 and 9. Diabetes. 2005; 54(10): 2988-94. http://doi.org/10.2337/diabetes.54.10.2988.
12. Kim D, Wang L, Beconi M et al. (2R)-4-oxo-4-3-(trifluoromethyl)-5,6-dihydro1,2,4triazolo4,3-apyrazin-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(1): 141-51. http://doi.org/10.1021/jm0493156.
13. Herman GA, Stein PP, Thornberry NA et al. Dipeptidyl peptidase-4 inhibitors for the treatment of type 2 diabetes: focus on sitagliptin. Clin Pharmacol Ther. 2007; 81(5): 761-7. http://doi.org/10.1038/sj.clpt.6100167.
14. Palalau AI, Tahrani AA, Piya MK et al. DPP-4 inhibitors in clinical practice. Postgrad Med. 2009; 121(6): 70-100. http://doi.org/10.3810/pgm.2009.11.2079.
15. 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(9548): 1696-705. http://doi.org/10.1016/S0140-6736(06)69705-5.
16.Hanefeld M, Herman GA, Wu M et al. Once-daily sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of patients with type 2 diabetes. Curr Med Res Opin. 2007; 23(6): 1329-39. http://doi.org/10.1185/030079907X188152.
17. Goldstein BJ, Feinglos MN, Lunceford JK 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(8): 1979-87. http://doi.org/10.2337/dc07-0627.
18.Migoya EM, Bergeron R, Miller JL et al. 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(6): 801-8. http://doi.org/10.1038/clpt.2010.184.
19.Mohan V, Yang W, Son H-Y et al. 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(1): 106-16. http://doi.org/10.1016/j.diabres.2008.10.009.
20. 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. http://doi.org/10.1007/s00125-006-0416-z.
21. 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. http://doi.org/10.2337/dc06-0706.
22.Bergenstal RM, Wysham C, MacConell L 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. 2010; 376(9739): 431-9. http://doi.org/10.1016/S0140-6736(10)60590-9.
23. 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(5): 733-45. http://doi.org/10.1111/j.1463-1326.2007.00744.x.
24. Rosenstock J, Brazg R, Andryuk PJ et al. 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(10): 1556-68. http://doi.org/10.1016/j.clinthera.2006.10.007.
25. Vilsbøll T, Rosenstock J, Yki-Järvinen H et al. Efficacy and safety of sitagliptin when added to insulin therapy in patients with type 2 diabetes. Diabetes Obes Metab. 2010; 12(2): 167-77. http://doi.org/10.1111/j.1463-1326.2009.01173.x.
26. Seck T, Nauck M, Sheng D et al. 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(5): 562-76. http://doi.org/10.1111/j.1742-1241.2010.02353.x.
27. Aschner P, Katzeff HL, Guo H et al. Efficacy and safety of monotherapy of sitagliptin compared with metformin in patients with type 2 diabetes. Diabetes Obes Metab. 2010; 12(3): 252-61. http://doi.org/10.1111/j.1463-1326.2009.01187.x.
28.Arechavaleta R, Seck T, Chen Y et al. 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(2): 160-8. http://doi.org/10.1111/j.1463-1326.2010.01334.x.
29. Scheen AJ, Charpentier G, Ostgren CJ et al. 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(7): 540-9. http://doi.org/10.1002/dmrr.1114.
30. Pratley RE, Nauck M, Bailey T et al. 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(9724): 1447-56. http://doi.org/10.1016/S0140-6736(10)60307-8.
31. DeFronzo RA, Okerson T, Viswanathan P et al. 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(10): 2943-52. http://doi.org/10.1185/03007990802418851.
32. Green JB, Bethel MA, Armstrong PW et al. Effect of Sitagliptin on Cardiovascular Outcomes in Type 2 Diabetes. N Engl J Med. 2015; 373(3): 232-42. http://doi.org/10.1056/NEJMoa1501352.
33. Nauck M, Stöckmann F, Ebert R et al. Reduced incretin effect in type 2 (non-insulin-dependent) diabetes. Diabetologia. 1986; 29(1): 46-52.