A review of sitagliptin with special emphasis on its use in moderate to severe renal impairment

Drug Design, Development and Therapy

Volumn 7, Issue , 2013, Pages 893-903

  Eligar, Vinay S ^a   Bain, Stephen C ^b  

^a UNIVERSITY HOSPITAL OF WALES   (United Kingdom)

^b SWANSEA UNIVERSITY   (United Kingdom)

Author keywords

Chronic kidney disease; CKD; Renal impairment; Sitagliptin

Indexed keywords

2,4 THIAZOLIDINEDIONE DERIVATIVE; ALOGLIPTIN; DIPEPTIDYL PEPTIDASE IV INHIBITOR; EXENDIN 4; GLIPIZIDE; GLUCAGON LIKE PEPTIDE 1; HEMOGLOBIN A1C; INCRETIN; INSULIN; LINAGLIPTIN; LIRAGLUTIDE; LIXISENATIDE; METFORMIN; PIOGLITAZONE; PLACEBO; PROINSULIN; ROSIGLITAZONE; SAXAGLIPTIN; SITAGLIPTIN; SULFONYLUREA DERIVATIVE; VILDAGLIPTIN;

ADD ON THERAPY; ALBUMINURIA; AREA UNDER THE CURVE; CARDIOVASCULAR DISEASE; CELL DAMAGE; CELL FUNCTION; CHRONIC KIDNEY DISEASE; DIABETES MELLITUS; DIABETOGENESIS; DISEASE ASSOCIATION; DISEASE COURSE; DISEASE SEVERITY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DOSE INCREASE; DRUG DOSE REDUCTION; DRUG DOSE TITRATION; DRUG EXCRETION; DRUG HALF LIFE; DRUG INDUCED HEADACHE; DRUG METABOLISM; GASTROINTESTINAL DISEASE; GENETIC PREDISPOSITION; GLYCEMIC CONTROL; HUMAN; HYPERGLYCEMIA; HYPOGLYCEMIA; INSULIN RESISTANCE; KIDNEY FAILURE; MAXIMUM PLASMA CONCENTRATION; METABOLIC SYNDROME X; MONOTHERAPY; NON INSULIN DEPENDENT DIABETES MELLITUS; NONHUMAN; PANCREAS ISLET BETA CELL; RENAL REPLACEMENT THERAPY; RESPIRATORY TRACT INFECTION; REVIEW; RHABDOMYOLYSIS; RHINOPHARYNGITIS; SIDE EFFECT; SINGLE DRUG DOSE; WEIGHT GAIN;

CHRONIC KIDNEY DISEASE; CKD; RENAL IMPAIRMENT; SITAGLIPTIN;

ANIMALS; DIABETES MELLITUS, TYPE 2; DIPEPTIDYL-PEPTIDASE IV INHIBITORS; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; HYPOGLYCEMIC AGENTS; PYRAZINES; RENAL INSUFFICIENCY, CHRONIC; SEVERITY OF ILLNESS INDEX; TRIAZOLES;

EID: 84883444066     PISSN: 11778881     EISSN: None     Source Type: Journal    
DOI: 10.2147/DDDT.S32331     Document Type: Review

References (63)

1. Diabetes UK [homepage on the Internet]. Available from http://www.diabetes.org.uk. Accessed July 1, 2013.
2. González EL, Johansson S, Wallander MA, Rodríguez LA. Trends in the prevalence and incidence of diabetes in the UK: 1996-2005. J Epidemiol Community Health. 2009;63(4):332-326.
3. National Diabetes Information Clearinghouse (NDIC). National Diabetes Statistics, 2011. Available from: http://diabetes.niddk.nih.gov/dm/pubs/statistics/. Accessed July 1, 2013.
4. Nathan DM, Buse JB, Davidson MB, et al; American Diabetes Association; European Association for Study of Diabetes. Medical management of hyperglycemia in type 2 diabetes: a consensus statement of the American Diabetes Association and the European Association for the Study of Diabetes. Diabetes Care. 2009;32:193-203.
5. National Institute for Health and Care Excellence (NICE). CG87 Type 2 diabetes-newer agents (a partial update of CG66): short guideline. Available from: http://www.nice.org.uk/nicemedia/live/12165/44318/44318.pdf. Accessed July 1, 2013.
6. National Kidney Foundation. KDOQI clinical practice guideline for diabetes and CKD: 2012 update. Am J Kidney Dis. 2012;60(5): 850-886.
7. National Institute for Health and Care Excellence (NICE). CG73 Chronic kidney disease: early identification and management of chronic kidney disease in adults in primary and secondary care. Available from: http://www.nice.org.uk/Guidance/CG73. Accessed July 1, 2013.
8. Hallan SI, Coresh J, Astor BC, et al. International comparison of the relationship of chronic kidney disease prevalence and ESRD risk. J Am Soc Nephrol. 2006;17(8):2275-2284.
9. Coresh J, Astor BC, Greene T, Eknoyan G, Levey AS. Prevalence of chronic kidney disease and decreased kidney function in the adult US population: Third National Health and Nutrition Examination Survey. Am J Kidney Dis. 2003;41(1):1-12.
10. Haroun MK, Jaar BG, Hoffman SC, Comstock GW, Klag MJ, Coresh J. Risk factors for chronic kidney disease: a prospective study of 23,534 men and women in Washington County, Maryland. J Am Soc Nephrol. 2003;14(11):2934-2941.
11. New JP, Middleton RJ, Klebe B, et al. Assessing the prevalence, monitoring and management of chronic kidney disease in patients with diabetes compared with those without diabetes in general practice. Diabet Med. 2007;24(4):364-369.
12. Hippisley-Cox J, Coupland C. Predicting the risk of chronic kidney disease in men and women in England and Wales: prospective derivation and external validation of the QKidney Scores. BMC Fam Pract. 2010;11:49.
13. United States Renal Data System. USRDS 2007 annual data report. Bethesda, MD: National Institute of Diabetes and Digestive and Kidney Diseases, National Institutes of Health, US Department of Health and Human Services; 2007.
14. Tonelli M, Muntner P, Lloyd A, et al; Alberta Kidney Disease Network. Using proteinuria and estimated glomerular filtration rate classify risk in patients with chronic kidney disease. A cohort study. Ann Intern Med. 2011;154:12-21.
15. Kidney Disease Improving Global Outcomes (KDIGO). 2012 clinical practice guidelines for the evaluation and management of chronic kidney disease. Kidney Int Suppl. 2013;3:1-150.
16. Liang J, Leung KK, Lam SY, Leung PS. Combined treatment with a dipeptidyl peptidase-IV inhibitor (sitagliptin) and an angiotensin II type 1 receptor blocker (losartan) promotes islet regeneration via enhanced differentiation of pancreatic progenitor cells. Diabetes Obes Metab. 2012;14(9):842-581.
17. Brazg R, Xu L, Dalla Man C, Cobelli C, Thomas K, Stein PP. Effect of adding sitagliptin, a dipeptidylpeptidase-4 inhibitor, to metformin on 24-h glycemic control and beta-cell function in patients with type 2 diabetes. Diabet Obes Metab. 2007;9:186-193.
18. Mu J, Petrov A, Eiermann GJ, et al. Inhibition of DPP-4 with sitagliptin improves glycemic control and restores islet cell mass and function in a rodent model of type 2 diabetes. Eur J Pharmacol. 2009;623:148-154.
19. Ahrén B, Winzell MS, Wierup N, Sundler F, Burkey B, Hughes TE. DPP-4 inhibition improves glucose tolerance and increases insulin and GLP-1 responses to gastric glucose in association with normalized islet topography in mice with beta-cell specific overexpression of human islet amyloid polypeptide. Regul Pept. 2007;143:97-103.
20. Williams-Herman D, Xu L, Teng R, et al. Effect of initial combination therapy with sitagliptin and metformin on β-cell function in patients with type 2 diabetes. Diabetes Obes Metab. 2012;14(1):67-76.
21. Karasik A, Aschner P, Katzeff H, Davies MJ, Stein PP. Sitagliptin, a DPP-4 inhibitor for the treatment of patients with type 2 diabetes: a review of recent clinical trials. Curr Med Res Opin. 2008;24(2): 489-496.
22. Zerilli T, Pyon EY. Sitagliptin phosphate: a DPP-4 inhibitor for the treatment of type 2 diabetes mellitus. Clin Ther. 2007;29(12): 2614-2634.
23. Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet. 2006;368:1696-1705.
24. Balas B, Baig MR, Watson C, et al. The dipeptidyl peptidase IV inhibitor vildagliptin suppresses endogenous glucose production and enhances islet function after single dose administration in type 2 diabetic patients. J Clin Endocrinol Metab. 2007;92:1249-1255.
25. Ahrén B, Simonsson E, Larsson H, et al. Inhibition of dipeptidyl peptidase IV improves metabolic control over a 4 week study period in type 2 diabetes. Diabetes Care. 2002;25:869-875.
26. Bergman A, Ebel D, Liu F, et al. Absolute bioavailability of sitagliptin, an oral dipeptidyl peptidase-4 inhibitor, in an oral dipeptidyl peptidase-4 inhibitor, in healthy volunteers. Biopharm Drug Dispos. 2007;28:315-322.
27. Ahrén B. DPP-4 inhibitors. Best Pract Res Clin Endocrinol Metab. 2007;21:517-533.
28. Ahrén B. Dipeptidyl peptidase-4 inhibitors: clinical data and clinical implications. Diabetes Care. 2007;30:1344-1350.
29. Ahrén B. Clinical results of treating type 2 diabetic patients with sitagliptin, vildagliptin or saxagliptin-diabetes control and potential adverse events. Best Pract Res Clin Endocrinol Metab. 2009;23:487-498.
30. JANUVIA (sitagliptin) [prescribing information]. Whitehouse Station, NJ: Merck and Co, Inc.
31. Herman GA, 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;78:675-688.
32. Herman GA, Bergman A, Stevens C, et al. Effect of single oral doses of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on incretin and plasma glucose levels following an oral glucose tolerance test in patients with type 2 diabetes. J Clin Endocrinol Metab. 2006;91:4612-4619.
33. Vincent SH, Reed JR, Bergman AJ, et al. Metabolism and excretion of the dipeptidyl peptidase 4 inhibitor [14C] sitagliptin in humans. Drug Metab Dispos. 2007;35:533-538.
34. Bergman AJ, Stevens C, Zhou Y, et al. 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.
35. Herman GA, Bergman A, Liu F, et al. Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol. 2006;46:876-886.
36. Hermansen K, Kipnes M, Luo E, Fanurik D, Khatami H, Stein P; Sitagliptin Study 035 Group. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor sitagliptin in patients with type 2 diabetes mellitus inadequately controlled on glimepiride alone or in combination with metformin. Diabetes Obes Metab. 2007;9:733-745.
37. 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):167-177.
38. Aschner P, Kipnes MS, Lunceford JK, Sanchez M, Mickel C, Williams-Herman DE. Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes. Diabetes Care. 2006;29:2632-2637.
39. 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;49:2564-25671.
40. Scott R, Wu L, 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;61:171-180.
41. Goldstein BJ, Feinglos MN, Lunceford JK, Johnson J, Williams-Herman DE. 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;30:1979-1987.
42. Qi DS, Teng R, Jiang M, et al. Two-year treatment with sitagliptin and initial combination therapy of sitagliptin and metformin provides substantial and durable glycemic control in patients with type 2 diabetes. Diabetologia. 2008;51:Suppl 1:S36.
43. Nonaka K, Kakikawa T, Sato A, et al. Efficacy and safety of sitagliptin monotherapy in Japanese patients with type 2 diabetes. Diabet Res Clin Pract. 2008;79:291-298.
44. Mohan V, Yang W, Son HY, et al. Efficacy and safety of sitagliptin inthe treatment of patients with type 2 diabetes in China, India and Korea. Diab Res Clin Pract. 2009;83:106-116.
45. Hanefeld M, Herman GA, Wu M, Mickel C, Sanchez M, Stein PP. Once-daily sitagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of patients with type 2 diabetes. Curr Med Res Opin. 2007;23(6):1329-1339.
46. Inzucchi SE, Bergenstal RM, Buse JB, et al. Management of hyperglycemia in type 2 diabetes: a patient-centered approach: position statement of the American Diabetes Association (ADA) and the European Association for the Study of Diabetes (EASD). Diabetes Care. 2012;35:1364-1379.
47. Charbonnel B, Karasik A, Liu J, Wu M, Meininger G. 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: 2638-2643.
48. Scott R, Loeys T, Davies MJ, Engel SS. Efficacy and safety of sitagliptin when added to ongoing metformin therapy in patients with type 2 diabetes. Diabetes Obes Metab. 2008;10:959-969.
49. Nauck MA, Meininger G, Sheng D, Terranella L, Stein PP. Efficacy and safety of the dipeptidyl peptidase-4 inhibitor, sitagliptin, compared with the sulfonylurea, glipizide, in patients with type 2 diabetes inadequately controlled on metformin alone: a randomized, double-blind, non-inferiority trial. Diabet Obes Metab. 2007;9:194-205.
50. 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): 562-576.
51. Lim S, An JH, Shin H, et al. Factors predicting therapeutic efficacy of combination treatment with sitagliptin and metformin in type 2 diabetic patients: the COSMETIC study. Clin Endocrinol (Oxf). 2012;77(2): 215-223.
52. Pérez-Monteverde A, Seck T, Xu L, et al. Efficacy and safety of sitagliptin and the fixed-dose combination of sitagliptin and metformin vs pioglitazone in drug-naïve patients with type 2 diabetes. Int J Clin Pract. 2011;65(9): 930-938.
53. Olansky L, Reasner C, Seck TL, et al. A treatment strategy implementing combination therapy with sitagliptin and metformin results in superior glycemic control versus metformin monotherapy due to a low rate of addition of antihyperglycemic agents. Diabetes Obes Metab. 2011;13(9):841-849.
54. Rosenstock J, Brazg RG, Andryuk PJ, Lu K, Stein P. 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. Clinical Ther. 2006;28:1556-1568.
55. Arjona Ferreira JC, Dobs A, Goldstein BJ, et al. Triple combination therapy with sitagliptin, metformin and rosiglitazone improves glycemic control in patients with type 2 diabetes. Diabetologia. 2008; 51 Suppl 1:S365.
56. Fonseca V, Staels B, Morgan JD 2nd, et al. Efficacy and safety of sitagliptin added to ongoing metformin and pioglitazone combination therapy in a randomized, placebo-controlled, 26-week trial in patients with type 2 diabetes. J Diabetes Complications. 2013;27(2):177-183.
57. Bergman AJ, Cote C, Yi B, et al. Effect of renal insufficiency on the pharmacokinetics of MK-0431 (sitagliptin), a selective dipeptidyl-peptidase-IV (DPP-IV) inhibitor. Clin Pharmacol Ther. 2006;79:75.
58. Bergman AJ, Cote C, Yi B, et al. Effect of Renal Insufficiency on the Pharmacokinetics of Sitagliptin, a Dipeptidyl Peptidase-4 Inhibitor. Diabetes Care. 2007;30(7):1862-1864.
59. Chan JC, Scott R, Arjona Ferreira JC, et al. Safety and efficacy of sitagliptin in patients with type 2 diabetes and chronic renal insufficiency. Diabetes Obes Metab. 2008;10(7):545-555.
60. Arjona Ferreira JC, Marre M, Barzilai N, et al. Efficacy and safety of sitagliptin versus glipizide in patients with type 2 diabetes and moderate-to-severe chronic renal insufficiency. Diabetes Care. 2013;36(5):1067-1073.
61. Arjona Ferreira JC, Corry D, Mogensen CE, et al. Efficacy and safety of sitagliptin in patients with type 2 diabetes and ESRD receiving dialysis: a 54-week randomized trial. Am J Kidney Dis. 2013;61(4):579-587.
62. Patil HR, Al Badarin FJ, Al Shami HA, et al. Meta-analysis of effect of dipeptidyl peptidase-4 inhibitors on cardiovascular risk in type 2 diabetes mellitus. Am J Cardiol. 2012;110:826-833.
63. Eurich DT, Simpson S, Senthilselvan A, Asche CV, Sandhu-Minhas JK, McAlister FA. Comparative safety and effectiveness of sitagliptin in patients with type 2 diabetes: retrospective population based cohort study. BMJ. 2013;346:2-10.