Drugs & Therapy Perspectives

, Volume 30, Issue 3, pp 92–99 | Cite as

Saxagliptin: a guide to its use in type 2 diabetes mellitus

  • Katherine A. Lyseng-Williamson
  • Lily P. H. Yang
Adis Drug Clinical Q&A


Oral saxagliptin (Onglyza®), a potent, selective dipeptidyl pepitase-4 inhibitor, is a useful option to improve glycaemic control in treatment-naïve and treatment-experienced patients with type 2 diabetes mellitus. The efficacy of saxagliptin 2.5 or 5 mg once daily as initial therapy and add-on therapy to various baseline antihyperglycaemic agents has been demonstrated in a number of clinical trials in patients with type 2 diabetes, including those with renal impairment. Saxagliptin is generally well tolerated, does not increase the risk of hypoglycaemia or cardiovascular outcomes relative to placebo or active comparators, and is generally weight neutral.



The manuscript was reviewed by: D.S.H. Bell, Division of Endocrinology, University of Alabama Medical School, Southside Endocrinology, Birmingham, AL, USA; G. Dimitriadis, 2nd Department of Internal Medicine, Research Institute and Diabetes Center, University of Athens Medical School, Attikon University Hospital, Athens, Greece; J.G. Eriksson, Department of General Practice and Primary Health Care, University of Helsinki, Helsinki, Finland.


This article was updated from Drugs 2012;72(2):229-48 [5]. The preparation of these reviews was not supported by any external funding. During the peer review process, the manufacturer of the agent under review was offered an opportunity to comment on the article. Changes resulting from comments received were made by the authors on the basis of scientific and editorial merit.


  1. 1.
    Tahrani AA, Bailey CJ, Del Prato S, et al. Management of type 2 diabetes: new and future developments in treatment. Lancet. 2011;378(9786):182–97.PubMedCrossRefGoogle Scholar
  2. 2.
    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 and the European Association for the Study of Diabetes. Diabetes Care. 2012;35(6):1364–9.PubMedCrossRefGoogle Scholar
  3. 3.
    Handelsman Y, Mechanick JI, Blonde L, et al. American Association of Clinical Endocrinologists Medical Guidelines for Clinical Practice for developing a diabetes mellitus comprehensive care plan. Endocr Pract. 2011;17(Suppl 2):1–53.PubMedCrossRefGoogle Scholar
  4. 4.
    Rodbard HW, Jellinger PS, Davidson JA, et al. Statement by an American Association of Clinical Endocrinologists/American College of Endocrinology consensus panel on type 2 diabetes mellitus: an algorithm for glycemic control. Endocr Pract. 2009;15(6):540–59.PubMedCrossRefGoogle Scholar
  5. 5.
    Yang LPH. Saxagliptin: a review of its use as combination therapy in the management of type 2 diabetes mellitus in the EU. Drugs. 2012;72(2):229–48.PubMedCrossRefGoogle Scholar
  6. 6.
    Onglyza® (saxagliptin) tablets, for oral use: US prescribing information. Princeton: Bristol-Myers Squibb Company; 2013.Google Scholar
  7. 7.
    Onglyza® (saxagliptin) coated tablets: Brazilian prescribing information [in Portugeuse]. São Paulo: Bristol-Myers Squibb Farmacêutica S.A.; 2013.Google Scholar
  8. 8.
    Wang A, Dorso C, Kopcho L, et al. Implications of the prolonged dissociation rate of saxagliptin, a highly potent and selective DPP4 inhibitor, on plasma DPP measurements [abstract no. 2088-PO]. Diabetes. 2008;57(Suppl. 1):A576–7.Google Scholar
  9. 9.
    Deacon CF. Dipeptidyl peptidase-4 inhibitors in the treatment of type 2 diabetes: a comparative review. Diabetes Obes Metab. 2011;13(1):7–18.PubMedCrossRefGoogle Scholar
  10. 10.
    Augeri DJ, Robl JA, Betebenner DA, et al. Discovery and preclinical profile of saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes. J Med Chem. 2005;48(15):5025–37.PubMedCrossRefGoogle Scholar
  11. 11.
    Drucker DJ. The role of gut hormones in glucose homeostasis. J Clin Invest. 2007;117(1):24–32.PubMedCentralPubMedCrossRefGoogle Scholar
  12. 12.
    Kirby M, Yu DMT, O’Connor SP, et al. Inhibitor selectivity in the clinical application of dipeptidyl peptidase-4 inhibition. Clin Sci (Lond). 2010;18(1):31–41.Google Scholar
  13. 13.
    Baetta R, Corsini A. Pharmacology of dipeptidyl peptidase-4 inhibitors: similarities and differences. Drugs. 2011;71(11):1441–67.PubMedCrossRefGoogle Scholar
  14. 14.
    Rosenstock J, Aguilar-Salinas C, Klein E, et al. Effect of saxagliptin monotherapy in treatment-naïve patients with type 2 diabetes. Curr Med Res Opin. 2009;25(10):2401–11.PubMedCrossRefGoogle Scholar
  15. 15.
    Jadzinsky M, Pfützner A, Paz-Pacheco E, et al. Saxagliptin given in combination with metformin as initial therapy improves glycaemic control in patients with type 2 diabetes compared with either monotherapy: a randomized controlled trial. Diabetes Obes Metab. 2009;11(6):611–22.PubMedCrossRefGoogle Scholar
  16. 16.
    DeFronzo RA, Hissa MN, Garber AJ, et al. The efficacy and safety of saxagliptin when added to metformin therapy in patients with inadequately controlled type 2 diabetes with metformin alone. Diabetes Care. 2009;32(9):1649–55.PubMedCrossRefGoogle Scholar
  17. 17.
    Chacra AR, Tan GH, Apanovitch A, et al. Saxagliptin added to a submaximal dose of sulphonylurea improves glycaemic control compared with uptitration of sulphonylurea in patients with type 2 diabetes: a randomised controlled trial. Int J Clin Pract. 2009;63(9):1395–406.PubMedCentralPubMedCrossRefGoogle Scholar
  18. 18.
    Hollander P, Li J, Allen E, et al. Saxagliptin added to a thiazolidinedione improves glycemic control in patients with type 2 diabetes and inadequate control on thiazolidinedione alone. J Clin Endocrinol Metab. 2009;94(12):4810–9.PubMedCrossRefGoogle Scholar
  19. 19.
    Dhillon S, Weber J. Saxagliptin. Drugs. 2009;69(15):2103–4.PubMedCrossRefGoogle Scholar
  20. 20.
    Hollander PA, Kushner P. Type 2 diabetes comorbidities and treatment challenges: rationale for DPP-4 inhibitors. Postgrad Med. 2010;122(3):71–80.PubMedCrossRefGoogle Scholar
  21. 21.
    Frederich R, McNeill R, Berglind N, et al. The efficacy and safety of the dipeptidyl peptidase-4 inhibitor saxagliptin in treatment-naive patients with type 2 diabetes mellitus: a randomized controlled trial. Diabetol Metab Syndr. 2012;4(1):36.PubMedCentralPubMedCrossRefGoogle Scholar
  22. 22.
    Barnett AH, Charbonnel B, Donovan M, et al. Effect of saxagliptin as add-on therapy in patients with poorly controlled type 2 diabetes on insulin alone or insulin combined with metformin. Curr Med Res Opin. 2012;28(4):513–23.PubMedCrossRefGoogle Scholar
  23. 23.
    Ravichandran S, DeFronzo R, Garber AJ, et al. Once-daily saxagliptin added to metformin is well tolerated and provides sustained glycaemic control over 102 weeks in patients with type 2 diabetes [abstract no. 132]. Diabetologia. 2009;52(Suppl. 1):S60.Google Scholar
  24. 24.
    Chacra AR, Tan GH, Ravichandran S, et al. Safety and efficacy of saxagliptin in combination with submaximal sulphonylurea versus up-titrated sulphonylurea over 76 weeks. Diab Vasc Dis Res. 2011;8(2):150–9.PubMedCrossRefGoogle Scholar
  25. 25.
    Hollander PL, Li J, Frederich R, et al. Safety and efficacy of saxagliptin added to thiazolidinedione over 76 weeks in patients with type 2 diabetes mellitus. Diab Vasc Dis Res. 2011;8(2):125–35.PubMedCrossRefGoogle Scholar
  26. 26.
    Barnett AH, Charbonnel B, Li J, et al. Saxagliptin add-on therapy to insulin with or without metformin for type 2 diabetes mellitus: 52-week safety and efficacy. Clin Drug Investig. 2013;33(10):707–17.PubMedCrossRefGoogle Scholar
  27. 27.
    Moses RG, Kalra S, Brook D, et al. A randomized controlled trial of the efficacy and safety of saxagliptin as add-on therapy in patients with type 2 diabetes and inadequate glycemic control on metformin plus a sulfonylurea. Diabetes Obes Metab. doi: 10.1111/dom.12234 [Epub 9 Nov 2013].
  28. 28.
    Göke B, Gallwitz B, Eriksson J, et al. Saxagliptin is non-inferior to glipizide in patients with type 2 diabetes mellitus inadequately controlled on metformin alone: a 52-week randomised controlled trial. Int J Clin Pract. 2010;64(12):1619–31.PubMedCrossRefGoogle Scholar
  29. 29.
    Scheen AJ, Charpentier G, Östgren 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.PubMedCrossRefGoogle Scholar
  30. 30.
    Hermans MP, Delibasi T, Farmer I, et al. Effects of saxagliptin added to sub-maximal doses of metformin compared with uptitration of metformin in type 2 diabetes: the PROMPT study. Curr Med Res Opin. 2012;28(10):1635–45.PubMedCrossRefGoogle Scholar
  31. 31.
    Göke B, Gallwitz B, Eriksson JG, et al. Saxagliptin vs. glipizide as add-on therapy in patients with type 2 diabetes mellitus inadequately controlled on metformin alone: long-term (52-week) extension of a 52-week randomised controlled trial. Int J Clin Pract. 2013;67(4):307–16.PubMedGoogle Scholar
  32. 32.
    Nowicki M, Rychlik I, Haller H, et al. Saxagliptin improves glycaemic control and is well tolerated in patients with type 2 diabetes mellitus and renal impairment. Diabetes Obes Metab. 2011;13(6):523–32.PubMedCrossRefGoogle Scholar
  33. 33.
    Nowicki M, Rychlik I, Haller H, et al. Long-term treatment with the dipeptidyl peptidase-4 inhibitor saxagliptin in patients with type 2 diabetes mellitus and renal impairment: a randomised controlled 52-week efficacy and safety study. Int J Clin Pract. 2011;65(12):1230–9.PubMedCrossRefGoogle Scholar
  34. 34.
    Rosenstock J, Gross JL, Aguilar-Salinas C, et al. Long-term 4-year safety of saxagliptin in drug-naive and metformin-treated patients with Type 2 diabetes. Diabet Med. 2013;30(12):1472–6.PubMedCrossRefGoogle Scholar
  35. 35.
    Chen R, Donovan M, Rusnak JM, et al. Saxagliptin used as monotherapy or in combination with other antihyperglycaemic agents does not significantly increase risk of hypoglycaemia [abstract no. 2082-PO]. In: 69th Annual Scientific Sessions of the American Diabetes Association; 5–9 Jun 2009; New Orleans.Google Scholar
  36. 36.
    Frederich R, Alexander JH, Fiedorek FT, et al. A systematic assessment of cardiovascular outcomes in the saxagliptin drug development program for type 2 diabetes. Postgrad Med. 2010;122(3):16–27.PubMedCrossRefGoogle Scholar
  37. 37.
    Scirica BM, Bhatt DL, Braunwald E, et al. Saxagliptin and cardiovascular outcomes in patients with type 2 diabetes mellitus. N Engl J Med. 2013;369(14):1317–26.PubMedCrossRefGoogle Scholar
  38. 38.
    Cook W, Bryzinski B, Slater J, et al. Saxagliptin efficacy and safety in patients with type 2 diabetes mellitus and cardiovascular disease history or cardiovascular risk factors: results of a pooled analysis of phase 3 clinical trials. Postgrad Med. 2013;125(3):145–54.PubMedCrossRefGoogle Scholar
  39. 39.
    Onglyza® (saxagliptin) film-coated tablets: summary of product characteristics. London: European Medicines Agency; 2013.Google Scholar

Copyright information

© Springer International Publishing Switzerland 2013

Authors and Affiliations

  • Katherine A. Lyseng-Williamson
    • 1
  • Lily P. H. Yang
    • 1
  1. 1.AdisNorth ShoreNew Zealand

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