Clinical overview of saxagliptin for Type 2 diabetes management

References

• Ong KL, Cheung BMY, Wong LYF et al. Prevalence, treatment, and control of diagnosed diabetes in the U.S. national health and nutrition examination survey 1999–2004. Ann. Epidemiol.18(3), 222–229 (2008).
   PubMed Web of Science ®Google Scholar
• Levy P. The current unmet need in Type 2 diabetes mellitus: addressing glycemia and cardiovascular disease. Postgrad. Med.121(3 Suppl. 1), 7–12 (2009).
   PubMed Web of Science ®Google Scholar
• Nathan DM, Buse JB, Davidson MB et al. 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 Care32(1), 193–203 (2009).
   PubMed Web of Science ®Google Scholar
• Byetta ®, package insert. Amylin Pharmaceuticals, Inc., San Diego, CA, USA.
   Google Scholar
• Resnick HE, Foster GL, Bardsley J, Ratner RE. Achievement of American Diabetes Association clinical practice recommendations among U.S. adults with diabetes, 1999–2002: the national health and nutrition examination survey. Diabetes Care29(3), 531–537 (2006).
   PubMed Web of Science ®Google Scholar
• Edelman SV, Henry RR. Diagnosis and Management of Type 2 Diabetes (Volume 8). Professional Communications Inc., NY, USA (2007).
   Google Scholar
• Canadian Diabetes Association Clinical Practice Guidelines Expert Committee. Canadian Diabetes Association 2008 clinical practice guidelines for the prevention and management of diabetes in Canada. Can. J. Diabetes.32(Suppl. 1), S1–S201 (2008).
   Web of Science ®Google Scholar
• 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.15(6), 541–559 (2009).
   Web of Science ®Google Scholar
• Pollack M, Chastek B, Williams SA. Impact of treatment complexity on adherence and glycemic control: an analysis of oral anti-diabetic agents. Presented at: International Society for Pharmacoeconomics and Outcomes Research 14th Annual International Meeting. Orlando, FL, USA, 16–20 May 2009.
   Google Scholar
• Thomas L, Eckhardt M, Langkopf E et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of action compared with other dipeptidyl peptidase-4 inhibitors. J. Pharmacol. Exp. Ther.325(1), 175–182 (2008).
   PubMed Web of Science ®Google Scholar
• Henry R, Smith S, Schwartz S et al. β-cell stimulation by saxagliptin in patients with Type 2 diabetes. Diabetes58(Suppl. 1), 447–P (2009).
   Google Scholar
• Rosenstock J, Foley JE, Rendell M et al. Effects of the dipeptidyl peptidase-IV inhibitor vildagliptin on incretin hormones, islet function, and postprandial glycemia in subjects with impaired glucose tolerance. Diabetes Care31(1), 30–35 (2008).
   PubMed Web of Science ®Google Scholar
• Rosenstock J, Zinman B. Dipeptidyl peptidase-4 inhibitors and the management of Type 2 diabetes mellitus. Curr. Opin. Endocrinol. Diabetes Obes.14(2), 98–107 (2007).
   PubMed Web of Science ®Google Scholar
• Rosenstock J. Reflecting on Type 2 diabetes prevention: more questions than answers! Diabetes Obes. Metab.9(Suppl. 1), 3–11 (2007).
   Google Scholar
• 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.122(3), 16–27 (2010).
   PubMed Web of Science ®Google Scholar
• Onglyza ™, package insert. Bristol-Myers Squibb, Princeton, NJ, USA & AstraZeneca, Wilmington, DE, USA.
   Google Scholar
• Rosenstock J, Aguilar-Salinas C, Klein E et al. Effect of saxagliptin monotherapy in treatment-naive patients with Type 2 diabetes. Curr. Med. Res. Opin.25(10), 2401–2411 (2009).
   PubMed Web of Science ®Google Scholar
• Jadzinsky M, Pfützner A, Paz-Pacheco E et al. Saxagliptin given in combination with metformin as initial therapy improves glycemic control in patients with Type 2 diabetes compared with either monotherapy: a randomized controlled trial. Diabetes Obes. Metab.11(6), 611–622 (2009).
   PubMed Web of Science ®Google Scholar
• 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.63(9), 1395–1406 (2009).
   PubMed Web of Science ®Google Scholar
• Hollander P, Li J, Allen E, Chen R; for the CV181–013 investigators. Saxagliptin added to a thiazolidinedione improves glycemic control in patients with Type 2 diabetes and inadequate control on thiazolidinedione alone. J. Clin. Endocrinol. Metab.94(12), 4810–4819 (2009).
   PubMed Web of Science ®Google Scholar
• DeFronzo RA, Hissa M, Garber AJ et al. The efficacy and safety of saxagliptin when added to metformin therapy in patients with inadequately controlled Type 2 diabetes on metformin alone. Diabetes Care32(9), 1649–1655 (2009).
   PubMed Web of Science ®Google Scholar
• 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.48(15), 5025–5037 (2005).
   PubMed Web of Science ®Google Scholar
• Metzler WJ, Yanchunas J, Weigelt C et al. Involvement of DPP-IV catalytic residues in enzyme-saxagliptin complex formation. Protein Sci.17(2), 240–250 (2008).
   PubMed Web of Science ®Google Scholar
• Kirby M, Yu DM, O’Connor SP, Gorrell MD. Inhibitor selectivity in the clinical application of dipeptidyl peptidase-4 inhibition. Clin. Sci.118(1), 31–41 (2010).
   Web of Science ®Google Scholar
• Drucker DJ. The role of gut hormones in glucose homeostasis. J. Clin. Invest.117(1), 24–32 (2007).
   PubMed Web of Science ®Google Scholar
• Kirby MS, Dorso C, Wang A et al. In vitro enzymologic characteristics of saxagliptin, a highly potent and selective DPP4 inhibitor with ‘slow binding’ characteristics. Clin. Chem. Lab. Med.46, (2008) (Abstract A29).
   Google Scholar
• Johnson KM. Dutogliptin, a dipeptidyl peptidase inhibitor for the treatment of Type 2 diabetes mellitus. Curr. Opin. Investig. Drugs11(4), 55–463 (2010).
   Google Scholar
• Boulton D, Geraldes M. Safety, tolerability, pharmacokinetics and pharmacodynamics of once-daily oral doses of saxagliptin for 2 weeks in Type 2 diabetic and healthy subjects. Diabetes56(Suppl. 1), (2007) (Abstract 606P).
   Google Scholar
• Ban K, Noyan-Ashraf MH, Hoefer J et al. Cardioprotective and vasodilatory actions of glucagon-like peptide 1 receptor are mediated through both glucagon-like peptide 1 receptor-dependent and -independent pathways. Circulation117(18), 2340–2350 (2008).
   PubMed Web of Science ®Google Scholar
• Patel CG, Zhang J, Li L et al. Effect of a high-fat meal on the pharmacokinetics of saxagliptin in healthy subjects. J. Clin. Pharmacol.50(10), 1211–1216. (2010).
   PubMed Web of Science ®Google Scholar
• Boulton DW, Li L, Frevert EU et al. Influence of renal or hepatic impairment on the pharmacokinetics of saxagliptin. Clin. Pharmacokinet. (In press).
   Google Scholar
• Patel C, Komoroski B, Brenner E, Li L, Boulton D. No meaningful pharmacokinetic drug–drug interactions between saxagliptin and metformin in healthy subjects. Presented at: American College of Clinical Pharmacy. Denver, CO, USA, 14–17 October 2007.
   Google Scholar
• Patel C, Komoroski B, Li L, Boulton D. No meaningful pharmacokinetic drug–drug interaction between saxagliptin and glyburide in healthy subjects. Presented at: American College of Clinical Pharmacy. Denver, CO, USA, 14–17 October 2007.
   Google Scholar
• Patel CG, Wolf RA, Komoroski B, Li L, Boulton AJ. No meaningful pharmacokinetic drug–drug interaction between saxagliptin and pioglitazone in healthy subjects. Presented at: American College of Clinical Pharmacy. Denver, CO, USA, 14–17 October 2007.
   Google Scholar
• Boulton DW, Li L, Patel CG. No pharmacokinetic interaction between saxagliptin and digoxin in healthy subjects. Clin. Pharmacol. Ther.83(Suppl. 1), S93 (2008) (Abstract PIII-69).
   Google Scholar
• Boulton DW, Adams D, Li L et al. Maalox max, famotidine or omeprazole do not meaningfully affect the pharmacokinetics of saxagliptin in healthy subjects. Clin. Pharmacol. Ther.83(Suppl. 1), S92 (2008).
   Google Scholar
• Patel CG, Boulton DW, Brenner E. Effect of ketoconazole on the pharmacokinetics of saxagliptin in healthy subjects. J. Clin. Pharmacol.47, 1183–1211 (2007) (Abstract 89).
   Google Scholar
• Onglyza ™ Europe, package insert. Bristol-Myers Squibb, Princeton, NJ, USA, & AstraZeneca, Wilmington, DE, USA.
   Google Scholar
• Rosenstock J, Sankoh S, List JF. Glucose-lowering activity of the dipeptidyl peptidase-4 inhibitor saxagliptin in drug-naïve patients with Type 2 diabetes. Diabetes Obes. Metab.10, 376–386 (2008).
   PubMed Web of Science ®Google Scholar
• Tahrani AA, Piya MK, Barnett AH. Saxagliptin: a new DPP-4 inhibitor for the treatment of Type 2 diabetes mellitus. Adv. Ther.26(3), 249–262 (2009).
   PubMed Web of Science ®Google Scholar
• DeFronzo R, Hissa MN, Garber AJ et al. Once daily saxagliptin added to metformin provides sustained glycemic control and is well tolerated over 102 weeks in patients with T2D. Diabetes58(Suppl. 1), (2009) (Abstract 547-P).
   Google Scholar
• Maheux P, Doucet J, Allen E et al. Efficacy and safety of saxagliptin 5 mg once-daily therapy in elderly patients with Type 2 diabetes mellitus. Diabetologia52, 1–550 (2008).
   Google Scholar
• Nesto RW, Bell D, Bonow RO et al. Thiazolidinedione use, fluid retention, and congestive heart failure: a consensus statement from the American Heart Association and American Diabetes Association. Diabetes Care27(1), 256–263 (2004).
   PubMed Web of Science ®Google Scholar
• Garber AJ, Schweizer A, Baron MA, Rochotte E, Dejager S. 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(2), 166–174 (2007).
   PubMed Web of Science ®Google Scholar
• Chen R, Donovan M, Rusnak JM. Saxagliptin used as monotherapy or in combination with other antihyperglycemic agents does not significantly increase risk of hypoglycemia. Diabetes58(Suppl. 1), A536 (2009).
   Google Scholar
• 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.9(5), 733–745 (2007).
   PubMed Web of Science ®Google Scholar
• Garber AJ, Foley JE, Banerji MA et al. Effects of vildagliptin on glucose control in patients with Type 2 diabetes inadequately controlled with a sulphonylurea. Diabetes Obes. Metab.10(11), 1047–1056 (2008).
   PubMed Web of Science ®Google Scholar
• US Department of Health and Human Services. Food and Drug Administration. FDA Approval 22–350. June (2008).
   Google Scholar
• Patel C, Castaneda L, Frevert U et al. Single-dose pharmacokinetics and safety of saxagliptin in subjects with hepatic impairment compared with healthy subjects. Diabetes57(Suppl. 1), (2008) (Abstract A160).
   Google Scholar
• Scheen AY, Charpentier G, Östgren CJ, Hellqvist Å, Gause-Nilsson I. 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.26(7), 540–549 (2010).
   PubMed Web of Science ®Google Scholar
• Januvia®, package insert. Merck & Co., Inc., Whitehouse Station, NJ, USA.
   Google Scholar
• Hinke SA, Kühn-Wache K, Hoffmann T et al. Metformin effects on dipeptidylpeptidase IV degradation of glucagon-like peptide-1. Biochem. Biophys. Res. Commun.291(5), 1302–1308 (2002).
   PubMed Web of Science ®Google Scholar
• 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.24(10), 2943–2952 (2008).
   PubMed Web of Science ®Google Scholar
• Vella A, Bock G, Giesler PD et al. Effects of dipeptidyl peptidase-4 inhibition on gastrointestinal function, meal appearance, and glucose metabolism in Type 2 diabetes. Diabetes56(5), 1475–1480 (2007).
   PubMed Web of Science ®Google Scholar