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Drug Safety Evaluation

Linagliptin for the treatment of type 2 diabetes mellitus: a drug safety evaluation

Bibliography

  • International Diabetes Federation. IDF Diabetes Atlas Sixth edition. 2013. Available from: http://www.idf.org/diabetesatlas [Accessed 16 July 2014]
  • Wild S, Roglic G, Green A, et al. Global prevalence of diabetes: estimates for the year 2000 and projections for 2030. Diabetes Care 2004;27:1047-53
  • Koopman RJ, Mainous AGIII, Diaz VA, Geesey ME. Changes in age at diagnosis of type 2 diabetes mellitus in the United States, 1988 to 2000. Ann Fam Med 2005;3:60-3
  • CDC. Centers for Disease Control and Prevention. Diabetes public health resource. Distribution of age at diagnosis of diabetes among adult incident cases aged 18–79 years, United States. 2011. Available from: http://www.cdc.gov/diabetes/statistics/age/fig1.htm [Accessed 16 July 2014]
  • 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;35:1364-79
  • Garber AJ; on behalf of the Taskforce. AACE comprehensive diabetes management algorithm 2013. Endocr Pract 2013;19:327-37
  • Scheen AJ. DPP-4 inhibitors in the management of type 2 diabetes: a critical review of head-to-head trials. Diabetes Metab 2012;38:89-101
  • Boehringer Ingelheim Pharmaceuticals, Inc. Trajenta. 2011. Available from: www.accessdata.fda.gov/drugsatfda_docs/label/2014/201280s009lbl.pdf [Accessed 16 July 2014]
  • Boehringer Ingelheim Pharmaceuticals, Inc. Jentadueto. 2012. Available from: www.accessdata.fda.gov/drugsatfda_docs/label/2013/201281s004lbl.pdf [Accessed 16 July 2014]
  • Drucker DJ, Nauck MA. The incretin system: glucagon-like peptide-1 receptor agonists and dipeptidyl peptidase-4 inhibitors in type 2 diabetes. Lancet 2006;368:1696-705
  • Deacon CF, Nauck MA, Toft-Nielsen M, et al. Both subcutaneously and intravenously administered glucagon-like peptide I are rapidly degraded from the NH2-terminus in type II diabetic patients and in healthy subjects. Diabetes 1995;44:1126-31
  • 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-ylm ethyl)-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 2008;325:175-82
  • Heise T, Graefe-Mody EU, Huttner S, et al. Pharmacokinetics, pharmacodynamics and tolerability of multiple oral doses of linagliptin, a dipeptidyl peptidase-4 inhibitor in male type 2 diabetes patients. Diabetes Obes Metab 2009;11:786-94
  • Scheen AJ. Linagliptin for the treatment of type 2 diabetes (pharmacokinetic evaluation). Expert Opin Drug Metab Toxicol 2011;7:1561-76
  • Scheen AJ. Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab 2010;12:648-58
  • Graefe-Mody U, Giessmann T, Ring A, et al. A randomized, open-label, crossover study evaluating the effect of food on the relative bioavailability of linagliptin in healthy subjects. Clin Ther 2011;33:1096-103
  • Blech S, Ludwig-Schwellinger E, Grafe-Mody EU, et al. The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin, in humans. Drug Metab Dispos 2010;38:667-78
  • Graefe-Mody U, Friedrich C, Port A, et al. Effect of renal impairment on the pharmacokinetics of the dipeptidyl peptidase-4 inhibitor linagliptin. Diabetes Obes Metab 2011;13:939-46
  • Graefe-Mody U, Rose P, Retlich S, et al. Pharmacokinetics of linagliptin in subjects with hepatic impairment. Br J Clin Pharmacol 2012;74:75-85
  • Fuchs H, Binder R, Greischel A. Tissue distribution of the novel DPP-4 inhibitor BI 1356 is dominated by saturable binding to its target in rats. Biopharm Drug Dispos 2009;30:229-40
  • Graefe-Mody U, Rose P, Ring A, et al. Assessment of the pharmacokinetic interaction between the novel DPP-4 inhibitor linagliptin and a sulfonylurea, glyburide, in healthy subjects. Drug Metab Pharmacokinet 2011;26:123-9
  • Graefe-Mody EU, Padula S, Ring A, et al. Evaluation of the potential for steady-state pharmacokinetic and pharmacodynamic interactions between the DPP-4 inhibitor linagliptin and metformin in healthy subjects. Curr Med Res Opin 2009;25:1963-72
  • Graefe-Mody EU, Jungnik A, Ring A, et al. Evaluation of the pharmacokinetic interaction between the dipeptidyl peptidase-4 inhibitor linagliptin and pioglitazone in healthy volunteers. Int J Clin Pharmacol Ther 2010;48:652-61
  • Friedrich C, Metzmann K, Rose P, et al. A randomized, open-label, crossover study to evaluate the pharmacokinetics of empagliflozin and linagliptin after coadministration in healthy male volunteers. Clin Ther 2013;35:A33-42
  • Graefe-Mody EU, Brand T, Ring A, et al. Effect of linagliptin on the pharmacokinetics and pharmacodynamics of warfarin in healthy volunteers. Int J Clin Pharmacol Ther 2011;49:300-10
  • Friedrich C, Ring A, Brand T, et al. Evaluation of the pharmacokinetic interaction after multiple oral doses of linagliptin and digoxin in healthy volunteers. Eur J Drug Metab Pharmacokinet 2011;36:17-24
  • Graefe-Mody U, Huettner S, Stahle H, et al. Effect of linagliptin (BI 1356) on the steady-state pharmacokinetics of simvastatin. Int J Clin Pharmacol Ther 2010;48:367-74
  • Friedrich C, Port A, Ring A, et al. Effect of multiple oral doses of linagliptin on the steady-state pharmacokinetics of a combination oral contraceptive in healthy female adults: an open-label, two-period, fixed-sequence, multiple-dose study. Clin Drug Investig 2011;31:643-53
  • Forst T, Uhlig-Laske B, Ring A, et al. The oral DPP-4 inhibitor linagliptin significantly lowers HbA1c after 4 weeks of treatment in patients with type 2 diabetes mellitus. Diabetes Obes Metab 2011;13:542-50
  • Del Prato S, Barnett AH, Huisman H, et al. Effect of linagliptin monotherapy on glycaemic control and markers of beta-cell function in patients with inadequately controlled type 2 diabetes: a randomized controlled trial. Diabetes Obes Metab 2011;13:258-67
  • Taskinen MR, Rosenstock J, Tamminen I, et al. Safety and efficacy of linagliptin as add-on therapy to metformin in patients with type 2 diabetes: a randomized, double-blind, placebo-controlled study. Diabetes Obes Metab 2011;13:65-74
  • Haak T, Meinicke T, Jones R, et al. Initial combination of linagliptin and metformin improves glycaemic control in type 2 diabetes: a randomized, double-blind, placebo-controlled study. Diabetes Obes Metab 2012;14:565-74
  • Bajaj M, Gilman R, Patel S, et al. Linagliptin improved glycaemic control without weight gain or hypoglycaemia in patients with Type 2 diabetes inadequately controlled by a combination of metformin and pioglitazone: a 24-week randomized, double-blind study. Diabet Med 2014. [Epub ahead of print]
  • Gomis R, Espadero RM, Jones R, et al. Efficacy and safety of initial combination therapy with linagliptin and pioglitazone in patients with inadequately controlled type 2 diabetes: a randomized, double-blind, placebo-controlled study. Diabetes Obes Metab 2011;13:653-61
  • Yki-Jarvinen H, Rosenstock J, Duran-Garcia S, et al. Effects of adding linagliptin to basal insulin regimen for inadequately controlled type 2 diabetes: a ≥52-week randomized, double-blind study. Diabetes Care 2013;36:3875-81
  • Owens DR, Swallow R, Dugi KA, Woerle HJ. Efficacy and safety of linagliptin in persons with type 2 diabetes inadequately controlled by a combination of metformin and sulphonylurea: a 24-week randomized study. Diabet Med 2011;28:1352-61
  • Lewin AJ, Arvay L, Liu D, et al. Efficacy and tolerability of linagliptin added to a sulfonylurea regimen in patients with inadequately controlled type 2 diabetes mellitus: an 18-week, multicenter, randomized, double-blind, placebo-controlled trial. Clin Ther 2012;34:1909-19; e15
  • Gomis R, Owens DR, Taskinen MR, et al. Long-term safety and efficacy of linagliptin as monotherapy or in combination with other oral glucose-lowering agents in 2121 subjects with type 2 diabetes: up to 2 years exposure in 24-week phase III trials followed by a 78-week open-label extension. Int J Clin Pract 2012;66:731-40
  • Haak T, Meinicke T, Jones R, et al. Initial combination of linagliptin and metformin in patients with type 2 diabetes: efficacy and safety in a randomised, double-blind 1-year extension study. Int J Clin Pract 2013;67:1283-93
  • Lehrke M, Marx N, Patel S, et al. Safety and tolerability of linagliptin in patients with type 2 diabetes: a comprehensive pooled analysis of 22 placebo-controlled studies. Clin Ther 2014;36(8):1130-46
  • Bloomfield HE, Greer N, Newman D, et al. Predictors and consequences of severe hypoglycemia in adults with diabetes - a systematic review of the evidence. VA-ESP Project #09-009;Washington (DC) - Department of Veterans Affairs; Washington DC, USA; 2012
  • Halimi S. Acute consequences of hypoglycaemia in diabetic patients. Diabetes Metab 2010;36(Suppl 3):S75-83
  • 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):S1-53
  • Holstein A, Hammer C, Hahn M, et al. Severe sulfonylurea-induced hypoglycemia: a problem of uncritical prescription and deficiencies of diabetes care in geriatric patients. Expert Opin Drug Saf 2010;9:675-81
  • Schejter YD, Turvall E, Ackerman Z. Characteristics of patients with sulphonurea-induced hypoglycemia. J Am Med Dir Assoc 2012;13:234-8
  • American Diabetes Association. Executive summary: standards of medical care in diabetes–2014. Diabetes Care 2014;37(Suppl 1):S5-13
  • Barnett AH, Huisman H, Jones R, et al. Linagliptin for patients aged 70 years or older with type 2 diabetes inadequately controlled with common antidiabetes treatments: a randomised, double-blind, placebo-controlled trial. Lancet 2013; 382:1413-23
  • Schernthaner G, Barnett AH, Patel S, et al. Safety and efficacy of the DPP-4 inhibitor linagliptin in elderly patients with type 2 diabetes: a comprehensive analysis of data from 1331 individuals aged ≥65 years. Diabetes Obes Metab 2014. [ Epub ahead of print]
  • Inzucchi SE, Nauck M, von Eynatten M, et al. Lower risk of hypoglycemia in elderly type 2 diabetes patients when linagliptin is added to basal insulin: an exploratory analysis. Diabetes 2013;62(Suppl 1):LB1
  • Schernthaner G, Schernthaner GH. Diabetic nephropathy: new approaches for improving glycemic control and reducing risk. J Nephrol 2013;26:975-85
  • Williams ME, Garg R. Glycemic management in ESRD and earlier stages of CKD. Am J Kidney Dis 2014;63(Suppl 2):S22-38
  • McGill JB, Sloan L, Newman J, et al. Long-term efficacy and safety of linagliptin in patients with type 2 diabetes and severe renal impairment: a 1-year, randomized, double-blind, placebo-controlled study. Diabetes Care 2013;36:237-44
  • Laakso M, Rosenstock J, Groop PH, et al. Linagliptin versus placebo followed by glimepiride in type 2 diabetes patients with moderate to severe renal impairment. Diabetes 2013;62(Suppl 1):A281-2
  • Groop PH, Cooper ME, Perkovic V, et al. Linagliptin lowers albuminuria on top of recommended standard treatment in patients with type 2 diabetes and renal dysfunction. Diabetes Care 2013;36:3460-8
  • MARLINA - T2DM : efficacy, safety & modification of albuminuria in type 2 diabetes subjects with renal disease with LINAgliptin. ClinicalTrials.gov Identifier: NCT01792518. 2013. Available from: www.clinicaltrials.gov/ct2/show/NCT01792518?term=MARLINA&rank=1 [Accessed 31 January 2014]
  • Kountz D. The dipeptidyl peptidase (DPP)-4 inhibitors for type 2 diabetes mellitus in challenging patient groups. Adv Ther 2013;30:1067-85
  • Kountz DS. Hypertension in black patients: an update. Postgrad Med 2013;125:127-35
  • Thrasher J, Daniels K, Patel S, et al. Efficacy and safety of linagliptin in black/african american patients with type 2 diabetes: a 6 month, randomized, double-blind, placebo-controlled study. Endocr Pract 2014;20:412-20
  • Zeng Z, Choi DS, Mohan V, et al. Linagliptin is efficacious and well tolerated in asian patients with inadequately controlled type 2 diabetes. J Diabetes Investig 2012;3:101
  • Davidson JA, Lajara R, Aguilar R, et al. Efficacy and safety of linagliptin in hispanic/latino patients with type 2 diabetes mellitus: a pooled analysis from six randomized placebo-controlled phase 3 trials. BMJ Open Diabetes Res Care 2014;2:e000020
  • Elashoff M, Matveyenko AV, Gier B, et al. Pancreatitis, pancreatic, and thyroid cancer with glucagon-like peptide-1-based therapies. Gastroenterology 2011;141:150-6
  • Singh S, Chang HY, Richards TM, et al. Glucagonlike peptide 1-based therapies and risk of hospitalization for acute pancreatitis in type 2 diabetes mellitus: a population-based matched case-control study. JAMA Intern Med 2013;173:534-9
  • Scirica BM, Bhatt DL, Braunwald E, et al. Saxagliptin and cardiovascular outcomes in patients with type 2 diabetes mellitus. N Engl J Med 2013;369:1317-26
  • White WB, Cannon CP, Heller SR, et al. Alogliptin after acute coronary syndrome in patients with type 2 diabetes. N Engl J Med 2013;369:1327-35
  • Egan AG, Blind E, Dunder K, et al. Pancreatic safety of incretin-based drugs--FDA and EMA assessment. N Engl J Med 2014;370:794-7
  • Go AS, Mozaffarian D, Roger VL, et al. Heart disease and stroke statistics–2013 update: a report from the American Heart Association. Circulation 2013;127:e6-245
  • Nissen SE, Wolski K. Effect of rosiglitazone on the risk of myocardial infarction and death from cardiovascular causes. N Engl J Med 2007;356:2457-71
  • U.S. Food and Drug Administration. Guidance for industry diabetes mellitus — evaluating cardiovascular risk in new antidiabetic therapies to treat type 2 diabetes. 2008. Available from: www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInformation/Guidances/ucm071627.pdf [Accessed 16 July 2014]
  • Johansen OE, Neubacher D, Seck T, et al. Cardiovascular (CV) safety of linagliptin in patients with type 2 diabetes (T2D): a pooled comprehensive analysis of prospectively adjudicated CV events in phase 3 studies. Diabetologia 2013;56(Suppl 1):S52
  • Rosenstock J, Marx N, Kahn SE, et al. Cardiovascular outcome trials in type 2 diabetes and the sulphonylurea controversy: rationale for the active-comparator CAROLINA trial. Diab Vasc Dis Res 2013;10:289-301
  • Lalau JD. Lactic acidosis induced by metformin: incidence, management and prevention. Drug Saf 2010;33:727-40
  • Scheen AJ, Paquot N. Metformin revisited: a critical review of the benefit-risk balance in at-risk patients with type 2 diabetes. Diabetes Metab 2013;39:179-90
  • Barnett AH, Patel S, Harper R, et al. Linagliptin monotherapy in type 2 diabetes patients for whom metformin is inappropriate: an 18-week randomized, double-blind, placebo-controlled phase III trial with a 34-week active-controlled extension. Diabetes Obes Metab 2012;14:1145-54
  • Gallwitz B, Rosenstock J, Rauch T, et al. 2-year efficacy and safety of linagliptin compared with glimepiride in patients with type 2 diabetes inadequately controlled on metformin: a randomised, double-blind, non-inferiority trial. Lancet 2012;380:475-83
  • 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;64:562-76
  • Matthews DR, Dejager S, Ahren B, et al. Vildagliptin add-on to metformin produces similar efficacy and reduced hypoglycaemic risk compared with glimepiride, with no weight gain: results from a 2-year study. Diabetes Obes Metab 2010;12:780-9

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