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Drug Evaluations

Linagliptin, a dipeptidyl peptidase-4 inhibitor with a unique pharmacological profile, and efficacy in a broad range of patients with type 2 diabetes

, MD &
Pages 101-110 | Published online: 09 Dec 2011

Bibliography

  • Shaw JE, Sicree RA, Zimmet PZ. Global estimates of the prevalence of diabetes for 2010 and 2030. Diabetes Res Clin Pract 2010;13(1):4-14
  • Sturm R. Stemming the global obesity epidemic: what can we learn from data about social and economic trends? Public Health 2008;122(8):739-46
  • Hill JO, Wyatt HR, Reed GW, Obesity and the environment: where do we go from here? Science 2003;299(5608):853-5
  • American Diabetes Association. Standards of medical care in diabetes—2011. Diabetes Care 2011;34(Suppl 1):S11-61
  • Rodbard HW, Jellinger PS, Davidson JA, 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
  • International Diabetes Federation Clinical Guidelines Task Force. Global guideline for type 2 diabetes. Brussels: International Diabetes Federation. Available from: http://www.idf.org/guidelines/type-2-diabetes [Last accessed 22 June 2011]
  • Ryden L, Standl E, Bartnik M, Guidelines on diabetes, pre-diabetes, and cardiovascular diseases: executive summary. The Task Force on Diabetes and Cardiovascular Diseases of the European Society of Cardiology (ESC) and of the European Association for the Study of Diabetes (EASD). Eur Heart J 2007;28(1):88-136
  • Orozco-Beltran D, Gil-Guillen VF, Quirce F, Control of diabetes and cardiovascular risk factors in patients with type 2 diabetes in primary care. The gap between guidelines and reality in Spain. Int J Clin Pract 2007;61(6):909-15
  • Hoerger TJ, Segel JE, Gregg EW, Is glycemic control improving in U.S. adults? Diabetes Care 2008;31(1):81-6
  • Jenssen TG, Tonstad S, Claudi T, The gap between guidelines and practice in the treatment of type 2 diabetes. A nationwide survey in Norway. Diabetes Res Clin Pract 2008;80(2):314-20
  • Patel A, MacMahon S, Chalmers J, Intensive blood glucose control and vascular outcomes in patients with type 2 diabetes. N Engl J Med 2008;358(24):2560-72
  • Gerstein HC, Miller ME, Byington RP, Effects of intensive glucose lowering in type 2 diabetes. N Engl J Med 2008;358(24):2545-59
  • Duckworth W, Abraira C, Moritz T, Glucose control and vascular complications in veterans with type 2 diabetes. N Engl J Med 2009;360(2):129-39
  • 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
  • Freeman JS. The pathophysiologic role of incretins. J Am Osteopath Assoc 2007;107(Suppl):S6-9
  • Nauck MA, Baller B, Meier JJ. Gastric inhibitory polypeptide and glucagon-like peptide-1 in the pathogenesis of type 2 diabetes. Diabetes 2004;53(Suppl 3):S190-6
  • Gallwitz B. The evolving place of incretin-based therapies in type 2 diabetes. Pediatr Nephrol 2010;25(7):1207-17
  • Ahren B. Gut peptides and type 2 diabetes mellitus treatment. Curr Diab Rep 2003;3(5):365-72
  • Drucker DJ, Philippe J, Mojsov S, Glucagon-like peptide I stimulates insulin gene expression and increases cyclic AMP levels in a rat islet cell line. Proc Natl Acad Sci USA 1987;84(10):3434-8
  • Deacon CF, Nauck MA, Toft-Nielsen M, 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(9):1126-31
  • Parkes D, Jodka C, Smith P, Pharmacokinetic actions of exendin-4 in the rat: comparison with glucagon-like peptide-1. Drug Dev Res 2001;53(4):260-7
  • Pospisilik JA, Martin J, Doty T, Dipeptidyl peptidase IV inhibitor treatment stimulates beta-cell survival and islet neogenesis in streptozotocin-induced diabetic rats. Diabetes 2003;52(3):741-50
  • Duttaroy A, Voelker F, Merriam K, The DPP-4 inhibitor vildagliptin increases pancreatic beta cell mass in neonatal rats. Eur J Pharmacol 2011;650(2-3):703-7
  • Del Prato S, Barnett AH, Huisman H, 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(3):258-67
  • Ban K, Noyan-Ashraf MH, Hoefer J, Cardioprotective and vasodilatory actions of glucagon-like peptide 1 receptor are mediated through both glucagon-like peptide 1 receptor-dependent and -independent pathways. Circulation 2008;117(18):2340-50
  • Anagnostis P, Athyros VG, Adamidou F, Glucagon-like peptide-1-based therapies and cardiovascular disease: looking beyond glycaemic control. Diabetes Obes Metab 2011;13(4):302-12
  • Verge D, Lopez X. Impact of GLP-1 and GLP-1 receptor agonists on cardiovascular risk factors in type 2 diabetes. Curr Diabetes Rev 2010;6(4):191-200
  • Gomis R, Espadero RM, Jones R, 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(7):653-61
  • Taskinen MR, Rosenstock J, Tamminen I, 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(1):65-74
  • Owens DR, Swallow R, Dugi KA, 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(11):1652-61
  • Rao AD, Kuhadiya N, Reynolds K, Is the combination of sulfonylureas and metformin associated with an increased risk of cardiovascular disease or all-cause mortality?: a meta-analysis of observational studies. Diabetes Care 2008;31(8):1672-8
  • Schramm TK, Gislason GH, Vaag A, Mortality and cardiovascular risk associated with different insulin secretagogues compared with metformin in type 2 diabetes, with or without a previous myocardial infarction: a nationwide study. Eur Heart J 2011; [Epub ahead of print]
  • Lincoff AM, Wolski K, Nicholls SJ, Pioglitazone and risk of cardiovascular events in patients with type 2 diabetes mellitus: a meta-analysis of randomized trials. JAMA 2007;298(10):1180-8
  • Dormandy JA, Charbonnel B, Eckland DJ, Secondary prevention of macrovascular events in patients with type 2 diabetes in the PROactive Study (PROspective pioglitAzone Clinical Trial In macroVascular Events): a randomised controlled trial. Lancet 2005;366(9493):1279-89
  • Forst T, Karagiannis E, Lubben G, Pleiotrophic and anti-inflammatory effects of pioglitazone precede the metabolic activity in type 2 diabetic patients with coronary artery disease. Atherosclerosis 2008;197(1):311-17
  • Boehringer Ingelheim Pharmaceuticals, Inc. Tradjenta™ (linagliptin) tablets US Prescribing Information. May 2011. Available from: http://bidocs.boehringer-ingelheim.com/BIWebAccess/ViewServlet.ser?docBase=renetnt&folderPath=/Prescribing+Information/PIs/Tradjenta/Tradjenta.pdf [Last accessed 22 June 2011]
  • Deacon CF, Holst JJ. Linagliptin, a xanthine-based dipeptidyl peptidase-4 inhibitor with an unusual profile for the treatment of type 2 diabetes. Expert Opin Investig Drugs 2010;19(1):133-40
  • 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(5):229-40
  • Heise T, Graefe-Mody EU, Huttner S, 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(8):786-94
  • Thomas L, Eckhardt M. Langkopf E, et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazoli n-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 2008;325(1):175-82
  • Eckhardt M, Langkopf E, Mark M, 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin -2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. J Med Chem 2007;50(26):6450-3
  • Huttner S, Graefe-Mody EU, Withopf B, Safety, tolerability, pharmacokinetics, and pharmacodynamics of single oral doses of BI 1356, an inhibitor of dipeptidyl peptidase 4, in healthy male volunteers. J Clin Pharmacol 2008;48(10):1171-8
  • Eckhardt M, Hauel N, Himmelsbach F, 3,5-Dihydro-imidazo[4,5-d]pyridazin-4-ones: a class of potent DPP-4 inhibitors. Bioorg Med Chem Lett 2008;18(11):3158-62
  • Scheen AJ. Pharmacokinetics of dipeptidylpeptidase-4 inhibitors. Diabetes Obes Metab 2010;12:648-58
  • Fuchs H, Tillement JP, Urien S, Concentration-dependent plasma protein binding of the novel dipeptidyl peptidase 4 inhibitor BI 1356 due to saturable binding to its target in plasma of mice, rats and humans. J Pharm Pharmacol 2009;61(1):55-62
  • Retlich S, Withopf B, Greischel A, Binding to dipeptidyl peptidase-4 determines the disposition of linagliptin (BI 1356)–investigations in DPP-4 deficient and wildtype rats. Biopharm Drug Dispos 2009;30(8):422-36
  • Blech S, Ludwig-Schwellinger E, Grafe-Mody EU, The metabolism and disposition of the oral dipeptidyl peptidase-4 inhibitor, linagliptin, in humans. Drug Metab Dispos 2010;38(4):667-78
  • Graefe-Mody U, Friedrich C, Port A, Effect of renal impairment on the pharmacokinetics of the dipeptidyl peptidase-4 inhibitor linagliptin(*). Diabetes Obes Metab 2011;13(10):939-46
  • Retlich S, Duval V, Ring A, Pharmacokinetics and pharmacodynamics of single rising intravenous doses (0.5 mg-10 mg) and determination of absolute bioavailability of the dipeptidyl peptidase-4 inhibitor linagliptin (BI 1356) in healthy male subjects. Clin Pharmacokinet 2010;49(12):829-40
  • Boehringer Ingelheim. Linagliptin phase III data. Fact Sheet. Available from: http://us.boehringer-ingelheim.com/content/dam/internet/opu/us_EN/documents/Media_Press_Releases/2010/linagliptin_phase3_facts.pdf [Last accessed 22 June 2011]
  • Baetta R, Corsini A. Pharmacology of dipeptidyl peptidase-4 inhibitors: similarities and differences. Drugs 2011;71(11):1441-67
  • Forst T, Uhlig-Laske B, Ring A, 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(6):542-50
  • Forst T, Uhlig-Laske B, Ring A, Linagliptin (BI 1356), a potent and selective DPP-4 inhibitor, is safe and efficacious in combination with metformin in patients with inadequately controlled Type 2 diabetes. Diabet Med 2010;27(12):1409-19
  • Hermansen K, Kipnes M, Luo E, 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
  • Pratley RE, Schweizer A, Rosenstock J, Robust improvements in fasting and prandial measures of beta-cell function with vildagliptin in drug-naive patients: analysis of pooled vildagliptin monotherapy database. Diabetes Obes Metab 2008;10(10):931-8
  • Rosenstock J, Aguilar-Salinas C, Klein E, Effect of saxagliptin monotherapy in treatment-naive patients with type 2 diabetes. Curr Med Res Opin 2009;25(10):2401-11
  • Xu L, Man CD, Charbonnel B, Effect of sitagliptin, a dipeptidyl peptidase-4 inhibitor, on beta-cell function in patients with type 2 diabetes: a model-based approach. Diabetes Obes Metab 2008;10(12):1212-20
  • Graefe-Mody U, Friedrich C, Brand T, Linagliptin has no pharmacokinetic interaction with commonly prescribed oral antidiabetic drugs. Presented at the 3rd World Congress on Controversies to Consensus in Diabetes, Obesity and Hypertension (CODHy); 13 – 16 May 2010; Prague, Czech Republic
  • Graefe-Mody U, Huettner S, Stahle H, Effect of linagliptin (BI 1356) on the steady-state pharmacokinetics of simvastatin. Int J Clin Pharmacol Ther 2010;48(6):367-74
  • Graefe-Mody U, Rose P, Ring A, The novel DPP-4 inhibitor linagliptin can be administered to patients with various degrees of hepatic impairment without dose adjustment. Abstracts of the 4th International Congress on Prediabetes and the Metabolic Syndrome; 6-9 April 2011; Madrid, Spain. J Diabetes 2011;3(Suppl s1):261
  • Bristol-Myers Squibb Co. ONGLYZA™ (saxagliptin) tablets. US Prescribing Information. February 2011. Available from: http://packageinserts.bms.com/pi/pi_onglyza.pdf [Last accessed 20 June 2011]
  • Merck Sharp & Dohme Corp. JANUVIA® (sitagliptin) tablets. US Prescribing Information. April 2011. Available from: http://www.merck.com/product/usa/pi_circulars/j/januvia/januvia_pi.pdf [Last accessed 22 June 2011]
  • Merck Sharp & Dohme Ltd. JANUVIA 100 mg film-coated tablets. Summary of Product Characteristics. 10 February 2011. electronic Medicines Compendium (eMC). Available from: http://www.medicines.org.uk/emc/document.aspx?documentid=19609&docType=SPC [Last accessed 22 June 2011]
  • Novartis Pharmaceuticals UK Ltd. Galvus 50 mg tablets. Summary of Product Characteristics. 28 February 2011. electronic Medicines Compendium (eMC). Available from: www.medicines.org.uk/emc/medicine/20734/SPC/ [Last accessed 21 June 2011]

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