Abstract
Linagliptin (Trajenta®; Tradjenta™), a dipeptidyl peptidase-4 inhibitor, is indicated for the treatment of type 2 diabetes mellitus. It has a favourable pharmacokinetic profile in terms of its primarily non-renal route of elimination. In clinical trials, oral linagliptin, as monotherapy or in combination with other oral antihyperglycaemic agents, improved glycaemic control.
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References
Scott LJ. Linagliptin in type 2 diabetes mellitus. Drugs 2011; 71(5): 611–24
Baetta R, Corsini A. Pharmacology of dipeptidyl peptidase-4 inhibitors: similarities and differences. Drugs 2011: 7(11): 1441–67
Trajenta®: summary of product characteristics. London: European Medicines Agency, 2011 Oct 6
Tradjenta™ (linagliptin): US prescribing information. Ridgefield (CT): Boehringer Ingelheim Pharmaceuticals, Inc., 2011 Jul
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 Oct; 13(10): 939–46
Graefe-Mody U, Rose P, Retlich S, et al. Pharmacokinetics of linagliptin in subjects with hepatic impairment. Br J Clin Pharmacol. Epub 2012 Jan 13
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 Aug; 33(8): 1096–103
Kawamori R, Inagaki N, Araki E, et al. Linagliptin monotherapy provides superior glycaemic control versus placebo or voglibose with comparable safety in Japanese patients with type 2 diabetes: a randomized, placebo and active comparator-controlled, double-blind study. Diabetes Obes Metab 2012 Apr; 14(4): 348–57
Del Prato S, Barnett AH, Huisman H, et al. Effect of linagliptin monotherapy on glycaemic control and markers of β-cell function in patients with inadequately controlled type 2 diabetes: a randomised controlled trial. Diab Obes Metab 2011; 13(3): 258–67
Barnett AH, Harper R, Toorawa R, et al. Linagliptin monotherapy improves glycaemic control in type 2 diabetes patients for whom metformin therapy is inappropriate [abstract no. 823]. Diabetologia 2010; 53 Suppl. 1: S327
Taskinen M, 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 Obesity Metab 2011; 13(1): 65–74
Gallwitz B, Uhlig-Laske B, Bhattacharaya S, et al. Linagliptin has similar efficacy to glimepiride but improved cardiovascular safety over 2 years in patients with type 2 diabetes inadequately controlled on metformin [abstract no. 39-LB]. 71st Annual Scientific Sessions of the American Diabetes Association; 2011 Jun 25–29; San Diego (CA)
Owens DR, Swallow R, Dugi KA. et al. 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 Nov; 28(11): 1352–61
Schernthaner G, Barnett AH, Emser A, et al. Safety and tolerability of linagliptin: a pooled analysis of data from randomized controlled trials in 3572 patients with type 2 diabetes mellitus. Diabetes Obes Metab. Epub 2012 Jan 23
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 Jul; 13(7): 653–61
Lewin AJ, Arvay L, Liu D, et al. Safety and efficacy of linagliptin as add-on therapy to a sulphonylurea in inadequately controlled type 2 diabetes [abstract no. 821]. 46th Annual Meeting of the European Association for the Study of Diabetes; 2010 Sep 20–24; Stockholm
Haak T, Meinicke T, Jones R et al. Initial combination of linagliptin and metformin improves glycaemic control in type 2 diabetes: a randomised, double-blind, placebo-controlled study. Diabetes Obes Metab. Epub 2012 Feb 22
Johansen OE, Neubacher D, von Eynatten M, et al. Cardiovascular safety with linagliptin in patients with type 2 diabetes mellitus: a prespecified, prospective, and adjudicated meta-analysis of a phase 3 programme. Cardiovasc Diabetol 2012 Jan 10; 11: 3
Boehringer Ingelheim Pharmaceuticals. CAROLINA: cardiovascular outcome study of linagliptin versus glimepiride in patients with type 2 diabetes [ClinicalTrials.gov identifier NCT01243424]. US National Institutes of Health, ClinicalTrials.gov [online]. Available from URL: http://clinicaltrials.gov [Accessed 2012 Mar 8]
Acknowledgements and Disclosure
This review was updated from Drugs 2011; 71 (5); 611–24,[1] and reviewed by J. Freeman, Division of Endocrinology and Metabolism, Philadelphia College of Osteopathic Medicine, Philadelphia, PA, USA.
The preparation of these articles 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 articles. Changes resulting from comments received were made by the authors on the basis of scientific and editorial merit.
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Scott, L.J., Lyseng-Williamson, K.A. Linagliptin: a guide to its use in type 2 diabetes mellitus. Drugs Ther Perspect 28, 1–5 (2012). https://doi.org/10.2165/11208000-000000000-00000
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DOI: https://doi.org/10.2165/11208000-000000000-00000