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Linagliptin: farmacology, efficacy and safety in type 2 diabetes treatment

Erika Paniago Guedes127*, Alexandre Hohl34, Thais Gomes de Melo5 and Felipe Lauand6

Author Affiliations

1 Endocrinologist Board of Metabolism Outpatient Clinic from the 481 State Institute for Diabetes and Endocrinology (IEDE/RJ), Rio de Janeiro, RJ, Brazil

2 Department of Endocrinology of Medical School of Graduate Studies, Pontifical Catholic University of Rio de Janeiro (PUC/RJ), Rio de Janeiro, RJ, Brazil

3 Federal University of Santa Catarina (UFSC), Florianopolis, SC, Brazil

4 Brazilian Society of Endocrinology and Metabolism - Santa Catarina state (SBEM-SC) - 2011/2012, Florianopolis, SC, Brazil

5 Boehringer Ingelheim, São Paulo, SP, Brazil

6 Eli Lilly, São Paulo, SP, Brazil

7 Avenida das Américas, no. 2901, sala 305, Edifício Barra Business, Barra da Tijuca, Rio de Janeiro, RJ, 489 22631-030, Brazil

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Diabetology & Metabolic Syndrome 2013, 5:25  doi:10.1186/1758-5996-5-25

Published: 22 May 2013


Type 2 diabetes mellitus (T2DM) has a high prevalence and incidence around the world. The complex pathophysiology mechanism is among the barriers for diabetes treatment. Type 2 diabetes patients have dysfunction in incretin hormones (as glucagon-like peptide-1 or GLP-1, and glucose-dependent insulinotropic polypeptide or GIP). By inhibiting the dipeptidyl peptidase-4 (DPP-4) enzyme, it is possible to slow the inactivation of GLP-1 and GIP, promoting blood glucose level reduction in a glucose-dependent manner. Linagliptin is a highly specific and potent inhibitor of DPP-4 that is currently indicated for the treatment of type 2 diabetes. Clinical studies with linagliptin demonstrated efficacy in reducing glycated hemoglobin (HbA1c) levels in type 2 diabetes patients, while maintaining a placebo-like safety and tolerability profile. Linagliptin has an interesting pharmacokinetic profile in terms of its predominantly non-renal elimination and the main implication of this characteristic is that no dose adjustment is necessary in patients with renal disease. Also, no dose adjustment is required in patients with hepatic insufficiency, as well in elderly or obese patients. This article will review the pharmacokinetic profile, efficacy data and safety aspects of linagliptin in type 2 diabetes patients.

DPP-4 inhibitor; Linagliptin; Efficacy; Safety; Renal impairment; Type 2 diabetes