Abstract
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.
Highlights
In recent decades, type 2 diabetes mellitus (T2DM) has reached epidemic proportions in all regions of the world, with increasing prevalence and incidence rates, in parallel to the obesity epidemic and the dissemination of occidental lifestyle [1]
This study suggested that the combination of metformin and linagliptin can be done safely in patients with T2DM, without requiring dose adjustment [20]
Patients (n = 2141) were grouped according to renal function, and it was found that reductions in Glycated hemoglobin (HbA1c) with linagliptin did not differ among groups, as well as adverse event occurrences that were similar to placebo [31,32]
Summary
Type 2 diabetes mellitus (T2DM) has reached epidemic proportions in all regions of the world, with increasing prevalence and incidence rates, in parallel to the obesity epidemic and the dissemination of occidental lifestyle [1]. This method of excretion may be in part because of the high plasma protein binding [9] The implication of this mode of linagliptin excretion is that in patients with kidney disease, no dose adjustment is required [8]. Clinical studies: efficacy assessment Monotherapy metformin is the first-line drug in the early pharmacological treatment of T2DM, some patients do not tolerate the drug, or exhibit contraindications [16]. In these cases, the DPP-4 inhibitors such as linagliptin can be an effective option for use as monotherapy. The percentage of patients achieving a reduction ≥ 0.5% in HbA1c with linagliptin (57.2%) was greater than those with voglibose (37.7%) (p < 0.0001) [10]
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