The pharmacokinetics and metabolism of linagliptin (BI1356, 8-(3R-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydro-purine-2,6-dione) were investigated in healthy volunteers. The 10- and 5-mg (14)C-labeled drug was administered orally or intravenously, respectively. Fecal excretion was the dominant excretion pathway with 84.7% (p.o.) and 58.2% (i.v.) of ...

The complex pathophysiologic mechanisms of type 2 diabetes are one of the barriers that make its treatment so difficult and it is also one of the responsible for the high prevalence of the disease around the world. Patients with T2DM have dysfunction in incretin hormones (such as glucagon-like peptide-1 or GLP-1 and glucose-dependent insulinotropic polypeptide or GIP). By inhibiting the dipepti...

INTRODUCTION Asian patients with type 2 diabetes (T2D) are younger, leaner, and more likely to develop renal dysfunction than White populations. In this multiethnic analysis of data from phase 3 trials, we investigated the efficacy and safety of the dipeptidyl peptidase-4 inhibitor linagliptin in Asians stratified by these subphenotypes. METHODS Data from randomized, double-blind, placebo-con...

A rapid, highly sensitive, economical and accurate RP-HPLC method was developed for simultaneous estimation of Metformin HCL and Linagliptin in Bulk and Pharmaceutical Dosage form. The separation was achieved by Hypersil C18 column (250 × 4.6 mm, 5 μ particle size) with mobile phase consisting of phosphate buffer (pH 5.6, diluted with orthophosphoric acid), methanol and acetonitrile in the rati...

Asia has a growing diabetic population. Linagliptin, a member of dipeptidyl peptidase-4 inhibitor class, is unique in its nonlinear pharmacokinetics with the characteristics of rapid attainment of steady state, little accumulation, predominantly nonrenal route of elimination, prolonged terminal half-life, and sustained inhibition of dipeptidyl peptidase-4 enzyme. No clinically relevant differen...

objective: druggability of a target protein depends on the interacting micro-environment between the target protein and drugs. therefore, a precise knowledge of the interacting micro-environment between the target protein and drugs is requisite for drug discovery process. to understand such micro-environment, we performed in silico interaction analysis between a human target protein, dipeptidyl...

INTRODUCTION The aim of this study was to investigate the efficacy and safety of linagliptin + low-dose (LD) metformin once daily versus high-dose (HD) metformin twice daily in treatment-naïve patients with type 2 diabetes. METHODS Patients (n = 689) were randomized (1:1) to double-blind treatment with linagliptin 5 mg + LD metformin (1000 mg) or HD metformin (2000 mg) for 14 weeks. Metformin...

BACKGROUND Use of dipeptidyl peptidase-4 inhibitors (DPP4-i) for the treatment of type 2 diabetes (T2D) has been associated with a possible increase in the risk for heart failure (HF). B-type natriuretic peptide (BNP), which is both a biomarker of HF and a hemodynamically active hormone, is a substrate of DPP-4. We herein tested the acute effects of the DPP-4i linagliptin on BNP and NT-proBNP i...

OBJECTIVE Druggability of a target protein depends on the interacting micro-environment between the target protein and drugs. Therefore, a precise knowledge of the interacting micro-environment between the target protein and drugs is requisite for drug discovery process. To understand such micro-environment, we performed in silico interaction analysis between a human target protein, Dipeptidyl ...