Context Patients with diabetes often have comorbidities such as hypertension. It is not known how individual characteristics influence response to dipeptidyl peptidase-4 (DPP4) inhibitors. Objective We tested the hypothesis that individual characteristics, sitagliptin dose, and genetic variability in DPP4 influence DPP4 activity during sitagliptin. Design and Setting Post hoc analysis of cl...

P-glycoprotein (P-gp) and cytochrome P450 3A4 (CYP3A4) play a significant role in the disposition and elimination of drugs. The objective of this study was to investigate the mechanism underlying the interaction between sitagliptin (substrate of P-gp and CYP3A4) and verapamil (known modulator of P-gp and CYP3A4) using in vivo, ex vivo and in situ models. Rats were treated with sitagliptin (10 m...

Simple, accurate and precise spectroflourometric and spectrophotometric methods have been developed and validated for the determination of sitagliptin phosphate monohydrate (STG) and metformin HCL (MET). Zero order, first derivative, ratio derivative spectrophotometric methods and flourometric methods have been developed. The zero order spectrophotometric method was used for the determination o...

Non-alcoholic fatty liver disease is a main complication of type 2 diabetes. Isoquercitrin are employed for antidiabetic therapies, but the effects on liver function and the hepatocytes are unclear. The aim of this study was to investigate the effects of isoquercitrin on the T2DM-induced hepatic injury in rats. Isoquercitrin (10 mg/kg/d, 30 mg/kg/d), sitagliptin phosphate (10 mg/kg/d) was given...

INTRODUCTION Dipeptidyl peptidase-4 (DPP-4) inhibitors reduce blood glucose in a dose-dependent manner, but the dose-dependent effect relationship between DPP-4 inhibitors and atherosclerosis has not been investigated. METHODS Patients with type 2 diabetes mellitus (T2DM) treated with insulin were randomized to the sitagliptin (n = 137) or conventional treatment group (n = 137). In the sitagl...

BACKGROUND Sitagliptin is one of the dipeptidyl peptidase-4 (DPP-4) inhibitors which prevent the inactivation of incretins, increasing the endogenous active incretin levels. Incretins stimulate insulin secretion from pancreatic β-cells and inhibit glucagon secretion from pancreatic α-cells, which is favorable for the treatment of diabetes. Sitagliptin is released on December, 2009, in Japan. We...

The metabolism and excretion of [C]sitagliptin, an orally active, potent and selective dipeptidyl peptidase 4 inhibitor, were investigated in humans after a single oral dose of 83 mg/193 Ci. Urine, feces, and plasma were collected at regular intervals for up to 7 days. The primary route of excretion of radioactivity was via the kidneys, with a mean value of 87% of the administered dose recovere...

Recently, the dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin, a major anti-hyperglycaemic agent, has received substantial attention as a therapeutic target for cardiovascular diseases via enhancing the number of circulating endothelial progenitor cells (EPCs). However, the direct effects of sitagliptin on EPC function remain elusive. In this study, we evaluated the proangiogenic effects o...

OBJECTIVE To compare the incidence of cardiovascular events and mortality in patients with type 2 diabetes mellitus treated with sitagliptin or non-sitagliptin comparators. METHODS A post hoc assessment of cardiovascular safety in 14,611 patients was performed by pooling data from 25 double-blind studies, which randomised patients at baseline to sitagliptin 100 mg/day or a non-sitagliptin com...