Preclinical and clinical aspects of the dipeptidyl peptidase-4 inhibitor anagliptin

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Dipeptidyl Peptidase-4 Inhibitor

In the United States, nearly 13% of adults aged 20 years and older have type 2 diabetes mellitus (T2DM), and its prevalence is still increasing (1,2). Microvascular and macrovascular abnormalities are common in patients with T2DM and are related to the severity and duration of hyperglycemia (3–5). Thus, treatment of hyperglycemia is an important way to prevent or delay diabetic vascular complic...

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Dipeptidyl Peptidase‐4 Inhibitor Anagliptin Prevents Intracranial Aneurysm Growth by Suppressing Macrophage Infiltration and Activation

BACKGROUND Chronic inflammation plays a key role in the pathogenesis of intracranial aneurysms (IAs). DPP-4 (dipeptidyl peptidase-4) inhibitors have anti-inflammatory effects, including suppressing macrophage infiltration, in various inflammatory models. We examined whether a DPP-4 inhibitor, anagliptin, could suppress the growth of IAs in a rodent aneurysm model. METHODS AND RESULTS IAs were...

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Mechanism of lipid‐lowering action of the dipeptidyl peptidase‐4 inhibitor, anagliptin, in low‐density lipoprotein receptor‐deficient mice

AIMS/INTRODUCTION Dipeptidyl peptidase-4 inhibitors are used for treatment of patients with type 2 diabetes. In addition to glycemic control, these agents showed beneficial effects on lipid metabolism in clinical trials. However, the mechanism underlying the lipid-lowering effect of dipeptidyl peptidase-4 inhibitors remains unclear. Here, we investigated the lipid-lowering efficacy of anaglipti...

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Dipeptidyl peptidase-4 inhibitor ameliorates status epilepticus seizures and cognitive disturbances in a rat model of temporal lobe epilepsy

Background and Objective: In temporal lobe epilepsy (TLE), recurrent seizures accompany with cognitive deficit. In some patients, the current medications cannot provide satisfactory control of seizures, therefore new drugs that act through different mechanisms are required. In the present study, the useful effect of dipeptidyl peptidase-4 inhibitor was evaluated in experimental model of tempora...

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Pharmacokinetics of the dipeptidyl peptidase 4 inhibitor saxagliptin in rats, dogs, and monkeys and clinical projections.

Saxagliptin is a potent, selective, reversible dipeptidyl peptidase 4 (DPP4) inhibitor specifically designed for extended inhibition of the DPP4 enzyme and is currently under development for the treatment of type-2 diabetes. The pharmacokinetics of saxagliptin were evaluated in rats, dogs, and monkeys and used to predict its human pharmacokinetics. Saxagliptin was rapidly absorbed and had good ...

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ژورنال

عنوان ژورنال: Folia Pharmacologica Japonica

سال: 2013

ISSN: 0015-5691,1347-8397

DOI: 10.1254/fpj.141.339