Preclinical and clinical findings of the dipeptidyl peptidase-4 inhibitor vildagliptin
نویسندگان
چکیده
منابع مشابه
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...
متن کاملHepatic Dipeptidyl Peptidase-4 Controls Pharmacokinetics of Vildagliptin In Vivo.
The main route of elimination of vildagliptin, which is an inhibitor of dipeptidyl peptidase-4 (DPP-4), in humans is cyano group hydrolysis to produce a carboxylic acid metabolite M20.7. Our in vitro study previously demonstrated that DPP-4 itself greatly contributed to the hydrolysis of vildagliptin in mouse, rat, and human livers. To investigate whether hepatic DPP-4 contributes to the hydrol...
متن کاملVildagliptin, a dipeptidyl peptidase-4 inhibitor, for the treatment of type 2 diabetes.
INTRODUCTION Vildagliptin is a dipeptidyl peptidase-4 inhibitor targeting the incretin system to improve glycemic control in type 2 diabetes. AREAS COVERED This review focuses on the pharmacokinetics, drug interactions and use of oral vildagliptin in special populations. Clinical efficacy and vildagliptin's role in the spectrum of therapeutics available are briefly addressed. EXPERT OPINION...
متن کاملAbsorption, metabolism, and excretion of [14C]vildagliptin, a novel dipeptidyl peptidase 4 inhibitor, in humans.
The absorption, metabolism, and excretion of (1-[[3-hydroxy-1-adamantyl) amino] acetyl]-2-cyano-(S)-pyrrolidine (vildagliptin), an orally active and highly selective dipeptidyl peptidase 4 inhibitor developed for the treatment of type 2 diabetes, were evaluated in four healthy male subjects after a single p.o. 100-mg dose of [(14)C]vildagliptin. Serial blood and complete urine and feces were co...
متن کاملDisposition of vildagliptin, a novel dipeptidyl peptidase 4 inhibitor, in rats and dogs.
The pharmacokinetics, absorption, metabolism, and excretion of vildagliptin, a potent and orally active inhibitor of dipeptidyl peptidase 4, were evaluated in male rats and dogs. Vildagliptin was rapidly absorbed with peak plasma concentrations occurring between 0.5 and 1.5 h. Moderate to high bioavailability was observed in both species (45-100%). The distribution and elimination half-lives of...
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ژورنال
عنوان ژورنال: Folia Pharmacologica Japonica
سال: 2010
ISSN: 0015-5691,1347-8397
DOI: 10.1254/fpj.136.299