Hepatic Dipeptidyl Peptidase-4 Controls Pharmacokinetics of Vildagliptin In Vivo
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چکیده
منابع مشابه
Hepatic 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...
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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 کاملDipeptidyl 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 کاملDipeptidyl peptidase-4 greatly contributes to the hydrolysis of vildagliptin in human liver.
The major metabolic pathway of vildagliptin in mice, rats, dogs, and humans is hydrolysis at the cyano group to produce a carboxylic acid metabolite M20.7 (LAY151), whereas the major metabolic enzyme of vildagliptin has not been identified. In the present study, we determined the contribution rate of dipeptidyl peptidase-4 (DPP-4) to the hydrolysis of vildagliptin in the liver. We performed hyd...
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: Drug Metabolism and Disposition
سال: 2016
ISSN: 0090-9556,1521-009X
DOI: 10.1124/dmd.116.073866