Vildagliptin

Abstract

Vildagliptin is an oral antidiabetic drug. It is an inhibitor of dipeptidyl peptidase‐4. The metabolism of vildagliptin was investigated in healthy male subjects after a single oral 100‐mg dose of [ 14 C]‐vildagliptin. The major circulating components were unchanged parent and the carboxylic metabolite, accounting 26 and 55% of the total plasma residues, respectively. Four major metabolic reactions were involved in the biotransformation of vildagliptin: hydrolysis of cyano group, amide bond hydrolysis, glucuronide conjugation, and hydroxylation/oxidation and opening of the pyrrolidine ring.