title: Absorption, distribution, metabolism and excretion of gemigliptin, a novel dipeptidyl peptidase IV inhibitor, in rats.
abstract: 1. The absorption, distribution, metabolism and excretion of a novel dipeptidyl peptidase IV inhibitor, gemigliptin, were examined following single oral administration of (14)C-labeled gemigliptin to rats. 2. The (14)C-labeled gemigliptin was rapidly absorbed after oral administration, and its bioavailability was 95.2% (by total radioactivity). Distribution to specific tissues other than the digestive organs was not observed. Within 7 days after oral administration, 43.6% of the administered dose was excreted via urine and 41.2% was excreted via feces. Biliary excretion of the radioactivity was about 17.7% for the first 24 h. After oral administration of gemigliptin to rats, the in vivo metabolism of gemigliptin was investigated with bile, urine, feces, plasma and liver samples. 3. The major metabolic pathway was hydroxylation, and the major circulating metabolites were a dehydrated metabolite (LC15-0516) and hydroxylated metabolites (LC15-0635 and LC15-0636).
authors.affiliation: Institute of Pharmaceutical Science and Technology and College of Pharmacy, Hanyang University , Ansan , Republic of Korea .
authors.forename: Yoon
authors.initials: Y
authors.lastname: Kim
authors.forename: Unyong
authors.initials: U
authors.lastname: Kim
authors.forename: In Sook
authors.initials: IS
authors.lastname: Kim
authors.forename: Sung-Hack
authors.initials: SH
authors.lastname: Lee
authors.forename: Jaeick
authors.initials: J
authors.lastname: Lee
authors.forename: Dong-Hyun
authors.initials: DH
authors.lastname: Kim
authors.forename: Hye Hyun
authors.initials: HH
authors.lastname: Yoo
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001646:Bile / Q000378:metabolism; D002250:Carbon Radioisotopes / Q000493:pharmacokinetics; D054873:Dipeptidyl-Peptidase IV Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D005243:Feces; D006900:Hydroxylation; D008658:Inactivation, Metabolic; D007408:Intestinal Absorption; D008297:Male; D010881:Piperidones / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D011743:Pyrimidines / Q000008:administration & dosage / Q000493:pharmacokinetics* / Q000652:urine; D017207:Rats, Sprague-Dawley; D014018:Tissue Distribution
chemical_list: D002250:Carbon Radioisotopes; D054873:Dipeptidyl-Peptidase IV Inhibitors; C534891:LC15-0444; C575080:LC15-0636; D010881:Piperidones; D011743:Pyrimidines
keywords: Absorption; distribution; excretion; gemigliptin; metabolism