Absorption, distribution, metabolism and excretion of gemigliptin, a novel dipeptidyl peptidase IV inhibitor, in rats
- Absorption, distribution, metabolism and excretion of gemigliptin, a novel dipeptidyl peptidase IV inhibitor, in rats
- 김윤; 김운용; 김인숙; 이승학; 이재익; 김동현; 유혜현
- Absorption; distribution; excretion; gemigliptin; metabolism
- Issue Date
- VOL 44, NO 7, 627-634
- 1. The absorption, distribution, metabolism and excretion of a novel dipeptidyl peptidase IV
inhibitor, gemigliptin, were examined following single oral administration of 14C-labeled
gemigliptin to rats.
2. The 14C-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
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