An Investigation of the Metabolism and Excretion of KD101 and Its Interindividual Differences: A Microtracing Mass Balance Study in Humans

Title
An Investigation of the Metabolism and Excretion of KD101 and Its Interindividual Differences: A Microtracing Mass Balance Study in Humans
Authors
유병용김언혜Stephen R. Dueker황준기윤장수이혜숙유경상이형기Sang-Won Lee
Keywords
KD101; AMS; Mass Balance; Metabolism; Microtracing
Issue Date
2021-01
Publisher
CTS-CLINICAL AND TRANSLATIONAL SCIENCE
Citation
VOL 14, NO 1-238
Abstract
The absorption, metabolism, and excretion (AME) profiles of KD101, currently under clinical development to treat obesity, were assessed in humans using accelerator mass spectrometry (AMS) after a single oral administration of KD101 at 400 mg and a microdose of 14C-KD101 at ~ 35.2 μg with a total radioactivity of 6.81 kBq. The mean total recovery of administered radioactivity was 85.2% with predominant excretion in the urine (78.0%). The radio-chromatographic metabolite profiling showed that most of the total radioactivity in the plasma and the urine was ascribable to metabolites. The UDPglucuronosyltransferase (UGT), including UGT1A1, UGT1A3, and UGT2B7, might have contributed to the interindividual variability in the metabolism and excretion of KD101. The microtracing approach using AMS is a useful tool to evaluate the AME of a drug under development without risk for high radiation exposure to humans.
URI
http://pubs.kist.re.kr/handle/201004/72447
ISSN
1752-8054
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KIST Publication > Article
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