Kim, Anhye Dueker, Stephen R. Hwang, Jun Gi Yoon, Jangsoo Lee, Sang-Won Lee, Hye Suk Yu, Byung-Yong Yu, Kyung-Sang Lee, Howard 2024-01-19T16:00:33Z 2024-01-19T16:00:33Z 2021-09-02 2021-01 1752-8054 https://pubs.kist.re.kr/handle/201004/117657 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 C-14-KD101 at similar to 35.2 mu g 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 UDP-glucuronosyltransferase (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. English WILEY LABORATORY-ANIMALS UDP-GLUCURONOSYLTRANSFERASES VALPROIC ACID PHARMACOKINETICS POLYMORPHISM LAMOTRIGINE SAMPLES PLASMA An Investigation of the Metabolism and Excretion of KD101 and Its Interindividual Differences: A Microtracing Mass Balance Study in Humans Article 10.1111/cts.12848 1 CTS-CLINICAL AND TRANSLATIONAL SCIENCE, v.14, no.1, pp.231 - 238 CTS-CLINICAL AND TRANSLATIONAL SCIENCE 14 1 231 238 scie scopus 000572689600001 2-s2.0-85091428782 Medicine, Research & Experimental Research & Experimental Medicine Article LABORATORY-ANIMALS UDP-GLUCURONOSYLTRANSFERASES VALPROIC ACID PHARMACOKINETICS POLYMORPHISM LAMOTRIGINE SAMPLES PLASMA KD101 AMS Mass Balance Metabolism Microtracing