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An Investigation of the Metabolism and Excretion of KD101 and Its Interindividual Differences: A Microtracing Mass Balance Study in Humans
- Source :
- Clinical and Translational Science, Vol 14, Iss 1, Pp 231-238 (2021), Clinical and Translational Science
- Publication Year :
- 2021
- Publisher :
- Wiley, 2021.
-
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 14 C-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 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.
- Subjects :
- Drug
Adult
Male
030213 general clinical medicine
Pharmacogenomic Variants
media_common.quotation_subject
Physiology
Administration, Oral
Urine
Absorption (skin)
030226 pharmacology & pharmacy
General Biochemistry, Genetics and Molecular Biology
Article
Excretion
03 medical and health sciences
Young Adult
0302 clinical medicine
MicroDose
Oral administration
Medicine
Humans
Carbon Radioisotopes
General Pharmacology, Toxicology and Pharmaceutics
Glucuronosyltransferase
media_common
Polycyclic Sesquiterpenes
business.industry
General Neuroscience
Research
lcsh:Public aspects of medicine
lcsh:RM1-950
lcsh:RA1-1270
General Medicine
Metabolism
Articles
Middle Aged
Healthy Volunteers
UGT2B7
Renal Elimination
lcsh:Therapeutics. Pharmacology
Biological Variation, Population
Gastrointestinal Absorption
Anti-Obesity Agents
business
Subjects
Details
- Language :
- English
- ISSN :
- 17528054 and 17528062
- Volume :
- 14
- Issue :
- 1
- Database :
- OpenAIRE
- Journal :
- Clinical and Translational Science
- Accession number :
- edsair.doi.dedup.....1d2c55eba91745e1b6ec101886866557