Characterization of fimasartan metabolites in human liver microsomes and human plasma
- Authors
- Lee, Ji-Yoon; Choi, Young Jae; Oh, Soo Jin; Chi, Yong Ha; Paik, Soo Heui; Lee, Ki Ho; Jung, Jae-Kyung; Ryu, Chang Seon; Kim, Kwon-Bok; Kim, Dong-Hyun; Yoon, Young-Ran; Kim, Sang Kyum
- Issue Date
- 2-1월-2016
- Publisher
- TAYLOR & FRANCIS LTD
- Keywords
- Fimasartan; metabolic stability; metabolite identification; qualitative and quantitative analysis
- Citation
- XENOBIOTICA, v.46, no.1, pp.40 - 51
- Indexed
- SCIE
SCOPUS
- Journal Title
- XENOBIOTICA
- Volume
- 46
- Number
- 1
- Start Page
- 40
- End Page
- 51
- URI
- https://scholar.korea.ac.kr/handle/2021.sw.korea/89843
- DOI
- 10.3109/00498254.2015.1047429
- ISSN
- 0049-8254
- Abstract
- 1.The metabolites of fimasartan (FMS), a new angiotensin II receptor antagonist, were characterized in human liver microsomes (HLM) and human subjects.2.We developed a method for a simultaneous quantitative and qualitative analysis using predictive multiple reaction monitoring information-dependent acquisition-enhanced product ion scanning. To characterize metabolic reactions, FMS metabolites were analyzed using quadrupole-time of flight mass spectrometer in full-scan mode.3.The structures of metabolites were confirmed by comparison of chromatographic retention times and mass spectra with those of authentic metabolite standards.4.In the cofactor-dependent microsomal metabolism study, the half-lives of FMS were 56.7, 247.9 and 53.3min in the presence of NADPH, UDPGA and NADPH+UDPGA, respectively.5.The main metabolic routes in HLM were S-oxidation, oxidative desulfuration, n-butyl hydroxylation and N-glucuronidation.6.In humans orally administered with 120mg FMS daily for 7 days, the prominent metabolites were FMS S-oxide and FMS N-glucuronide in the 0-8-h pooled plasma sample of each subject.7.This study characterizes, for the first time, the metabolites of FMS in humans to provide information for its safe use in clinical medicine.
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