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p Metabolite Identification in the Preclinical and Clinical Phase of Drug Development

文献类型：期刊论文

作者Wu, Yali1,2; Pan, Lulu1,2; Chen, Zhendong1; Zheng, Yuandong1; Diao, Xingxing1,2; Zhong, Dafang1,2
刊名CURRENT DRUG METABOLISM
出版日期2021
卷号22期号:11页码:838-857
ISSN号1389-2002
关键词Metabolite identification drug toxicity drug exposure covalent-binding drug drug safety natural medicines
DOI10.2174/1389200222666211006104502
通讯作者Diao, Xingxing(xxdiao@simm.ac.cn) ; Zhong, Dafang(dfzhong@simm.ac.cn)
英文摘要Metabolite identification plays a critical role in the phases during drug development. Drug metabolites can contribute to efficacy, toxicity, and drug-drug interaction. Thus, the correct identification of metabolites is essential to understand the behavior of drugs in humans. Drug administration authorities (e.g., FDA, EMA, and NMPA) emphasize evaluating the safety of human metabolites with exposure higher than 10% of the total drugrelated components. Many previous reviews have summarized the various methods, tools, and strategies for the appropriate and comprehensive identification of metabolites. In this review, we focus on summarizing the importance of identifying metabolites in the preclinical and clinical phases of drug development. Summarized scenarios include the role of metabolites in pharmacokinetics/pharmacodynamics (PK/PD) analysis, disproportional exposure of metabolites that contribute to drug toxicity, changes in metabolite exposure in renal-impaired patients, covalent tyrosine kinase inhibitors (anticancer drugs), and metabolite identification of drug candidates from natural medicines. This review is aimed to provide meaningful insight into the significant role of metabolite identification in drug development.
WOS关键词MASS-SPECTROMETRIC CHARACTERIZATION ; INTESTINAL 1ST-PASS METABOLISM ; HUMAN SERUM-ALBUMIN ; IN-VITRO ; COVALENT BINDING ; 3-N-BUTYLPHTHALIDE NBP ; LIQUID-CHROMATOGRAPHY ; HUMANS IDENTIFICATION ; TYROSINE KINASE ; AMYLOID-BETA
资助项目National Natural Science Foundation of China[81903701] ; National Natural Science Foundation of China[81521005]
WOS研究方向Biochemistry & Molecular Biology ; Pharmacology & Pharmacy
语种英语
出版者BENTHAM SCIENCE PUBL LTD
WOS记录号WOS:000745114300002
源URL[http://119.78.100.183/handle/2S10ELR8/300583]  
专题新药研究国家重点实验室
通讯作者Diao, Xingxing; Zhong, Dafang
作者单位1.Chinese Acad Sci, State Key Lab Drug Res, Shanghai Inst Mat Med, Shanghai 201210, Peoples R China
2.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
推荐引用方式
GB/T 7714		 Wu, Yali,Pan, Lulu,Chen, Zhendong,et al. p Metabolite Identification in the Preclinical and Clinical Phase of Drug Development[J]. CURRENT DRUG METABOLISM,2021,22(11):838-857.
APA Wu, Yali,Pan, Lulu,Chen, Zhendong,Zheng, Yuandong,Diao, Xingxing,&Zhong, Dafang.(2021).p Metabolite Identification in the Preclinical and Clinical Phase of Drug Development.CURRENT DRUG METABOLISM,22(11),838-857.
MLA Wu, Yali,et al."p Metabolite Identification in the Preclinical and Clinical Phase of Drug Development".CURRENT DRUG METABOLISM 22.11(2021):838-857.

入库方式： OAI收割

来源：上海药物研究所

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