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Current Drug Metabolism


ISSN (Print): 1389-2002
ISSN (Online): 1875-5453

Mini-Review Article

Metabolite Identification in the Preclinical and Clinical Phase of Drug Development

Author(s): Yali Wu, Lulu Pan, Zhendong Chen, Yuandong Zheng, Xingxing Diao* and Dafang Zhong*

Volume 22, Issue 11, 2021

Published on: 05 October, 2021

Page: [838 - 857] Pages: 20

DOI: 10.2174/1389200222666211006104502

Price: $65


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.

Keywords: Metabolite identification, drug toxicity, drug exposure, covalent-binding drug, drug safety, natural medicines.

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