a Department of Chemical Engineering and Analytical Chemistry , University of Barcelona , Barcelona , Spain.
Expert Opin Drug Discov. 2019 May;14(5):469-483. doi: 10.1080/17460441.2019.1582638. Epub 2019 Feb 27.
The identification and characterization of the metabolites during the early stages of discovery and development of new drug candidates are essential to establish the metabolic clearance as well as the potential pharmacological and/or toxicological effects. Hence, feasible methods of analysis, preferably rapid and simple, are required to satisfy the increasing demand of metabolite profiling studies. Areas covered: This paper reviews the topic of metabolite profiling in drug discovery based on liquid chromatography, with especial emphasis on chromatographic modes and detectors. Features and possibilities of the different options are critically discussed. Expert opinion: High performance analytical techniques are fundamental to gain unambiguous information on metabolites of new drugs. In this regard, liquid chromatography hyphenated to mass spectrometric detection is the most popular approach. The diversity of chromatographic modes and the great variety of separation columns available offer innumerable analytical possibilities to characterize and quantify compounds with a broad range of physicochemical properties.
在新药候选物的发现和开发的早期阶段,对代谢物进行鉴定和特征分析对于确定代谢清除率以及潜在的药理学和/或毒理学效应至关重要。因此,需要可行的分析方法,最好是快速简单的方法,以满足日益增长的代谢物分析研究的需求。
本文综述了基于液相色谱的药物发现中的代谢物分析专题,特别强调了色谱模式和检测器。批判性地讨论了不同选择的特点和可能性。
高性能分析技术是获得新药代谢物明确信息的基础。在这方面,液相色谱与质谱检测联用是最受欢迎的方法。色谱模式的多样性和可用的分离柱种类繁多,为具有广泛物理化学性质的化合物的特征分析和定量提供了无数的分析可能性。