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低分子量候选药物高通量药代动力学筛选方法。

Approaches for high-throughput pharmacokinetic screening of low-molecular-weight drug candidates.

作者信息

Fontana Stefano

机构信息

DMPK, Aptuit , Via A. Fleming, 4, 37135 Verona , Italy +39 0458219605 ; +39 0458218153 ;

出版信息

Expert Opin Drug Metab Toxicol. 2014 Feb;10(2):139-42. doi: 10.1517/17425255.2014.870153. Epub 2013 Dec 13.

DOI:10.1517/17425255.2014.870153
PMID:24329157
Abstract

In the face of advancing technology in combinatorial synthesis and high-throughput screening, the drug discovery process continues to evolve. Drug metabolism and pharmacokinetics (DMPK) studies play a key role in lead identification and optimization. This fast-paced development process has imposed an enormous burden on the analytical chemist to design faster and more sensitive assay techniques to aid the drug discovery and development. Various strategies aimed at increasing the throughput and reducing sample numbers in discovery DMPK have been developed for both in vitro and in vivo experiments. However, quantity and speed, often associated with technology development, do not always guarantee quality but a clear strategic focus in the spirit of 'Fit for Purpose' approach is required to implement systems to generate high-quality data and to drive research in new directions.

摘要

面对组合化学合成和高通量筛选技术的不断进步,药物研发过程持续演变。药物代谢和药代动力学(DMPK)研究在先导化合物的发现与优化中发挥着关键作用。这种快节奏的发展进程给分析化学家带来了巨大负担,他们需要设计出更快且更灵敏的检测技术,以助力药物研发。针对体外和体内实验,已开发出各种旨在提高发现阶段DMPK的通量并减少样品数量的策略。然而,通常与技术发展相关的数量和速度并不总能保证质量,而是需要秉持“适用为目的”的理念,有明确的战略重点,才能实施生成高质量数据并推动新方向研究的系统。

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