Ward Keith W
Bausch & Lomb, Global Preclinical Development, Rochester, NY 14603, USA.
Expert Opin Drug Metab Toxicol. 2005 Dec;1(4):583-94. doi: 10.1517/17425255.1.4.583.
The early characterisation of drug metabolism and pharmacokinetic (DMPK) properties of new chemical entities plays a key role in the pharmaceutical industry's effort to reduce attrition. Specifically, a major goal of early DMPK studies is to accurately predict the behaviour of new chemical entities in humans, thus allowing likely failures to be terminated rapidly and resource to be placed on molecules most likely to succeed. The present review summarises progress over the past several years in the key technologies used in the pharmaceutical industry to achieve these goals: namely, in vivo, in vitro and in silico/computational tools. The limitations of the various assays are discussed, with attention also given to likely future directions in this field.
新化学实体的药物代谢和药代动力学(DMPK)特性的早期表征在制药行业减少研发失败方面发挥着关键作用。具体而言,早期DMPK研究的一个主要目标是准确预测新化学实体在人体内的行为,从而能够迅速终止可能失败的项目,并将资源投入到最有可能成功的分子上。本综述总结了制药行业为实现这些目标所使用的关键技术在过去几年中的进展:即体内、体外和计算机模拟/计算工具。讨论了各种分析方法的局限性,并关注了该领域未来可能的发展方向。