Pharmacokinetics (PK), which describes the disposition of a drug in the body, should be a primary consideration in the selection of a drug candidate, ultimately contributing to its eventual clinical success or failure. Accordingly, a sound understanding of PK concepts and an appreciation of the judicious use of PK and related (e.g., metabolism, transporter) data in drug discovery can be beneficial to those involved in the process. This review defines important PK parameters (e.g., clearance, volume of distribution, half-life), describes methods of PK data analysis (noncompartmental vs. compartmental) and provides an overview of additional concepts such as allometric scaling, PK/pharmacodynamic modeling, and nonlinear PK. Furthermore, the role and strategic use of PK screens in drug discovery are discussed.

中文翻译：

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药代动力学及其在小分子药物发现研究中的作用。

描述体内药物配置的药代动力学（PK）应该是选择候选药物时的主要考虑因素，最终有助于其最终的临床成败。因此，对PK概念的透彻理解以及对PK和药物发现中相关（例如，新陈代谢，转运蛋白）数据的明智使用的赞赏，对于参与该过程的人员可能是有益的。这篇综述定义了重要的PK参数（例如，清除率，分布量，半衰期），描述了PK数据分析的方法（非房室vs.房室），并概述了其他概念，例如异速比结垢，PK /药效学建模和非线性PK。此外，讨论了PK筛选在药物发现中的作用和战略用途。