Lin Kedan, Tibbitts Jay, Shen Ben-Quan
Early Development Pharmacokinetics and Pharmacodynamics, Genentech Inc., South San Francisco, CA, USA.
Methods Mol Biol. 2013;1045:117-31. doi: 10.1007/978-1-62703-541-5_7.
Pharmacokinetic and absorption, distribution, metabolism, and excretion (ADME) characterization of antibody-drug conjugates (ADCs) reflects the dynamic interactions between the biological system and ADC, and provides critical assessments in lead selection, optimization, and clinical development. Understanding the pharmacokinetics (PK), ADME properties and consequently the pharmacokinetic-pharmacodynamic properties of ADCs is critical for their successful development. This chapter discusses the PK properties of ADCs, types of PK and ADME studies in supporting different stages of development, general design of PK/ADME studies with a focus on ADC-specific characteristics, and interpretation of PK parameters.
抗体药物偶联物（ADC）的药代动力学以及吸收、分布、代谢和排泄（ADME）特征反映了生物系统与ADC之间的动态相互作用，并为先导化合物的筛选、优化及临床开发提供了关键评估。了解ADC的药代动力学（PK）、ADME特性以及由此产生的药代动力学-药效学特性对于其成功开发至关重要。本章讨论了ADC的PK特性、支持不同开发阶段的PK和ADME研究类型、侧重于ADC特定特征的PK/ADME研究的总体设计以及PK参数的解读。
