抗体药物偶联物（ADC）已成为抗肿瘤药物研发的关键领域。它们通过将单克隆抗体的肿瘤靶向能力与小分子药物的细胞毒作用相结合，为肿瘤治疗提供了创新的可能性。药理学是一门重要学科，通过建模和模拟整合临床试验数据，有助于全面了解 ADC 的药代动力学特征。然而，由于ADC结构复杂，其建模方法仍不清楚。在这篇综述中，我们分析了已发表的 ADC 群体药代动力学模型，并将其分为单分析物模型、二分析物模型和三分析物模型。我们还描述了每个模型的优点、局限性和建议。此外，我们建议ADC群体药代动力学模型的开发应根据四个关键方面进行严格考虑和建立：（1）研究目标； (2) 可用的体外和动物数据； (3) 可获取的临床信息； (4)生物分析方法的能力。该综述为指导药理学在 ADC 临床研究中的应用提供了见解，从而有助于更有效的治疗开发。© 2024。作者，获得 Springer Nature Switzerland AG 的独家许可。

Antibody-drug conjugates (ADCs) have become a pivotal area in the research and development of antitumor drugs. They provide innovative possibilities for tumor therapy by integrating the tumor-targeting capabilities of monoclonal antibodies with the cytotoxic effect of small molecule drugs. Pharmacometrics, an important discipline, facilitates comprehensive understanding of the pharmacokinetic characteristics of ADCs by integrating clinical trial data through modeling and simulation. However, due to the complex structure of ADCs, their modeling approaches are still unclear. In this review, we analyzed published population pharmacokinetic models for ADCs and classified them into single-analyte, two-analyte, and three-analyte models. We also described the benefits, limitations, and recommendations for each model. Furthermore, we suggested that the development of population pharmacokinetic models for ADCs should be rigorously considered and established based on four key aspects: (1) research objectives; (2) available in vitro and animal data; (3) accessible clinical information; and (4) the capability of bioanalytical methods. This review offered insights to guide the application of pharmacometrics in the clinical research of ADCs, thereby contributing to more effective therapeutic development.© 2024. The Author(s), under exclusive licence to Springer Nature Switzerland AG.