抗体偶联药物的分子特点及其药代动力学研究考虑

随着我国药物研发和临床试验水平的不断提高,近年来抗体偶联药物(Antibody-Drug Conjugate, ADC)的相关研究和注册申报也正在增多。ADC类药物由抗体、连接子和小分子毒素组成,在兼具高度靶向性和高细胞毒性优势的同时,由于其结构的多样性和复杂性,以及循环系统中释放的小分子毒素含量较低等特殊性,给其药代动力学研究带来了诸多挑战。本文将从ADC药物的分子设计、药代动力学特征和目标分析物等方面讨论,以期帮助读者更好的理解ADC药物的药代动力学研究。

Characteristics and considerations for pharmacokinetics of antibody-drug conjugates

As the continuous improvement of drug development and clinical research in China, related research and registration of antibody-drug conjugate(ADC) are increasing in recent years. ADC drugs have the advantages of high targeting and strong cytotoxicity, but their structural diversity and complexity, and the low concentration of small molecule drugs released in circulatory system resulting in challenges in the pharmacokinetics studies of ADC. In order to have a better understanding of the pharmacokinetics of ADC drugs, here we will have a discussion on the molecular design, pharmacokinetic characteristics and target analyte of ADC drugs.