单克隆抗体药代动力学研究进展及应用

Advances in pharmacokinetic studies of therapeutic monoclonal antibodies and their application

单克隆抗体药物在肿瘤治疗领域表现出显著疗效。单克隆抗体药物的结构和生物活性与小分子药物存在显著差异,故体内的吸收、分布、代谢、排泄及毒性过程均表现出与小分子药物不同的药代动力学(pharmacokinetics,PK)特征。本文对单克隆抗体药物PK特征进行总结,并结合抗体免疫原性、糖基化修饰、不同给药方式等因素,对单克隆抗体药物PK特性进行讨论;简述其药代动力学/药效学(pharmacodynamics,PD)(PK/PD)模型在抗肿瘤靶向药物中的研究情况。

Monoclonal antibody (mAb) drugs have recently shown significant efficacy in the field of cancer therapy. Their structure and biological activity are significantly different from those of small molecule drugs. Therefore, their absorption, distribution, metabolism, excretion and toxicity processes in the body show different pharmacokinetics (PK) characteristics from small molecule drugs. The unique PK characteristics of mAbs are summarized and discussed in combination with factors such as antibody immunogenicity, glycosylation modification and different modes of administration. The pharmacokinetic/ pharmacodynamic (PK/PD) model in the function of anti-tumor targeted drug study is also outlined.