抗體藥物偶聯(lián)物（ADC）是由具有靶向特異性的單抗和具有高毒性的小分子結(jié)合而成的新藥，與單抗和小分子藥物相比，具有特異性高和毒性低的特征。由于這種特性，用于ADC的藥動(dòng)學(xué)（PK）研究的生物分析方法>的建立和選擇具有挑戰(zhàn)性。同時(shí)大分子抗體和小分子組分的藥物，生物分析方法的組合對(duì)了解ADC的體外與體內(nèi)過(guò)程，認(rèn)識(shí)藥物運(yùn)送到作用部位和暴露反應(yīng)關(guān)系十分重要。因此，對(duì)ADC的開發(fā)策略、新生物分析方法的開發(fā)、建立和驗(yàn)證，以及臨床前和臨床PK、PK/PD研究的問(wèn)題的挑戰(zhàn)和機(jī)遇必須有足夠認(rèn)識(shí)。就ADC的藥動(dòng)學(xué)研究的進(jìn)展和難點(diǎn)予以介紹，以期與從事該類藥物的研究者一起討論和分析。

Antibody drug conjugate (ADC) therapeutics utilized the specificity of monoclonal antibodies (mAbs) and potency of highly toxic small molecules. ADCs are typically composed of an mAb with a cytotoxin conjugated to it, resulting in a new eterogeneous mixture of mAb with various numbers of toxins. Due to this heterogeneity characterized by the therapeutic drug-to-antibody ratio, the selection of bioanalytical methods used to understand and develop ADCs can be challenging. Since the therapeutic drugs have both large- and small-molecule components, and one can use bioanalytical methods in both spaces. A combination of bioanalytical methods is typically used to understand the ADC in vitro/in vivo, to understand payload delivery to the site of action, and to establish an exposure-response relationship. Therefore, many challenges and opportunities to learn are involved with this approach, including issues related to ADC analysis strategies and application of these methods to ADC development, analytical establishment and validation, preclinical and clinical PK, PK/PD studies. In this paper, we introduced the progress and difficulties on pharmacokinetic studies of the ADC in order to engage researchers to discuss and analyze the issues on ADC pharmacokinetic studies.