蛋白激酶抑制剂（PKIs）的靶向治疗代表了非小细胞肺癌（NSCLC）的重要治疗选择之一。它显著提高了患者的生存率和生活质量。尽管已知患者间药物动力学变异性较大且可能需要个体化剂量，但这些抗癌药物以固定剂量口服给药。为了优化和个体化PKIs的剂量，从而增加治疗的效果和安全性，治疗性药物监测（TDM）是最常提及的方法。与其他医学领域不同，由于缺乏PKIs的浓度-效应关系证据或数据，TDM在肿瘤学实践中相对较少。因此，本综述的目的是总结PKIs的药物动力学特征，并提供支持使用TDM对NSCLC患者进行个体化治疗的证据。

Targeted therapy with protein kinase inhibitors (PKIs) represents one of the important treatment options for non-small cell lung cancer (NSCLC). It has contributed to improve patients' survival and quality of life significantly. These anticancer drugs are administrated orally in flat-fixed doses despite the well-known large interpatient pharmacokinetic variability and the possible need for dose individualization. To optimize and individualize dosing of PKIs, and thereby increasing the effectiveness and safety of the treatment, therapeutic drug monitoring (TDM) is the most frequently mentioned method. Unlike other areas of medicine, TDM has been rather exceptional in oncological practise since there is a little evidence or no data for concentration-effect relationships of PKIs. Therefore, the aim of this review is to summarize the pharmacokinetic characteristics of PKIs and provide the evidence supporting the use of TDM for personalised treatment of patients with NSCLC.