虽然激酶抑制剂（KI）经常表现出较大的患者间变异性，但仍经常使用“一刀切”的疗程。与此同时，针对几种激酶抑制剂已经建立了暴露-反应和暴露-毒性的关系，因此，这种疗程可能导致不必要的毒性以及亚最佳的疗效。因此，基于测量的全身药物药代动力学水平进行剂量调整，即治疗药物监测（TDM），有望改善治疗疗效并减少毒性发生率。因此，本综合综述的目的是对目前已获得FDA/EMA批准的77种激酶抑制剂进行治疗药物监测的证据进行概述（截至2023年7月1日），这些激酶抑制剂在血液学和肿瘤科学中应用。我们对这些激酶抑制剂的暴露-反应和暴露-毒性关系进行详细阐述，并在可能的情况下提供TDM的实际建议并讨论相应的药代动力学靶标。© 2023年，作者。

Although kinase inhibitors (KI) frequently portray large interpatient variability, a 'one size fits all' regimen is still often used. In the meantime, relationships between exposure-response and exposure-toxicity have been established for several KIs, so this regimen could lead to unnecessary toxicity and suboptimal efficacy. Dose adjustments based on measured systemic pharmacokinetic levels-i.e., therapeutic drug monitoring (TDM)-could therefore improve treatment efficacy and reduce the incidence of toxicities. Therefore, the aim of this comprehensive review is to give an overview of the available evidence for TDM for the 77 FDA/EMA kinase inhibitors currently approved (as of July 1st, 2023) used in hematology and oncology. We elaborate on exposure-response and exposure-toxicity relationships for these kinase inhibitors and provide practical recommendations for TDM and discuss corresponding pharmacokinetic targets when possible.© 2023. The Author(s).