酪氨酸激酶抑制剂的群体药动学研究进展

    Advances of Population Pharmacokinetics in Tyrosine Kinase Inhibitors

    • 摘要: 以酪氨酸激酶抑制剂(tyrosine kinase inhibitors,TKIs)为代表的小分子靶向抗肿瘤药物以其高选择性和低毒性等优势已成为肿瘤治疗药物研究的新热点,关于TKIs的群体药动学(population pharmacokinetics,PPK)研究报道也日益增多。本研究综述常见肿瘤TKIs药物的PPK研究进展,列举了各类药物的PPK模型结构参数及其协变量,并总结了药物是否需要根据相关影响因素进行给药方案的调整,以期为临床合理使用TKIs药物及药动-药效学(pharmacokinetic-pharmacodynamics,PK-PD)研究提供参考。

       

      Abstract: Small molecule targeted anti-tumor drugs represented by tyrosine kinase inhibitors(TKIs) have become a new hotspot in the research of cancer therapeutic drugs due to their high selectivity and low toxicity, and more and more studies of population pharmacokinetics (PPK) in TKIs are reported. This article summarize the progress of PPK research on TKIs used in common tumor, listed the PPK model structure parameters and covariates, and summarized whether they need to be adjusted according to relevant influencing factors, in order to provide reference for rationally use of TKIs in clinical and pharmacokinetic- pharmacodynamics(PK-PD) studies.

       

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