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一种UPLC-MS/MS方法的开发及其在老鼠中对regorafenib的药理学分析的应用

Filip Otto¹, Viktoriia Propisnova², Hanna Urjasz¹

¹Department of Clinical Pharmacy and Biopharmacy, Poznań University of Medical Sciences, Rokietnicka 3, Poznań, 60-806, Poland.

Scientific reports

|February 20, 2026

概括

这项研究开发了一种经过验证的UPLC-MS/MS方法来量化regorafenib (REG) 和其代谢物. 与特拉美丁尼布 (TRA) 的同时使用显著增加了大鼠的 REG 系统暴露.

科学领域:

药理学药理学是指药理学的学科.
生物分析是一种生物分析.
药物新陈代谢药物新陈代谢

背景情况:

雷戈拉芬尼 (Regorafenib,REG) 是一种用于治疗肝细胞癌等癌症的多酶抑制剂,但个体变异性会影响其疗效.
EG的不良影响和不足的疗效可能来自于可变的血度.

研究的目的:

开发和验证一种生物分析方法,用于在大鼠血中量化REG及其代谢物 (M-2,M-5).
评估特拉美丁尼 (TRA) 对 REG 和其代谢物的药理动力学影响.

主要方法:

超高性能液态染色学与并联质谱学 (UPLC-MS/MS) 被用于量化.
雷戈拉费尼布D3作为内部标准,用于在大鼠血中检测REG,M-2和M-5.
经过验证的方法应用于大鼠的药理动力学和药物相互作用研究.

主要成果:

该UPLC-MS/MS方法表现出卓越的线性,精度,准确性和稳定性,符合EMA的指导方针.
与特拉美替尼 (TRA) 联合使用显著增加了REG的Cmax和AUC0-∞,分别增加了375%和553%.
TRA的使用导致M-2水平显著下降 (52%和44%),M-5水平显著增加 (779%).

结论:

成功建立了一种可靠的UPLC-MS/MS方法,用于在老鼠血中量化REG,M-2和M-5.
当Trametinib与Regorafenib同时使用时,Trametinib显著增加了对Regorafenib的全身暴露.

关键词:

甲基 N- 甲基 N- 氧化物regorafenib.药理动力学药理动力学雷戈拉费尼布的使用情况雷戈拉费尼布N-氧化物特拉美提尼布 (Trametinib) 是一种药物.在 UPLC-MS/MS 中使用.

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