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低剂量阿帕蒂尼布在患有功能障碍的人群中:一个药理动力学研究
Jishi Liu1, Wei Li1, Kaiqian Zhang1
1Department of Nephrology, The Third Xiangya Hospital, Central South University No. 138, Tongzipo Road, Changsha, 410013, Hunan Province, China.
概括
这项研究发现,轻度至中度功能障碍不会显著改变阿帕蒂尼布的药理动力学或其主要代谢物. 因此,对于服用低剂量阿帕蒂尼布的轻度或中度功能障碍患者,剂量调整是不必要的.
科学领域:
- 药理学 药理学是指药理学的学科.
- 腎臟病學 (nephrology) 是一種醫學專業.
- 在瘤学瘤学.
背景情况:
- 阿帕提尼布是一种用于癌症治疗的氨酸激酶抑制剂.
- 功能障碍可能会影响药物的药理动力学.
- 功能障碍对阿帕蒂尼布及其代谢物的影响需要研究.
研究的目的:
- 在不同程度的功能患者中研究阿帕蒂尼布及其主要代谢物的药理学.
- 为了确定是否需要对轻度或中度功能障碍患者的阿帕蒂尼布进行剂量调整.
主要方法:
- 一次250毫克口服阿帕蒂尼布剂量给正常,轻度和中度功能障碍的受试者.
- 药理动力学样本是在剂量后96小时内收集的.
- 使用非分组分析计算药理动力学参数.
主要成果:
- 轻度和中度功能障碍对阿帕蒂尼布的药理动力学没有显著影响 (Cmax,AUC0-t,AUC0-inf).
- 代谢物M1-1,M1-2和M1-6的药理动力学没有受到功能障碍的显著影响.
- 观察到对代谢物M9-2的暴露增加,但由于缺乏抑制作用,因此被认为在临床上无关紧要.
结论:
- 患有轻度至中度功能障碍的患者不需要对250毫克阿帕蒂尼布的剂量进行调整.
- 在研究剂量下,阿帕提尼布在患有轻度至中度功能障碍的患者中通常耐受良好.
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