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内源性血里博夫拉不是人类可行的BCRP生物标志物

John P Savaryn¹, Ryota Kikuchi¹, Yuli Qian²

¹Quantitative, Translational and ADME Sciences, AbbVie Inc., North Chicago, Illinois, USA.

Clinical and translational science

|December 17, 2024

概括

血里博夫拉不是人类乳腺癌抵抗蛋白 (BCRP) 抑制的可行的生物标志物. 一项临床研究发现,在服用BCRP抑制剂后, рибофлавин水平没有增加.

科学领域:

药理学药理学是指药理学的学科.
生物标志物发现发现
药物新陈代谢药物新陈代谢

背景情况:

最近的报道表明,血里博夫拉是抑制BCRP的潜在生物标志物.
支持这一假设的临床数据有限,仅有两项先前的研究表明,黎波弗拉水平的适度增加.

研究的目的:

调查内源性血里博夫拉作为人类BCRP抑制生物标志物的实用性.
为了验证先前的有限研究中的发现,使用一种具有良好特征的BCRP抑制剂.

主要方法:

从临床药物相互作用研究中使用的样本,涉及BCRP抑制剂cedirogant.
测量了11名参与者在服用cedirogant (375毫克每天服用一次) 之前和之后的血里博夫拉水平.
通过测量罗斯瓦斯塔丁暴露和甲酸I水平的变化来评估cedirogant的BCRP抑制作用.

主要成果:

基剂的使用显著增加了罗斯瓦斯塔丁的暴露,证实了其作为临床BCRP抑制剂的作用.
血里博夫拉水平在24小时内表现出极小的个体内变化 (1-10 ng/mL).
与假设相反,cedirogant治疗没有导致血里博夫拉水平显著增加.

结论:

内源性血里博夫拉不是评估人类BCRP抑制的可行的生物标志物.
缺乏相关性表明,其他因素影响了与BCRP活性无关的血里博夫拉水平.

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