一个第一阶段的,开放标签,质量平衡研究[14C]-伊伯多米德在健康受试者
Yiming Cheng1, Xiaomin Wang1, Liangang Liu2
1Clinical Pharmacology, Pharmacometrics, Disposition and Bioanalysis, Bristol Myers Squibb, Princeton, NJ, USA.
European journal of drug metabolism and pharmacokinetics
|March 24, 2024
概括
伊伯多米德是一种新型的大脑调节剂,在人类中经历生物转化,主要通过尿液和便作为不变药物和代谢物分泌. 这项研究描述了其代谢途径和分泌特征.
科学领域:
- 药理学 药理学是指药理学的学科.
- 药物代谢和药理动力学
- 临床药理学 临床药理学
背景情况:
- 伊伯多米德是一种新型脑细胞调节剂 (CELMoD®),正在临床开发中,用于血液恶性瘤.
- 进行了一项人体质量平衡研究,以描述 iberdomide (NCT03294603) 的生物转化和分泌途径.
研究的目的:
- 在健康人体中描述 iberdomide 的生物转化和分泌途径.
- 为了评估一次口服剂量放射性标记的伊伯多米德的质量平衡和药理动力学特征.
主要方法:
- 六名健康受试者接受了一次口服剂量1毫克的放射性标记的 [14C]-iberdomide.
- 收集了血液,尿液和便样本,以分析放射性,药理动力学和临床实验室评估.
主要成果:
- 单次口服剂量易贝尔多米德的耐受性良好.
- 放射性总回收率为88.5%,尿液为45.9%,便为42.6%.
- 伊伯多米德及其主要代谢物M12分别占循环放射性的约59%和14%. 大约27%以不变的伊伯多米德和62%的代谢产物形式分泌.
结论:
- 人类对伊伯多米德的生物转化涉及氧化和水解途径.
- 伊伯多米德是主要的循环成分,M12是主要的代谢物.
- 来自伊伯多米德的放射性物质在尿液和便中分泌的数量相似.
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