首页> 美国卫生研究院文献>Clinical and Translational Science >An Investigation of the Metabolism and Excretion of KD101 and Its Interindividual Differences: A Microtracing Mass Balance Study in Humans
【2h】

An Investigation of the Metabolism and Excretion of KD101 and Its Interindividual Differences: A Microtracing Mass Balance Study in Humans

机译:KD101新陈代谢和排泄的调查及其间差异:人类的微量滑梯大规模平衡研究

代理获取
本网站仅为用户提供外文OA文献查询和代理获取服务,本网站没有原文。下单后我们将采用程序或人工为您竭诚获取高质量的原文,但由于OA文献来源多样且变更频繁,仍可能出现获取不到、文献不完整或与标题不符等情况,如果获取不到我们将提供退款服务。请知悉。

摘要

The absorption, metabolism, and excretion (AME) profiles of KD101, currently under clinical development to treat obesity, were assessed in humans using accelerator mass spectrometry (AMS) after a single oral administration of KD101 at 400 mg and a microdose of 14C‐KD101 at ~ 35.2 μg with a total radioactivity of 6.81 kBq. The mean total recovery of administered radioactivity was 85.2% with predominant excretion in the urine (78.0%). The radio‐chromatographic metabolite profiling showed that most of the total radioactivity in the plasma and the urine was ascribable to metabolites. The UDP‐glucuronosyltransferase (UGT), including UGT1A1, UGT1A3, and UGT2B7, might have contributed to the interindividual variability in the metabolism and excretion of KD101. The microtracing approach using AMS is a useful tool to evaluate the AME of a drug under development without risk for high radiation exposure to humans.
机译:KD101的吸收,新陈代谢和排泄和排泄(AME)曲线在临床开发下进行治疗肥胖症,在400mg的单一口服施用KD101和14C-KD101的微鼠里在〜35.2μg,总放射性为6.81 kbq。施用放射性的平均总回收率为85.2%,尿液中的主要排泄(78.0%)。无线电色谱代谢物分析显示,血浆中的大多数总放射性和尿液均可归c原代谢物。 UDP-葡萄糖醇糖基转移酶(UGT),包括UGT1A1,UGT1A3和UGT2B7可能有助于代谢和KD101排泄中的接触性变异性。使用AMS的微路径方法是一种有用的工具,可以在没有高辐射暴露于人类的情况下进行开发中的药物的AME。

著录项

相似文献

  • 外文文献
  • 中文文献
  • 专利
代理获取

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号