Evaluation of the tissue distribution, excretion, and cytochrome P450 induction studies of a potential antitumor agent, TM-2, in animals using LC-MS/MS

排泄 药理学 体内 分布(数学) 药代动力学 细胞色素P450 脾脏 微粒体 毒性 化学 内科学 生物 内分泌学 新陈代谢 医学 生物化学 数学分析 生物技术 数学
作者
Lei Men,Yunli Zhao,Hongxin Lin,Xing Tang,Zhiguo Yu
出处
期刊:Xenobiotica [Taylor & Francis]
卷期号:47 (9): 800-806 被引量:2
标识
DOI:10.1080/00498254.2016.1232446
摘要

1. TM-2 is a promising novel semi-synthetic taxane derivative with greater antitumor activity especially against resistant tumors and lower toxicity compared with docetaxel. Information on distribution and excretion of the pharmaceutical in animals, as well as biochemical information relevant to potential drug interactions should normally be evaluated prior to human clinical trials. 2. The present study investigated the tissue distribution and excretion of TM-2 in animals following intravenous administration for further advancement of the molecule. The potential inductive effect of TM-2 on cytochrome P450 iso-enzymes CYP 3A1 in rats was also evaluated. 3. The tissue distribution study in mice showed that TM-2 was rapidly dispersed in the various tissues and peak concentration levels were achieved within 0.083-1 h. The highest concentration was detected in pancreas, followed by lung, kidney, spleen, heart and liver. TM-2 was mainly excreted in the feces via the bile (0.14% of the dose) and urinary excretion was minimal (0.007%). TM-2 increased CYP3A1 enzyme activities with time and dose dependence in rat liver microsome. 4. This important data serve as a useful resource to support further research of TM-2 and allow intelligent assessment of toxicology and in vivo activity testing performed in animals.
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