Pharmacokinetics of icotinib，a novel anti-tumor agent，and its tissue distribution in preclinical species
文献类型：期刊论文
| 作者 | Zhang Yifan3 ; Guan Zhongmin1; Chen Xiaoyan3; Hu Yunyan2; Wang Yinxiang2; Zhong Dafang3
|
| 刊名 | Chinese Journal New Drugs
 |
| 出版日期 | 2014 |
| 卷号 | 23期号:2页码:235-240 |
| 关键词 | icotinib pharmacokinetics EGFR-TKIs |
| ISSN号 | 1003-3734 |
| 其他题名 | 抗肿瘤新药埃克替尼在动物体内的药动学和组织分布研究 |
| 文献子类 | Article |
| 英文摘要 | Objective；To evaluate the pharmacokinetics of icotinib and its tissue distribution in preclinical species. Methods：The pharmacokinetic profiles were characterized in single oral and intravenous doses to rats and dogs as suspension and solution formulations. Tissue distribution was assessed following a single oral dose in rats and the extent of protein binding was determined in rat and human plasma. Biological samples from the in vivo and in vitro studies were analyzed using HPLC-UV and LC/MS/MS methods for the quantification of icotinib. Results：Icotinib declined both in rat and dog systemic circulation，with a terminal t_(1/2) of 3.23 and 5.6h and a relatively low clearance of 8.95 and 9.57mL·min~(-1)·kg~(-1)，respectively. It showed an approximately linear pharmacokinetic profile over the tested dosage range following oral administration. The absolute oral bioavailability of icotinib given as suspension was 51.3% in rats and 27.4% in dogs，respectively，and that given as solution was 62.8% in dogs. The exposure of icotinib was 3 to 5-fold higher in female than in male rats，but no sex difference was found in dogs. Icotinib exhibited high plasma protein binding(>98%)which was concentration and species independent. Tissue distribution studies in rats showed that icotinib distributed to tissues rapidly and extensively. Stomach，intestine and liver showed higher exposure than plasma within 4h post dose. Conclusion：Icotinib exhibits good pharmacokinetic profile in preclinical species，which supports its development in human. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5047573 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/269352]  |
| 专题 | 上海药物代谢研究中心 |
| 通讯作者 | Zhang Yifan; Zhong Dafang |
| 作者单位 | 1.Shenyang Pharmaceutical University, Shenyang, Liaoning 110016, China.; 2.Zhejiang Beta Pharma Inc., Hangzhou, Zhejiang 311100, China. 3.Shanghai Institute of Materia Medica，Chinese Academy of Sciences, Shanghai 201203, China.; |
| 推荐引用方式 GB/T 7714 | Zhang Yifan,Guan Zhongmin,Chen Xiaoyan,等. Pharmacokinetics of icotinib，a novel anti-tumor agent，and its tissue distribution in preclinical species[J]. Chinese Journal New Drugs,2014,23(2):235-240. |
| APA | Zhang Yifan,Guan Zhongmin,Chen Xiaoyan,Hu Yunyan,Wang Yinxiang,&Zhong Dafang.(2014).Pharmacokinetics of icotinib，a novel anti-tumor agent，and its tissue distribution in preclinical species.Chinese Journal New Drugs,23(2),235-240. |
| MLA | Zhang Yifan,et al."Pharmacokinetics of icotinib，a novel anti-tumor agent，and its tissue distribution in preclinical species".Chinese Journal New Drugs 23.2(2014):235-240. |
入库方式： OAI收割
来源：上海药物研究所
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