Pharmacokinetics and tissue distribution in rats of a novel anticancer platinum compound LLC-1903
Pharmacokinetics and tissue distribution in rats of a novel anticancer platinum compound LLC-1903
复制标题
新型抗癌铂化合物LLC-1903在大鼠体内的药代动力学和组织分布
DOI：
10.1080/00498254.2020.1728421
复制
发表时间：
2020-02-18
期刊：
影响因子：
1.8
通讯作者：
Liu, Qingfei
中科院分区：
文献类型：
--
作者：
Li, Yingxue;Meng, Fanzhuo;Liu, Qingfei
Abstract LLC-1903, a novel anticancer compound, was synthesized by optimizing the structure, which was derived from altering the leaving group of lobaplatin. It has an excellent in vitro anti-cancer activity, high water solubility, high stability in solution and low in vivo toxicity according to our former study. The plasma pharmacokinetics (PK) and tissue distribution of LLC-1903 and lobaplatin in rats were determined after intravenous administration of a single dose (0.06 mmol/kg body weight). Inductively coupled plasma mass spectrometry (ICP-MS) was used to measure the concentration of platinum (Pt) in plasma and tissue samples. Most PK parameters of the Pt in LLC-1903 showed a significant difference from those of lobaplatin. The plasma level of LLC-1903 is only half of that of lobaplatin (p < 0.01) which could be the direct result of faster drug clearance. The tissue distribution showed that both LLC-1903 and lobaplatin were mainly found in the liver and kidney, and less in other organs. At four time points (0.083, 0.5, 1 and 4 h) after administration, the tissue concentrations of LLC-1903 were almost always significantly higher than those of lobaplatin (p < 0.05 or p < 0.01).
