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).

通过优化结构，合成了一种新型的抗癌化合物LLC-1903，该结构是通过改变洛铂的离去基团而得到的。根据我们以前的研究，它具有出色的体外抗癌活性，高水溶性，溶液稳定性高和体内毒性低。

在静脉内注射单剂量（0.06 mmol / kg体重）后，确定LLC-1903和洛巴铂在大鼠中的血浆药代动力学（PK）和组织分布。电感耦合等离子体质谱法（ICP-MS）用于测量血浆和组织样品中的铂（Pt）浓度。

LLC-1903中Pt的大多数PK参数显示出与洛巴铂的显着差异。LLC-1903的血浆水平仅为洛巴铂的血浆水平的一半（p  <0.01），这可能是药物清除速度更快的直接结果。组织分布表明，LLC-1903和洛巴铂均主要存在于肝和肾中，其他器官中较少。给药后四个时间点（0.083、0.5、1和4小时），LLC-1903的组织浓度几乎总是显着高于洛巴铂的组织浓度（p  <0.05或p  <0.01）。