Hartinger Christian G, Jakupec Michael A, Zorbas-Seifried Stefanie, Groessl Michael, Egger Alexander, Berger Walter, Zorbas Haralabos, Dyson Paul J, Keppler Bernhard K
University of Vienna, Institute of Inorganic Chemistry, Waehringer Strasse 42, A-1090 Vienna, (phone: +43-1-4277-52600; fax: +43-1-4277-52680).
Institut des Sciences et Ingénierie Chimiques, Ecole Polytechnique Fédérale de Lausanne (EPFL), CH-1015 Lausanne.
Chem Biodivers. 2008 Oct;5(10):2140-2155. doi: 10.1002/cbdv.200890195.
The promising drug candidate indazolium trans-[tetrachlorobis(1H-indazole)ruthenate(III)] (KP1019) is the second Ru-based anticancer agent to enter clinical trials. In this review, which is an update of a paper from 2006 (Hartinger et al., J. Inorg. Biochem. 2006, 100, 891-904), the experimental evidence for the proposed mode of action of this coordination compound is discussed, including transport into the cell via the transferrin cycle and activation by reduction. The results of the early clinical development of KP1019 are summarized in which five out of six evaluated patients experienced disease stabilization with no severe side effects.
有前景的候选药物吲唑鎓反式-四氯双(1H-吲唑)钌(III)是第二种进入临床试验的钌基抗癌药物。本综述是2006年一篇论文(Hartinger等人，《无机生物化学杂志》2006年，100，891 - 904)的更新版，讨论了这种配位化合物作用模式的实验证据，包括通过转铁蛋白循环进入细胞以及通过还原激活。总结了KP1019早期临床开发的结果，其中六名评估患者中有五名病情稳定，且无严重副作用。
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