Nishikawa Makiya, Takakura Yoshinobu, Hashida Mitsuru
Department of Biopharmaceutics and Drug Metabolism, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.
Cancer Sci. 2008 May;99(5):856-62. doi: 10.1111/j.1349-7006.2008.00774.x. Epub 2008 Feb 19.
Cancer gene therapy, in which pharmacologically active compounds are administered to cancer patients in a genetic form, has been examined not only in animals but also in cancer patients. Viral vector-induced severe side effects in patients have greatly underscored the importance of non-viral gene transfer methods. Even though the importance of pharmacokinetics is undoubtedly understood in the development of anticancer therapies, its importance has been less well recognized in non-viral cancer gene therapy. When transgene products express their activity within transduced cells, such as herpes simplex virus type 1 thymidine kinase and short hairpin RNA, the pharmacokinetics of the vectors and the expression profiles of the transgenes will determine the efficacy of gene transfer. The percentage of cells transduced is highly important if few by-stander effects are expected. If transgene products are secreted from cells into the blood circulation, such as interferons and interleukins, the pharmacokinetics of transgenes becomes a matter of significant importance. Then, any approach to increasing the level and duration of transgene expression will increase the therapeutic effects of cancer gene therapy. Here we review the pharmacokinetics of both non-viral vectors and transgene products, and discuss what should be done to achieve safer and more effective non-viral cancer gene therapy.
癌症基因治疗是将具有药理活性的化合物以基因形式给予癌症患者,目前不仅在动物身上进行了研究,也在癌症患者身上进行了试验。病毒载体在患者身上引发的严重副作用极大地凸显了非病毒基因传递方法的重要性。尽管在抗癌治疗的发展过程中,药代动力学的重要性无疑已得到认可,但在非病毒癌症基因治疗中,其重要性尚未得到充分认识。当转基因产物在转导细胞内发挥活性时,如单纯疱疹病毒1型胸苷激酶和短发夹RNA,载体的药代动力学和转基因的表达谱将决定基因传递的效果。如果预期旁观者效应较少,转导细胞的百分比就非常重要。如果转基因产物从细胞分泌到血液循环中,如干扰素和白细胞介素,那么转基因的药代动力学就变得至关重要。因此,任何提高转基因表达水平和持续时间的方法都将增强癌症基因治疗的疗效。在此,我们综述非病毒载体和转基因产物的药代动力学,并讨论为实现更安全、更有效的非病毒癌症基因治疗应采取的措施。