正电子核素~(89)Zr:药物化学及其生物体内行为评价的研究新进展

~(89)Zr是近年来刚刚兴起的正电子核素,其半衰期长(78.4h),特别适合标记抗体、纳米等具有较长生物半衰期的药物载体以及需长时间观测显像的载体。~(89)Zr生产成本低,体内稳定性较好,能滞留在肿瘤细胞中,更重要的是~(89)Zr在PET显像中分辨率高,因此~(89)Zr在PET显像领域具有广阔的应用前景。本文从~(89)Zr的生产和纯化、溶液配位化学以及与抗体的键连方法学等药物化学基本性质出发,再通过~(89)Zr的生物分布、临床前及临床应用等生物体内行为评价,较为全面地综述正电子核素~(89)Zr的最新研究进展。

Positron-Emitting Radionuclide 89Zr: Medicinal Chemistry and in Vivo Biological Behavior Evaluation

Positron-emitting radionuclide ⁸⁹Zr is just emerging in recent years. It has a half-life of 78.4 h, and is especially suitable for labelling antibodies, or nanoparticles, and other carriers of long time observation. ⁸⁹Zr is cheap to produce, stable in vivo, and residualizes in tumors, and importantly has high resolution of PET images, therefore it will have wide application prospect in the field of PET imaging. This paper provides a comprehensive research progress of ⁸⁹Zr medicinal chemistry and in vivo biological behavior evaluation, including the production and purification of ⁸⁹Zr, the solution coordination chemistry of ⁸⁹Zr, new bioconjugation strategies, the preclinical imaging studies of ⁸⁹Zr based agents, and the clinical applications of ⁸⁹Zr labeled radiopharmaceuticals.