McDevitt M R, Sgouros G, Finn R D, Humm J L, Jurcic J G, Larson S M, Scheinberg D A
Memorial Sloan-Kettering Cancer Center, New York, NY 10021, USA.
Eur J Nucl Med. 1998 Sep;25(9):1341-51. doi: 10.1007/s002590050306.
This review discusses the application of alpha particle-emitting radionuclides in targeted radioimmunotherapy. It will outline the production and chemistry of astatine-211, bismuth-212, lead-212, actinium-225, bismuth-213, fermium-255, radium-223 and terbium-149, which at present are the most promising alpha-emitting isotopes available for human clinical use. The selective cytotoxicity offered by alpha particle-emitting radioimmunoconstructs is due to the high linear energy transfer and short particle path length of these radionuclides. Based upon the pharmacokinetics of alpha particle-emitting radioimmunoconstructs, both stochastic and conventional dosimetric methodology is discussed, as is the preclinical and initial clinical use of these radionuclides conjugated to monoclonal antibodies for the treatment of human neoplasia.
本综述讨论了发射α粒子的放射性核素在靶向放射免疫治疗中的应用。它将概述砹-211、铋-212、铅-212、锕-225、铋-213、镄-255、镭-223和铽-149的生产和化学性质，这些目前是最有前景的可用于人类临床的发射α粒子的同位素。发射α粒子的放射免疫构建体所提供的选择性细胞毒性归因于这些放射性核素的高线性能量传递和短粒子路径长度。基于发射α粒子的放射免疫构建体的药代动力学，讨论了随机和传统剂量学方法，以及这些与单克隆抗体偶联的放射性核素在治疗人类肿瘤方面的临床前和初始临床应用。
