Laboratoire Subatech, UMR 6457, Ecole des Mines de Nantes / Universite de Nantes / CNRS-IN2P3, 4 Rue A. Kastler, BP 20722, F-44307 Nantes Cedex 3, France.
Curr Top Med Chem. 2012;12(23):2642-54. doi: 10.2174/1568026611212230002.
Alpha-particles are of considerable growing interest for Targeted Alpha Therapy (TAT). TAT gains more attention as new targets, chemical labeling techniques and α-particle emitters are developed but translation of TAT into the clinic has been slow, in part because of the limited availability and the short physical half-lives of some of the available α-particle emitters. This article is an up-to-date overview of the literature concerning α-emitters used for TAT of cancer. It briefly describes the nuclear characteristics, the production parameters (targets, extraction and purification), the complexation properties of these radionuclides to chelates and biological vectors and finally draws-upon the preclinical and clinical studies that have been performed over the past two decades. Radiobiology and dosimetry aspects are also presented in this paper.
α-粒子在靶向α治疗(TAT)中引起了相当大的兴趣。随着新靶点、化学标记技术和α-粒子发射体的发展,TAT 受到了更多的关注,但 TAT 的临床转化进展缓慢,部分原因是一些可用的α-粒子发射体的供应有限和物理半衰期短。本文是一篇关于用于癌症 TAT 的α-发射体的文献综述。它简要描述了这些放射性核素的核特性、生产参数(靶标、提取和纯化)、与螯合物和生物载体的络合特性,最后总结了过去二十年进行的临床前和临床研究。本文还介绍了放射生物学和剂量学方面的内容。