Department of Chemical Sciences, University of Padova, 35131 Padova, Italy.
Department of Chemical Sciences, University of Padova, 35131 Padova, Italy.
Nucl Med Biol. 2022 Nov-Dec;114-115:168-188. doi: 10.1016/j.nucmedbio.2022.06.002. Epub 2022 Jun 17.
Current interest in the α-emitting bismuth radionuclides, bismuth-212 (Bi) and bismuth-213 (Bi), stems from their great potential for targeted alpha therapy (TAT), an expanding and promising approach for the treatment of micrometastatic disease and the eradication of single malignant cells. To selectively deliver their emission to the cancer cells, these radiometals must be firmly coordinated by a bifunctional chelator (BFC) attached to a tumour-seeking vector. This review provides a comprehensive overview of the current state-of-the-art chelating agents for bismuth radioisotopes. Several aspects are reported, from their 'cold' chelation chemistry (thermodynamic, kinetic, and structural properties) and radiolabelling investigations to the preclinical and clinical studies performed with a variety of bioconjugates. The aim of this review is to provide both a guide for the rational design of novel optimal platforms for the chelation of these attractive α-emitters and emphasize the prospects of the most encouraging chelating agents proposed so far.
目前，人们对发射 α 粒子的铋放射性核素铋-212（Bi）和铋-213（Bi）产生了浓厚的兴趣，这主要源于它们在靶向 α 治疗（TAT）方面的巨大潜力，TAT 是一种不断发展且有前途的治疗微转移疾病和消除单个恶性细胞的方法。为了将其发射选择性地递送到癌细胞，这些放射性金属必须通过与肿瘤靶向载体相连的双功能螯合剂（BFC）牢固地配位。本综述全面概述了当前用于铋放射性同位素的螯合剂。从“冷”螯合化学（热力学、动力学和结构特性）和放射性标记研究到各种生物缀合物的临床前和临床研究，报告了几个方面。本综述的目的是为合理设计新型最佳平台提供指导，以螯合这些有吸引力的α发射器，并强调迄今为止提出的最有前途的螯合剂的前景。
