PDF(Pubmed)
Abstract：
Targeted alpha particle therapy (TAT) has emerged as a promising strategy for the treatment of prostate cancer (PCa). Actinium-225 (225Ac), a potent alpha-emitting radionuclide, may be incorporated into targeting vectors, causing robust and in some cases sustained antitumor responses. The development of radiolabeling techniques involving EDTA, DOTA, DOTPA, and Macropa chelators has laid the groundwork for advancements in this field. At the forefront of clinical trials with 225Ac in PCa are PSMA-targeted TAT agents, notably [225Ac]Ac-PSMA-617, [225Ac]Ac-PSMA-I&T and [225Ac]Ac-J591. Ongoing investigations spotlight [225Ac]Ac-hu11B6, [225Ac]Ac-YS5, and [225Ac]Ac-SibuDAB, targeting hK2, CD46, and PSMA, respectively. Despite these efforts, hurdles in 225Ac production, daughter redistribution, and a lack of suitable imaging techniques hinder the development of TAT. To address these challenges and additional advantages, researchers are exploring alpha-emitting isotopes including 227Th, 223Ra, 211At, 213Bi, 212Pb or 149Tb, providing viable alternatives for TAT.
摘要：
靶向α粒子疗法(TAT)已成为治疗前列腺癌(PCa)的有希望的策略。Actinium-225（225Ac），一种有效的发射α的放射性核素,可以整合到靶向载体中，引起强烈的，在某些情况下持续的抗肿瘤反应。涉及EDTA的放射性标记技术的发展，DOTA,DOTPA,Macropa螯合剂为这一领域的发展奠定了基础。在PCa中使用225Ac的临床试验的最前沿是PSMA靶向TAT药物，特别是[225Ac]Ac-PSMA-617、[225Ac]Ac-PSMA-I&T和[225Ac]Ac-J591。正在进行的调查聚焦[225Ac]Ac-hu11B6，[225Ac]Ac-YS5和[225Ac]Ac-SibuDAB，靶向hK2、CD46和PSMA，分别。尽管做出了这些努力,225Ac生产的障碍，女儿再分配,缺乏合适的成像技术阻碍了TAT的发展。为了应对这些挑战和其他优势，研究人员正在探索包括227Th在内的α发射同位素，223Ra,211At,213Bi,212Pb或149Tb，为TAT提供可行的替代方案。
