A review of recent advancements in Actinium-225 labeled compounds and biomolecules for therapeutic purposes

Maria Hassan, Tanveer Hussain Bokhari, Nadeem Ahmed Lodhi, Muhammad Kaleem Khosa, Muhammad Usman
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引用次数: 1

Abstract

In nuclear medicine, cancers that cannot be cured or can only be treated partially by traditional techniques like surgery or chemotherapy are killed by ionizing radiation as a form of therapeutic treatment. Actinium-225 is an alpha-emitting radionuclide that is highly encouraging as a therapeutic approach and more promising for targeted alpha therapy (TAT). Actinium-225 is the best candidate for tumor cells treatment and has physical characteristics such as high (LET) linear energy transfer (150 keV per μm), half-life (t1/2 = 9.92d), and short ranges (400–100 μm) which prevent the damage of normal healthy tissues. The introduction of various new radiopharmaceuticals and radioisotopes has significantly assisted the advancement of nuclear medicine. Ac-225 radiopharmaceuticals continuously demonstrate their potential as targeted alpha therapeutics. 225Ac-labeled radiopharmaceuticals have confirmed their importance in medical and clinical areas by introducing [225Ac]Ac-PSMA-617, [225Ac]Ac-DOTATOC, [225Ac]Ac-DOTA-substance-P, reported significantly improved response in patients with prostate cancer, neuroendocrine, and glioma, respectively. The development of these radiopharmaceuticals required a suitable buffer, incubation time, optimal pH, and reaction temperature. There is a growing need to standardize quality control (QC) testing techniques such as radiochemical purity (RCP). This review aims to summarize the development of the Ac-225 labeled compounds and biomolecules. The current state of their reported resulting clinical applications is also summarized as well.

Abstract Image

用于治疗目的的锕-225标记化合物和生物分子的最新进展综述。
在核医学中,不能治愈或只能通过手术或化疗等传统技术部分治疗的癌症,会被电离辐射作为一种治疗方法杀死。锕-225是一种发射α的放射性核素,作为一种治疗方法非常令人鼓舞,在靶向α治疗(TAT)方面更有前景。肌动蛋白-225是治疗肿瘤细胞的最佳候选者,具有高(LET)线性能量转移(150 keV/μm),半衰期(t1/2 = 9.92d)和短距离(400-100 μm),防止对正常健康组织的损伤。各种新的放射性药物和放射性同位素的引入极大地促进了核医学的发展。Ac-225放射性药物不断展示其作为靶向α疗法的潜力。225 Ac标记的放射性药物通过引入[225 Ac]Ac-PSMA-617、[225 Ac]Ac-DOTATOC、[225 Ac]Ac-DOTA-底物-P,证实了其在医学和临床领域的重要性,报告分别显著改善了前列腺癌症、神经内分泌和神经胶质瘤患者的反应。这些放射性药物的开发需要合适的缓冲液、孵育时间、最佳pH和反应温度。越来越需要标准化质量控制(QC)测试技术,如放射化学纯度(RCP)。本文综述了Ac-225标记化合物和生物分子的研究进展。还总结了其所报道的临床应用的现状。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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