用于治疗目的的 Actinium-225 标记化合物和生物分子的最新进展综述,Chemical Biology & Drug Design

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用于治疗目的的 Actinium-225 标记化合物和生物分子的最新进展综述
Chemical Biology & Drug Design ( IF 3.2 ) Pub Date : 2023-09-15 , DOI: 10.1111/cbdd.14311
Maria Hassan ₁ , Tanveer Hussain Bokhari ₁ , Nadeem Ahmed Lodhi ₂ , Muhammad Kaleem Khosa ₁ , Muhammad Usman ₁

Affiliation

在核医学中，无法治愈或只能通过手术或化疗等传统技术部分治疗的癌症可以通过电离辐射作为一种治疗形式来杀死。Actinium-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，并且对于靶向 α 疗法 (TAT) 更有前景。Actinium-225 是肿瘤细胞治疗的最佳候选者，具有高 (LET) 线性能量转移（150 keV/μm）、半衰期（t _1/2 = 9.92d）和短射程（400– 100μm），防止正常健康组织受损。各种新型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进步。Ac-225 放射性药物不断证明其作为靶向 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-substance-P 已证实其在医学和临床领域的重要性，报告显着改善了反应分别用于前列腺癌、神经内分泌癌和神经胶质瘤患者。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 值和反应温度。对放射化学纯度 (RCP) 等质量控制 (QC) 测试技术标准化的需求日益增长。本综述旨在总结Ac-225标记化合物和生物分子的发展。还总结了他们报告的临床应用的现状。

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

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 (t_1/2 = 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.

更新日期：2023-09-15

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