在核医学中，那些传统技术如手术或化疗无法治愈或只能部分治疗的癌症，通过离子辐射来实施治疗。钍-225是一种高度鼓舞人心的α放射性同位素，对靶向α疗法（TAT）更具前景。钍-225是治疗肿瘤细胞的最佳候选药物，具有高线性能量转移（150 keV/μm）、半衰期（t1/2 = 9.92天）和短程（400-100 μm）等物理特性，能够防止对正常健康组织的伤害。引入各种新的放射性药物和放射性同位素极大地推动了核医学的发展。钍-225放射性药物一直显示出它们作为靶向α治疗药物的潜力。通过引入[225 Ac]Ac-PSMA-617、[225 Ac]Ac-DOTATOC和[225 Ac]Ac-DOTA-substance-P，钍-225标记的放射性药物在前列腺癌、神经内分泌瘤和胶质瘤患者中报告了明显改善的治疗反应。这些放射性药物的发展需要适当的缓冲液、孵育时间、最佳pH值和反应温度。对于放射性纯度（RCP）等质量控制（QC）测试技术的标准化需求不断增长。本综述旨在总结钍-225标记化合物和生物分子的发展情况，并总结其报道的临床应用状况。© 2023 John Wiley & Sons Ltd.

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. 225 Ac-labeled radiopharmaceuticals have confirmed their importance in medical and clinical areas by introducing [225 Ac]Ac-PSMA-617, [225 Ac]Ac-DOTATOC, [225 Ac]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.© 2023 John Wiley & Sons Ltd.