Progress of 225Ac-Labelled Radiopharmaceuticals for Cancer Treatment
225Ac with the advantages of longer half-life(10 d),shorter range(＜100 μm)and high energy deposition(80-100 keV/pm)compared with other medical isotopes,is one of the most important alpha-emitting nuclides.The a particles emitted by 225 Ac can cause DNA double-strand breaks in tumor cells,which is more favourable in clinical application.This review delineates the decay characteristics and production methodologies of 225Ac,alongside detailing the conjugation of 225Ac with target-specific ligands through various chelation strat-egies.It encapsulates the advancements in research and clinical applications of 225 Ac-labeled compounds,including 225Ac-prostate-specific membrane antigen(PSMA)-617,225Ac-PSMA-I&T,225Ac-1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid(DOTA)-SP,and 225Ac-1,4,7,10-tetraazacyclododecane-N,N',N",N(")-tetraacetic acid d-phenylalanine1-tyrosine3-octreotide(DOTATE),in the therapeutic regimes for prostate cancer,gliomas,breast carcinoma,and pulmonary malignancies.The difficulties and challenges of 225Ac-labelled radiopharmaceutical are also forecasted,in order to provide reference for the research and application of 225Ac-labelled radiopharmaceuticals in the treatment of malignant tumors.
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