靶向PSMA放射性小分子药物研究进展

Research Progress of PSMA-Targeted Small Molecule Drugs

前列腺癌(PCa)是男性死亡的常见诱因,严重危害着人们的生命健康。随着靶向前列腺特异性膜抗原(PSMA)的放射性药物在PET/CT和SPECT/CT中的应用,前列腺癌诊断的灵敏度与精确度得到了有效提高。本文首先对靶向PSMA小分子药物的核心结构单元进行介绍,然后重点介绍基于脲基发展而来的靶向PSMA放射性药物(放射性核素包括:^(68)Ga、^(18)F、^(11)C、^(99m)Tc、^(64)Cu、^(123)I、^(125)I、^(131)I、^(177)Lu、^(225)Ac、^(213)Bi和^(212)Pb等),以及在前列腺癌中的诊断与治疗研究进展,最后对该研究领域进行总结与展望。

Prostate cancer(PCa)is one of the most common reasons for male death,seriously endangering human life and health.With the application of prostate specific membrane antigen PSMA-targeted radiopharmaceuticals in PET/CT and SPECT/CT,the sensitivity and accuracy of diagnosis have been efficiently improved.In this paper,we firstly introduce the core structures of PSMA-targeted small molecule drugs.Then urea-based PSMA-targeted radiopharmaceuticals(radionuclides include ^(68)Ga,^(18)F,^(11)C,^(99m)Tc,^(64)Cu,^(123)I,^(125)I,^(131)I,^(177)Lu,^(225)Ac,^(213)Bi,^(212)Pb,etc.)and recent progress in diagnosis and therapy are highlighted.Finally,this research field is summarized and prospected.