核化学与放射化学2026，Vol.48Issue(3)：246-258,13.DOI:10.7538/hhx.2026.48.03.0246
212Pb放射性药物的研究现状及应用前景
Research Progress and Application Prospect of 212Pb Radiopharmaceuticals
摘要
Abstract
Due to the specific characteristics of high linear energy transfer(80-100 keV/μm),short penetration distance(40-100 μm),strong cytotoxic and few reverse effects,α radionuclides has a promising prospect for the therapy of micro-tumors,primary and micro-metastatic cancers.As the parent nuclide of the alpha-emitting radioisotope 212Bi,212Pb has been attracted much attention in the application of targeted alpha therapy.Compared with 225Ac,212Pb only involves one alpha decay.This ensures that therapeutic energy is delivered precisely and reduces the damage to the surrounding healthy tissues.In addition,Pb has a strong coordination ability and is more likely to combine with small molecule ligands to form stable targeted drugs.Thus,in recent years,researchers have prepared 212Pb radiopharmaceuticals by combining 212Pb with monoclonal antibodies,peptides,nanoparticles,etc.This paper summarizes the properties and preparation techniques of 212Pb nuclides,and the properties of chelators between 212Pb and targeted ligands.Three different ways of preparation technologies for separating and extracting of 212Pb are described:through 232Th or 232U,reactor irradiation of 226Ra.In contrast,there are some advantages to produce 212Pb by the third method.The extraction efficiency of 228Th can be increased and the loss of 226Ra is extremely low during the preparation process.Then,this article describes the 212Pb-complexes with DOTA,NOTA,TCMC,p-SCN-Bn-TCMC.The research progress and current clinical application of 212Pb radiopharmaceuticals,such as 212Pb-DOTAMTATE,212Pb-ADVC001,212Pb-DOTAM-GRPR1,212Pb-VMT-α-NET,are also discussed.In addition,203Pb,as an easily accessible diagnostic nuclide,can be used in combination to provide accurate data for the 212Pb treatment,which can further increase the application of 212Pb radiopharmaceuticals in the clinical.The rapid development of 212Pb radiopharmaceuticals has highlighted their potential as a form of radiotherapy and their remarkable effects in treating a variety of diseases.It is expected to be a support for providing references for the researches and applications in the treatment of malignant tumors in the future.Meanwhile,it should be noted that a large amount of research is still needed before it can be used for human treatment in the hospital,including production and transportation of 212Pb nuclides,the recoil phenomenon of decayed nuclides,the visual monitoring of drug distribution during treatment,the estimation of radiation doses,the assessment of toxicity,and the setting of standard doses,etc.Although large-scale clinical research is still needed,we should believe that 212Pb radiopharmaceuticals can play a significant role in the future with the continuous development of nuclear and medical technologies.关键词
212Pb/螯合剂/α放射性核素靶向治疗/癌症/制备技术Key words
212Pb/chelating agents/targeted alpha therapy/cancer/preparation techniques分类
医药卫生引用本文复制引用
李沁芝,李波,张劲松,陈云明,罗宁,胡映江,吴建荣..212Pb放射性药物的研究现状及应用前景[J].核化学与放射化学,2026,48(3):246-258,13.基金项目
中核集团稳定支持科研基金(WDZC-2023-GJZX-002) （WDZC-2023-GJZX-002）
