Strategies for Innovative Development of Tumor-targeted Theranostic Radiopharmaceuticals

Radiopharmaceutical is an essential component of nuclear medicine and have demonstrated significant potential in disease diagnosis and treatment. In recent years, several tumor-targeted theranostic radiopharmaceuticals have been approved for market launch, ushering in a new era of targeted radionucl...

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Main Author: HUANG Xuhu1, 2, 3, CHEN Huan1, 2, 3, LI Kexin1, 2, 3, WANG Ning1, 2, 3, ZHUANG Jin1, 2, 3, LI Hongyu1, 2, 3, DU Jin2, 3, 4
Format: Article
Language:English
Published: Editorial Board of Atomic Energy Science and Technology 2025-04-01
Series:Yuanzineng kexue jishu
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Online Access:https://yznkxjs.xml-journal.net/article/doi/10.7538/yzk.2025.youxian.0191
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author HUANG Xuhu1, 2, 3, CHEN Huan1, 2, 3, LI Kexin1, 2, 3, WANG Ning1, 2, 3, ZHUANG Jin1, 2, 3, LI Hongyu1, 2, 3, DU Jin2, 3, 4
author_facet HUANG Xuhu1, 2, 3, CHEN Huan1, 2, 3, LI Kexin1, 2, 3, WANG Ning1, 2, 3, ZHUANG Jin1, 2, 3, LI Hongyu1, 2, 3, DU Jin2, 3, 4
author_sort HUANG Xuhu1, 2, 3, CHEN Huan1, 2, 3, LI Kexin1, 2, 3, WANG Ning1, 2, 3, ZHUANG Jin1, 2, 3, LI Hongyu1, 2, 3, DU Jin2, 3, 4
collection DOAJ
description Radiopharmaceutical is an essential component of nuclear medicine and have demonstrated significant potential in disease diagnosis and treatment. In recent years, several tumor-targeted theranostic radiopharmaceuticals have been approved for market launch, ushering in a new era of targeted radionuclide therapy and theranostics. The global radiopharmaceutical industry is experiencing vigorous growth, and the research and development of tumor-targeted radiopharmaceuticals in China is transitioning from generic drugs to innovative drugs. The innovation of tumor-targeted radiopharmaceuticals is a complex systematic engineering task which requires comprehensive consideration and synergistic optimization of multiple aspects, including target, radionuclide, chelator, linker, and targeting ligand. In this paper, the above five aspects were reviewed to provide insights for the innovative development of radiopharmaceuticals. First, the strategies for selecting target and radionuclide were summarized and the development strategies of chelator for novel radionuclides were analyzed. Subsequently, taking PSMA-targeted radiopharmaceuticals based on small molecules as examples, the development strategies for targeting ligand and linker were discussed. Additionally, the emerging novel technologies and strategies for the development of theranostic radiopharmaceuticals, including radiohybrid strategies, dual-target strategies and covalent strategies were described. Finally, the challenges faced by the innovative development of tumor targeted radiopharmaceuticals were summarized and analyzed, and the future direction was prospected, with the hope of providing reference for the innovative development of radiopharmaceuticals in China.
format Article
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institution Kabale University
issn 1000-6931
language English
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publisher Editorial Board of Atomic Energy Science and Technology
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series Yuanzineng kexue jishu
spelling doaj-art-6d9ec484e0804a88b6819b5fefcb41232025-08-20T03:52:32ZengEditorial Board of Atomic Energy Science and TechnologyYuanzineng kexue jishu1000-69312025-04-0159476978210.7538/yzk.2025.youxian.0191Strategies for Innovative Development of Tumor-targeted Theranostic RadiopharmaceuticalsHUANG Xuhu1, 2, 3, CHEN Huan1, 2, 3, LI Kexin1, 2, 3, WANG Ning1, 2, 3, ZHUANG Jin1, 2, 3, LI Hongyu1, 2, 3, DU Jin2, 3, 401. HTA Co., Ltd., Beijing 102413, China 2. CAEA Center of Excellence on Nuclear Technology Applications for Engineering and Industrialization of Radiopharmaceuticals, Beijing 102413, China 3. CNNC Engineering Research Center of Radiopharmaceuticals, Beijing 102413, China 4. China Isotope & Radiation Corporation, Beijing 100089, ChinaRadiopharmaceutical is an essential component of nuclear medicine and have demonstrated significant potential in disease diagnosis and treatment. In recent years, several tumor-targeted theranostic radiopharmaceuticals have been approved for market launch, ushering in a new era of targeted radionuclide therapy and theranostics. The global radiopharmaceutical industry is experiencing vigorous growth, and the research and development of tumor-targeted radiopharmaceuticals in China is transitioning from generic drugs to innovative drugs. The innovation of tumor-targeted radiopharmaceuticals is a complex systematic engineering task which requires comprehensive consideration and synergistic optimization of multiple aspects, including target, radionuclide, chelator, linker, and targeting ligand. In this paper, the above five aspects were reviewed to provide insights for the innovative development of radiopharmaceuticals. First, the strategies for selecting target and radionuclide were summarized and the development strategies of chelator for novel radionuclides were analyzed. Subsequently, taking PSMA-targeted radiopharmaceuticals based on small molecules as examples, the development strategies for targeting ligand and linker were discussed. Additionally, the emerging novel technologies and strategies for the development of theranostic radiopharmaceuticals, including radiohybrid strategies, dual-target strategies and covalent strategies were described. Finally, the challenges faced by the innovative development of tumor targeted radiopharmaceuticals were summarized and analyzed, and the future direction was prospected, with the hope of providing reference for the innovative development of radiopharmaceuticals in China.https://yznkxjs.xml-journal.net/article/doi/10.7538/yzk.2025.youxian.0191tumor-targetedtheranostic radiopharmaceuticalsinnovative strategies
spellingShingle HUANG Xuhu1, 2, 3, CHEN Huan1, 2, 3, LI Kexin1, 2, 3, WANG Ning1, 2, 3, ZHUANG Jin1, 2, 3, LI Hongyu1, 2, 3, DU Jin2, 3, 4
Strategies for Innovative Development of Tumor-targeted Theranostic Radiopharmaceuticals
Yuanzineng kexue jishu
tumor-targeted
theranostic radiopharmaceuticals
innovative strategies
title Strategies for Innovative Development of Tumor-targeted Theranostic Radiopharmaceuticals
title_full Strategies for Innovative Development of Tumor-targeted Theranostic Radiopharmaceuticals
title_fullStr Strategies for Innovative Development of Tumor-targeted Theranostic Radiopharmaceuticals
title_full_unstemmed Strategies for Innovative Development of Tumor-targeted Theranostic Radiopharmaceuticals
title_short Strategies for Innovative Development of Tumor-targeted Theranostic Radiopharmaceuticals
title_sort strategies for innovative development of tumor targeted theranostic radiopharmaceuticals
topic tumor-targeted
theranostic radiopharmaceuticals
innovative strategies
url https://yznkxjs.xml-journal.net/article/doi/10.7538/yzk.2025.youxian.0191
work_keys_str_mv AT huangxuhu123chenhuan123likexin123wangning123zhuangjin123lihongyu123dujin234 strategiesforinnovativedevelopmentoftumortargetedtheranosticradiopharmaceuticals