1
基本信息
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题目:
Elevating theranostics: The emergence and promise of radiopharmaceutical cell-targeting heterodimers in human cancers
作者及单位：
Claudia Chambers1,2,3, Broc Chitwood1, Charles J. Smith1,2,4,5*, Yubin Miao6*
1
Molecular Imaging and Theranostics Center, Columbia, Missouri, USA
2
Research Division, Harry S. Truman Memorial Veterans' Hospital, Columbia, Missouri, USA
3
Department of Chemistry, University of Missouri, Columbia, Missouri, USA
4
Department of Radiology, University of Missouri School of Medicine, Columbia, Missouri, USA
5
University of Missouri Research Reactor Center, University of Missouri, Columbia, Missouri, USA
6
Department of Radiology, University of Colorado Denver, Aurora, Colorado, USA
引用格式：
Chambers C, Chitwood B, Smith CJ, Miao Y. Elevating theranostics: the emergence and promise of radiopharmaceutical cell-targeting heterodimers in human cancers. iRADIOLOGY. 2024; 2(2): 128–55. https://doi.org/10.1002/ird3.62
原文链接：
https://onlinelibrary.wiley.com/doi/10.1002/ird3.62
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2
主要内容
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Optimal therapeutic and diagnostic efficacy is essential for healthcare's global mission of advancing oncologic drug development. Accurate diagnosis and detection are crucial prerequisites for effective risk stratification and personalized patient care in clinical oncology. A paradigm shift is emerging with the promise of multi-targeting compounds. While existing detection and staging methods have demonstrated some success, the traditional approach of monotherapy is being reevaluated to enhance therapeutic effectiveness. Heterodimeric site-specific agents are a versatile solution by targeting two distinct biomarkers with a single theranostic agent. This review describes the innovation of dual-targeting compounds, examining their design strategies, therapeutic implications, and the promising path they present for addressing complex diseases.
CONCLUSION：
The field of personalized nuclear medicine is currently undergoing a transformative shift due to the introduction of multimeric peptide-based radiopharmaceuticals. Although considerable progress has been achieved in recent years by conventional techniques involving monovalent bioactive peptides, nanoparticles, or antibodies, researchers are increasingly embracing a heterobivalent strategy to enhance the radiotracer's pharmacological properties and theranostic potential. As the scientific community shifts toward heterobivalent approaches, greater leaps will be made in new drug delivery systems in the fight against cancer. Advances in radiochemistry and chelation chemistry have further allowed precise tuning of these peptides for radiolabeling with various radionuclides, catering to a wide array of medical applications within nuclear oncology. As research continues to evolve, these insights pave the way for the continued development and implementation of innovative radiopharmaceuticals into the clinical arena.
While traditional monovalent approaches have continued commendable achievements, they lack the ability to face limitations with the intricate, heterogeneous nature of tumors. Not all cancers are the same and can vary in type and amount depending on the individual patient or the stage of cancer. The bivalent radiotracers described herein provide substantial evidence in displaying the advantages of amalgamating the dual receptor-targeting actions of emerging theranostic radiopharmaceuticals. While the synthesis of heterobivalent ligands is acknowledged for its complexity and time-consuming nature, streamlined methods of synthesis are ongoing expedite the difficult process. It is believed the potential benefits of these radiopharmaceuticals outweigh the inherent challenges associated with their synthesis. By utilizing a single agent to target multiple known biomarkers, the potential impact encompasses broader patient coverage, precise staging, customized treatment design, and the potential for improved patient outcomes and quality of life.
In conclusion, employing bivalency to engage multiple targets simultaneously holds the potential to surpass the capabilities of monovalent peptide-based radiopharmaceuticals. As the scientific community gradually embraces the usage for heterobivalent approaches, successful strategies to effectively combat cancer across diverse patient profiles and varying cancer stages will be developed. Harnessing the combined potential between multiple targeting strategies, these approaches could unlock new dimensions of accuracy, sensitivity, and specificity of disease.
期刊推荐
● iRADIOLOGY《融合影像学（英文）》(Online ISSN: 2834-2879，Print ISSN: 2834-2860)是中国生物物理学会分子影像学分会的官方出版物，由中国工程院院士于金明、中国科学院院士滕皋军、中国科学院田捷教授、北京医院陈敏教授担任期刊顾问，中国工程院院士董家鸿、贵州医科大学附属医院李海洋教授担任期刊名誉主编，中国科学院上海药物研究所分子影像中心程震教授担任主编，贵州医科大学附属医院左石教授担任共同主编，贵州医科大学附属医院高波教授担任执行主编，北京大学王凡教授等担任副主编。
● 本刊由清华大学、贵州医科大学附属医院共同主办，清华大学出版社和Wiley出版发行，是一本国际性同行评议和开放获取的多学科交叉融合的医学影像英文期刊。
● 该刊物主要关注功能和分子影像学及以影像学为基础的治疗学方面的基础、转化和临床研究进展，内容涵盖生物医学成像、新技术开发和应用、功能和分子成像以及人工智能等诸多领域。文章类型包括：社论、论著、综述、短篇报道、病例图片、指南和共识、评论。
● 本刊的创办发行，将为我国放射医学领域的科研工作者提供优秀的学术交流平台，有力推动我国放射医学事业发展。
● 本刊已被国际知名数据库DOAJ、CAS（美国化学文摘）收录。
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