From targeted delivery to precision strike: The next-generation innovative radiopharmaceuticals for cancer theranostics
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GRAPHICAL ABSTRACT
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PUBLIC SUMMARY
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Radiopharmaceuticals combine tumor-targeting molecules with radiation to image and treat cancer in one step.
The field is moving from β emitters to potent, precise α emitters.
Artificial intelligence (AI) and imaging analytics enable personalized, image-guided radiation dosing.
Wider access now hinges on secure isotope supply chains and coordinated regional production networks.
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ABSTRACT
This review provides a comprehensive analysis of the evolution of radiopharmaceuticals, tracing their development from fundamental physical chemistry to the global industrial chain. First, the article elucidates the central role of radionuclide decay physics in diagnostic and therapeutic applications, while discussing the decisive impact of coordination chemistry and chelator selection on in vivo stability. Regarding drug design, it analyzes the evolution of targeting vehicles from rapid diffusion small molecules to long-circulating monoclonal antibodies, and the optimization of pharmacokinetics via linkers that modulate polarity. The review further surveys a diverse target landscape, exploring the biological mechanisms of bystander and abscopal effects in overcoming tumor heterogeneity. It emphasizes the critical value of artificial intelligence (AI) and radiomics in achieving personalized biological effective dose predictions. Finally, the article dissects the clinical regulatory frameworks for radiation protection, analyses the challenges of the global nuclide supply chain, and gives a comparative perspective in regional ecosystems. -
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REFERENCES
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Zhao L., Li L., Zhang T., et al. (2026). From targeted delivery to precision strike: The next-generation innovative radiopharmaceuticals for cancer theranostics. The Innovation Drug Discovery 1:100030. https://doi.org/10.59717/j.xinn-drugdisc.2026.100030
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Zhao L., Li L., Zhang T., et al. (2026). From targeted delivery to precision strike: The next-generation innovative radiopharmaceuticals for cancer theranostics. The Innovation Drug Discovery 1:100030. https://doi.org/10.59717/j.xinn-drugdisc.2026.100030
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Content
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Figure 1.
The historical and projected evolution of nuclear medicine
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Figure 2.
A simplified schematic intended to illustrate the category and characterization of nuclides
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Figure 3.
The chelator evaluation and characterization
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Figure 4.
Schematic images of various vehicles
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Figure 5.
Linkers for radiopharmaceuticals
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Figure 6.
Chemical structures of representative target ligands. Created with ChemDraw
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Figure 7.
Representative targets for advanced radiopharmaceuticals and enhanced targeting mechanisms
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Figure 8.
Key mechanisms, therapeutic strategies, and the role of AI in targeted radionuclide therapy
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Figure 9.
The production, distribution, and challenges faced in the radiopharmaceutical industry
