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Life sciences · Journal article
Holistic Integrative Oncology · November 4, 2026
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Abstract Target-specific radiopharmaceuticals utilize molecular targeting vectors to selectively localize cancer cells, thereby providing a personalized theranostic approach for cancer therapy by integrating matched diagnostic and therapeutic radionuclides. Consequently, theranostic radiopharmaceuticals constitute an essential framework for delivering precision medicine in nuclear oncology. The successful clinical application of FDA-approved therapeutic radiopharmaceuticals and their corresponding imaging probes provides a validated roadmap for the development of novel targeted radiotracers. Moreover, a substantial number of novel target-specific molecular probes are currently being evaluated in clinical trials. In targeted radionuclide therapy, beta-emitting radionuclides remain the most widely used agents in clinical practice, and several of them have demonstrated substantial therapeutic efficacy. However, alpha-emitting radionuclides possess a higher linear energy transfer, which leads to greater cytotoxic potency than beta particles. Therefore, targeted alpha therapy represents a cutting-edge paradigm in precision oncology, offering potent and highly selective radiopharmaceutical strategies. This review highlights the significant progress achieved in the development of targeted radiopharmaceuticals, such as agents targeting fibroblast activation protein and trophoblast cell surface antigen 2, from preclinical research to clinical translation. Despite persistent challenges such as target heterogeneity and potential toxicity, the future application of multi-omics-guided personalized design and novel radionuclides is expected to reshape the landscape of precision cancer therapy with targeted radiopharmaceuticals.