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Targeted radiopharmaceuticals have become a cornerstone of modern nuclear medicine, significantly enhancing both diagnostic and therapeutic capabilities. The development of novel radiopharmaceuticals, including theranostic agents, has opened up new frontiers in targeted medicine. With the rapid pace of research and the growing availability of these radiopharmaceuticals, nuclear medicine is emerging as a critical component of personalized medicine. This chapter provides an overview of the current trends, recent advances, and challenges in targeted radiopharmaceuticals covering radionuclide production and radiolabeling with target-specific ligands. It also discusses the established and investigational diagnostic radiopharmaceuticals that are changing the paradigm of the management of various diseases. Additionally, the chapter explores the potential of targeted radiopharmaceutical therapies as a promising approach for personalized, precise, and effective cancer treatment, while addressing the challenges these therapies face.

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