From targeted delivery to precision strike: The next-generation innovative radiopharmaceuticals for cancer theranostics

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.