Gallium‐Containing Agents for Tumor Diagnosis and Therapy: Current Status and Future Prospects

ABSTRACT Ga‐containing agents show great promise in tumor theranostics due to their unique physicochemical and biological features. Recent studies have extensively explored Ga‐containing radiopharmaceuticals, therapeutic compounds, and multifunctional formulations, clarifying their interactions with the tumor microenvironment and antitumor mechanisms. Clinically, Ga imaging agents, especially 68 Ga‐labeled probes, have become standard tools for precise diagnosis of prostate cancer, neuroendocrine tumors, and other malignancies, while Ga therapeutic agents act by interfering with DNA metabolism, regulating tumor immunity, and inhibiting angiogenesis. This review summarizes the current research status of Ga‐containing agents in tumor diagnosis and therapy, covering imaging/therapeutic mechanisms and clinical applications, and clarifies their advantages and limitations. To promote their clinical translation, future efforts should focus on AI‐assisted multimodal imaging, personalized theranostics, intelligent targeted delivery systems and standardized multicenter clinical promotion.