Dual-Labeled Small Peptides in Cancer Imaging and Fluorescence-Guided Surgery: Progress and Future Perspectives

Dual-labeled compounds that combine radiolabeling and fluorescence labeling represent a significant advancement in precision oncology. Their clinical implementation enhances patient care and outcomes by leveraging the high sensitivity of radioimaging for tumor detection and taking advantage of fluorescence-based optical visualization for surgical guidance. Non-invasive radioimaging facilitates immediate identification of both primary tumors and metastases, while fluorescence imaging assists in decision-making during surgery by offering a spatial distinction between malignant and non-malignant tissue. These advancements hold promise for enhancing patient outcomes and personalization of cancer treatment. The development of dual-labeled molecular probes targeting various cancer biomarkers is crucial in addressing the heterogeneity inherent in cancer pathology and recent studies had already demonstrated the impact of dual-labeled compounds in surgical decision-making (NCT03699332, NCT03407781). This review focuses on the development and application of small dual-labeled peptides in the imaging and treatment of various cancer types. It summarizes the biomarkers targeted to date, tracing their development from initial discovery to the latest advancements in peptidomimetics. Through comprehensive analysis of recent preclinical and clinical studies, the review demonstrates the potential of these dual-labeled peptides to improve tumor detection, localization, and resection. Additionally, it highlights the evolving landscape of dual-modality imaging, emphasizing its critical role in advancing personalized and effective cancer therapy. This synthesis of current research underscores the promise of dual-labeled peptides in enhancing diagnostic accuracy and therapeutic outcomes in oncology.