Future of radiotheranostics

Radiotheranostics is reshaping precision oncology by integrating molecular imaging with targeted radionuclide therapy through matched diagnostic-therapeutic radiopharmaceutical pairs. Landmark clinical successes, including Lutetium-177-DOTATATE (¹⁷⁷Lu-DOTATATE) and ¹⁷⁷Lu-prostate-specific membrane antigen-617 (¹⁷⁷Lu-PSMA-617), have validated this approach and accelerated the shift from empiric dosing towards evidence-based practice supported by randomised trials. Beyond established somatostatin receptor and PSMA paradigms, emerging platforms targeting tumour-stroma and lineage-associated biology, such as fibroblast activation protein and other receptor systems, are broadening applications across diverse malignancies. In parallel, advances in radionuclide science, including next-generation β-emitters and targeted α-particle therapies, are enabling strategies with higher biological effectiveness and potential advantages in small-volume and micrometastatic disease. Innovations in ligand and vector engineering (including half-life extension and multivalent constructs) aim to improve tumour retention and therapeutic index. Finally, quantitative imaging, personalised dosimetry (from organ-based to voxel-level approaches) and artificial intelligence (AI)-enabled workflows are laying the foundation for scalable, individualised treatment planning and response assessment. This review synthesises key developments in molecular targeting, radiochemistry, dosimetry, AI and combination strategies, outlining the priorities required to translate next-generation radiotheranostics into durable, multidisciplinary cancer care.