Introduction: Theranostic radiopharmaceuticals represent a significant advancement in personalized medicine, particularly in oncology. By integrating diagnostic imaging and targeted radionuclide therapy within a single molecular platform, these agents enable selective delivery of cytotoxic radiation to tumor cells. This integrated 'diagnose-then-treat' paradigm enables precise patient selection, individualized treatment planning, and response assessment.
Areas covered: A comprehensive literature search was performed using major biomedical databases, including PubMed, Scopus, and Web of Science. Clinical successes such as peptide receptor radionuclide therapy for neuroendocrine tumors (NETs), and Prostate-specific membrane antigen (PSMA)-targeted radioligand therapy (RLT) for metastatic castration-resistant prostate cancer underline the promise of radiotheranostics. Rapid innovation is driving personalized dosimetry from research into clinical practice, improving the balance between efficacy and toxicity. Furthermore, improved target selection using PET imaging is becoming essential for optimal patient selection and clinical trial design.
Expert opinion: Despite these advances, critical challenges persist, including toxicity management and heterogeneous target expression; additionally, radionuclide production, supply logistics, and cold-chain requirements remain significant barriers to widespread adoption; finally, standardization issues, harmonized imaging protocols, and clear response criteria further complicate patient selection. The field's advancement will rely on robust randomized clinical trials and innovative combination strategies to address tumor heterogeneity and resistance.
Keywords: Clinical challenges; Radiotheranostics; clinical perspectives; precision medicine; radiopharmaceutical; solid tumors.