The use of radiopharmaceuticals in targeted cancer therapy: a narrative review

Abstract

Radiopharmaceutical therapy (RPT) is an advanced targeted cancer treatment that delivers radiation through specialized radiolabeled compounds to selectively destroy cancer cells while minimizing damage to healthy tissues. This theranostic approach integrates diagnosis and therapy, enhancing treatment precision and improving the therapeutic index compared to conventional chemotherapy. RPT agents consist of a radioactive isotope conjugated to a targeting molecule, enabling specific binding to cancer-associated antigens or receptors. Upon binding, these agents induce cell death through DNA damage caused by ionizing radiation. The choice of radionuclide, including beta and alpha emitters, plays a crucial role in determining therapeutic efficacy and potential side effects. This study aims to provide a comprehensive analysis of RPT, focusing on its mechanisms of action, clinical applications, and emerging challenges. We discuss the therapeutic potential of various radionuclides and highlight key clinical trials demonstrating efficacy across different malignancies. Additionally, we address critical issues such as optimizing delivery systems, managing radiotoxicity, and refining the dose-response relationship. Future directions include the development of novel radiopharmaceuticals and personalized treatment approaches. Further investigation is essential to overcome existing limitations and maximize the clinical benefits of RPT for patients with advanced cancers. Our findings contribute to a deeper understanding of RPT and offer insights into strategies for improving therapeutic outcomes and patient care.