Targeted Radiopharmaceutical Therapies: Cutting-Edge Advances

Dear Colleagues,

The past decade has witnessed a paradigm shift in oncology with the emergence of targeted radiopharmaceutical therapies (TRT), also known as molecular radiotherapy or targeted radionuclide therapy. By delivering cytotoxic radiation directly to malignant tissues via molecularly targeted vectors, TRT offers a refined alternative to external beam radiotherapy and systemic chemotherapy. This approach enables selective tumor destruction while minimizing off-target effects and toxicities—aligning with the principles of precision medicine.

Therapeutic radioisotopes such as α-emitters (225Ac, 213Bi, 211At, 212Pb, 149Tb) and β-emitters (177Lu, 90Y, 131I, 67Cu, 161Tb) have demonstrated transformative potential in treating a range of solid tumors and hematologic malignancies. The clinical success of agents like [177Lu]Lu-DOTATATE for neuroendocrine tumors and [177Lu]Lu-PSMA-617 for metastatic prostate cancer has validated the theranostic model—where imaging-guided therapy enables patient selection, dosimetry optimization, and treatment response monitoring.

However, despite this rapid clinical progress, several scientific and translational challenges remain unresolved. These include isotope production scalability, logistical supply chain constraints, chelation chemistry stability, radiobiology of alpha emitters, dosimetry standardization, combination therapies, and clinical trial design for regulatory harmonization. Addressing these gaps is essential for expanding access and achieving broader therapeutic impact.

This Special Issue aims to bring together multidisciplinary expertise from radiochemistry, medical physics, radiobiology, oncology, nuclear medicine, and pharmaceutical sciences to highlight current advancements and emerging strategies in targeted radiopharmaceutical therapy. The focus will include innovations spanning molecular design, isotope production, radionuclide delivery technologies, preclinical evaluation, clinical translation, and regulatory considerations.

Aim and Scope

This Special Issue invites original research articles, reviews, and short communications on topics including but not limited to:

• Emerging therapeutic radioisotopes: production, purification, and supply chain strategies
• Chelation chemistry and bioconjugation for improved in vivo stability
• Alpha vs beta emitters: physical properties, radiobiology, and clinical rationale
• Novel targeting platforms (small molecules, peptides, antibodies, nanoparticles, engineered scaffolds)
• Theranostics and personalized dosimetry-guided therapy
• Mechanisms of radiation-induced DNA damage and bystander effects
• Radiopharmaceutical combinations with immunotherapy, chemotherapy, or radiosensitizers
• Translational case studies and first-in-human studies
• Toxicity management, organ protection, and safety strategies
• Regulatory, GMP manufacturing, and clinical trial frameworks
• Future directions in precision oncology and adaptive radiopharmaceutical therapy

Significance

This Special Issue will serve as a timely and authoritative platform to:

• Highlight state-of-the-art developments in TRT
• Explore innovations driving personalized oncology
• Facilitate knowledge exchange between academia, clinical centers, and industry
• Accelerate translational pathways and clinical adoption
• Promote international collaboration in radionuclide science and theranostic development

Dr. Noeen Malik
Guest Editor

Manuscript Submission Information

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• targeted radiopharmaceutical therapies (TRT)
• radiopharmaceuticals
• radionuclide therapy
• molecular radiotherapy
• radioisotopes
• radiochemistry
• isotope production
• radionuclide delivery
• preclinical evaluation
• clinical translation