Recent advances in radionuclide drug conjugates (RDCs) for cancer theranostics: From targeted design to clinical translation

Bioorg Chem. 2025 Dec:167:109240. doi: 10.1016/j.bioorg.2025.109240.

Liu Xijing ¹, Binbin Cheng ²

Affiliations

1 School of Environmental Science and Engineering, Hubei Polytechnic University, Huangshi 435003, China.
2 Hubei Key Laboratory for Kidney Disease Pathogenesis and Intervention, Hubei Engineering Research Center for Immunotherapy Drug Studies on Renal Tumors, Hubei Polytechnic University, Huangshi, Hubei 435003, China; Central Laboratory, Wenzhou Medical University Lishui Hospital, Lishui People's Hospital, Lishui, Zhejiang 323000, China. Electronic address: [email protected].

PMID: 41240619 DOI: 10.1016/j.bioorg.2025.109240

Abstract

Conjugated drugs, such as antibody-drug conjugates (ADCs) and peptide drug conjugates (PDCs), which deliver therapeutic payloads via targeted moieties, have revolutionized Cancer therapy but face several limitations such as payload-related off-target toxicity. These risks are primarily attributed to the premature release of toxic payloads due to the instability of the conjugation structures. Radionuclide drug conjugates (RDCs) address these issues by covalently combining diagnostic/therapeutic radionuclides with tumor-targeting vectors rather than a toxic molecule, enabling precision theranostics. Their unique capacity to quantify target expression, monitor therapeutic response, and deliver localized radiation has established RDCs as a transformative paradigm for tumor staging, molecular classification, and treatment optimization in modern oncology. This review categorizes key RDC targets, analyzes the mechanisms involved, and discusses the challenges/future directions, providing a focused update on recent breakthroughs that differ from prior reviews.

Keywords

Precision medicine; Radionuclide drug conjugates; cancer therapy.

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