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Peer-reviewedCC BY 4.0Frontiers in Oncology

Targeted radioligand therapy in oncology: clinical development across targets and platforms

  1. 1Rutgers Institute for Pharmaceutical Industry Fellowships, Ernest Mario School of Pharmacy, Rutgers University
  2. 2Department of Radiation Oncology, Rutgers Cancer Institute, Rutgers Robert Wood Johnson Medical School, Rutgers University

Abstract

Radioligand therapy (RLT) has gained increasing prominence as an important therapeutic modality in oncology. By coupling a tumor-targeting ligand with a therapeutic radionuclide, therapeutic targeted RLT enables selective radiation delivery to a malignant site. Clinical validation of prostate-specific membrane antigen (PSMA)- and somatostatin receptor (SSTR)-directed therapies, together with the regulatory approvals of lutetium Lu 177 dotatate and lutetium Lu 177 vipivotide tetraxetan, has established proof of clinical utility for this approach and driven a broader expansion of RLT development across oncology. In this review, we outline the major emitter classes for therapeutic RLT, provide an overview of the active clinical development landscape with emphasis on different targeting strategies, discuss the toxicity considerations relevant to this modality, and conclude with a perspective on the major challenges and future directions shaping the field.

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BibTeX
@article{an2026targeted,
  title = {{Targeted radioligand therapy in oncology: clinical development across targets and platforms}},
  author = {Jiaxin An and Xiaolei Meng and Lara Hathout and Ronald Ennis and Xinxin Zhang and Ning J. Yue and Matthew P. Deek and Salma K. Jabbour},
  journal = {Frontiers in Oncology},
  year = {2026},
  month = oct,
  doi = {10.3389/fonc.2026.1886049},
  url = {https://www.frontiersin.org/articles/10.3389/fonc.2026.1886049/full},
  note = {CC BY 4.0},
}
RIS
TY  - JOUR
TI  - Targeted radioligand therapy in oncology: clinical development across targets and platforms
AU  - Jiaxin An
AU  - Xiaolei Meng
AU  - Lara Hathout
AU  - Ronald Ennis
AU  - Xinxin Zhang
AU  - Ning J. Yue
AU  - Matthew P. Deek
AU  - Salma K. Jabbour
PY  - 2026
DA  - 2026/10/26
JO  - Frontiers in Oncology
DO  - 10.3389/fonc.2026.1886049
UR  - https://www.frontiersin.org/articles/10.3389/fonc.2026.1886049/full
AB  - Radioligand therapy (RLT) has gained increasing prominence as an important therapeutic modality in oncology. By coupling a tumor-targeting ligand with a therapeutic radionuclide, therapeutic targeted RLT enables selective radiation delivery to a malignant site. Clinical validation of prostate-specific membrane antigen (PSMA)- and somatostatin receptor (SSTR)-directed therapies, together with the regulatory approvals of lutetium Lu 177 dotatate and lutetium Lu 177 vipivotide tetraxetan, has established proof of clinical utility for this approach and driven a broader expansion of RLT development across oncology. In this review, we outline the major emitter classes for therapeutic RLT, provide an overview of the active clinical development landscape with emphasis on different targeting strategies, discuss the toxicity considerations relevant to this modality, and conclude with a perspective on the major challenges and future directions shaping the field.
SN  - 2234-943X
ER  -