2. Academic Validation
  3. Radioligand Therapy in Cancer Management: A Global Perspective

Radioligand Therapy in Cancer Management: A Global Perspective

  • Cancers (Basel). 2025 Oct 23;17(21):3412. doi: 10.3390/cancers17213412.
Gaia Ninatti 1 2 3,  Sze Ting Lee 1 2 4 5,  Andrew M Scott 1 2 4 6
Affiliations

Affiliations

  • 1 Olivia Newton-John Cancer Research Institute, Heidelberg, Melbourne, VIC 3084, Australia.
  • 2 Department of Molecular Imaging and Therapy, Austin Health, Heidelberg, Melbourne, VIC 3084, Australia.
  • 3 School of Medicine and Surgery, University of Milano-Bicocca, 20900 Monza, Italy.
  • 4 School of Cancer Medicine, La Trobe University, Bundoora, Melbourne, VIC 3086, Australia.
  • 5 School of Health and Biomedicine, RMIT University, Melbourne, VIC 3000, Australia.
  • 6 Faculty of Medicine, University of Melbourne, Parkville, Melbourne, VIC 3052, Australia.
PMID: 41228206 DOI: 10.3390/cancers17213412
Abstract

Radioligand therapy (RLT) is a targeted treatment modality that combines a tumour-specific ligand with a therapeutic radionuclide. Once administered, the radiopharmaceutical binds selectively to cancer-associated targets, delivering cytotoxic radiation directly to tumour cells while sparing surrounding tissues. Two RLT agents, [177Lu]Lu-DOTA-TATE (Lutathera®) and [177Lu]Lu-PSMA-617 (Pluvicto®), have received regulatory approval for the treatment of advanced gastroenteropancreatic neuroendocrine tumours and metastatic castration-resistant prostate Cancer, respectively. As of July 2025, more than 400 clinical trials are registered, exploring novel molecular targets such as FAP, CAIX, and GRPR, as well as alternative radionuclides and combination regimens in both solid and haematologic malignancies. In this review, we describe the design principles and mechanisms of action of RLT, summarise clinical evidence for approved and emerging radiopharmaceuticals, and discuss current global disparities in access and availability. Finally, we outline the main clinical challenges, including fixed dosing regimens, resistance, toxicity, and variability in patient selection and response assessment. Continued research to optimise radiopharmaceutical design, together with investment in infrastructure, workforce capacity, and international collaboration, will be essential to expand access and realise the full potential of RLT as a leading treatment strategy in modern oncology.

Keywords

[177Lu]Lu-DOTA-TATE; [177Lu]Lu-PSMA-617; neuroendocrine tumours; prostate cancer; radioligand therapy; theranostics.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-W1126504
    99.91%, DLL3 Ligand