Radioligand therapy is an innovative approach to treating certain types of cancer. It delivers radiation to cancer cells in a targeted and precise way, with a minimal effect on healthy cells,1 which allows for greater efficiency.

What are radioligands?

A radioligand is made of two parts: a ligand, which can find cancer cells that have a particular surface molecule, and a radioisotope, which emits therapeutic radiation to kill these cells. The radioligand can target cells anywhere in the body.

The radioligand can be customised for diagnostic (imaging) or therapeutic (treatment) purposes by changing the type of radioisotope. Combining the diagnostic and treatment processes is known as theranostics.1 2 Alternatively, changing the ligand can allow targeting of different types of cancer or even other diseases.

About radioligand therapy

Despite progress in many areas of cancer care, important gaps remain. Many people do not have effective treatment options, particularly for aggressive or rare forms of cancer.3 New strategies are needed to improve not just survival, but quality of life.4 One emerging type of treatment is radioligand therapy. It has been shown to improve overall survival and quality of life for many people with neuroendocrine cancers and metastatic castration-resistant prostate cancer that has spread to the bone.1 4-7 However, it has only recently been introduced into cancer care guidelines for these types of tumours.8-17 Radioligand therapy has potential to treat other aggressive or rare forms of cancer.3

Current use of radioligand therapy is variable. Integrating it into clinical practice requires new models of care and multidisciplinary coordination. Download the full report to learn more about radioligand therapy and the actions that may support its greater introduction into cancer care.

The evolution of radioligand therapy

Targeted radiation has existed for decades. Radioiodine was first used to treat overactive thyroid glands and subsequently thyroid cancer in the 1940s.18-21 Because the thyroid absorbs significantly more iodine than any other organ, radioiodine is taken directly to the thyroid and delivers radiation to kill cancerous cells. Radioiodine remains central to thyroid cancer treatment today.

This principle of targeted radiation has evolved from organ-level precision to cellular-level precision in line with scientific advances. Radioligands bind to certain types of cancer cells wherever they are located in the body, so they can be used for targeted diagnosis and treatment.

Exciting opportunities for cancer care

Cancer is currently the second highest cause of mortality and morbidity in Europe, and its burden is expected to continue rising. As our understanding of cancer’s complexity and diversity grows, it becomes increasingly clear that we must have a broad range of adaptable tools. Current cancer care often fails to meet the needs of people with rare cancers, or cancers that are resistant to treatments or have metastasised (spread to other parts of the body).

Radioligand therapy may help to address this gap and provide life-enhancing treatment for people with limited treatment options, playing an important role in realising the potential of personalised, targeted healthcare. However, its uptake across Europe is highly variable. Many people who might benefit from radioligand therapy are unable to access it or face restrictions to its appropriate use.

Optimal cancer care will look different for each individual, but personalisation and multidisciplinary working are essential. People with cancer benefit from a team of experts who can respond in a way that best meets their specific needs. The nature of radioligand therapy makes it highly adaptable, but also necessitates multidisciplinary working between oncologists, nuclear medicine specialists and others. Efforts to facilitate radioligand therapy therefore go hand in hand with wider efforts to improve access to multidisciplinary cancer care.

It is up to decision-makers to act now to ensure that every person with cancer receives appropriate and adaptable care as soon as they need it – including, where appropriate, radioligand therapy. Read our recommendations for better integrating radioligand therapy into cancer care at the link below.

About this project

This policy report has been drafted by The Health Policy Partnership, an independent research organisation, with input from a multi‑stakeholder steering committee. Its aim is to create greater awareness of radioligand therapy as an innovative component of cancer care. The steering committee had full editorial control over content, which reflects consensus among the group. All members provided their time for free. The outputs of this project are intended for educational purposes only and do not relate to any particular product.

This project was supported by a grant from Advanced Accelerator Applications, a Novartis company, with additional support from Curium.

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  2. Herrmann K, Larson SM, Weber WA. 2017. Theranostic Concepts: More Than Just a Fashion Trend-Introduction and Overview. J Nucl Med 58(Suppl 2): 1s-2s
  3. Rahbar K, Bode A, Weckesser M, et al. 2016. Radioligand Therapy With 177Lu-PSMA-617 as A Novel Therapeutic Option in Patients With Metastatic Castration Resistant Prostate Cancer. Clin Nucl Med 41(7): 522-8
  4. Khan S, Krenning EP, van Essen M, et al. 2011. Quality of life in 265 patients with gastroenteropancreatic or bronchial neuroendocrine tumors treated with [177Lu-DOTA0,Tyr3]octreotate. J Nucl Med 52(9): 1361-8
  5. Baum RP, Kulkarni HR, Singh A, et al. 2018. Results and adverse events of personalized peptide receptor radionuclide therapy with (90)Yttrium and (177)Lutetium in 1048 patients with neuroendocrine neoplasms. Oncotarget 9(24): 16932-50
  6. Hirmas N, Jadaan R, Al-Ibraheem A. 2018. Peptide Receptor Radionuclide Therapy and the Treatment of Gastroentero-pancreatic Neuroendocrine Tumors: Current Findings and Future Perspectives. Nucl Med Mol Imaging 52(3): 190-99
  7. Nilsson S. 2016. Radionuclide Therapies in Prostate Cancer: Integrating Radium-223 in the Treatment of Patients With Metastatic Castration-Resistant Prostate Cancer. Curr Oncol Rep 18(2): 14
  8. Falconi M, Eriksson B, Kaltsas G, et al. 2016. ENETS Consensus Guidelines Update for the Management of Patients with Functional Pancreatic Neuroendocrine Tumors and Non-Functional Pancreatic Neuroendocrine Tumors. Neuroendocrinology 103(2): 153-71
  9. Pavel M, O’Toole D, Costa F, et al. 2016. ENETS Consensus Guidelines Update for the Management of Distant Metastatic Disease of Intestinal, Pancreatic, Bronchial Neuroendocrine Neoplasms (NEN) and NEN of Unknown Primary Site. Neuroendocrinology 103(2): 172-85
  10. National Comprehensive Cancer Network. 2019. NCCN Clinical Practice Guidelines in Oncology: Neuroendocrine and Adrenal Tumors. Washington, DC: NCCN
  11. European Association of Urology. 2019. Prostate Cancer Oncology Guideline. Available from: [Accessed 08/10/19]
  12. National Institute for Health and Care Excellence. 2018. Lutetium (177Lu) oxodotreotide for treating unresectable or metastatic neuroendocrine tumours. [Updated 28/08/18]. Available from: [Accessed 6/12/19]
  13. Parker C, Gillessen S, Heidenreich A, et al. 2015. Cancer of the prostate: ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up. Ann Oncol 26(suppl_5): v69-v77
  14. Poeppel TD, Handkiewicz-Junak D, Andreeff M, et al. 2018. EANM guideline for radionuclide therapy with radium-223 of metastatic castration-resistant prostate cancer. Eur J Nucl Med Mol Imaging 45(5): 824-45
  15. Basch E, Loblaw DA, Oliver TK, et al. 2014. Systemic therapy in men with metastatic castration-resistant prostate cancer:American Society of Clinical Oncology and Cancer Care Ontario clinical practice guideline. J Clin Oncol 32(30): 3436-48
  16. National Comprehensive Cancer Network. 2019. NCCN CLinical Practice Guidelines in Oncology: Prostate Cancer. Washington, DC: NCCN
  17. National Institute for Health and Care Excellence. 2019. Prostate Cancer: diagnosis and management. [Updated 01/05/19]. Available from: [Accessed 03/10/19]
  18. Levine R, Krenning EP. 2017. Clinical history of the theranostic radionuclide approach to neuroendocrine tumors and other types of cancer: historical review based on an interview of Eric P. Krenning by Rachel Levine. J Nucl Med 58(Supplement 2): 3S-9S
  19. McCready VR. 2017. Radioiodine – the success story of Nuclear Medicine. Eur J Nucl Med Mol Imaging 44(2): 179-82
  20. Mitchell AL, Gandhi A, Scott-Coombes D, et al. 2016. Management of thyroid cancer: United Kingdom National Multidisciplinary Guidelines. J Laryngol Otol 130(S2): S150-S60
  21. Filetti S, Durante C, Hartl D, et al. 2019. Thyroid cancer: ESMO Clinical Practice Guidelines for diagnosis, treatment and follow-up. Ann Oncol: 10.1093/annonc/mdz400

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