Optimisation of radioligand therapy in neuroendocrine tumours: Current and evolving evidence

Gnanasegaran, Gopinath; Grossman, Ashley

doi:10.1111/jne.13208

Cited by 4 publications

(1 citation statement)

References 58 publications

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“…Hypoxia's impact is expected to be significantly reduced with high linear energy transfer (LET) due to the direct effect on the DNA. Furthermore, this is linked to the production of reactive oxygen species (ROS), leading to indirect toxic effects predominantly in non-hypoxic cells (Navalkissoor et al 2022 ; Jiao et al 2022 ). The advantages of using alpha-emitters after a limited effect with beta-emitters has been shown in several studies (Feuerecker et al 2021 ).…”

Section: Clinical Targeted Alpha Therapymentioning

confidence: 99%

Implementing Ac-225 labelled radiopharmaceuticals: practical considerations and (pre-)clinical perspectives

Hooijman,

Radchenko,

Ling

et al. 2024

EJNMMI radiopharm. chem.

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Background In the past years, there has been a notable increase in interest regarding targeted alpha therapy using Ac-225, driven by the observed promising clinical anti-tumor effects. As the production and technology has advanced, the availability of Ac-225 is expected to increase in the near future, making the treatment available to patients worldwide. Main body Ac-225 can be labelled to different biological vectors, whereby the success of developing a radiopharmaceutical depends heavily on the labelling conditions, purity of the radionuclide source, chelator, and type of quenchers used to avoid radiolysis. Multiple (methodological) challenges need to be overcome when working with Ac-225; as alpha-emission detection is time consuming and highly geometry dependent, a gamma co-emission is used, but has to be in equilibrium with the mother-nuclide. Because of the high impact of alpha emitters in vivo it is highly recommended to cross-calibrate the Ac-225 measurements for used quality control (QC) techniques (radio-TLC, HPLC, HP-Ge detector, and gamma counter). More strict health physics regulations apply, as Ac-225 has a high toxicity, thereby limiting practical handling and quantities used for QC analysis. Conclusion This overview focuses specifically on the practical and methodological challenges when working with Ac-225 labelled radiopharmaceuticals, and underlines the required infrastructure and (detection) methods for the (pre-)clinical application.

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Section: Clinical Targeted Alpha Therapymentioning

confidence: 99%

Implementing Ac-225 labelled radiopharmaceuticals: practical considerations and (pre-)clinical perspectives

Hooijman,

Radchenko,

Ling

et al. 2024

EJNMMI radiopharm. chem.

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Somatostatin receptor‐linked α‐particle therapy in neuroendocrine tumours

Navalkissoor,

Grossman

2024

J Neuroendocrinology

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The incidence and prevalence of neuroendocrine tumours (NETs) are on the rise, but to date, only complete surgical resection is curative. Among the various therapeutic options for metastatic disease, peptide receptor radionuclide therapy (PRRT), linking a radioactive moiety to an octreotide derivative, has been shown to be highly efficacious and a well‐tolerated therapy, improving progression‐free survival and prolonging overall survival. Nevertheless, complete responses are rare, and the current β‐particle emitters have non‐optimal radiobiological properties. A new generation of α‐particle‐emitting radionuclides is being developed, with the advantages of very high energy and a short path length. We survey the most recent developments in this field, summarising the result of currently performed studies in this potentially ground‐breaking novel form of therapy for NETs.

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Approach to the Patient: Concept and Application of Targeted Radiotherapy in the Paraganglioma Patient

Pacak,

Taieb,

Lin

et al. 2024

The Journal of Clinical Endocrinology &Amp; Metabolism

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Paragangliomas can metastasize, posing potential challenges in both symptomatic management and disease control. Systemic targeted radiotherapies using 131I-MIBG and 177Lu-DOTATATE are a mainstay in the treatment of metastatic paragangliomas. This clinical scenario and discussion aim to enhance physicians’ knowledge of the stepwise approach to treat these patients with paraganglioma targeted radiotherapies. It comprehensively discusses current approaches to selecting paraganglioma patients for targeted radiotherapies and how to choose between the two radiotherapies based on specific patient and tumor characteristics, when either therapy is feasible, or one is superior to another one. The safety, efficacy, toxicity profiles, and optimization of these radiotherapies are also discussed, along with other therapeutic options including radiotherapies, available for patients besides these two therapies. As conclusion, perspectives in radiotherapies of paraganglioma patients are outlined since they hold near future promising approaches that can improve patient outcomes.

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Optimisation of radioligand therapy in neuroendocrine tumours: Current and evolving evidence

Cited by 4 publications

References 58 publications

Implementing Ac-225 labelled radiopharmaceuticals: practical considerations and (pre-)clinical perspectives

Implementing Ac-225 labelled radiopharmaceuticals: practical considerations and (pre-)clinical perspectives

Somatostatin receptor‐linked α‐particle therapy in neuroendocrine tumours

Approach to the Patient: Concept and Application of Targeted Radiotherapy in the Paraganglioma Patient

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