Targeted Alpha-emitter Therapy of Neuroendocrine Tumors using 212Pb-octreotate (AlphaMedix TM)

Tworowska, Izabela; Bolek, Luke; Shanoon, Farah; Sgouros, George; Frey, Eric; He, Bin; Muzammil, Ali; Ghaly, Michael; Stallons, Tania A. Rozgaja; Saidi, Amal; Torgue, Julien

doi:10.1016/j.jmir.2019.03.104

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“…Esta terapia es particularmente promisoria en el tratamiento de los TNEs bien diferenciados. Otra estrategia en desarrollo es el uso de emisores alfa unidos a análogos de somatostatina (Pb 212 -Octreotate, actualmente en estudio) 40 .…”

Section: Radiofármacos (Prrt)unclassified

Tumores Neuroendocrinos: un desafío transversal

et al. 2021

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Section: Radiofármacos (Prrt)unclassified

Tumores Neuroendocrinos: un desafío transversal

et al. 2021

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Targeted α-therapy in non-prostate malignancies

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Colletti

2021

Eur J Nucl Med Mol Imaging

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Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

et al. 2020

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Identified in 1973, somatostatin (SST) is a cyclic hormone peptide with a short biological half-life. Somatostatin receptors (SSTRs) are widely expressed in the whole body, with five subtypes described. The interaction between SST and its receptors leads to the internalization of the ligand–receptor complex and triggers different cellular signaling pathways. Interestingly, the expression of SSTRs is significantly enhanced in many solid tumors, especially gastro-entero-pancreatic neuroendocrine tumors (GEP-NET). Thus, somatostatin analogs (SSAs) have been developed to improve the stability of the endogenous ligand and so extend its half-life. Radiolabeled analogs have been developed with several radioelements such as indium-111, technetium-99 m, and recently gallium-68, fluorine-18, and copper-64, to visualize the distribution of receptor overexpression in tumors. Internal metabolic radiotherapy is also used as a therapeutic strategy (e.g., using yttrium-90, lutetium-177, and actinium-225). With some radiopharmaceuticals now used in clinical practice, somatostatin analogs developed for imaging and therapy are an example of the concept of personalized medicine with a theranostic approach. Here, we review the development of these analogs, from the well-established and authorized ones to the most recently developed radiotracers, which have better pharmacokinetic properties and demonstrate increased efficacy and safety, as well as the search for new clinical indications.

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Targeted Alpha-emitter Therapy of Neuroendocrine Tumors using 212Pb-octreotate (AlphaMedix TM)

Cited by 3 publications

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Tumores Neuroendocrinos: un desafío transversal

Tumores Neuroendocrinos: un desafío transversal

Targeted α-therapy in non-prostate malignancies

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

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