Preclinical Evaluation of the α-Particle Generator Nuclide 225Ac for Somatostatin Receptor Radiotherapy of Neuroendocrine Tumors

Miederer, Matthias; Henriksen, Gjermund; Alke, Andrea; Moßbrugger, Ilona; Quintanilla-Martı́nez, Leticia; Senekowitsch–Schmidtke, Reingard; Essler, Markus

doi:10.1158/1078-0432.ccr-07-4647

Cited by 135 publications

(101 citation statements)

References 18 publications

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“…As a result, 213 Bi-DOTA-PESIN and 213 Bi-AMBA have ideal properties for targeted a-particle therapy. Previously published experience with receptor-targeted radiopeptide a-therapy is limited (39)(40)(41)(42). In this study, we present the preclinical evaluation of 2 peptides labeled with 213 Bi for future receptor-targeted radiopeptide therapy in prostate cancer patients.…”

Section: Discussionmentioning

confidence: 99%

Alpha- versus Beta-Particle Radiopeptide Therapy in a Human Prostate Cancer Model (213Bi-DOTA-PESIN and 213Bi-AMBA versus177Lu-DOTA-PESIN)

et al. 2011

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Recurrent prostate cancer presents a challenge to conventional treatment, particularly so to address micrometastatic and small-volume disease. Use of a-radionuclide therapy is considered as a highly effective treatment in such applications due to the shorter range and exquisite cytotoxicity of a-particles as compared with b-particles. 213 Bi is considered an a-emitter with high clinical potential, due to its short half-life (45.6 minutes) being well matched for use in peptide-receptor radionuclide a-therapy; however, there is limited knowledge available within this context of use. In this study, two novel 213 Bi-labeled peptides, DOTA-PEG 4 -

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Section: Discussionmentioning

confidence: 99%

Alpha- versus Beta-Particle Radiopeptide Therapy in a Human Prostate Cancer Model (213Bi-DOTA-PESIN and 213Bi-AMBA versus177Lu-DOTA-PESIN)

et al. 2011

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“…A number of studies have been conducted in preclinical models providing evidence that conjugates of such radionuclides with antibodies or peptides are effective in treatment of tumour xenografts of prostate [1,2], ovarian [3,4], breast [5][6][7], bladder [8], colon [9] and gastric [10,11] cancer, as well as in lymphoma [12,13] and somatostatin receptor-positive pancreatic tumours [14,15]. Other possible future applications of α-emitter conjugates include killing of tumour neovasculature [16] and nonmyeloablative conditioning for haematopoietic stem cell transplantation [17].…”

Section: Introductionmentioning

confidence: 99%

Therapeutic efficacy and toxicity of 225Ac-labelled vs. 213Bi-labelled tumour-homing peptides in a preclinical mouse model of peritoneal carcinomatosis

Essler

Gärtner

Neff

et al. 2012

Eur J Nucl Med Mol Imaging

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“…Therapy has been suggested/performed in animals and patients using SS analogues labelled with various radionuclides, e.g. the Auger and conversion electron emitters 111 In and 103m Rh (low electron energy) [46,72], the β-emitters 177 Lu, 153 Sm, and 161 Tb (medium electron energy) [23,24,26,42,44,51,73,74,75] and 90 Y, and 188 Re (high electron energy) [76,77,78] and the α-particle emitters 225 Ac, 211 At and 213 Bi [66,67,68,79]. For radionuclides with a higher electron energy and thus longer range, the absorbed fraction/dose in small tumours will be lower than in larger tumours and tissue surrounding the tumours will be more highly exposed.…”

Section: General Methods Including Individualizationmentioning

confidence: 99%

Radionuclide Therapy via SSTR: Future Aspects from Experimental Animal Studies

Forssell-Aronsson¹,

Spetz²,

Ahlman

2012

Neuroendocrinology

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There is need for better therapeutic options for neuroendocrine tumours. The aim of this review was to summarize results of experimental animal studies and raise ideas for future radionuclide therapy based on high expression of somatostatin (SS) receptors by many neuroendocrine tumours. In summary, one of the major options is individualized treatment for each patient, including choice of SS analogues, radionuclides and treatment schedules. Other options are methods to increase the treatment effect on tumour tissue (increasing tumour uptake and retention by upregulation of receptor expression and avoiding saturation of receptor binding), methods to increase the tumour tissue response (by choice of radionuclides, SS analogues or combined therapies), and methods to reduce side effects (diminished uptake and retention in critical organs and reduced normal tissue response). Furthermore, combination therapy with other radiopharmaceuticals, cytotoxic drugs or radiosensitizers can be considered to enhance the effects of radiolabelled SS analogues.

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Preclinical Evaluation of the α-Particle Generator Nuclide 225Ac for Somatostatin Receptor Radiotherapy of Neuroendocrine Tumors

Cited by 135 publications

References 18 publications

Alpha- versus Beta-Particle Radiopeptide Therapy in a Human Prostate Cancer Model (213Bi-DOTA-PESIN and 213Bi-AMBA versus177Lu-DOTA-PESIN)

Alpha- versus Beta-Particle Radiopeptide Therapy in a Human Prostate Cancer Model (213Bi-DOTA-PESIN and 213Bi-AMBA versus177Lu-DOTA-PESIN)

Therapeutic efficacy and toxicity of 225Ac-labelled vs. 213Bi-labelled tumour-homing peptides in a preclinical mouse model of peritoneal carcinomatosis

Radionuclide Therapy via SSTR: Future Aspects from Experimental Animal Studies

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