Differences in Biodistribution Between 99mTc-Depreotide, 111In-DTPA-Octreotide, and 177Lu-DOTA-Tyr3-Octreotate in a Small Cell Lung Cancer Animal Model

Schmitt, Anneli; Bernhardt, Peter; Nilsson, Ola; Ahlman, Håkan; Kölby, Lars; Forssell-Aronsson, Eva

doi:10.1089/cbr.2005.20.231

Cited by 31 publications

(23 citation statements)

References 13 publications

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“…The tumor/normal-tissue activity concentration ratio was highest for blood (12)(13)(14)(15)(16)(17)(18)(19)(20)(21)(22)(23)(24)(25)(26), and muscle vs. all other tissues (Table II). The lowest tumor/normal-tissue value was Table I.…”

Section: Biodistribution Ofmentioning

confidence: 99%

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Biodistribution of 177Lu-octreotate and 111In-minigastrin in female nude mice transplanted with human medullary thyroid carcinoma GOT2

et al. 2011

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Abstract.To be able to evaluate new radiopharmaceuticals and optimize diagnostic and therapeutic procedures, relevant animal models are required. The aim of this study was to evaluate the medullary thyroid carcinoma GOT2 animal model by analyzing the biodistribution of 177 Lu-octreotate and 111 In-minigastrin (MG0). BALB/c nude mice, subcutaneously transplanted with GOT2, were intravenously injected with either 177 Lu-octreotate or 111 In-MG0, with or without excess of unlabeled human minigastrin simultaneously with 111 In-MG0. Animals were sacrificed 1-7 days after injection in the 177 Lu-octreotate study and 1 h after injection of 111 In-MG0. The activity concentrations in organs and tissues were determined and mean absorbed doses from 177 Lu were calculated. There was a specific tumor uptake of either 177 Lu-octreotate or 111 In-MG0. 177 Lu-octreotate samples showed high activity concentrations in tissues expressing somatostatin receptors (SSTR). For both radiopharmaceuticals the highest activity concentrations were found in the kidneys. Compared to results from similar studies in mice with another MTC cell line (TT) the biodistribution was favorable (higher tumor uptake) for the GOT2 model, while compared to other animal models expressing SSTR, the tumor uptake of 177 Lu-octreotate was modest. In conclusion, the GOT2 animal model is a valuable model for evaluation and optimization of diagnostic and therapeutic procedures using radiolabeled somatostatin, CCK2 and gastrin analogues prior to clinical studies.

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Section: Biodistribution Ofmentioning

confidence: 99%

“…Numerous studies on radiolabeled octreotide, or octreotate, have been made on nude mice xenografted with GOT1 (14)(15)(16)(17) or NCI-H69 (18)(19)(20)(21). Studies using radioiodinated meta-iodobenzylguanidine (MIBG) have been performed in vitro or on nude mice xenografted with BON tumors (22,23).…”

Section: Introductionmentioning

confidence: 99%

Biodistribution of 177Lu-octreotate and 111In-minigastrin in female nude mice transplanted with human medullary thyroid carcinoma GOT2

et al. 2011

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“…The affinity and internalization of a radiolabelled SS analogue depend on the entire molecule, including chelating agent and radionuclide. Animal studies demonstrated higher SSTR affinity of DOTATATE versus DOTATOC, resulting in higher tumour/normal tissue (T/NT) ratios and better therapeutic effects [24,50,51]. 177 Lu-DOTATATE had a higher tumour uptake in CA20948-bearing rats than 88 Y- and 111 In-labelled analogues [24].…”

Section: General Methods Including Individualizationmentioning

confidence: 99%

“…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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“…99m Tc]depreotide, 19,20 have been successfully developed and used in the clinic for somatostatin receptor imaging. In addition, several radiolabeled peptides, such as [ Tclabeled bombesin analogues for tumor imaging, 22 and [ 64 Cu]RGD for a V b 3 integrin imaging, 23 have shown promising results.…”

Section: Introductionmentioning

confidence: 99%

Development of radiolabeled peptides to target p185HER2/neu receptors of cancer

2006

Labelled Comp Radiopharmac

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Differences in Biodistribution Between ^99mTc-Depreotide, ¹¹¹In-DTPA-Octreotide, and ¹⁷⁷Lu-DOTA-Tyr³-Octreotate in a Small Cell Lung Cancer Animal Model

Cited by 31 publications

References 13 publications

Biodistribution of 177Lu-octreotate and 111In-minigastrin in female nude mice transplanted with human medullary thyroid carcinoma GOT2

Biodistribution of 177Lu-octreotate and 111In-minigastrin in female nude mice transplanted with human medullary thyroid carcinoma GOT2

Radionuclide Therapy via SSTR: Future Aspects from Experimental Animal Studies

Development of radiolabeled peptides to target p185HER2/neu receptors of cancer

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