A Comparison of High- Versus Low-Linear Energy Transfer Somatostatin Receptor Targeted Radionuclide Therapy In Vitro

2005 ◽  
Vol 20 (1) ◽  
pp. 52-57 ◽  
Author(s):  
Tapan Nayak ◽  
Jeffrey Norenberg ◽  
Tamara Anderson ◽  
Robert Atcher
Keyword(s):  
Energy Transfer ◽  
Linear Energy Transfer ◽  
Radionuclide Therapy ◽  
Somatostatin Receptor ◽  
Targeted Radionuclide Therapy

scholarly journals Multifunctional Cyanine-Based Theranostic Probe for Cancer Imaging and Therapy

2021 ◽  
Vol 22 (22) ◽  
pp. 12214
Author(s):  
Cheng-Liang Peng ◽  
Ying-Hsia Shih ◽  
Ping-Fang Chiang ◽  
Chun-Tang Chen ◽  
Ming-Cheng Chang
Keyword(s):  
Photothermal Therapy ◽  
Radionuclide Therapy ◽  
Nuclear Imaging ◽  
Biological Evaluation ◽  
Targeted Radionuclide Therapy ◽  
Nir Fluorescence ◽  
Tumor Accumulation ◽  
Selective Accumulation

Cancer is one of the leading causes of death in the world. A cancer-targeted multifunctional probe labeled with the radionuclide has been developed to provide multi-modalities for NIR fluorescence and nuclear imaging (PET, SPECT), for photothermal therapy (PTT), and targeted radionuclide therapy of cancer. In this study, synthesis, characterization, in vitro, and in vivo biological evaluation of the cyanine-based probe (DOTA-NIR790) were demonstrated. The use of cyanine dyes for the selective accumulation of cancer cells were used to achieve the characteristics of tumor markers. Therefore, all kinds of organ tumors can be targeted for diagnosis and treatment. The DOTA-NIR790 labeled with lutetium-111 could detect original or metastatic tumors by using SPECT imaging and quantify tumor accumulation. The β-emission of 177Lu-DOTA-NIR790 can be used for targeted radionuclide therapy of tumors. The DOTA-NIR790 enabled imaging by NIR fluorescence and by nuclear imaging (SPECT) to monitor in real-time the tumor accumulation and the situation of cancer therapy, and to guide the surgery or the photothermal therapy of the tumor. The radionuclide-labeled heptamethine cyanine based probe (DOTA-NIR790) offers multifunctional modalities for imaging and therapies of cancer.

scholarly journals Therapeutic Potential of 47Sc in Comparison to 177Lu and 90Y: Preclinical Investigations

Pharmaceutics ◽  
2019 ◽  
Vol 11 (8) ◽  
pp. 424 ◽  
Author(s):  
Klaudia Siwowska ◽  
Patrycja Guzik ◽  
Katharina A. Domnanich ◽  
Josep M. Monné Rodríguez ◽  
Peter Bernhardt ◽  
...  
Keyword(s):  
Radionuclide Therapy ◽  
Therapeutic Potential ◽  
Folate Receptor ◽  
Tumor Growth Inhibition ◽  
Therapeutic Effects ◽  
Targeted Radionuclide Therapy ◽  
Decay Properties ◽  
Therapeutic Properties ◽  
Folate Conjugate

Targeted radionuclide therapy with 177Lu- and 90Y-labeled radioconjugates is a clinically-established treatment modality for metastasized cancer. 47Sc is a therapeutic radionuclide that decays with a half-life of 3.35 days and emits medium-energy β−-particles. In this study, 47Sc was investigated, in combination with a DOTA-folate conjugate, and compared to the therapeutic properties of 177Lu-folate and 90Y-folate, respectively. In vitro, 47Sc-folate demonstrated effective reduction of folate receptor-positive ovarian tumor cell viability similar to 177Lu-folate, but 90Y-folate was more potent at equal activities due to the higher energy of emitted β−-particles. Comparable tumor growth inhibition was observed in mice that obtained the same estimated absorbed tumor dose (~21 Gy) when treated with 47Sc-folate (12.5 MBq), 177Lu-folate (10 MBq), and 90Y-folate (5 MBq), respectively. The treatment resulted in increased median survival of 39, 43, and 41 days, respectively, as compared to 26 days in untreated controls. There were no statistically significant differences among the therapeutic effects observed in treated groups. Histological assessment revealed no severe side effects two weeks after application of the radiofolates, even at double the activity used for therapy. Based on the decay properties and our results, 47Sc is likely to be comparable to 177Lu when employed for targeted radionuclide therapy. It may, therefore, have potential for clinical translation and be of particular interest in tandem with 44Sc or 43Sc as a diagnostic match, enabling the realization of radiotheragnostics in future.

scholarly journals [177Lu-DOTA0,Tyr3]octreotate for somatostatin receptor-targeted radionuclide therapy

2001 ◽  
Vol 92 (5) ◽  
pp. 628-633 ◽  
Author(s):  
Marion de Jong ◽  
Wout A.P. Breeman ◽  
Bert F. Bernard ◽  
Willem H. Bakker ◽  
Michael Schaar ◽  
...  
Keyword(s):  
Radionuclide Therapy ◽  
Somatostatin Receptor ◽  
Targeted Radionuclide Therapy

Somatostatin receptor-targeted radionuclide therapy of tumors: Preclinical and clinical findings

2002 ◽  
Vol 32 (2) ◽  
pp. 133-140 ◽  
Author(s):  
Marion de Jong ◽  
Roelf Valkema ◽  
Francois Jamar ◽  
Larry K. Kvols ◽  
Dik J. Kwekkeboom ◽  
...  
Keyword(s):  
Radionuclide Therapy ◽  
Somatostatin Receptor ◽  
Clinical Findings ◽  
Targeted Radionuclide Therapy

scholarly journals Somatostatin-receptor-targeted radionuclide therapy for progressive meningioma: benefit linked to68Ga-DOTATATE/-TOC uptake

2016 ◽  
pp. now060 ◽  
Author(s):  
Katharina Seystahl ◽  
Veit Stoecklein ◽  
Ulrich Schüller ◽  
Elisabeth Rushing ◽  
Guillaume Nicolas ◽  
...  
Keyword(s):  
Radionuclide Therapy ◽  
Somatostatin Receptor ◽  
Targeted Radionuclide Therapy

scholarly journals Targeted Radionuclide Therapy Using Auger Electron Emitters: The Quest for the Right Vector and the Right Radionuclide

Pharmaceutics ◽  
2021 ◽  
Vol 13 (7) ◽  
pp. 980
Author(s):  
Malick Bio Idrissou ◽  
Alexandre Pichard ◽  
Bryan Tee ◽  
Tibor Kibedi ◽  
Sophie Poty ◽  
...  
Keyword(s):  
Radionuclide Therapy ◽  
Auger Electron ◽  
Nuclear Dna ◽  
Clonogenic Survival ◽  
Targeted Radionuclide Therapy ◽  
Nuclear Uptake ◽  
Tat Peptides ◽  
Electron Emitters ◽  
The Right

Auger electron emitters (AEEs) are attractive tools in targeted radionuclide therapy to specifically irradiate tumour cells while sparing healthy tissues. However, because of their short range, AEEs need to be brought close to sensitive targets, particularly nuclear DNA, and to a lower extent, cell membrane. Therefore, radioimmunoconjugates (RIC) have been developed for specific tumour cell targeting and transportation to the nucleus. Herein, we assessed, in A-431CEA-luc and SK-OV-31B9 cancer cells that express low and high levels of HER2 receptors, two 111In-RIC consisting of the anti-HER2 antibody trastuzumab conjugated to NLS or TAT peptides for nuclear delivery. We found that NLS and TAT peptides improved the nuclear uptake of 111In-trastuzumab conjugates, but this effect was limited and non-specific. Moreover, it did not result in a drastic decrease of clonogenic survival. Indium-111 also contributed to non-specific cytotoxicity in vitro due to conversion electrons (30% of the cell killing). Comparison with [125I]I-UdR showed that the energy released in the cell nucleus by increasing the RIC’s nuclear uptake or by choosing an AEE that releases more energy per decay should be 5 to 10 times higher to observe a significant therapeutic effect. Therefore, new Auger-based radiopharmaceuticals need to be developed.

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