Production and quality control of [166Ho]-DOTA-bevacizumab for therapeutic applications

Khorami-Moghadam, Alireza; Jalilian, Amir Reza; Yavari, Kamal; Bolouri, Bahram; Bahrami-Samani, Ali; Ghannadi‐Maragheh, Mohammad

doi:10.1007/s10967-012-1640-2

Cited by 6 publications

(5 citation statements)

References 25 publications

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“…After 24 h, 30000 cpm of 111 In-DOTA-trastuzumab were added to each well and incubated at 37°C. At various times (4,8,12,16,24,30 and 36 h), RPMI medium in wells were removed and the cells, half of wells, were then exposed to 1 ml solution of 0.1 M NaOH and half of wells were exposed to 1 ml solution of 0.1 M acetic acid pH 4.0. After 15 min, the radioactivity content of the supernatant was measured by γ-counter.…”

Section: Immunoreactivity Of Radiolabeled Trastuzumab Towards Skbr3 Cmentioning

confidence: 99%

“…[1] Various radio labeled DOTA-immunoconjugates have been developed successfully recently. [2][3][4] In order to develop herceptin radio immunoconjugates for using in imaging studies, DOTA-trastuzumab was labeled by In-111 chloride for preliminary bio-distribution studies in rats and tumor-bearing mice.…”

Section: Introductionmentioning

confidence: 99%

“…

Context: Herceptin and its fragments have been radiolabeled and used in the imaging of human epidermal growth factor receptor 2 (HER2)/neu-positive tumors and development of diagnostic kits is of great importance in radiopharmacy.Aims: In this study, 4,7,4,7, In-DOTA-trastuzumab) was successively prepared and evaluated for ultimate use in the HER2 antigen imaging in oncology.Settings and Design: The conjugate was prepared, labeled and evaluated using in vitro (radioimmunoassay [RIA], enzyme-linked immunosorbent assay (ELISA), stability, binding, internalization)/in vivo (bio-distribution, single-photon emission computed tomography [SPECT]) experiments.Materials and Methods: 111 In-DOTA-trastuzumab was prepared followed by determination of radiochemical purity (RCP), integrity of protein, immunoreactivity of radiolabeled antibody with HER2/neu antigen (by SkBr3 cell line binding and RIA methods) were determined followed by stability tests, internalization studies and the tissue bio-distribution determination in wild-type rats as well as SPECT imaging in SkBr3-bearing mice.Statistical Analysis Used: All values were expressed as mean ± standard deviation (mean ± SD) and the data were compared using Student's t-test. Statistical significance was defined as P < 0.05.

Results: 111 In-DOTA-trastuzumab was prepared (RCP >95 ± 0.5%, S.A. 5.3 µCi/µg) with the average number of chelators per antibody of 6:1 showing significant immune-reactivity retention using ELISA.

…”

mentioning

confidence: 99%

“…Aims: In this study, 4,7,4,7, In-DOTA-trastuzumab) was successively prepared and evaluated for ultimate use in the HER2 antigen imaging in oncology.…”

mentioning

confidence: 99%

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Preclinical evaluation of [ ¹¹¹ In]-DOTA-trastuzumab for clinical trials

et al. 2014

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Section: Immunoreactivity Of Radiolabeled Trastuzumab Towards Skbr3 Cmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

“…

…”

mentioning

confidence: 99%

“…Aims: In this study, 4,7,4,7, In-DOTA-trastuzumab) was successively prepared and evaluated for ultimate use in the HER2 antigen imaging in oncology.…”

mentioning

confidence: 99%

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Preclinical evaluation of [ ¹¹¹ In]-DOTA-trastuzumab for clinical trials

et al. 2014

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“…In particular, suitable gamma energy enables us to track targeting agent both in vitro and in vivo [11,12].…”

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confidence: 99%

Anti-Angiogenesis Therapy of Cancer Cells using 153Sm-Bevasesomab

Yavari¹

2018

ESJ

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Purpose: Angiogenesis is essential for tumor growth or metastasis. Avastin is a monoclonal antibody that is used in treating angiogenesis. We labelled this monoclonal antibody with samarium153 and performed in vitro quality control tests as a first step in the production of a new radiopharmaceutical.Material and Methods: For a successful radiolabeling, we chose DOTA-NHS as the bifunctional chelating agent and optimized radiolabeling condition with modifications of the factors such as reaction time and molar ratio which are known to be very critical in radiolabeling. The efficiency and in vitro stability of antibody labelling were determined using thin layer chromatography. The integrity of the radiolabeled antibody was checked by SDS-PAGE. Biodistribution study of 153Sm-DOTA -avastin was carried out in BALB/c mice at 2, 24, 48 and 72 hours after injection. Immunoreactivity and toxicity of the complex were tested on colon cancer cell line by MTT.Results: The efficiency of antibody labelling was more than 99%. The in vitro stability of the labelled product in human serum after 120h was 78 ±2%. There was no fragmentation in the labelled antibody during SDS-PAGE protocol. The highest of %ID/g was observed in the blood, liver, lungs and spleen. The immunoreactivity of the complex was 89±1.4%. At a concentration of 1 nM, the complex killed 70±3% of SW480 cells. At 1.9 nM, 90±5% of the cells were killed.Discussion: The monoclonal antibody avastin against angiogenesis was effectively radiolabeled with 153Sm. The results showed that the new complex could be considered a promising tracer for noninvasive delineation of angiogenesis.

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Preclinical evaluation of holmium‐166 labeled anti‐VEGF‐A(Bevacizumab)

Khorami-Moghadam

Bolouri

Jalilian

et al. 2013

Labelled Comp Radiopharmac

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Radiolabeled antiangiogenic monoclonal antibodies are potential agents for targeted therapy in specific types of malignancies. In this study, (166)Ho-DOTA-Bevacizumab was used in biodistribution studies using single-photon emission computed tomography (SPECT) to acquire dosimetric aspects of the radiolabeled antibody in mice. The liver toxicity of the radiolabeled antibody was also determined using serum glutamic pyruvic transaminase, serum glutamic oxaloacetic transaminase and alkaline phosphatase assay 2-7 days post-injection. The SPECT biodistribution demonstrated a similar pattern as the other radiolabeled anti-vascular endothelial growth factor A (VEGF-A) immunoconjugates. (166)Ho-DOTA-Bevacizumab was revealed as a potential compound for therapy/imaging of VEGF-A expression in oncology.

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Production and quality control of [166Ho]-DOTA-bevacizumab for therapeutic applications

Cited by 6 publications

References 25 publications

Preclinical evaluation of [ ¹¹¹ In]-DOTA-trastuzumab for clinical trials

Preclinical evaluation of [ ¹¹¹ In]-DOTA-trastuzumab for clinical trials

Anti-Angiogenesis Therapy of Cancer Cells using 153Sm-Bevasesomab

Preclinical evaluation of holmium‐166 labeled anti‐VEGF‐A(Bevacizumab)

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Production and quality control of [166Ho]-DOTA-bevacizumab for therapeutic applications

Cited by 6 publications

References 25 publications

Preclinical evaluation of [ 111 In]-DOTA-trastuzumab for clinical trials

Preclinical evaluation of [ 111 In]-DOTA-trastuzumab for clinical trials

Anti-Angiogenesis Therapy of Cancer Cells using 153Sm-Bevasesomab

Preclinical evaluation of holmium‐166 labeled anti‐VEGF‐A(Bevacizumab)

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Preclinical evaluation of [ ¹¹¹ In]-DOTA-trastuzumab for clinical trials

Preclinical evaluation of [ ¹¹¹ In]-DOTA-trastuzumab for clinical trials