Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease

Durante, Ana Claudia R.; Sobral, Danielle Vieira; Miranda, Ana Cláudia Camargo; Almeida, Érika V.; Fuscaldi, Leonardo Lima; Barboza, Marycel Rosa Felisa Figols de; Malavolta, Luciana

doi:10.3390/ph12010025

Cited by 17 publications

(100 citation statements)

References 26 publications

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“…The P of [ 68 Ga]Ga-PSMA-11 was determined using the shake flask method, as previously described [ 44 , 45 ]. Briefly, an aliquot of [ 68 Ga]Ga-PSMA-11 (50 µL/~1 MBq) was added to a mixture of n -octanol/water (1:1) ( n = 14).…”

Section: Methodsmentioning

confidence: 99%

Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer

et al. 2021

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Prostate-specific membrane antigen (PSMA) is a glycoprotein present in the prostate, that is overexpressed in prostate cancer (PCa). Recently, PSMA-directed radiopharmaceuticals have been developed, allowing the pinpointing of tumors with the Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) imaging techniques. The aim of the present work was to standardize and validate an automatic synthesis module-based radiolabeling protocol for [68Ga]Ga-PSMA-11, as well as to produce a radiopharmaceutical for PET imaging of PCa malignancies. [68Ga]Ga-PSMA-11 was evaluated to determine the radiochemical purity (RCP), stability in saline solution and serum, lipophilicity, affinity to serum proteins, binding and internalization to lymph node carcinoma of the prostate (LNCaP) cells, and ex vivo biodistribution in mice. The radiopharmaceutical was produced with an RCP of 99.06 ± 0.10%, which was assessed with reversed-phase high-performance liquid chromatography (RP-HPLC). The product was stable in saline solution for up to 4 h (RCP > 98%) and in serum for up to 1 h (RCP > 95%). The lipophilicity was determined as −3.80 ± 0.15, while the serum protein binding (SPB) was <17%. The percentages of binding to LNCaP cells were 4.07 ± 0.51% (30 min) and 4.56 ± 0.46% (60 min), while 19.22 ± 2.73% (30 min) and 16.85 ± 1.34% (60 min) of bound material was internalized. High accumulation of [68Ga]Ga-PSMA-11 was observed in the kidneys, spleen, and tumor, with a tumor-to-contralateral-muscle ratio of >8.5 and a tumor-to-blood ratio of >3.5. In conclusion, an automatic synthesis module-based radiolabeling protocol for [68Ga]Ga-PSMA-11 was standardized and the product was evaluated, thus verifying its characteristics for PET imaging of PCa tumors in a clinical environment.

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Section: Methodsmentioning

confidence: 99%

Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer

et al. 2021

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“…Devido à elevada afinidade pelo receptor HER2, o AcM humanizado trastuzumabe tem sido alvo de estudos de radiomarcação com o intuito de radioimunodiagnóstico (RID) e radioimunoterapia (RIT). Levando-se em consideração a possível influência dos agentes quelantes bifuncionais, da razão molar anticorpo:quelante e dos radionuclídeos, nas propriedades físico-químicas e biológicas do radioimunoconjugado (RIC), este trabalho teve por objetivo desenvolver e comparar o potencial teranóstico do trastuzumabe-DTPA- 111 In e do trastuzumbe-DOTA- 177 Lu. Os resultados evidenciaram que os diferentes agentes quelantes, razões molares e radionuclídeos não influenciaram nas seguintes propriedades: integridade e estabilidade dos imunoconjugados; processo de radiomarcação e estabilidade dos RICs, estabilidade em soro, ligação às proteínas séricas, internalização e imunorreatividade.…”

Section: A a Ag G Gr R Ra A Ad D De E Ec C Ci I Im M Me E En N Nt T To O Os S Sunclassified

“…Em contrapartida, observou-se influência no caráter lipofílico dos RICs, na ligação às células que expressam receptores HER2, no perfil de biodistribuição e na captação tumoral. Estes dados permitem concluir que, em nível nacional, o trastuzumabe-DTPA- 111 In e o trastuzumabe-DOTA- 177 Lu é um par teranóstico com potencial aplicação em futuros estudos clínicos (RID e RIT) de cânceres que superexpressam receptores de HER2, em especial, o câncer de mama.…”

Section: A a Ag G Gr R Ra A Ad D De E Ec C Ci I Im M Me E En N Nt T To O Os S Sunclassified

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Desenvolvimento de radioimunoconjugados como agentes teranósticos baseados no anticorpo monoclonal anti-HER2 (trastuzumabe): influência dos agentes quelantes e dos radionuclídeos nas propriedades biológicas

Miranda¹

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MIRANDA, Ana C. C. Development of radioimmunoconjugates as theranostic agents based on the anti-HER2 monoclonal antibody (trastuzumab): influence of chelating agents and radionuclides on biological properties. 166 p. Tese (Doutorado em Tecnologia Nuclear) Instituto de Pesquisas Energéticas e Nucleares -IPEN-CNEN/SP. São Paulo: 2020. Breast cancer is the second leading cause of mortality worldwide. HER2 positive tumors occur in 20 to 30% of breast cancers and are characterized as the second worst prognosis compared to the other subtypes. It indicates a more aggressive clinical behavior, with the worst response to conventional therapies. In this context, the development of noninvasive imaging techniques using monoclonal antibodies (MAbs) is a fast developing field. Due to the high affinity to HER2 receptors, the humanized MAb trastuzumab has been radiolabeled and studied, aiming radioimmunodiagnosis (RID) and radioimmunotherapy (RIT). Taking into account the potential influence of bifunctional chelating agents, antibody:chelator molar ratio and radionuclides, in the physicochemical and biological properties of radioimmunoconjugate (RIC), this work aimed to develop and to compare the theranostic potential of 111 In-DTPA-trastuzumab and 177 Lu-DOTAtrastuzumab. The results showed that the different chelating agents, molar ratios and radionuclides did not influence in the following properties: integrity and stability of the immunoconjugates; radiolabeling process and stability of RICs, serum stability, serum proteins binding, internalization and immunoreactivity. On the other hand, there was an influence on the lipophilic feature of RICs, HER2 positive cells binding, biodistribution profile and tumor uptake. These data indicate that 111 In-DTPA-trastuzumab and 177 Lu-DOTA-trastuzumab is a theranostic pair with potential for future clinical studies in RID and RIT of cancers that overexpress HER2 receptors, especially breast cancer.

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Assessment of bioactive peptides derived from laminin-111 as prospective breast cancer-targeting agents

Mendonça,

Sobral,

Durante

et al. 2024

Amino Acids

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Breast cancer remains a pressing public health issue primarily affecting women. Recent research has spotlighted bioactive peptides derived from laminin-111, implicated in breast tumor development. Remarkably, the sequences IKVAV, YIGSR, and KAFDITYVRLKF from the α1, β1, and γ1 chains, respectively, have garnered significant attention. This study aims to assess the potential of these radiolabeled peptides as targeting agents for breast cancer. The three peptides were synthesized using the Fmoc strategy, purified via reversed-phase high-performance liquid chromatography (RP-HPLC), and characterized through mass spectrometry. Iodine-131 (131I) radiolabeling was performed using the chloramine T method, exhibiting high radiochemical yield and stability for [131I]I-YIKVAV and [131I]I-YIGSR. Conversely, [131I]I-KAFDITYVRLKF demonstrated low radiochemical yield and stability and was excluded from the biological studies. The lipophilicity of the compounds ranged from − 2.12 to − 1.10. Serum protein binding assay for [131I]I-YIKVAV and [131I]I-YIGSR reached ≅ 48% and ≅ 25%, respectively. Affinity for breast cancer cells was evaluated using MDA-MB-231 and MCF-7 tumor cell lines, indicating the affinity of the radiopeptides with these tumor cells. Ex vivo biodistribution profiles of the radiopeptides were assessed in the MDA-MB-231 breast tumor animal model, revealing tumor tissue accumulation, supported by a high tumor-to-contralateral muscle ratio and autoradiography. These results signify the effective penetration of YIKVAV and YIGSR into tumor tissue. Therefore, the synthesized α1 and β1 peptide fragments exhibit favorable characteristics as potential breast cancer-targeting agents, promising future exploration as radiopharmaceuticals for breast cancer.

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Comparative Study of Two Oxidizing Agents, Chloramine T and Iodo-Gen®, for the Radiolabeling of β-CIT with Iodine-131: Relevance for Parkinson’s Disease

Cited by 17 publications

References 26 publications

Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer

Standardization of the [68Ga]Ga-PSMA-11 Radiolabeling Protocol in an Automatic Synthesis Module: Assessments for PET Imaging of Prostate Cancer

Desenvolvimento de radioimunoconjugados como agentes teranósticos baseados no anticorpo monoclonal anti-HER2 (trastuzumabe): influência dos agentes quelantes e dos radionuclídeos nas propriedades biológicas

Assessment of bioactive peptides derived from laminin-111 as prospective breast cancer-targeting agents

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