Comparative preclinical evaluation of 68Ga-NODAGA and 68Ga-HBED-CC conjugated procainamide in melanoma imaging

Trencsényi, György; Dénes, Noémi; Nagy, Gábor; Kis, Anna; Vida, András; Farkas, F; Szabó, Judit P.; Kovàcs, Tündé; Berényi, Ervin; Garai, Ildikó; Bai, Péter; Hunyadi, J.; Kertész, István

doi:10.1016/j.jpba.2017.02.049

Cited by 16 publications

(7 citation statements)

References 34 publications

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“…Furthermore, low SPB values were observed, which were in agreement with the obtained Log p value [ 36 ]. These results are in accordance with previously published data for the same or similar molecules [ 37 , 38 , 39 ].…”

Section: Discussionsupporting

confidence: 94%

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: Discussionsupporting

confidence: 94%

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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“…To facilitate Ga-68 labeling effectively, a variety of bifunctional chelating agents (BFCAs) have been developed and used [6–10]. Many studies have shown NODAGA (1,4,7-triazacyclononane-1-glutamic acid-4,7-diacetic acid) superiority over other BFCAs such as DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid), or HBED-CC (N,N′-bis-[2-hydroxy-5-(carboxyethyl) benzyl] ethylenediamine-N,N’-diacetic acid) [11, 12]. Our previous study has reported that NODAGA has faster labeling kinetics and permits Ga-68 labeling at room temperature under acidic conditions [13].…”

Section: Introductionmentioning

confidence: 99%

Evaluating Ga-68 Peptide Conjugates for Targeting VPAC Receptors: Stability and Pharmacokinetics

et al. 2018

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“…Benzamide derivatives for PET comprise radiolabeled benzamide and an aliphatic structure that includes an alkyl linker and an amine residue (11,(21)(22)(23)(24)(25)32,33). Many researchers have modified the structure, especially the benzene ring, to improve radiochemical yield, melanin-targeting ability, or pharmacokinetic properties.…”

Section: Discussionmentioning

confidence: 99%

“…These probes were evaluated in B16 murine melanoma-bearing mice and showed tumor-specific uptake; however, improvements to their targeting ability were needed before they could be applied in clinical trials. In recent years, the PET radionuclides 68 Ga and 18 F, which provide higher spatial resolution, have been used to radiolabel benzamide derivatives (11,(20)(21)(22)(23)(24)(25). Among them, 18 F-P3BZA was evaluated in melanoma patients as a preliminary clinical application and suggested a potential use for melanoma diagnosis (26).…”

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confidence: 99%

N-(2-(Dimethylamino)Ethyl)-4-¹⁸F-Fluorobenzamide: A Novel Molecular Probe for High-Contrast PET Imaging of Malignant Melanoma

Pyo

Kim

et al. 2018

J Nucl Med

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Malignant melanoma is an aggressive and serious form of skin cancer, with prognosis and treatment outcome depending heavily on the clinical stage of the disease at the time of diagnosis. Here, we synthesized a novel 18 F-labeled benzamide derivative to target melanoma and then evaluated its biologic characteristics in small-animal models. Methods: N-(2-(dimethylamino)ethyl)-4-18 F-fluorobenzamide ( 18 F-DMFB) was synthesized by reaction of N-succinimidyl 4-18 Ffluorobenzoate with N,N-dimethylethylenediamine. The binding affinity of 18 F-DMFB was measured in B16F10 (mouse melanoma) cells with or without L-tyrosine. Small-animal PET imaging with 18 F-DMFB was performed on B16F10 xenograft and metastasis mouse models. Results: The overall non-decay-corrected radiochemical yield of 18 F-DMFB was approximately 10%-15%. Uptake of 18 F-DMFB was melanin-specific, as cellular uptake in B16F10 increased more than 18-fold in the presence of L-tyrosine. Biodistribution studies revealed that 18 F-DMFB accumulated, and was retained, in B16F10 xenografts for 120 min (10, 30, 60, and 120 min: 9.24, 10.80, 13.0, and 10.59 percentage injected dose/g, respectively) after radiotracer injection. Liver uptake of 18 F-DMFB decreased from 10 to 120 min and showed fast clearance (10, 30, 60, and 120 min: 11.19, 5.7, 2.47, and 0.4 percentage injected dose/g). Furthermore, 18 F-DMFB allowed visualization of metastatic lesions immediately after injection and was retained in lesions for over 60 min, with a high tumor-to-background ratio. Conclusion: 18 F-DMFB demonstrated a high melanin-targeting ability and tumor-specific tumor uptake in both primary and metastatic lesions in animal models bearing malignant melanoma. 18 F-DMFB may be a potential PET imaging agent for melanoma.

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Comparative preclinical evaluation of 68Ga-NODAGA and 68Ga-HBED-CC conjugated procainamide in melanoma imaging

Cited by 16 publications

References 34 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

Evaluating Ga-68 Peptide Conjugates for Targeting VPAC Receptors: Stability and Pharmacokinetics

N-(2-(Dimethylamino)Ethyl)-4-¹⁸F-Fluorobenzamide: A Novel Molecular Probe for High-Contrast PET Imaging of Malignant Melanoma

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Comparative preclinical evaluation of 68Ga-NODAGA and 68Ga-HBED-CC conjugated procainamide in melanoma imaging

Cited by 16 publications

References 34 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

Evaluating Ga-68 Peptide Conjugates for Targeting VPAC Receptors: Stability and Pharmacokinetics

N-(2-(Dimethylamino)Ethyl)-4-18F-Fluorobenzamide: A Novel Molecular Probe for High-Contrast PET Imaging of Malignant Melanoma

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N-(2-(Dimethylamino)Ethyl)-4-¹⁸F-Fluorobenzamide: A Novel Molecular Probe for High-Contrast PET Imaging of Malignant Melanoma