Radiopharmaceutical Research and Production in Brazil: A 30-Year History of Participation in the Nuclear Medicine Scenario

Santos-Oliveira, Ralph; Antunes, Leila Jorge

doi:10.2967/jnmt.111.088450

Cited by 3 publications

(2 citation statements)

References 3 publications

(1 reference statement)

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“…18 F-FDG PET/CT has been routinely used for repetitive and noninvasive monitoring of chemotherapy responses both in small animals and in human. The short radioactive half-life (110 minutes) of 18 F (42) also permits repetitive imaging for before and after 1A12 treatment. Baseline 18 F-FDG uptake in tumor-bearing mice was determined before and after 1A12 treatment.…”

Section: Resultsmentioning

confidence: 99%

Syntheses and Discovery of a Novel Class of Cinnamic Hydroxamates as Histone Deacetylase Inhibitors by Multimodality Molecular Imaging in Living Subjects

Chan

Smith

et al. 2014

Cancer Research

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Histone deacetylases (HDAC) that regulate gene expression are being explored as cancer therapeutic targets. In this study, we focused on HDAC6 based on its ability to inhibit cancerous Hsp90 chaperone activities by disrupting Hsp90/p23 interactions. To identify novel HDAC6 inhibitors, we used a dual-luciferase reporter system in cell culture and living mice by bioluminescence imaging (BLI). On the basis of existing knowledge, a library of hydrazone compounds was generated for screening by coupling cinnamic hydroxamates with aldehydes and ketones. Potency and selectivity were determined by in vitro HDAC profiling assays, with further evaluation to inhibit Hsp90(α/β)/p23 interactions by BLI. In this manner, we identified compound 1A12 as a dose-dependent inhibitor of Hsp90(α/β)/p23 interactions, UKE-1 myeloid cell proliferation, p21waf1 upregulation, and acetylated histone H3 levels. 1A12 was efficacious in tumor xenografts expressing Hsp90(α)/p23 reporters relative to carrier control–treated mice as determined by BLI. Small animal 18F-FDG PET/CT imaging on the same cohort showed that 1A12 also inhibited glucose metabolism relative to control subjects. Ex vivo analyses of tumor lysates showed that 1A12 administration upregulated acetylated-H3 by approximately 3.5-fold. Taken together, our results describe the discovery and initial preclinical validation of a novel selective HDAC inhibitor.

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Section: Resultsmentioning

confidence: 99%

Syntheses and Discovery of a Novel Class of Cinnamic Hydroxamates as Histone Deacetylase Inhibitors by Multimodality Molecular Imaging in Living Subjects

Chan

Smith

et al. 2014

Cancer Research

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“…Radiopharmaceuticals are a heterogeneous class of medicinal products characterized by containing one or more radioactive isotopes. Those isotopes decay spontaneously with the emission of ionizing radiation that is used for various medical purposes [1,2]. Iodine −131 radionuclide (I −131 ) (t 1/2 = 8.04d), as an example, has important applications in nuclear medicine; especially it is the drug of choice for the diagnosis and treatment of thyroid carcinoma.…”

Section: Introductionmentioning

confidence: 99%

Adaptation of hard gelatin capsules for oral delivery of aqueous radiopharmaceuticals

Omar

Abdel-Rashid

AlAssaly³

et al. 2019

DARU J Pharm Sci

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Purpose Oral administration of Iodine −131 (I −131) solutions causes high risk of contamination for patients and dispensers. The objective of the study was to adapt hard gelatin capsules (HGCs) for filling with radiopharmaceutical solutions without deformation. Methods Polystyrene (PS) internally lining films with different thicknesses were used to protect HGCs. The insulated HGCs were evaluated for their physicochemical characteristics and rupturing time in different dissolution media. HGCs internally lined with PS were examined for withstand loading with different volumes and radioactivities of I −131 solutions. Radioactivity release was studied in deionized water and acidic media. Quality control of released I −131 was inspected for radiochemical purities. Results There was a directly proportion between PS lining thickness and stability of HGCs after filling with 500 μl aqueous methylene blue solution. HGCs internally lined with PS 100 μm thickness withstand deformation for ˃ two months; however showed fast in-vitro rupturing time in different dissolution media. Internally lined HGCs loaded with different volumes and radioactivities of I −131 solutions resisted for one week without radioactive leakage. Yet, revealed complete release of I −131 after 20 min in dissolution media with great radiochemical purity. Conclusion The study promises safely I −131 aqueous solution delivery via adapted HGCs.

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Technetium-99m metastable radiochemistry for pharmaceutical applications: old chemistry for new products

Costa

İlem-Özdemir

Santos-Oliveira

2019

Journal of Coordination Chemistry

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Radiopharmaceutical Research and Production in Brazil: A 30-Year History of Participation in the Nuclear Medicine Scenario

Abstract: This article describes the 30-y history of nuclear medicine in Brazil, including reactors, production of radiopharmaceuticals, and trends.

Cited by 3 publications

References 3 publications

Syntheses and Discovery of a Novel Class of Cinnamic Hydroxamates as Histone Deacetylase Inhibitors by Multimodality Molecular Imaging in Living Subjects

Syntheses and Discovery of a Novel Class of Cinnamic Hydroxamates as Histone Deacetylase Inhibitors by Multimodality Molecular Imaging in Living Subjects

Adaptation of hard gelatin capsules for oral delivery of aqueous radiopharmaceuticals

Technetium-99m metastable radiochemistry for pharmaceutical applications: old chemistry for new products

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