Background: Approaches targeting the sodium-glucose cotransporter (SGLT) could represent a promising future therapeutic strategy for numerous oncological and metabolic diseases. In this study, we evaluated the safety, biodistribution and radiation dosimetry of the glucose analogue positron emission tomography (PET) agent [F] labeled alpha-methyl-4-deoxy-4-[F]fluoro-D-glucopyranoside ([F]Me4FDG) with high sodium-glucose cotransporter and low glucose transporter (GLUT) affinity. For this purpose, five healthy volunteers (1 man, 4 women) underwent multiple whole-body PET/computed tomography (CT) examinations starting with injection and up to 4 h after injection of averaged (2.4 ± 0.1) MBq/kg (range: 2.3-2.5 MBq/kg) administered activity. The PET/CT scans were conducted in 5 separate sessions, blood pressure and temperature were measured, and blood and urine samples were collected before the scans and one hour after injection to assess toxicity. Measurements of [F]Me4FDG radioactivity in organs of interest were determined from the PET/CT scans at 5 time points. Internal dosimetry was performed on voxel level using a fast Monte Carlo approach.
Results: All studied volunteers could well tolerate the [F]Me4FDG and no adverse event was reported. The calculated effective dose was (0.013 ± 0.003) mSv/MBq. The organs with the highest absorbed dose were the kidneys with 0.05 mSv/MBq per kidney. The brain showed almost no uptake. After 60 min, (12 ± 15) % of the administered dose was excreted into the bladder.
Conclusion: Featuring an effective dose of only 0.013 ± 0.003 mSv/MBq and no occurrence of side effects, the glucose analogue [F]Me4FDG seems to be a safe radio-tracer with a favorable biodistribution for PET imaging and also within several consecutive scans.
Trial Registration Number: NCT03557138, Registered 22 February 2017, https://ichgcp.net/clinical-trials-registry/NCT03557138 .
Download full-text PDF |
Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC11096136 | PMC |
| http://dx.doi.org/10.1186/s13550-024-01098-2 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Future Prospect of Low-Molecular-Weight Prostate-Specific Membrane Antigen Radioisotopes Labeled as Theranostic Agents for Metastatic Castration-Resistant Prostate Cancer.
Molecules
December 2024
Department of Analysis and Medicinal Chemistry, Faculty of Pharmacy, Universitas Padjadjaran, Sumedang 45363, Indonesia.
Prostate cancer ranks as the fourth most common cancer among men, with approximately 1.47 million new cases reported annually. The emergence of prostate-specific membrane antigen (PSMA) as a critical biomarker has revolutionized the diagnosis and treatment of prostate cancer.
View Article and Find Full Text PDFEndothelialization of coronary stents after intra-luminal adenoviral VEGF-A gene transfer in a preclinical porcine restenosis model - Studies with optical coherence tomography, angioscopy, multiphoton and scanning electron microscopy.
J Mol Cell Cardiol
December 2024
A.I.Virtanen Institute for Molecular Sciences, University of Eastern Finland, Kuopio, Finland; Heart Centre and Gene Therapy Unit, Kuopio University Hospital, Kuopio, Finland. Electronic address:
Background: Coronary stenting operations have become the main option for the treatment of coronary heart disease. Vessel recovery after stenting has emerged as a critical factor in reducing possible complications. In this study, we evaluated the feasibility, safety and efficacy of locally administered intraluminal gene therapy delivered using a specialized infusion balloon catheter.
View Article and Find Full Text PDFLocalized In Vivo Prodrug Activation Using Radionuclides.
J Nucl Med
January 2025
Center for Systems Biology, Massachusetts General Hospital, Boston, Massachusetts;
Radionuclides used for imaging and therapy can show high molecular specificity in the body with appropriate targeting ligands. We hypothesized that local energy delivered by molecularly targeted radionuclides could chemically activate prodrugs at disease sites while avoiding activation in off-target sites of toxicity. As proof of principle, we tested whether this strategy of radionuclide-induced drug engagement for release (RAiDER) could locally deliver combined radiation and chemotherapy to maximize tumor cytotoxicity while minimizing off-target exposure to activated chemotherapy.
View Article and Find Full Text PDFComparison of a Series of Ga-Labeled DOTA-LLP2A Conjugates for Positron Emission Tomography Imaging of Very Late Antigen-4 in Melanoma.
Mol Pharm
January 2025
NHC Key Laboratory of Nuclear Medicine, Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China.
Melanoma, with its steadily rising global incidence, is characterized by high invasiveness, leading to poor prognosis in advanced stages. There remains an unmet clinical need for the development of radiolabeled PET imaging probes for the early diagnosis of melanoma. Integrin VLA-4, a key factor in melanoma metastasis, presents a promising protein target to address the specificity shortcomings of existing probes in melanoma imaging.
View Article and Find Full Text PDFPiperine-loaded mesoporous silica nanoparticles as a promising strategy for targeting Echinococcus granulosus protoscoleces.
Sci Rep
January 2025
Department of Parasitology and Mycology, School of Medicine, Shiraz University of Medical Sciences, Shiraz, Iran.
Medical and surgical treatments for cystic echinococcosis (CE) are challenged by various complications. This study evaluates in vitro protoscolicidal activity of piperine-loaded mesoporous silica nanoparticles (PIP-MSNs) against protoscoleces of Echinococcus granulosus. MSNs were prepared by adding tetraethyl orthosilicate to cetyltrimethylammonium bromide and NaOH, and then loaded with PIP.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!