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Group name EquipeJPP
Item Type Journal Article
Title Dosimetry and Toxicity Studies of the Novel Sulfonamide Derivative of Sulforhodamine 101([18F]SRF101) at a Preclinical Level
Creator Kreimerman et al.
Author Ingrid Kreimerman
Author Erick Mora-Ramirez
Author Laura Reyes
Author Manuel Bardiès
Author Eduardo Savio
Author Henry Engler
Abstract BACKGROUND: The SR101 N-(3-[18F]Fluoropropyl) sulfonamide ([18F]SRF101) is a Sulforhodamine 101 derivative that was previously synthesised by our group. The fluorescent dye SR101 has been reported as a marker of astroglia in the neocortex of rodents in vivo. OBJECTIVE: The aim of this study was to perform a toxicological evaluation of [18F]SRF101 and to estimate human radiation dosimetry based on preclinical studies. METHODS: Radiation dosimetry studies were conducted based on biokinetic data obtained from a mouse model. A single-dose toxicity study was carried out. The toxicological limit chosen was <100 ?g, and allometric scaling with a safety factor of 100 for unlabelled SRF101 was selected. RESULTS: The absorbed and effective dose estimated using OLINDA/EXM V2.0 for male and female dosimetric models presented the same tendency. The highest total absorbed dose values were for different sections of the intestines. The mean effective dose was 4.03 x10-3 mSv/MBq and 5.08 x10-3 mSv/MBq for the male and female dosimetric models, respectively, using tissue-weighting factors from ICRP-89. The toxicity study detected no changes in the organ or whole-body weight, food consumption, haematologic or clinical chemistry parameters. Moreover, lesions or abnormalities were not found during the histopathological examination. CONCLUSION: The toxicological evaluation of SRF101 verified the biosafety of the radiotracer for human administration. The dosimetry calculations revealed that the radiation-associated risk of [18F]SRF101 would be of the same order as other 18F radiopharmaceuticals used in clinical applications. These study findings confirm that the novel radiotracer would be safe for use in human PET imaging.
Publication Current Radiopharmaceuticals
Volume 12
Issue 1
Pages 40-48
Date 2019
Journal Abbr Curr Radiopharm
Language eng
DOI 10.2174/1874471011666180830145304
ISSN 1874-4729
Library Catalog PubMed
Extra Number: 1 PMID: 30173658
Tags Animals, Female, Fluorodeoxyglucose F18, Male, Mice, original, PET radiotracers, Preclinical evaluation, Radiation Dosage, Radiometry, Radiopharmaceuticals, Rhodamines, Scientific, Sulfonamides, tissue-weighting factors, toxicity., [18F]SRF101
Date Added 2023/11/23 - 12:44:37
Date Modified 2024/12/15 - 11:41:59
Notes and Attachments PubMed entry (Attachment)


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