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Assessment of the novel estrogen receptor PET tracer 4-fluoro-11β-methoxy-16α-[(18)F]fluoroestradiol (4FMFES) by PET imaging in a breast cancer murine model.
- Source :
-
Molecular imaging and biology [Mol Imaging Biol] 2013 Oct; Vol. 15 (5), pp. 625-32. - Publication Year :
- 2013
-
Abstract
- Purpose: The aim of this study was to compare the in vivo stability, uptake, and positron emission tomography (PET) imaging performance of a novel estrogen receptor PET tracer, 4-fluoro-11β-methoxy-16α-[(18)F]fluoroestradiol (4FMFES), with 16α-[(18)F]fluoroestradiol (FES).<br />Procedures: MC7-L1 and MC4-L2 (ER+) cell lines and their ERα-knockdown variants (ERαKD) were implanted subcutaneously in Balb/c mice. After 21 days, mice were imaged using either FES or 4FMFES. One hour post-injection, static images were acquired for 30 min and the tumor %ID/g uptake values were derived. Biodistribution data were also obtained 1 h following the injection of either FES or 4FMFES. Blood samples were taken at different times and analyzed on thin-layer chromatography to quantify the presence of radiometabolites for each radiotracer. To assess specific targeting to the estrogen receptors, mice bearing only ER+ tumors were treated with the competitive ER inhibitor fulvestrant 48 h prior to imaging with 4FMFES.<br />Results: Metabolic stability was found to be similar for both tracers in mice. Both FES and 4FMFES differentiated ER+ tumors from ERαKD tumors in biodistribution and PET imaging studies. 4FMFES achieved a significantly higher %ID/g uptake in ER+ tumors and MC4-L2 ERαKD tumors than FES in the PET imaging studies. Also, tumor-to-background ratio was higher in ER+ tumors using 4FMFES compared to FES. Dissection data showed a significantly higher %ID/g in all tested cell lines and ER-rich tissues using 4FMFES versus FES. Fulvestrant-treated mice had either low or undetectable tumor uptake.<br />Conclusion: In a tumor-bearing mouse model, 4FMFES achieves better specific tumor uptake and better contrast than FES, making it a promising candidate for ER imaging.
- Subjects :
- Animals
Cell Line, Tumor
Contrast Media
Disease Models, Animal
Estradiol pharmacology
Female
Fulvestrant
Humans
Mammary Neoplasms, Animal pathology
Mice
Mice, Inbred BALB C
Tissue Distribution
Estradiol analogs & derivatives
Mammary Neoplasms, Animal diagnostic imaging
Positron-Emission Tomography
Receptors, Estrogen metabolism
Subjects
Details
- Language :
- English
- ISSN :
- 1860-2002
- Volume :
- 15
- Issue :
- 5
- Database :
- MEDLINE
- Journal :
- Molecular imaging and biology
- Publication Type :
- Academic Journal
- Accession number :
- 23619898
- Full Text :
- https://doi.org/10.1007/s11307-013-0638-7