Assessment of the Novel Estrogen Receptor PET Tracer 4-Fluoro-11β-methoxy-16α-[18F]fluoroestradiol (4FMFES) by PET Imaging in a Breast Cancer Murine Model View Full Text


Ontology type: schema:ScholarlyArticle     


Article Info

DATE

2013-10

AUTHORS

Michel Paquette, Serge Phoenix, René Ouellet, Réjean Langlois, Johan E. van Lier, Éric E. Turcotte, Francois Bénard, Roger Lecomte

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). 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. 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. 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. More... »

PAGES

625-632

Identifiers

URI

http://scigraph.springernature.com/pub.10.1007/s11307-013-0638-7

DOI

http://dx.doi.org/10.1007/s11307-013-0638-7

DIMENSIONS

https://app.dimensions.ai/details/publication/pub.1053704473

PUBMED

https://www.ncbi.nlm.nih.gov/pubmed/23619898


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