Characterization of the uptake of 16α-([18F]fluoro)-17β-estradiol in DMBA-induced mammary tumors☆
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Cited by (58)
The quest for improving the management of breast cancer by functional imaging: The discovery and development of 16α-[<sup>18</sup>F]fluoroestradiol (FES), a PET radiotracer for the estrogen receptor, a historical review
2021, Nuclear Medicine and BiologyCitation Excerpt :Following our first report in 1984 of the favorable biodistribution characteristics of FES in immature female rats [10], we imaged a series of DMBA-induced mammary tumors in adult female rats. We examined as a function of time, metabolism and tumor uptake of FES, as well as blood volume and blood flow in tumors and possible correlations between uptake and ER levels in tumors and in the uterus, finding that the relationships among these factors were complex [73]. We also performed a dose-response study of FES in immature female rats [74]; increasing doses of FES were obtained by adding progressively larger quantities of unlabeled FES.
Development of Companion Diagnostics
2016, Seminars in Nuclear MedicineCitation Excerpt :The binding characteristics of this positron-emitting radiopharmaceutical are similar to estradiol for both the ER and SHBG,59 making it an excellent marker of ER expression. Like estradiol, most of FES within the blood is bound to protein, primarily SHBG and albumin, and the exact ratio depends on the concentration of SHBG.60-62 As with any other steroid, FES is metabolized by the liver.60
16α-[<sup>18</sup>F]-fluoro-17ß-oestradiol ([<sup>18</sup>F]FES): A biomarker for imaging oestrogen receptor expression with positron emission tomography (PET)
2015, Medecine NucleaireCitation Excerpt :Analogues of oestradiol must display a good affinity for SHBG and albumin. In rats and in humans, about 95% of [18F]FES are bound to plasma proteins (either SBG or albumin) [20,21]. Even though most of [18F]FES initially binds to albumin right after intravenous administration, very quickly thereafter the tracer is transferred to SBG [22].
Comparative pharmacokinetics and tissue distribution analysis of systemically administered 17-β-estradiol and its metabolites in vivo delivered using a cationic nanoemulsion or a peptide-modified nanoemulsion system for targeting atherosclerosis
2014, Journal of Controlled ReleaseCitation Excerpt :Thus, within an hour of intravenous administration of 17-βE using the solution, and the DOTAP nanoemulsion system, the circulating levels of the parent compound as well as the metabolites decreased to less than 5% of the injected dose. Similar PK parameters and distribution profile of 17-βE solution have been observed in humans and rats with slight species based differences on systemic administration of 17-βE solution [29–31]. However, in our study, at all time points, the circulating levels of both the parent compound and metabolites ESS and EST in plasma were significantly greater when administered using the CREKA-peptide modified nanoemulsion system relative to the solution as well as the DOTAP nanoemulsion system.
PET imaging of oestrogen receptors in patients with breast cancer
2013, The Lancet OncologyCitation Excerpt :After the initial rapid decline, the activity of unconjugated 18F-FES blood declines slowly, over around 50 min, and by 60 min reaches less than 5% of peak value. The presence of conjugated 18F-FES metabolites is unlikely to affect tumour 18F-FES uptake because they cannot bind oestrogen receptors and their polarity prevents penetration of cell membranes.23,59 Unconjugated 18F-FES is bound to carrier proteins SHBG (45%) and albumin (45%) in serum, and the remainder circulates in free form.56
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This work was supported by DOE Grant DE-FG02-84ER60218 and NIH Grants HL13851 and CA25836.