Analysis of blood clearance and labeled metabolites for the estrogen receptor tracer [F-18]-16α-Fluorestradiol (FES)

Nuclear Medicine and Biology

Volumn 24, Issue 4, 1997, Pages 341-348

  Mankoff, David A ^a   Tewson, Timothy J ^a   Eary, Janet F ^a  

^a UNIVERSITY OF WASHINGTON   (United States)

Author keywords

Estrogen receptor; FES; Metabolites; Protein binding

Indexed keywords

16ALPHA FLUOROESTRADIOL F 18; ESTRADIOL; UNCLASSIFIED DRUG;

ADULT; AGED; ARTICLE; BREAST CANCER; CLINICAL ARTICLE; CONTROLLED STUDY; FEMALE; HUMAN; PLASMA CLEARANCE;

ADULT; AGED; ERYTHROCYTES; ESTRADIOL; FEMALE; FLUORINE RADIOISOTOPES; HUMANS; METABOLIC CLEARANCE RATE; MIDDLE AGED; PROTEIN BINDING; RECEPTORS, ESTROGEN;

EID: 0030786893     PISSN: 09698051     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0969-8051(97)00002-4     Document Type: Article

References (26)

1. Bernstein S. and S. Solomon. (1970) Chemical and Biological Aspects of Steroid Conjugation, Springer-Verlag, New York.
2. Campbell F. C., Elston C. W., Blarney R. W., Morris A. H., Nicholson R. I., Griffeths K. and Haybittle J. L. (1981) Quantitative oestradiol receptor values in primary breast cancer and response of metastases to endocrine therapy. Lancet 1, 1317-1319.
3. Dehdashti F., Mortimer J. E., Siegel B. A., et al. (1995) Positron tomographic assessment of estrogen receptors in breast cancer: Comparison with FDG-PET and in vitro receptor assays. J. Nucl. Med. 36, 1766-1774.
4. Flanagan F. L., Dedashti F., Mortimer J. E., Siegel B. A., Johnson S. and Welch M. J. (1996) PET assessment of response to tamoxifen therapy in patients with metastatic breast cancer. J. Nucl. Med. 37, 99P (Abstract).
5. Hanna W. and Mobbs B. C. (1989) Comparative evaluation of ER-ICA and enzyme immunoassay for the quantitation of estrogen receptors in breast cancer. Am. J. Clin. Pathol. 91, 182-186.
6. Honig S. H. and Swain S. M. (1993) Hormonal manipulation in the adjuvant treatment of breast cancer. In: Important Advances in Oncology (Edited by DeVita V.T., Hellman S. and Rosenberg S.A.), pp. 103-123. Lippincott, Philadelphia.
7. Hortobagyi G. N. and Buzdar A. U. (1995) Current status of adjuvant systemic therapy for primary breast cancer: Progress and controversy. CA Cancer J. Clin. 45, 199-226.
8. Jaiyesimi I. A., Buzdar A. U., Decker D. A. and Hortobagyi G. N. (1995) Use of tamoxifen for breast cancer: Twenty-eight years later. Semin. Clin. Oncol. 13, 513-529.
9. Kamby C., Rasmussen B. B. and Kristensen B. (1989) Oestrogen receptor status of primary breast carcinomas and their metastases: Relation to pattern of spread and survival after recurrence. Br. J. Cancer. 60, 252-257.
10. Katzenellenbogen J. A. (1995) Designing steroid receptor-based radiotracers to image breast and prostate tumors. J. Nucl. Med. 36(6 Suppl), 8S-13S.
11. Katzenellenbogen J. A., MathiasC. J., Vanbrocklin H. F., Brodack J. W. and Welch M. J. (1993) Titration of the in vivo uptake of 16α-[F-18]fluoroestradiol by target tissues in the rat: Competition by tamoxifen, and implications for quantitating estrogen receptors in vivo and the use of animal models in receptor-binding radiopharmaceutical development. Nucl. Med. Biol. 20, 735-745.
12. Kiesewetter D.O., Kilbourn M. R., Landvatter S.W., Heiman D. F., Katzenellenbogen J. A. and Welch M. J. (1984) Preparation of four fluorine-18-labeled estrogens and their selective uptakes in target tissue of immature rats. J. Nucl. Med. 25, 1212-1221.
13. Lim J. L., Zheng L., Berridge M. S. and Tewson T. J. (1996) The use of 3-methoxymethyl-16β,17β-epiestriol-O-cyclic sulfone as the precursor in the synthesis of F-18 16α-fluoroestradiol. Nucl. Med. Biol. 23, 911-915.
14. Mankoff D. A., Shields A. F., Graham M. M., Link J. M. and Krohn K. A. (1996) A graphical analysis method to estimate blood-tissue transfer constants for systems with labeled metabolites. J. Nucl. Med. 37, 2049-2057.
15. Mathias C. J., Welch M. J., Katzenellenbogen J. A., Brodack J. W., Kilbourn M. R., Carlson K. E. and Kiesewetter D. O. (1987) Characterization of the uptake of 16α-([F-18]fluoro)-17β-estradiol in DMBA-induced mammary tumors. Nucl. Med. Biol. 14, 15-25.
16. McClelland R. A., Berger U., Miller L. S., Pawles T. J. and Coombes R. C. (1986) Immunocytochemical assay for estrogen receptor in patients with breast cancer: Relationship to a biochemical assay and to outcome of therapy.J. Clin. Oncol. 4, 1171-1176.
17. McGuire A. H., Dehdashti F., Siegel B. A., Lyss A. P., Brodack J. W., Mathias C. J., Mintun M. A., Katzenellenbogen J. A. and Welch M. J. (1991) Positron tomographic assessment of 16α-[F-18]-fluoro-17β-estradiol uptake in metastastic breast carcinoma. J. Nucl. Med. 32, 1526-1531.
18. Mintun M. A., Welch M. J., Siegel B. A., Mathias C. J., Brodack J. W., McGuire A. H. and Katzenellenbogan J. A. (1988) Breast cancer: PET imaging of estrogen receptors. Radiology 169, 45-48.
19. Murad F. and Kuret J. (1990) Estrogens and progestins. In: Goodman and Oilman's The Pharamacological Basis for Therapeutics (Edited by Oilman A. G. et al.), pp. 1384-1412. Pergamon, Elmsford, NY.
20. Petra P. H. (1991) The plasma sex-steroid binding protein (SBP or SHBG): A critical review of recent developments on the structure, molecular biology and function. J. Steroid Biochem. Mol. Biol. 40, 1991.
21. 18F reaction. Radiochim. Acta 26, 21-25.
22. Santen R. J., Manni A., Harvey H. and Redmond C. (1990) Endocrine treatment of breast cancer in women. Endocr. Rev. 11, 221-265.
23. Schlyer D., Bastos M., Alexoff D. and Ap W. (1990) Separation of [F-18] fluoride from [O-18]water using anion exchange resin. Appl. Radiat. Isot. 41(6), 531-533.
24. Strel'chyonok, O.A., Avvakumov G. V. and Survilo L. I. (1984) A recognition system for sex-hormone-binding protein-estradiol complex in human decidual endometrium plasma membranes. Biochim. Biophys. Acta 802(3), 459-466.
25. Tewson T. J. (1995) The routine synthesis of fluorine-18 16α-fluoroestradiol: The use of 3-methoxymethyl-epiestriol-16β,17β-cyclic sulfate as the starting substrate. J. Lab. Compd. Radiopharm. 37, 589-591.
26. Wolf D.M. and Jordan V. C. (1993) Drug resistance to tamoxifen during breast cancer therapy. Breast Cancer Res. Treat. 27, 27-40.