Abstract
The non-steroidal anti-oestrogen, tamoxifen [I], is currently used extensively in treatment of metastatic breast cancer and other disseminated oestrogen-dependent tumours, as well as in the ‘adjuvant’ context. It is extensively metabolized in man to two major biologically active products: the N-desmethyl [II] and 4-hydroxy [III] derivatives [1–3] (see overleaf). The former has estrogenic activity while the latter is strongly anti-oestrogenic [4]. The relative binding affinities of I, II and III for oestrogen receptors [4] and relative blood levels in patients [2, 4, 5] who had received the drug
Access this chapter
Tax calculation will be finalised at checkout
Purchases are for personal use only
Preview
Unable to display preview. Download preview PDF.
References
Adam, H.K., Douglas, E.J. & Kemp, J.V. (1979) Biochem. Pharmacol. 28, 145–147. [Cf. #D-2, this vol.-Ed.]
Fabian, C., Sternson, L.A. & Barnett, M. (1980) Cancer Treat. Rep. 64, 765 – 773.
Fromson, J.M., Pearson, S. & Braman, S. (1973) Xenobiotica 3, 711 – 714.
Fabian, C., Tilzer, L. & Sternson, L.A. (1981) Biopharm. Drug Dis. 2, 381 – 390.
Fabian, C. & Sternson, L.A. (1981) Reviews on Endocrine Related Cancer, Suppl. 9, ICI Pharm. Div., pp. 158 –168.
Meltzer, N., Stang, P. & Sternson, L.A. (1984) Biochem. Pharmacol. 33, 115 – 123.
Mendenhall, D.W., Kobayashi, H., Shih, F.M.L. & Sternson, L.A. (1978) Clin. Chem. 24, 1518 – 1524.
Golander, Y. & Sternson, L.A. (1980) J. Chromatog. 181, 41– 49.
Thaaker, K., Higuchi, T. & Sternson, L.A. (1979) J. Pharm. Sci.63, 93 – 95.
Ternson, L.A., Meltzer, N. & Shih, F.M.L (1981) Anal. Lett. 14, 583–600.
Bedford, G.R., Walpole, A.L. & Wright, B. (1974) J. Med. Chem. 17, 147 – 149.
Mendenhall, D.W. (1978) Ph. D. Thesis, Dept. of Pharmaceutical Chemistry, University of Kansas, Lawrence, KA.
Stermite, F.R. (1967) in Organic Photochemistry, Vol. 1 (Chapman, O.L., ed.), Dekker, New York, pp. 247–282.
Doyle, T.D., Filipescu, N., Benson, W.R. & Banes, D. (1970) J. Am. Chem. Soc. 92, 6371–6372
Author information
Authors and Affiliations
Editor information
Editors and Affiliations
Rights and permissions
Copyright information
© 1984 Plenum Press, New York
About this chapter
Cite this chapter
Sternson, L.A. (1984). HPLC Methodology for Therapeutic Monitoring of Tamoxifen and Two Major Metabolites in Blood and Tissues. In: Reid, E., Wilson, I.D. (eds) Drug Determination in Therapeutic and Forensic Contexts. Methodological Surveys in Biochemistry and Analysis, vol 14. Springer, Boston, MA. https://doi.org/10.1007/978-1-4613-2397-6_28
Download citation
DOI: https://doi.org/10.1007/978-1-4613-2397-6_28
Publisher Name: Springer, Boston, MA
Print ISBN: 978-1-4612-9462-7
Online ISBN: 978-1-4613-2397-6
eBook Packages: Springer Book Archive