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Serum elimination half-life of tamoxifen and its metabolites in patients with advanced breast cancer

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  • Tamoxifen, Advanced Breast Cancer
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Summary

In breast cancer patients discontinuing chronic tamoxifen therapy, the serum elimination of metabolites X, Y and E paralleled that of tamoxifen, whereas that of metabolite Z did not. The serum elimination of tamoxifen and metabolites X and B was increased by amino-glutethimide treatment, whereas that of metabolites Z, Y, and E was not.

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References

  1. Adam HK, Patterson JS, Kemp JV (1980) Studies in the metabolism and pharmacokinetics of tamoxifen in normal volunteers. Cancer Treat Rep 64: 761

    Google Scholar 

  2. Al-Turk WA, Stohs SJ (1983) Kinetics of tamoxifen inhibition of aryl-carbon hydroxylase activity of intestinal and hepatic microsomes from male rats. Res Commun Chem Pathol Pharmacol 39: 69

    Google Scholar 

  3. Vos D de, Mould G, Stevenson D (1989) The bioavailability of tamoxifen: new findings and their clinical implications. Curr Ther Res 46: 703

    Google Scholar 

  4. Furr BJA, Jordan VC (1984) The pharmacology and clinical uses of tamoxifen. Pharmacol Ther 25: 127

    Google Scholar 

  5. Golander Y, Sternson LA (1980) Paired-ion chromatographic analysis of tamoxifen and two major metabolites in plasma. J Chromatogr 181: 41

    Google Scholar 

  6. Guelen PJM, Stevenson D, Briggs RJ, Vos D de (1987) The bioavailability of Tamoplex (tamoxifen): 2. A single dose cross-over study in healthy male volunteers. Methods Find Exp Clin Pharmacol 9: 685

    Google Scholar 

  7. Jordan VC (1982) Metabolites of tamoxifen in animals and man: identification, pharmacology, and significance. Breast Cancer Res Treat 2: 123

    Google Scholar 

  8. Lien EA, Solheim E, Kvinnsland S, Ueland PM (1988) Identification of 4-hydroxy-N-desmethyltamoxifen as a metabolite of tamoxifen in human bile. Cancer Res 48: 2304

    Google Scholar 

  9. Lien EA, Solheim E, Lea OA, Lundgren S, Kvinnsland S, Ueland PM (1989) Distribution of 4-hydroxy-N-desmethyltamoxifen and other tamoxifen metabolites in human biological fluids during tamoxifen treatment. Cancer Res 49: 2175

    Google Scholar 

  10. Lien EA, Anker G, Lønning PE, Solheim E, Ueland PM (1990) Decreased serum concentrations of tamoxifen and its metabolites induced by aminoglutethimide. Cancer Res 50: 5851

    Google Scholar 

  11. Lien EA, Wester K, Lønning PE, Solheim E, Ueland PM (1991) Distribution of tamoxifen and metabolites into brain tissue and brain metastases in breast cancer patients. Br J Cancer 63: 641

    Google Scholar 

  12. Lønning PE (1990) Aminoglutethimide enzyme induction: pharmacological and endocrinological implications. Cancer Chemother Pharmacol 26: 241

    Google Scholar 

  13. Lundgren S, Lønning PE, Aakvaag A, Kvinnsland S (1990) Influence of aminoglutethimide on the metabolism of medroxyprogesterone acetate and megestrol acetate in postmenopausal patients with advanced breast cancer. Cancer Chemother Pharmacol 27: 101

    Google Scholar 

  14. Meltzer NM, Stang P, Sternson LA (1984) Influence of tamoxifen and its N-desmethyl and 4-hydroxy metabolites on rat liver microsomal enzymes. Biochem Pharmacol 33: 115

    Google Scholar 

  15. Nayfield SG, Karp JE, Ford LG, Dorr FA, Kramer BS (1991) Potential role of tamoxifen in prevention of breast cancer. J Natl Cancer Inst 31: 1450

    Google Scholar 

  16. Patterson JS, Settatree RS, Adam HK, Kemp JV (1980) Serum concentrations of tamoxifen and major metabolite during long-term Nolvadex therapy, correlated with clinical response. In: Mouridsen H, Palshof T (eds) Breast cancer: experimental and clinical aspects. Pergamon, London, p 89

    Google Scholar 

  17. Ruenitz PC, Bagley JR, Pape CW (1984) Some chemical and biochemical aspects of liver microsomal metabolism of tamoxifen. Drug Metab Dispos 12: 478

    Google Scholar 

  18. Stevenson D, Briggs R, Mould GP (1985) A bioequivalence study of two preparations of tamoxifen after single doses. J Pharm Biomed Anal 4: 191

    Google Scholar 

  19. Stevenson D, Chapman D, Briggs R, Vos D de (1988) Determination of tamoxifen and five metabolites in plasma and urine. J Pharm Biomed Anal 6: 1065

    Google Scholar 

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Authors and Affiliations

  1. Medical Department, Pharmachemie B.V., P. O. Box 552, 2003 RN, Haarlem, The Netherlands

    Dick de Vos

  2. St. Antonius Hospital, Nieuwegein, The Netherlands

    Peter H. Th. J. Slee

  3. The Robens Institute, University of Surrey, Guildford, England

    Derek Stevenson & Ray J. Briggs

Authors
  1. Dick de Vos
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  2. Peter H. Th. J. Slee
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  3. Derek Stevenson
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  4. Ray J. Briggs
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de Vos, D., Slee, P.H.T.J., Stevenson, D. et al. Serum elimination half-life of tamoxifen and its metabolites in patients with advanced breast cancer. Cancer Chemother. Pharmacol. 31, 76–78 (1992). https://doi.org/10.1007/BF00695998

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  • DOI: https://doi.org/10.1007/BF00695998

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