Distribution of Tamoxifen and Its Metabolites in Rat and Human Tissues during Steady-State Treatment

Cancer Research

Volumn 51, Issue 18, 1991, Pages 4837-4844

  Ueland, Per M ^b,c   Solheim, Einar ^a  

^a Department of Pharmacology and Toxicology ^*  (Norway)

^b Department of Pharmacology and Toxicology ^*  (Norway)

^c UNIVERSITY OF BERGEN   (Norway)

Author keywords

[No Author keywords available]

Indexed keywords

TAMOXIFEN;

ADIPOSE TISSUE; ANIMAL; ARTICLE; BRAIN; COMPARATIVE STUDY; DRUG ADMINISTRATION; EXPERIMENTAL NEOPLASM; FEMALE; HUMAN; HYDROXYLATION; LIVER; LUNG; MALE; METABOLISM; ORAL DRUG ADMINISTRATION; PANCREAS; RAT; RAT STRAIN; TISSUE DISTRIBUTION;

ADIPOSE TISSUE; ADMINISTRATION, ORAL; ANIMAL; BRAIN; COMPARATIVE STUDY; DRUG ADMINISTRATION SCHEDULE; FEMALE; HUMAN; HYDROXYLATION; LIVER; LUNG; MALE; NEOPLASMS, EXPERIMENTAL; PANCREAS; RATS; RATS, INBRED STRAINS; SUPPORT, NON-U.S. GOV'T; TAMOXIFEN; TISSUE DISTRIBUTION;

EID: 0026425653     PISSN: 00085472     EISSN: 15387445     Source Type: Journal    
DOI: None     Document Type: Article

References (56)

1. Jordan, V. C. Long-term adjuvant tamoxifen therapy for breast cancer. Breast Cancer Res. Treat., 15:125-136,1990.
2. Buckley, M. M-T., and Goa K. L. Tamoxifen. A reappraisal of its pharmacodynamic and pharmacokinetic properties, and therapeutic use. Drugs, 37: 451-490,1989.
3. Bakkevold, K. E., Pettersen, A., Amesjø;, B., and Espehaug, B. Tamoxifen therapy in unresectable adenocarcinoma of the pancreas and the papilla of Vater. Br. J. Surg., 77:725-730, 1990.
4. Gazet, J. C. Tamoxifen prophylaxis for women at high risk of breast cancer. Lancet, 2: 1119,1985.
5. Robertson, D. W., Katzenellenbogen, J. A., Long, D. J., Rorke, E. A., and Katzenellenbogen, B. S. Tamoxifen antiestrogens. A comparison of the activity, pharmacokinetics, and metabolic activation of the cis and trans isomers of tamoxifen. J. Steroid Biochem., 16:1-13,1982.
6. Lien, E. A., Solheim, E., Lea, O. A., Lundgren, S., Kvinnsland, S., and Ueland, P. M. Distribution of 4-hydroxy-N-desmethyltamoxifen and other tamoxifen metabolites in human biological fluids during tamoxifen treatment. Cancer Res., 49:2175-2183,1989.
7. Cole, M. P., Jones, C. T. A., and Todd, I. D. H. A new anti-oestrogenic agent in late breast cancer. An early clinical appraisal of ICI46474. Br. J. Cancer, 25: 1971.
8. Patterson, J. S., Settatree, R. S., Adam, H. K., and Kemp, J. V. Serum concentrations of tamoxifen and major metabolite during long term Nolvadex therapy, correlated with clinical response. In: H. T. Mouridsen and T. Palshof (eds.). Breast Cancer-Experimental and Clinical Aspects, pp. 89-92. Oxford: Pergamon Press, 1980.
9. Daniel, C. P., Gaskell, S. J., and Nicholson, R. I. The measurement of tamoxifen and metabolites in the rat and relationship to the response of DMBA-induced mammary tumours. Eur. J. Cancer Clin. Oncol., 20: 137-143, 1984.
10. Reddel, R. R., Murphy, L. C., and Sutherland, R. L. Factors affecting the sensitivity of T-47D human breast cancer cells to tamoxifen. Cancer Res., 4:2398-2405, 1984.
11. Reddel, R. R., Murphy, L. C., and Sutherland, R. L. Effects of biologically active metabolites of tamoxifen on the proliferation kinetics of MCF-7 human breast cancer cells in vitro. Cancer Res., 43:4618-4624, 1983.
12. Sutherland, R. L., Hall, R. E., and Taylor, L.W. Cell proliferation kinetics of MCF-1 human mammary carcinoma cells in culture and effects of tamoxifen on exponentially growing and plateau-phase cells. Cancer Res., 43:3998-4006,1983.
13. Grénman, R., Virolainen, E., Shapira, A., and Carey, T. E. In vitro effects of tamoxifen on UM-scc head and neck cancer cell lines: correlation with the estrogen and progesterone receptor content Int. J. Cancer, 39:77-81,1987.
14. Robinson, S. P., Langan-Fahey, S. M., and Jordan, V. C. Implications of tamoxifen metabolism in the athymic mouse for the study of antitumor effects upon human breast cancer xenografts. Eur. J. Cancer Clin. Oncol., 25:1769-1776, 1989.
15. Major, J. S., Green, B., and Heald, P. J. Interactions of oestradiol-1719 and tamoxifen in the uterus of the pregnant rat. J. Endocrinol., 71: 315-324, 1976.
16. Fromson, J. M., Pearson, S., and Bramah, S. The metabolism of tamoxifen (I. C. I. 46,474). Part I: In laboratory animals. Xenobiotica, 3: 693-709, 1973.
17. Wilking, N., Appelgren, L-E., Carlström, K., Pousette, Å., and Theve, N. O. The distribution and metabolism of *-labelled tamoxifen in spayed female mice. Acta Pharmacol. Toxicol., 50:161-168,1982.
18. DeGregorio, M. W., Coronado, E., and Osborne, C. K. Tumor and serum tamoxifen concentrations in the athymic nude mice. Cancer Chemother. Pharmacol., 23:68-70, 1989.
19. Gottardis, M. M., Robinson, S. P., Satyaswaroop, P. G., and Jordan, V. C. Contrasting actions of tamoxifen on endometrial and breast tumor growth in the athymic mouse. Cancer Res., 48:812-815,1988.
20. Ruenitz, P. C., and Bagley, J. R. Comparative fates of clomiphene and tamoxifen in the immature female rat. Drug Metab. Dispos., 13: 582-586, 1985.
21. Fromson, J. M., Pearson, S., and Bramah, S. The metabolism of tamoxifen. (I. C. I. 46,474) Part II: In female patients. Xenobiotica, 3:711-714,1973.
22. Fromson, J. M., and Sharp, D. S. The selective uptake of tamoxifen by human uterine tissue. J. Obstet. Gynaecol. Br. Commonw., 81: 321-323, 1974.
23. Daniel, P., Gaskell, S. J., Bishop, H., Campbell, C., and Nicholson, R. I. Determination of tamoxifen and biologically active metabolites in human breast tumours and plasma. Eur. J. Cancer Clin. Oncol., 17: 1183-1189, 1981.
24. Milano, G., Etienne, M. C., Frenay, M., Khater, R., Formento, J. L., Renee, N., Moll, J. L., Francoual, M., Berto, M., and Namer, M. Optimised analysis of tamoxifen and its main metabolites in the plasma and cytosol of mammary tumours. Br. J. Cancer, 55: 509-512, 1987.
25. Robinson, S. P., Langan-Fahey, S. M., Johnson, D. A., and Jordan, V. C. Metabolites, pharmacodynamics, and pharmacokinetics of tamoxifen in rats and mice compared to the breast cancer patient. Drug Metab. Dispos., 19: 36-43,1991.
26. Lien, E. A., Solheim, E., Kvinnsland, S., and Ueland, P. M. Identification of 4-hydroxy-N-desmethyltamoxifen as a metabolite of tamoxifen in human bile. Cancer Res., 48:2304-2308, 1988.
27. Lien, E. A., Ueland, P. M., Solheim, E., and Kvinnsland, S. Determination of tamoxifen and four metabolites in serum by low-dispersion liquid chromatography. Clin. Chem., 33:1608-1614,1987.
28. Robinson, S. P., and Jordan, V. C. Metabolism of steroid-modifying anticancer agents. Pharmacol. Ther., 36:41-103,1988.
29. Langan-Fahey, S. M., Douglass, C., Tormey, D. C., and Jordan, V. C. Tamoxifen metabolites in patients on long-term adjuvant therapy for breast cancer. Eur. J. Cancer, 26:883-888, 1990.
30. Murphy, C., Fotsis, T., Pantzar, P., Adlercreutz, H., and Martin, P. Analysis of tamoxifen and its metabolites in human plasma by gas chromatography-mass spectrometry (GC-MS) using selected ion monitoring (SIM). J. Steroid Biochem., 26: 547-555, 1987.
31. Lyman, S. D., and Jordan, V. C. Metabolism of nonsteroidal antiestrogens. in: V. C. Jordan (ed.), Estrogen/Antiestrogen Action and Breast Cancer Therapy, pp. 191-219. Madison: University of Wisconsin Press, 1986.
32. Siddick, Z. H., Tnish, M. A., and Gram, T. E. Drug absorption and distribution. In: C. R. Craig and R. E. Stitzel (eds.). Modem Pharmacology, pp. 20-36. Boston: Little, Brown and Co., 1982.
33. Browne, T. R., Greenblatt, D. J., Schumacher, G. E., Szabo, G. K., Evans, J. E., and Evans, B. A. New pharmacokinetic methods. III. Two simple tests for **deep pool efTect.** J. Oin. Pharmacol., 30:680-685,1990.
34. Dumin, J. V. G. A., and Womersley, J. Body fat assessed from total body density and its estimation from skinfold thickness: measurements on 481 men and women aged from 16 to 72 years. Br. J. Nutr., 32:77-97, 1974.
35. Rowland, M., and Tozer, T. N. Clinical Pharmacokinetics: Concepts and Applications. Philadelphia: Lea & Febiger, 1989.
36. Roerig, D. L., Kotrly, K. J., Dawson, C. A., Ahlf, S. B., Gualtieri, J. F., and Kampine, J. P. First-pass uptake of verapamil, diazepam, and thiopental in human lung. Anesth. Analg., 69:461-466, 1989.
37. Roth, R. R., and Vinegar, A. Action by the lungs on circulating xenobiotic agents, with a case study of physiologically based pharmacokinetic modeling of benz(a)pyrene disposition. Pharmacol. Ther., 48:143-155,1990.
38. Pasqualini, J. R., Geliy, C., and Nguyen, B-L. Metabolism and biologic response of estrogen sulfates in hormone-dependent and hormone-independent mammary cancer cell lines. Effect of antiestrogens. Ann. NY Acad. Sci., 595:106-116, 1990.
39. Sutherland, R. L., Murphy, L. C., Foo, M. S., Green, M. D., and Whyboume, A. M. High-affinity anti-oestrogen binding site distinct from the oestrogen receptor. Nature (Lond.), 288:273-275,1980.
40. Ruenitz, P. C., and Bagley, J. R. Affmity of ligands other than triarylethylenes for liver microsomal antiestrogen binding sites. Biochem. Pharmacol., 34: 2807-2809,1985.
41. Batra, S. Interaction of antiestrogens with binding sites for muscarinic cholinergic drugs and calcium channel blockers in cell membranes. Cancer Chemother. Pharmacol., 26:310-312,1990.
42. Pasqualini, J. R., Sumida, C., and Giambiagi, N. Pharmacodynamic and biological effects of anti-estrogens in different models. J. Steroid. Biochem., 11: 613-643, 1988.
43. Clarke, R., van den Berg, H. W., and Murphy, R. F. Reduction of the membrane fluidity of human breast cancer cells by tamoxifen and 17-estradiol. J. Natl. Cancer Inst., 82:1702-1705,1990.
44. Controlled trial of tamoxifen as single adjuvant agent in management of early breast cancer. Analysis at six years by Nolvadex adjuvant trial organisation. Lancet, 1: 836-839, 1985.
45. Breast Cancer Trials Committee, Scottish Cancer Trials Office. Adjuvant tamoxifen in the management of operable breast cancen the Scottish trial. Lancet, 2:171-175,1987.
46. Rose, C., and Mouridsen, H. T. Endocrine management of advanced breast cancer. Horm. Res., 32 (Suppl. IX* 189-197, 1989.
47. Fomander, T., Rutqvist, L. E., and Glas, U. Response to tamoxifen and fluoxymesterone in a group of breast cancer patients with disease recurrence after cessation of adjuvant tamoxifen. Cancer Treat. Rep., 71: 685-688, 1987.
48. Lien, E. A., Wester, K., Uinning, P. E., Solheim, E., and Ueland, P. M. Distribution of tamoxifen and metabolites into brain tissue and brain metas-tases in breast cancer patients. Br. J. Cancer, 63:641-645,1991.
49. Colomer, R., Casas, D., Del Campo, J. M., Boada, M., Rubio, D., and Salvador, L. Brain metastases from breast cancer may respond to endocrine therapy. Breast Cancer Res. Treat., 12:83-86,1988.
50. Hansen, S. B., Galsgvd, H., von Eyben, F. E., Westergaard-Nielsen, V., and Wolf-Jensen, J. Tamoxifen for brain metastases from breast cancer. Ann. Neurol., 20:544-545,1986.
51. Carey, R. W., Davis, J. M., and Zervas, N. T. Tamoxifen-induced regression of cerebral metastases in breast carcinoma. Cancer Treat. Rep., 65:793-795, 1981.
52. Greenway, B., Iqbal, M. J., Johnson, P. J., and Williams, R. Oestrogen receptor proteins in malignant and fetal pancreas. Br. Med. J., 283: 751-753, 1981.
53. Andren-Sandberg, A. Estrogens and pancreatic cancer: some recent aspects. Scand. J. Gastroenterol., 21:129-133,1986.
54. Eriksen, E. F., Colvard, D. S., Berg, N. J., Graham, M. L., Mann, K. G., Spelsberg, T. C., and Riggs, B. L. Evidence of estrogen receptors in normal human osteoblast-like cells. Science (Washington DC), 241:84-86,1988.
55. Jordan, V. C., and Murphy, C. S. Endocrine pharmacology of antiestrogens as antitumor agents. Endocrine Rev., II: 578-610,1990.
56. Spicer, D. V., Pike, M. C., Henderson, B. E., and Groshen, S. Tamoxifen and estrogen replacement therapy as agents of disease prevention. J. Natl. Cancer Inst., 83:63-64,1991.