Fulvestrant: A new type of estrogen receptor antagonist for the treatment of advanced breast cancer

Drugs of Today

Volumn 40, Issue 9, 2004, Pages 751-764

  Buzdar, Aman U ^a  

^a UNIVERSITY OF TEXAS MD ANDERSON CANCER CENTER   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANASTROZOLE; ANDROGEN; ANTIESTROGEN; AROMATASE INHIBITOR; ESTROGEN; ESTROGEN RECEPTOR; EXEMESTANE; FADROZOLE; FULVESTRANT; HORMONE RECEPTOR; LETROZOLE; MEGESTROL ACETATE; PROGESTERONE RECEPTOR; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; TOREMIFENE;

ADVANCED CANCER; ARTHRALGIA; ARTHRITIS; ARTHROPATHY; ASTHENIA; BONE PAIN; BREAST CANCER; CANCER HORMONE THERAPY; CEREBROVASCULAR ACCIDENT; CLINICAL TRIAL; CROSS RESISTANCE; DEEP VEIN THROMBOSIS; DIGESTIVE SYSTEM FUNCTION DISORDER; DRUG EFFICACY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG TOLERABILITY; HEADACHE; HOT FLUSH; HUMAN; LUNG EMBOLISM; NAUSEA; OSTEOARTHRITIS; PAIN; POSTMENOPAUSE; REVIEW; SIDE EFFECT; SIGNAL TRANSDUCTION; THROMBOEMBOLISM; URINARY TRACT INFECTION; VAGINITIS; VASODILATATION; WEIGHT GAIN;

ANIMALS; ANTINEOPLASTIC AGENTS, HORMONAL; BREAST NEOPLASMS; ESTRADIOL; HORMONE ANTAGONISTS; HUMANS; RECEPTORS, ESTROGEN;

EID: 8344241101     PISSN: 16993993     EISSN: 16994019     Source Type: Journal    
DOI: 10.1358/dot.2004.40.9.850495     Document Type: Review

References (45)

1. Osborne, C.K., Pippen, J., Jones, S.E. et al. Double-blind, randomized trial comparing the efficacy and tolerability of fulvestrant versus anastrozole in postmenopausal women with advanced breast cancer progressing on prior endocrine therapy: Results of a North American trial. J Clin Oncol 2002, 20: 3386-95.
2. Buzdar, A.U. Endocrine therapy in the treatment of metastatic breast cancer. Semin Oncol 2001, 28: 291-304.
3. Bertelli, G., Pronzato, P., Amoroso, D. et al. Adjuvant tamoxifen in primary breast cancer: Influence on plasma lipids and antithrombin III levels. Breast Cancer Res Treat 1988, 12: 307-10.
4. Love, R.R., Barden, H.S., Mazess, R.B., Epstein, S., Chappell, R.J. Effect of tamoxifen on lumbar spine bone mineral density in postmenopausal women after 5 years. Arch Intern Med 1994, 154: 2585-8.
5. Morales, M., Santana, N., Soria, A. et al. Effects of tamoxifen on serum lipid and apolipoprotein levels in postmenopausal patients with breast cancer. Breast Cancer Res Treat 1996, 40: 265-70.
6. Fisher, B., Costantino, J.P., Redmond, C.K., Fisher, E.R., Wickerham, D.L., Cronin, W.M. Endometrial cancer in tamoxifen-treated breast cancer patients: Findings from the National Surgical Adjuvant Breast and Bowel Project (NSABP) B-14. J Natl Cancer Inst 1994, 86: 527-37.
7. Fisher, B., Dignam, J., Bryant, J. et al. Five versus more than five years of tamoxifen therapy for breast cancer patients with negative lymph nodes and estrogen receptor-positive tumors. J Natl Cancer Inst 1996, 88: 1529-42.
8. Early Breast Cancer Trialists' Collaborative Group. Tamoxifen for early breast cancer: An overview of the randomised trials. Lancet 1998, 351: 1451-67.
9. Howell, A. Preliminary experience with pure antiestrogens. Clin Cancer Res 2001, 7: 4369s-75s.
10. The ATAC Trialists' Group. Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early breast cancer: First results of the ATAC randomised trial. Lancet 2002, 359: 2131-9.
11. Goss, P.E. Emerging role of aromatase inhibitors in the adjuvant setting. Am J Clin Oncol 2003, 26: S27-S33.
12. Coombes, R.C., Hall, E., Gibson, L.J. et al. A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer. N Engl J Med 2004, 350: 1081-92.
13. Boccardo, F., Rubagotti, A., Amoroso, D. et al. Anastrozole appears to be superior to tamoxifen in women already receiving adjuvant tamoxifen treatment. Breast Cancer Res Treat 2003, 82 (Suppl. 1): S6, Abstr. 3.
14. Wakeling, A.E., Dukes, M., Bowler, J. A potent specific pure antiestrogen with clinical potential. Cancer Res 1991, 51: 3867-73.
15. Wakeling, A.E. Use of pure antioestrogens to elucidate the mode of action of oestrogens. Biochem Pharmacol 1995, 49: 1545-9.
16. Wakeling, A.E. Similarities and distinctions in the mode of action of different classes of antioestrogens. Endocr Relat Cancer 2000, 7: 17-28.
17. McClelland, R.A., Manning, D.L., Gee, J.M. et al. Effects of short-term antiestrogen treatment of primary breast cancer on estrogen receptor mRNA and protein expression and on estrogen-regulated genes. Breast Cancer Res Treat 1996, 41: 31-41.
18. Horwitz, K.B., McGuire, W.L. Estrogen control of progesterone receptor and estrogen receptor in human breast cancer. J Biol Chem 1978, 253: 2223-38.
19. Hutcheson, I.R., Knowlden, J.M., Madden, T.-A. et al. Oestrogen receptor-mediated modulation of the EGFR/MAPK pathway in tamoxifen-resistant MCF-7 cells. Breast Cancer Res Treat 2003, 81: 81-93.
20. Hu, X.F., Veroni, M., De Luise, M. et al. Circumvention of tamoxifen resistance by the pure anti-estrogen ICI 182,780. Int J Cancer 1993, 55: 873-6.
21. Lykkesfeldt, A.E., Larsen, S.S., Briand, P. Human breast cancer cell lines resistant to pure anti-estrogens are sensitive to tamoxifen treatment. Int J Cancer 1995, 61: 529-34.
22. Osborne, C.K., Jarman, M., McCague, R., Coronado, E.B., Hilsenbeck, S.G., Wakeling, A.E. The importance of tamoxifen metabolism in tamoxifen-stimulated breast tumor growth. Cancer Chemother Pharmacol 1994, 34: 89-95.
23. Osborne, C.K., Coronado-Heinsohn, E.B., Hilsenbeck, S.G. et al. Comparison of the effects of a pure steroidal antiestrogen with those of tamoxifen in a model of human breast cancer. J Natl Cancer Inst 1995, 87: 746-50.
24. Dukes, M., Miller, D., Wakeling, A.E., Waterton, J.C. Antiuterotrophic effects of a pure antioestrogen, ICI 182,780: Magnetic resonance imaging of the uterus in ovariectomized monkeys. J Endocrinol 1992, 135: 239-47.
25. Addo, S., Yates, R.A., Laight, A. A phase I trial to assess the pharmacology of the new oestrogen receptor antagonist fulvestrant on the endometrium in healthy postmenopausal volunteers. Br J Cancer 2002, 87: 1354-9.
26. Robertson, J.F.R. Faslodex (ICI 182, 780), a novel estrogen receptor downregulator - Future possibilities in breast cancer. J Steroid Biochem 2001, 79: 209-12.
27. Howell, A., DeFriend, D.J., Robertson, J.F. et al. Pharmacokinetics, pharmacological and antitumour effects of the specific anti-oestrogen ICI 182780 in women with advanced breast cancer. Br J Cancer 1996, 74: 300-8.
28. Howell, A., Robertson, J.F.R., Quaresma Albano, J. et al. Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment. J Clin Oncol 2002, 20: 3396-403.
29. Robertson, J.F., Osborne, C.K., Howell, A. et al. Fulvestrant versus anastrozole for the treatment of advanced breast carcinoma in postmenopausal women - A prospective combined analysis of two multicenter trials. Cancer 2003, 98: 229-38.
30. Mauriac, L., Pippen, J.E., Quaresma Albano, J., Gertler, S.Z., Osborne, C.K. Fulvestrant (Faslodex) versus anastrozole for the second-line treatment of subgroups of postmenopausal women with visceral and non-visceral metastases: combined results from two multicentre trials. Eur J Cancer 2003, 39: 1228-33.
31. Pippen, J., Osborne, C.K., Howell, A., Robertson, J.F.R. Fulvestrant (Faslodex) versus anastrozole (Arimidex) for the treatment of advanced breast cancer: A prospective combined survival analysis of two multicenter trials. Breast Cancer Res Treat 2003, 82 (Suppl 1): S101.
32. Howell, A., Robertson, J.F.R., Abram, P. et al. Comparison of fulvestrant v tamoxifen for the treatment of advanced breast cancer in postmenopausal women previously untreated with endocrine therapy: A multinational, double-blind, randomized trial. J Clin Oncol 2004, 22: 1605-13.
33. Steger, G., Bartsch, R., Wenzel, C. et al. Fulvestrant (Faslodex®) in metastatic breast cancer. Breast Cancer Res Treat 2003, 82 (Suppl 1): S104.
34. Franco, S., Perez, A., Tan-Chiu, E., Frankel, C., Vogel, C.L. Fulvestrant (Faslodex®) demonstrates clinical benefit in heavily pretreated postmenopausal women with advanced breast cancer: A single-center experience. Breast Cancer Res Treat 2003, 82 (Suppl. 1): S105.
35. Petruzelka, L., Zimovjanova, M. Fulvestrant in postmenopausal women with metastatic breast cancer progressing on prior endocrine therapy - Results from an expanded access programme. 4th European Breast Cancer Conference, (March 16-24, Hamburg) 2004, Poster 264.
36. Buzdar, A.U., Marcus, C., Holmes, F. Phase II evaluation of LY156758 in metastatic breast cancer. Oncology 1988, 45: 344-5.
37. Gradishar, W., Glusman, J., Lu, Y., Vogel, C., Cohen, F.J., Sledge, G.W., Jr. Effects of high dose raloxifene in selected patients with advanced breast carcinoma. Cancer 2000, 88: 2047-53.
38. Vogel, C.L., Shemano, I., Schoenfelder, J., Gams, R.A., Green, M.R. Multicenter phase II efficacy trial of toremifene in tamoxifen-refractory patients with advanced breast cancer. J Clin Oncol 1993, 11: 345-50.
39. Pyrhonen, S., Valavaara, R., Vuorinen, J., Hajba, A. High dose toremifene in advanced breast cancer resistant to or relapsed during tamoxifen treatment. Breast Cancer Res Treat 1994, 29: 223-8.
40. Perey, L., Thürlimann, B., Hawle, H. et al. Fulvestrant ('Faslodex') as hormonal treatment in postmenopausal patients with advanced breast cancer progressing after treatment with tamoxifen and aromatase inhibitors. Breast Cancer Res Treat 2002, 76 (Suppl. 1): S72, Abstr. 249.
41. Howell, A., Robertson, J.F.R. Sensitivity to endocrine therapy is maintained in both fulvestrant- and tamoxifen-treated postmenopausal women with advanced breast cancer. Ann Oncol 2002, 13 (Suppl. 5): 46, Abstr. 173P.
42. Vergote, I., Robertson, J.F.R., Kleeberg, U., Burton, G., Osborne, C.K., Mauriac, L. Postmenopausal women who progress on fulvestrant ('Faslodex') remain sensitive to further endocrine therapy. Breast Cancer Res Treat 2003, 79: 207-11.
43. Robertson, J.F.R., Semiglazov, V., Gee, J.M., Armstrong, J. Effects of fulvestrant in premenopausal women with oestrogen receptor-positive primary breast cancer. Eur J Cancer Supplement 2004, 2: 73, Abstr. 59.
44. The ATAC Trialists' Group. Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early-stage breast cancer. Results of the ATAC (Arimidex, Tamoxifen, Alone or in Combination) trial efficacy and safety update analyses. Cancer 2003, 98: 1802-10.
45. Robertson, J.F., Nicholson, R.I., Bundred, N.J. et al. Comparison of the short-term biological effects of 7alpha-[9-(4,4,5,5,5-pentafluoropentylsulfinyl) -nonyl]estra-1,3,5, (10)-triene-3,17beta-diol (Faslodex) versus tamoxifen in postmenopausal women with primary breast cancer. Cancer Res 2001, 61: 6739-46.