Cancer Treatment Reviews
Volume 31 , Pages S3-S9 , 2005

Clinical development of fulvestrant (‘Faslodex’)

  • Anthony Howell

      Affiliations

    • CRUK Department of Medical Oncology, University of Manchester, Christie Hospital NHS Trust, Wilmslow Road, Manchester M20 4BX, UK
    • Corresponding Author InformationCorresponding author. Tel.: +44 161 446 8037; fax: + 44 161 446 8000.
    • ,
  • Paul Abram

      Affiliations

    • Belvoir Park Hospital, Belfast, UK

References 

  1. Beatson GT. On the treatment of inoperable cases of carcinoma of the mamma: suggestions for a new method of treatment, with illustrative cases. Lancet. 1896;2:105–107
  2. Dodds EC, Golberg L, Lawson W, Robinson R. Oestrogenic activity of certain synthetic compounds. Nature. 1938;141:247–248
  3. Schrager S, Potter BE. Diethylstilbestrol exposure. Am Fam Physician. 2004;69:2395–2400
  4. Lonning PE, Taylor PD, Anker G, et al. High-dose estrogen treatment in postmenopausal breast cancer patients heavily exposed to endocrine therapy. Breast Cancer Res Treat. 2001;67:111–116
  5. Early Breast Cancer Trialists’ Collaborative Group. Tamoxifen for early breast cancer: an overview of the randomised trials. Lancet. 1998;351:1451–1467
  6. Hasmann M, Rattel B, Loser R. Preclinical data for droloxifene. Cancer Lett. 1994;84:101–116
  7. Johnston SR, Riddler S, Haynes BP, et al. The novel anti-oestrogen idoxifene inhibits the growth of human MCF-7 breast cancer xenografts and reduces the frequency of acquired anti-oestrogen resistance. Br J Cancer. 1997;75:804–809
  8. Robinson SP, Parker CJ, Jordan VC. Preclinical studies with toremifene as an antitumor agent. Breast Cancer Res Treat. 1990;16(Suppl.):S9–S17
  9. Stenbygaard LE, Herrstedt J, Thomsen JF, Svendsen KR, Engelholm SA, Dombernowsky P. Toremifene and tamoxifen in advanced breast cancer – a double-blind cross-over trial. Breast Cancer Res Treat. 1993;25:57–63
  10. Buzdar A, Hayes D, et al. Phase III randomized trial of droloxifene and tamoxifen as first-line endocrine treatment of ER/PgR-positive advanced breast cancer. Breast Cancer Res Treat. 2002;73:161–175
  11. Lee ES, Schafer JM, Yao K, et al. Cross resistance of triphenylethylene-type antiestrogens but not ICI 182,780 in tamoxifen-stimulated breast tumors grown in athymic mice. Clin Cancer Res. 2000;6:4893–4899
  12. Holli K, Valavaara R, Blanco G, et al. Safety and efficacy results of a randomized trial comparing adjuvant toremifene and tamoxifen in postmenopausal patients with node-positive breast cancer. Finnish Breast Cancer Group. J Clin Oncol. 2000;18:3487–3494
  13. Marttunen MB, Hietanen P, Tiitinen A, Ylikorkala O. Comparison of effects of tamoxifen and toremifene on bone biochemistry and bone mineral density in postmenopausal breast cancer patients. J Clin Endocrinol Metab. 1998;83:1158–1162
  14. Marttunen MB, Cacciatore B, Hietanen P, et al. Prospective study on gynaecological effects of two antioestrogens tamoxifen and toremifene in postmenopausal women. Br J Cancer. 2001;84:897–902
  15. Gradishar WJ, Glusman JE, Vogel C, et al. Raloxifene HCI, a new endocrine agent, is active in estrogen receptor positive (ER+) metastatic breast cancer. Breast Cancer Res Treat. 1997;20(Suppl.):53;[abstract 209]
  16. Munster PN, Buzdar A, Dhingra K, et al. Phase I study of a third-generation selective estrogen receptor modulator, LY353381.HCL, in metastatic breast cancer. J Clin Oncol. 2001;19:2002–2009
  17. Cotreau MM, Stonis L, Dykstra KH, et al. Multiple-dose, safety, pharmacokinetics, and pharmacodynamics of a new selective estrogen receptor modulator, ERA-923, in healthy postmenopausal women. J Clin Pharmacol. 2002;42:157–165
  18. Wakeling AE, Bowler J. Steroidal pure antioestrogens. J Endocrinol. 1987;112:R7–R10
  19. Wakeling AE, Dukes M, Bowler J. A potent specific pure antiestrogen with clinical potential. Cancer Res. 1991;51:3867–3873
  20. Osborne CK. Steroid hormone receptors in breast cancer management. Breast Cancer Res Treat. 1998;51:227–238
  21. Hu XF, Veroni M, De Luise M, et al. Circumvention of tamoxifen resistance by the pure anti-estrogen ICI 182,780. Int J Cancer. 1993;55:873–876
  22. McClelland RA, Gee JM, Francis AB, et al. Short-term effects of pure anti-oestrogen ICI 182780 treatment on oestrogen receptor, epidermal growth factor receptor and transforming growth factor-alpha protein expression in human breast cancer. Eur J Cancer A. 1996;32:413–416
  23. Nicholson RI, Gee JM, Francis AB, Manning DL, Wakeling AE, Katzenellenbogen BS. Observations arising from the use of pure antioestrogens on oestrogen-responsive (MCF-7) and oestrogen growth-independent (K3) human breast cancer cells. Endocr Relat Cancer. 1995;2:115–121
  24. Muller V, Jensen EV, Knabbe C. Partial antagonism between steroidal and nonsteroidal antiestrogens in human breast cancer cell lines. Cancer Res. 1998;58:263–267
  25. Osborne CK, Jarman M, McCague R, Coronado EB, Hilsenbeck SG, Wakeling AE. The importance of tamoxifen metabolism in tamoxifen-stimulated breast tumor growth. Cancer Chemother Pharmacol. 1994;34:89–95
  26. Robertson JF, Nicholson RI, Bundred NJ, 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;61:6739–6746
  27. Dukes M, Waterton JC, Wakeling AE. Antiuterotrophic effects of the pure antioestrogen ICI 182,780 in adult female monkeys (Macaca nemestrina): quantitative magnetic resonance imaging. J Endocrinol. 1993;138:203–210
  28. Addo S, Yates RA, 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;87:1354–1359
  29. Howell A, Osborne CK, Morris C, Wakeling AE. ICI 182,780 (Faslodex™): development of a novel, “pure” antiestrogen. Cancer. 2000;89:817–825
  30. Howell A, DeFriend DJ, Robertson JF, et al. Pharmacokinetics, pharmacological and anti-tumour effects of the specific anti-oestrogen ICI 182780 in women with advanced breast cancer. Br J Cancer. 1996;74:300–308
  31. Lundeen SG, Carver JM, McKean M-L, Winneker RC. Characterization of the ovariectomized rat model for the evaluation of estrogen effects on plasma cholesterol levels. Endocrinology. 1997;138:1552–1558
  32. Wade GN, Blaustein JD, Gray JM, Meredith JM. ICI 182,780: a pure antiestrogen that affects behaviors and energy balance in rats without acting in the brain. Am J Physiol. 1993;265(6 Pt 2):R1392–R1398
  33. Robertson JF, Osborne CK, 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;98:229–238
  34. Mauriac L, Pippen JE, Quaresma Albano J, Gertler SZ, Osborne CK. Fulvestr ant (Faslodex) versus anastrozole for the second-line treatment of advanced breast cancer in subgroups of postmenopausal women with visceral and non-visceral metastases: combined results from two multicentre trials. Eur J Cancer. 2003;39:1228–1233
  35. Howell A, Pippen J, Elledge R, et al. Fulvestrant versus anastrozole for the treatment of advanced breast cancer: a prospectively planned combined survival analysis of two multicenter trials. Cancer. 2005;104:236–239
  36. Howell A, Robertson JFR, Abram P, et al. Comparison of fulvestrant versus 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;22:1605–1613
  37. Perey L, Paridaens R, Nolé F, et al. Fulvestrant (Faslodex™) as hormonal treatment in postmenopausal patients with advanced breast cancer (ABC) progressing after treatment with tamoxifen and aromatase inhibitors: update of a phase II SAKK trial. Breast Cancer Res Treat. 2004;88(Suppl. 1):S236;[abstract 6048]
  38. Ingle JN, Rowland KM, Suman VJ, et al. Evaluation of fulvestrant in women with advanced breast cancer and progression on prior aromatase inhibitor therapy: a phase II trial of the North Central Cancer Treatment Group. In: Poster presentation at the San Antonio breast cancer symposium, 8–11 December, San Antonio, TX, USA; 2004 [poster 409].
  39. Ingle JN, Rowland KM, Suman VJ, et al. Evaluation of fulvestrant in women with advanced breast cancer and progression on prior aromatase inhibitor therapy: a phase II trial of the North Central Cancer Treatment Group. Breast Cancer Res Treat. 2004;88(Suppl. 1):S38;[abstract 409]
  40. Robertson JFR, Howell A, Gorbunova VA, Watanabe T, Pienkowski T, Lichinitser MR. Sensitivity to further endocrine therapy is retained following progression on first-line fulvestrant. Breast Cancer Res Treat. 2005;92:169–174
  41. Vergote I, Robertson JFR, Kleeberg U, Burton G, Osborne CK, Mauriac L. Postmenopausal women who progress on fulvestrant (‘Faslodex’) remain sensitive to further endocrine therapy. Breast Cancer Res Treat. 2003;79:207–211
  42. Paridaens R, Dirix L, Lohrisch C, et al. Mature results of a randomized phase II multicenter study of exemestane versus tamoxifen as first-line hormone therapy for postmenopausal women with metastatic breast cancer. Ann Oncol. 2003;14:1391–1398
  43. Kaufmann M, Bajetta E, Dirix LY, et al. Exemestane is superior to megestrol acetate after tamoxifen failure in postmenopausal women with advanced breast cancer: results of a phase III randomized double-blind trial. The Exemestane Study Group. J Clin Oncol. 2000;18:1399–1411

PII: S0305-7372(05)00140-4

doi: 10.1016/j.ctrv.2005.08.010

Cancer Treatment Reviews
Volume 31 , Pages S3-S9 , 2005

Article Tools

* Image Usage & Resolution