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THE SELECTIVE ESTROGEN RECEPTOR DOWNREGULATOR FASLODEX® (FULVESTRANT)

Bundred N et al. ICI 182,780 (Faslodex) an estrogen receptor downregulator reduces cell turnover index more effectively than tamoxifen. Proc ASCO 2001;Abstract 1660.

Cicatiello L et al. The antiestrogen ICI 182,780 inhibits proliferation of human breast cancer cells by interfering with multiple, sequential estrogen-regulated processes required for cell cycle completion. Mol Cell Endocrinol 2000;165:199-209. Abstract

Curran M, Wiseman L. Fulvestrant. Drugs 2001;61:807-13; discussion 814. Abstract

Diel P et al. Treatment with the pure antiestrogen Faslodex (ICI 182780) increases the sensitivity of MCF-7 breast cancer cells against fas induced apoptosis. Breast Ca Res Treat 2000;Abstract 376.

England GM, Jordan VC. Pure antiestrogens as a new therapy for breast cancer. Oncol Res 1997;9:397-402. Abstract

Erikstein B et al. ICI 182,780 (‘Faslodex’) 250 mg monthly intramuscular (i.m.) injection shows consistent pk profile when given as either 1 x 5ml or 2 x 2.5 ml injections in postmenopausal women with advanced breast cancer (ABC). Proc ASCO 2001;Abstract 2025.

Gradishar WJ, Jordan VC. Clinical potential of new antiestrogens. J Clin Oncol 1997;15:840-52. Abstract

Howell A et al. Comparison of efficacy and tolerability of fulvestrant (Faslodex) with anastrozole (Arimidex) in post-menopausal women with advanced breast cancer. Breast Ca Res Treat 2000;64(1):Abstract 6. No Abstract Available.

Howell A et al. ICI 182,780 (Faslodex): Development of a novel, “pure” antiestrogen. Cancer 2000;89(4):817-825. Abstract

Howell A et al. Response to a specific antioestrogen (ICI 182780) in tamoxifen-resistant breast cancer. Lancet 1995;345:29-30. No Abstract Available.

Howell A 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;74:300-8. Abstract

Long BJ et al. The steroidal antiestrogen ICI 182,780 is an inhibitor of cellular aromatase activity. J Steroid Biochem Mol Biol 1998;67:293-304. Abstract

McClelland RA et al. Enhanced epidermal growth factor receptor signaling in MCF7 breast cancer cells after long-term culture in the presence of the pure antiestrogen ICI 182,780 (Faslodex). Endocrinology 2001;142:2776-88. Abstract

O'Regan RM et al. Effects of the antiestrogens tamoxifen, toremifene, and ICI 182,780 on endometrial cancer growth. J Natl Cancer Inst 1998;90: 1552-8. Abstract

Osborne CK 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. Abstract

Osborne CK. A Double-blind randomized trial comparing the efficacy and tolerability of Faslodex™ (fulvestrant) with Arimidex™ (anastrozole) in post-menopausal (PM) women with advanced breast cancer (ABC). Breast Ca Res Treat 2000;64(1):Abstract 7.No Abstract Available.

Osborne CK et al. Selective estrogen receptor modulators: Structure, function, and clinical use. J Clin Oncol 2000;18(17):3172-3186. Abstract

Robertson JFR et al. The pharmacokinetics of single dose Faslodex ™ (ICI 182,780) in postmenopausal primary breast cancer - relationship with estrogen receptor (ER) down regulation. Proc ASCO 2000;Abstract 362.

Robertson JF 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 Sep 15;61(18):6739-46. Abstract

Robertson JFR. A comparison of the single-dose pharmacokinetics (PK) of 'Faslodex' (fulvestrant) 250 mg when given as either a one x 5-ml intramuscular (i.m.) injection or two x 2.5-ml injections in postmenopausal (PM) women with advanced breast cancer (ABC). Breast Ca Res Treat 2000; Abstract 172. No Abstract Available.

Robertson JFR et al. Duration of remission to ICI 182,780 compared to megestrol acetate in tamoxifen-resistant breast cancer. Breast 1997;6:186-9. No Abstract Available.

Rosenberg Z et al. Is ICI 182,780 an antiprogestin in addition to being an antiestrogen? Breast Cancer Res Treat 2000;60:1-8. No Abstract Available.

SLIDE PRESENTATIONS

Targeting the estrogen receptor for destruction: New therapeutic opportunities in the treatment of breast cancer. Richard M. Elledge, MD, Baylor College of Medicine. Presented at the Chemotherapy Foundation Symposium XVIII Web link

ICI 182,780 ('Faslodex'): An estrogen receptor downregulator — Targeted therapy for breast cancer. V Craig Jordan, PhD, DSc Web link

FIRST-TIME HORMONAL THERAPY FOR ADVANCED BREAST CANCER

Buzdar A et al. Phase III, multicenter, double-blind, randomized study of letrozole, an aromatase inhibitor, for advanced breast cancer versus megestrol acetate. J Clin Oncol 2001;19:3357-3366. Abstract

Buzdar A et al. Anastrozole versus megestrol acetate in the treatment of postmenopausal women with advanced breast carcinoma: Results of a survival update based on a combined analysis of data from two mature phase III trials. Arimidex Study Group. Cancer 1998;83:1142-1152. Abstract

Bonneterre JB et al. Anastrazole versus tamoxifen as first-line therapy for advanced breast cancer in 668 postmenopausal women: Results of the Tamoxifen or Arimidex Randomized Group Efficacy and Tolerability study. J Clin Oncol 2000;18:3748-3757. Abstract

Bonneterre J et al. Anastrozole is superior to tamoxifen as first-line therapy in hormone receptor-positive advanced breast carcinoma: Results of two randomized trials designed for combined analysis. Cancer 2001;92(9):2247- 2258. Abstract

Mouridsen H et al. Superior efficacy of letrozole versus tamoxifen as first-line therapy for postmenopausal women with advanced breast cancer: Results of a phase III study of the International Letrozole Breast Cancer Group. J Clin Oncol 2001;19(10):2596-606. Abstract

Nabholtz JM et al. Anastrozole is superior to tamoxifen as first-line therapy for advanced breast cancer in postmenopausal women: Results of a North American multicenter randomized trial. Arimidex Study Group. J Clin Oncol 2000;18(22):3758-67. Abstract

Vergote IJ et al. Randomised study of anastrozole versus tamoxifen as firstline therapy for advanced breast cancer in postmenopausal women. Eur J Cancer 2000;36(Suppl 4):S84-85. Abstract

OTHER RESOURCES

National Comprehensive Cancer Network (NCCN) Website Web Link

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