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[Cancer Research 51, 3867-3873, August 1, 1991]
© 1991 American Association for Cancer Research

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A Potent Specific Pure Antiestrogen with Clinical Potential

Alan E. Wakeling1, Michael Dukes and Jean Bowler

Bioscience I [A. E. W., M. D.] and Chemistry I [J. B.], ICI Pharmaceuticals, Mereside, Alderley Park, Macclesfield, Cheshire SK10 4TG, United Kingdom

Previous studies from this laboratory have described a series of 7{alpha}-alkylamide analogues of estradiol with pure antiestrogenic activity, exemplified by ICI 164,384. A new compound, 7{alpha}-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]estra-1,3,5(10)-triene-3,17ß-diol (ICI 182,780) has now been identified which has significantly increased antiestrogenic potency and retains pure estrogen antagonist activity. The antiuterotrophic potency of ICI 182,780 in the immature rat was more than 10-fold greater than that of ICI 164,384 (50% effective doses of 0.06 and 0.9 mg/kg, respectively). This order of magnitude increase of in vivo potency was also reflected, in part, by intrinsic activity at the estrogen receptor. The relative binding affinities of ICI 182,780 and ICI 164,384 were 0.89 and 0.19, respectively, compared with that of estradiol (1.0). Similarly, the in vitro growth-inhibitory potency of ICI 182,780 exceeded that of ICI 164,384 in MCF-7 human breast cancer cells, where 50% inhibitory concentrations of 0.29 and 1.3 nM, respectively, were recorded. ICI 182,780 was a more effective inhibitor of MCF-7 growth than 4'-hydroxytamoxifen, producing an 80% reduction of cell number under conditions where 4'-hydroxytamoxifen achieved a maximum of 50% inhibition. This increased efficacy was reflected by a greater reduction of the proportion of cells engaged in DNA synthesis in ICI 182,780-treated cell cultures compared with tamoxifen-treated cells.

Sustained antiestrogenic effects, following a single parenteral dose of ICI 182,780 in oil suspension, were apparent in both rats and pigtail monkeys. In vivo, antitumor activity of ICI 182,780 was demonstrated with xenografts of MCF-7 and Br10 human breast cancers in nude mice. A single injection of ICI 182,780 provided antitumor efficacy equivalent to that of daily tamoxifen treatment for at least 4 weeks.

The properties of ICI 182,780 identify this pure antiestrogen as a prime candidate with which to evaluate the potential therapeutic benefits of complete estrogen withdrawal in endocrine-responsive human breast cancer.

1 To whom requests for reprints should be addressed.

Received 4/10/91. Accepted 5/21/91.




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J. Pharmacol. Exp. Ther.Home page
E. A. Booth, M. Marchesi, E. J. Kilbourne, and B. R. Lucchesi
17{beta}-Estradiol as a Receptor-Mediated Cardioprotective Agent
J. Pharmacol. Exp. Ther., October 1, 2003; 307(1): 395 - 401.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
J. S. Carroll, D. K. Lynch, A. Swarbrick, J.-M. Renoir, B. Sarcevic, R. J. Daly, E. A. Musgrove, and R. L. Sutherland
p27Kip1 Induces Quiescence and Growth Factor Insensitivity in Tamoxifen-treated Breast Cancer Cells
Cancer Res., August 1, 2003; 63(15): 4322 - 4326.
[Abstract] [Full Text] [PDF]


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Arch SurgHome page
K. E. Calhoun, R. F. Pommier, P. Muller, W. S. Fletcher, and S. Toth-Fejel
Dehydroepiandrosterone Sulfate Causes Proliferation of Estrogen Receptor-Positive Breast Cancer Cells Despite Treatment With Fulvestrant
Arch Surg, August 1, 2003; 138(8): 879 - 883.
[Abstract] [Full Text] [PDF]


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Ann OncolHome page
M. Piccart, L. M. Parker, and K. I. Pritchard
Oestrogen receptor downregulation: an opportunity for extending the window of endocrine therapy in advanced breast cancer
Ann. Onc., July 1, 2003; 14(7): 1017 - 1025.
[Abstract] [Full Text] [PDF]


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J. Biol. Chem.Home page
S. T. Pearce, H. Liu, and V. C. Jordan
Modulation of Estrogen Receptor alpha Function and Stability by Tamoxifen and a Critical Amino Acid (Asp-538) in Helix 12
J. Biol. Chem., February 21, 2003; 278(9): 7630 - 7638.
[Abstract] [Full Text] [PDF]


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Clin. Cancer Res.Home page
M. Dowsett
Preoperative Models to Evaluate Endocrine Strategies for Breast Cancer
Clin. Cancer Res., January 1, 2003; 9(1): 502s - 510s.
[Abstract] [Full Text]


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CarcinogenesisHome page
M. S. Cotroneo, J. Wang, W. A. Fritz, I.-E. Eltoum, and C. A. Lamartiniere
Genistein action in the prepubertal mammary gland in a chemoprevention model
Carcinogenesis, September 1, 2002; 23(9): 1467 - 1474.
[Abstract] [Full Text] [PDF]


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JCOHome page
C.K. Osborne, J. Pippen, S.E. Jones, L.M. Parker, M. Ellis, S. Come, S.Z. Gertler, J.T. May, G. Burton, I. Dimery, 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., August 15, 2002; 20(16): 3386 - 3395.
[Abstract] [Full Text] [PDF]


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JCOHome page
A. Howell, J.F.R. Robertson, J. Quaresma Albano, A. Aschermannova, L. Mauriac, U.R. Kleeberg, I. Vergote, B. Erikstein, A. Webster, and C. Morris
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., August 15, 2002; 20(16): 3396 - 3403.
[Abstract] [Full Text] [PDF]


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J. Pharmacol. Exp. Ther.Home page
L. M. Ickenstein and S. M. Bandiera
Persistent Suppression of Hepatic CYP2A1 Expression and Serum Triiodothyronine Levels by Tamoxifen in Intact Female Rats: Dose-Response Analysis and Comparison with 4-Hydroxytamoxifen, Fulvestrant (ICI 182,780), and 17beta -Estradiol-3-benzoate
J. Pharmacol. Exp. Ther., August 1, 2002; 302(2): 584 - 593.
[Abstract] [Full Text] [PDF]


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Toxicol SciHome page
G. D. Charles, C. Gennings, T. R. Zacharewski, B. B. Gollapudi, and E. W. Carney
An Approach for Assessing Estrogen Receptor-Mediated Interactions in Mixtures of Three Chemicals: A Pilot Study
Toxicol. Sci., August 1, 2002; 68(2): 349 - 360.
[Abstract] [Full Text] [PDF]


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EndocrinologyHome page
C. J. Thompson, N. N. C. Tam, J. M. Joyce, I. Leav, and S.-m. Ho
Gene Expression Profiling of Testosterone and Estradiol-17{beta}-Induced Prostatic Dysplasia in Noble Rats and Response to the Antiestrogen ICI 182,780
Endocrinology, June 1, 2002; 143(6): 2093 - 2105.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
J. S. Carroll, A. Swarbrick, E. A. Musgrove, and R. L. Sutherland
Mechanisms of Growth Arrest by c-myc Antisense Oligonucleotides in MCF-7 Breast Cancer Cells: Implications for the Antiproliferative Effects of Antiestrogens
Cancer Res., June 1, 2002; 62(11): 3126 - 3131.
[Abstract] [Full Text] [PDF]


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Am. J. Respir. Cell Mol. Bio.Home page
T. S. Sherman, K. L. Chambliss, L. L. Gibson, M. C. Pace, M. E. Mendelsohn, S. L. Pfister, and P. W. Shaul
Estrogen Acutely Activates Prostacyclin Synthesis in Ovine Fetal Pulmonary Artery Endothelium
Am. J. Respir. Cell Mol. Biol., May 1, 2002; 26(5): 610 - 616.
[Abstract] [Full Text] [PDF]


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J. Appl. Physiol.Home page
S. G. Hayes, N. B. Moya Del Pino, and M. P. Kaufman
Estrogen attenuates the cardiovascular and ventilatory responses to central command in cats
J Appl Physiol, April 1, 2002; 92(4): 1635 - 1641.
[Abstract] [Full Text] [PDF]


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HypertensionHome page
M. E. Beyer, G. Yu, H. Hanke, and H. M. Hoffmeister
Acute Gender-Specific Hemodynamic and Inotropic Effects of 17{beta}-Estradiol on Rats
Hypertension, November 1, 2001; 38(5): 1003 - 1010.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
J. F. Robertson, R. I. Nicholson, N. J. Bundred, E. Anderson, Z. Rayter, M. Dowsett, J. N. Fox, J. M. W. Gee, A. Webster, A. E. Wakeling, et al.
Comparison of the Short-Term Biological Effects of 7{alpha}-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)-nonyl]estra-1,3,5, (10)-triene-3,17{beta}-diol (Faslodex) versus Tamoxifen in Postmenopausal Women with Primary Breast Cancer
Cancer Res., September 1, 2001; 61(18): 6739 - 6746.
[Abstract] [Full Text] [PDF]


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Clin. Cancer Res.Home page
T. W. Chan, M. Pollak, and H. Huynh
Inhibition of Insulin-like Growth Factor Signaling Pathways in Mammary Gland by Pure Antiestrogen ICI 182,780
Clin. Cancer Res., August 1, 2001; 7(8): 2545 - 2554.
[Abstract] [Full Text] [PDF]


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JCBHome page
E. Bonnelye, L. Merdad, V. Kung, and J.E. Aubin
The Orphan Nuclear Estrogen Receptor-Related Receptor {alpha} (Err{alpha}) Is Expressed Throughout Osteoblast Differentiation and Regulates Bone Formation in Vitro
J. Cell Biol., May 28, 2001; 153(5): 971 - 984.
[Abstract] [Full Text] [PDF]


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J. Pharmacol. Exp. Ther.Home page
G. A. Figtree, C. M. Webb, and P. Collins
Tamoxifen Acutely Relaxes Coronary Arteries by an Endothelium-, Nitric Oxide-, and Estrogen Receptor-Dependent Mechanism
J. Pharmacol. Exp. Ther., November 1, 2000; 295(2): 519 - 523.
[Abstract] [Full Text]


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Am. J. Physiol. Cell Physiol.Home page
M. E. Nuttall, G. B. Stroup, P. W. Fisher, D. P. Nadeau, M. Gowen, and L. J. Suva
Distinct mechanisms of action of selective estrogen receptor modulators in breast and osteoblastic cells
Am J Physiol Cell Physiol, November 1, 2000; 279(5): C1550 - C1557.
[Abstract] [Full Text] [PDF]


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JCOHome page
C. K. Osborne and S. A. W. Fuqua
Selective Estrogen Receptor Modulators: Structure, Function, and Clinical Use
J. Clin. Oncol., September 17, 2000; 18(17): 3172 - 3186.
[Abstract] [Full Text] [PDF]


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JNCI J Natl Cancer InstHome page
X. Chen, C. Danes, M. Lowe, T. W. Herliczek, and K. Keyomarsi
Activation of the Estrogen-Signaling Pathway by p21WAF1/CIP1 in Estrogen Receptor-Negative Breast Cancer Cells
J Natl Cancer Inst, September 6, 2000; 92(17): 1403 - 1413.
[Abstract] [Full Text] [PDF]


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Toxicol SciHome page
J. Odum and J. Ashby
Neonatal Exposure of Male Rats to Nonylphenol Has No Effect on the Reproductive Tract
Toxicol. Sci., August 1, 2000; 56(2): 400 - 404.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
A. Gandhi, P. A. Holland, W. F. Knox, C. S. Potten, and N. J. Bundred
Effects of a Pure Antiestrogen on Apoptosis and Proliferation within Human Breast Ductal Carcinoma in Situ
Cancer Res., August 1, 2000; 60(15): 4284 - 4288.
[Abstract] [Full Text]


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Arterioscler. Thromb. Vasc. Bio.Home page
P. Parini, B. Angelin, A. Stavreus-Evers, B. Freyschuss, H. Eriksson, and M. Rudling
Biphasic Effects of the Natural Estrogen 17{beta}-Estradiol on Hepatic Cholesterol Metabolism in Intact Female Rats
Arterioscler Thromb Vasc Biol, July 1, 2000; 20(7): 1817 - 1823.
[Abstract] [Full Text] [PDF]


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J Am Coll CardiolHome page
G. A. Figtree, H. Griffiths, Y.-Q. Lu, C. M. Webb, K. MacLeod, and P. Collins
Plant-derived estrogens relax coronary arteries in vitro by a calcium antagonistic mechanism
J. Am. Coll. Cardiol., June 1, 2000; 35(7): 1977 - 1985.
[Abstract] [Full Text] [PDF]


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Toxicol SciHome page
G. D. Charles, M. J. Bartels, T. R. Zacharewski, B. B. Gollapudi, N. L. Freshour, and E. W. Carney
Activity of Benzo[a]pyrene and Its Hydroxylated Metabolites in an Estrogen Receptor-{alpha} Reporter Gene Assay
Toxicol. Sci., June 1, 2000; 55(2): 320 - 326.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
K.-M. Lau, M. LaSpina, J. Long, and S.-M. Ho
Expression of Estrogen Receptor (ER)-{{alpha}} and ER-{beta} in Normal and Malignant Prostatic Epithelial Cells: Regulation by Methylation and Involvement in Growth Regulation
Cancer Res., June 1, 2000; 60(12): 3175 - 3182.
[Abstract] [Full Text]


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Toxicol PatholHome page
S. Kennedy
Endocrine Disruptors: Overview and a Pathologist's Perspective
Toxicol Pathol, May 1, 2000; 28(3): 418 - 419.
[PDF]


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BloodHome page
J. Komi and O. Lassila
Nonsteroidal anti-estrogens inhibit the functional differentiation of human monocyte-derived dendritic cells
Blood, May 1, 2000; 95(9): 2875 - 2882.
[Abstract] [Full Text] [PDF]


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Toxicol SciHome page
L. C. Hodges, J. S. Bergerson, D. S. Hunter, and C. L. Walker
Estrogenic Effects of Organochlorine Pesticides on Uterine Leiomyoma Cells in Vitro
Toxicol. Sci., April 1, 2000; 54(2): 355 - 364.
[Abstract] [Full Text] [PDF]


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CirculationHome page
A. Huang, D. Sun, A. Koller, and G. Kaley
17{beta}-Estradiol Restores Endothelial Nitric Oxide Release to Shear Stress in Arterioles of Male Hypertensive Rats
Circulation, January 4, 2000; 101(1): 94 - 100.
[Abstract] [Full Text] [PDF]


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Mol Hum ReprodHome page
K. C. Reinhart, R. K. Dubey, P. J. Keller, U. Lauper, and M. Rosselli
Xeno-oestrogens and phyto-oestrogens induce the synthesis of leukaemia inhibitory factor by human and bovine oviduct cells
Mol. Hum. Reprod., October 1, 1999; 5(10): 899 - 907.
[Abstract] [Full Text] [PDF]


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Proc. Natl. Acad. Sci. USAHome page
M. Sabbah, D. Courilleau, J. Mester, and G. Redeuilh
Estrogen induction of the cyclin D1 promoter: Involvement of a cAMP response-like element
PNAS, September 28, 1999; 96(20): 11217 - 11222.
[Abstract] [Full Text] [PDF]


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CirculationHome page
G. A. Figtree, Y.-q. Lu, C. M. Webb, and P. Collins
Raloxifene Acutely Relaxes Rabbit Coronary Arteries In Vitro by an Estrogen Receptor–Dependent and Nitric Oxide–Dependent Mechanism
Circulation, September 7, 1999; 100(10): 1095 - 1101.
[Abstract] [Full Text] [PDF]


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Cancer Res.Home page
J. I. MacGregor Schafer, H. Liu, D. A. Tonetti, and V. C. Jordan
The Interaction of Raloxifene and the Active Metabolite of the Antiestrogen EM-800 (SC 5705) with the Human Estrogen Receptor
Cancer Res., September 1, 1999; 59(17): 4308 - 4313.
[Abstract] [Full Text] [PDF]


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EndocrinologyHome page
D. Ghosh, J. A. Taylor, J. A. Green, and D. B. Lubahn
Methoxychlor Stimulates Estrogen-Responsive Messenger Ribonucleic Acids in Mouse Uterus through a Non-Estrogen Receptor (Non-ER){alpha} and Non-ER{beta} Mechanism
Endocrinology, August 1, 1999; 140(8): 3526 - 3533.
[Abstract] [Full Text]




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