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Oncology and Molecular Endocrinology Research Center, Laval University Medical Center and Laval University, Québec, Canada G1V 4G2
Address all correspondence and requests for reprints to: Professor Fernand Labrie, Oncology and Molecular Endocrinology Research Center, Laval University Medical Center (CHUL), 2705 Laurier Boulevard, Quebec City, Quebec, Canada G1V 4G2. E-mail: fernand.labrie{at}crchul.ulaval.ca.
The Women’s Health Initiative Study and other reports have created major uncertainty among postmenopausal women and physicians concerning hormone replacement therapy. We have thus investigated the possibility of replacing the progestin in hormone replacement therapy by a novel selective estrogen receptor (ER) modulator having potent and pure antiestrogenic activity in the mammary gland and uterus. As measured by changes in histology and Cdc47 labeling in the rat model, the present study shows that the stimulatory effect of estradiol in the mammary gland and uterus is efficiently blocked by simultaneous administration of the novel selective ER modulator EM-652, but bone mineral density is preserved and serum cholesterol is decreased. After the administration of 14C-labeled EM-652, we observed that there is no detectable radioactivity in the brain. Moreover, ER
immunoreactivity remained constant in the hypothalamus after EM-652 treatment, whereas ER became almost undetectable in the mammary gland and uterus. The present data show the poor or absent access of EM-652 to the brain, whereas the effects of estrogens are efficiently neutralized in the mammary gland and uterus. Such data support the exciting possibility of a novel approach that could meet most of the needs of women’s health at menopause, namely control of hot flushes and prevention of breast, uterine, and ovarian cancer as well as osteoporosis and potentially helping brain function and preventing Alzheimer’s disease with no identifiable risk or negative effect.
This article has been cited by other articles:
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  F Labrie Future perspectives of selective estrogen receptor modulators used alone and in combination with DHEA. Endocr. Relat. Cancer, June 1, 2006; 13(2): 335 - 355. [Abstract] [Full Text] [PDF]
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 V. Luu-The, P. Tremblay, and F. Labrie Characterization of Type 12 17{beta}-Hydroxysteroid Dehydrogenase, an Isoform of Type 3 17{beta}-Hydroxysteroid Dehydrogenase Responsible for Estradiol Formation in Women Mol. Endocrinol., February 1, 2006; 20(2): 437 - 443. [Abstract] [Full Text] [PDF]
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 F Labrie, V Luu-The, A Belanger, S-X Lin, J Simard, G Pelletier, and C Labrie Is dehydroepiandrosterone a hormone? J. Endocrinol., November 1, 2005; 187(2): 169 - 196. [Abstract] [Full Text] [PDF]
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 D. G. Rudmann, I. R. Cohen, M. R. Robbins, D. E. Coutant, and J. W. Henck Androgen Dependent Mammary Gland Virilism in Rats Given the Selective Estrogen Receptor Modulator LY2066948 Hydrochloride Toxicol Pathol, October 1, 2005; 33(6): 711 - 719. [Abstract] [Full Text] [PDF]
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 J. L. Turgeon, D. P. McDonnell, K. A. Martin, and P. M. Wise Hormone Therapy: Physiological Complexity Belies Therapeutic Simplicity Science, May 28, 2004; 304(5675): 1269 - 1273. [Abstract] [Full Text] [PDF]
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 G. E. Hoffman and S. L. Zup Good Versus Evil: Changing the Approach to Hormone Replacement Therapy Endocrinology, November 1, 2003; 144(11): 4698 - 4699. [Full Text] [PDF]
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