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2002 1
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Page 1
Clinical Trial of Acolbifene in Premenopausal Women at High Risk for Breast Cancer.
Fabian CJ, Kimler BF, Zalles CM, Phillips TA, Metheny T, Petroff BK, Havighurst TC, Kim K, Bailey HH, Heckman-Stoddard BM. Fabian CJ, et al. Cancer Prev Res (Phila). 2015 Dec;8(12):1146-55. doi: 10.1158/1940-6207.CAPR-15-0109. Epub 2015 Sep 21. Cancer Prev Res (Phila). 2015. PMID: 26391916 Free PMC article. Clinical Trial.
The purpose of this study was to assess the feasibility of using the selective estrogen receptor modulator (SERM) acolbifene as a breast cancer prevention agent in premenopausal women. ...Ki-67 decreased from a median of 4.6% [interquartile range (IQR), 3.1%-8.5%] at basel …
The purpose of this study was to assess the feasibility of using the selective estrogen receptor modulator (SERM) acolbifene as a bre …
Bioactivation of the selective estrogen receptor modulator acolbifene to quinone methides.
Liu J, Liu H, van Breemen RB, Thatcher GR, Bolton JL. Liu J, et al. Chem Res Toxicol. 2005 Feb;18(2):174-82. doi: 10.1021/tx0497752. Chem Res Toxicol. 2005. PMID: 15720121
The majority of GSH conjugates resulted from reaction of the classical acolbifene quinone methide with GSH. Incubations of acolbifene with GSH and either tyrosinase or human and rat liver microsomes also produced acolbifene quinone methide-GSH conjugates. ... …
The majority of GSH conjugates resulted from reaction of the classical acolbifene quinone methide with GSH. Incubations of acolbif …
Emerging hormonal treatments for menopausal symptoms.
Genazzani AR, Komm BS, Pickar JH. Genazzani AR, et al. Expert Opin Emerg Drugs. 2015 Mar;20(1):31-46. doi: 10.1517/14728214.2015.986093. Epub 2015 Jan 5. Expert Opin Emerg Drugs. 2015. PMID: 25557757 Review.
Investigational treatments discussed include two new vaginal estrogen products (TX-004HR, WC-3011); the first combination of estradiol and progesterone, and a novel combination of dehydroepiandrosterone and acolbifene. We also review a new selective estrogen receptor modul …
Investigational treatments discussed include two new vaginal estrogen products (TX-004HR, WC-3011); the first combination of estradiol and p …
Synthesis and structure-activity relationships of analogs of EM-652 (acolbifene), a pure selective estrogen receptor modulator. Study of nitrogen substitution.
Gauthier S, Cloutier J, Dory YL, Favre A, Mailhot J, Ouellet C, Schwerdtfeger A, Mérand Y, Martel C, Simard J, Labrie F. Gauthier S, et al. J Enzyme Inhib Med Chem. 2005 Apr;20(2):165-77. doi: 10.1080/14756360500043448. J Enzyme Inhib Med Chem. 2005. PMID: 15968821
EM-652 (acolbifene) analogs have been synthesized as selective estrogen receptor modulators. ...
EM-652 (acolbifene) analogs have been synthesized as selective estrogen receptor modulators. ...
Identification of novel proteins induced by estradiol, 4-hydroxytamoxifen and acolbifene in T47D breast cancer cells.
Al-Dhaheri MH, Shah YM, Basrur V, Pind S, Rowan BG. Al-Dhaheri MH, et al. Steroids. 2006 Nov;71(11-12):966-78. doi: 10.1016/j.steroids.2006.07.006. Epub 2006 Sep 1. Steroids. 2006. PMID: 16949628
Six proteins were identified that were differentially regulated by 17beta-estradiol, 4-hydroxytamoxifen and the pure antagonist acolbifene (EM-652); calreticulin, synapse associated protein 1 (SYAP1), CD2 antigen binding protein 2 (CD2BP2), nucleosome assembly protein 1 li …
Six proteins were identified that were differentially regulated by 17beta-estradiol, 4-hydroxytamoxifen and the pure antagonist acolbifen …
Hypocholesterolemic action of the selective estrogen receptor modulator acolbifene in intact and ovariectomized rats with diet-induced hypercholesterolemia.
Lemieux C, Gélinas Y, Lalonde J, Labrie F, Richard D, Deshaies Y. Lemieux C, et al. Metabolism. 2006 May;55(5):605-13. doi: 10.1016/j.metabol.2005.11.016. Metabolism. 2006. PMID: 16631436
Acolbifene (ACOL) is a fourth-generation selective estrogen receptor modulator (SERM) that has strong and pure antiestrogenic properties toward estrogen-sensitive cancers, but improves energy and lipid metabolism in an estrogen-like fashion in rodent models. ...Intact and …
Acolbifene (ACOL) is a fourth-generation selective estrogen receptor modulator (SERM) that has strong and pure antiestrogenic propert …
Hypolipidemic action of the SERM acolbifene is associated with decreased liver MTP and increased SR-BI and LDL receptors.
Lemieux C, Gélinas Y, Lalonde J, Labrie F, Cianflone K, Deshaies Y. Lemieux C, et al. J Lipid Res. 2005 Jun;46(6):1285-94. doi: 10.1194/jlr.M400448-JLR200. Epub 2005 Mar 1. J Lipid Res. 2005. PMID: 15741653 Free article.
This study aimed to identify the mechanisms of the hypolipidemic action of the selective estrogen receptor modulator (SERM) acolbifene (ACOL). Four weeks of treatment with ACOL reduced fasting and postprandial plasma triglycerides (TGs), an effect associated with lower VLD …
This study aimed to identify the mechanisms of the hypolipidemic action of the selective estrogen receptor modulator (SERM) acolbifene …
The selective estrogen receptor modulator acolbifene reduces cholesterolemia independently of its anorectic action in control and cholesterol-fed rats.
Lemieux C, Gélinas Y, Lalonde J, Labrie F, Richard D, Deshaies Y. Lemieux C, et al. J Nutr. 2005 Sep;135(9):2225-9. doi: 10.1093/jn/135.9.2225. J Nutr. 2005. PMID: 16140902 Free article.
The cancer-preventing selective estrogen receptor modulator (SERM) acolbifene (ACOL) exerts a potent and pure antiestrogenic action in the mammary gland and uterus, yet it displays beneficial, estrogen-like actions on energy and lipid metabolism in rodents. ...
The cancer-preventing selective estrogen receptor modulator (SERM) acolbifene (ACOL) exerts a potent and pure antiestrogenic action i …
Activity and safety of the antiestrogen EM-800, the orally active precursor of acolbifene, in tamoxifen-resistant breast cancer.
Labrie F, Champagne P, Labrie C, Roy J, Laverdière J, Provencher L, Potvin M, Drolet Y, Pollak M, Panasci L, L'Espérance B, Dufresne J, Latreille J, Robert J, Samson B, Jolivet J, Yelle L, Cusan L, Diamond P, Candas B. Labrie F, et al. J Clin Oncol. 2004 Mar 1;22(5):864-71. doi: 10.1200/JCO.2004.05.122. J Clin Oncol. 2004. PMID: 14990642 Clinical Trial.
PURPOSE: To determine the efficacy and safety of EM-800 (SCH-57050), the precursor of acolbifene, a new, highly potent, orally active, pure antiestrogen in the mammary gland and endometrium, for the treatment of tamoxifen-resistant breast cancer. ...
PURPOSE: To determine the efficacy and safety of EM-800 (SCH-57050), the precursor of acolbifene, a new, highly potent, orally active …
Estrogen receptors as therapeutic targets in breast cancer.
Ariazi EA, Ariazi JL, Cordera F, Jordan VC. Ariazi EA, et al. Curr Top Med Chem. 2006;6(3):181-202. Curr Top Med Chem. 2006. PMID: 16515478 Review.
Other SERMs approved or under development for use against breast cancer or osteoporosis include toremifene, GW5638, GW7604 (the active metabolite of GW5638), idoxifene, lasofoxifene, arzoxifene, bazedoxifene, EM-800 and acolbifene (the active metabolite of EM-800). Aromata …
Other SERMs approved or under development for use against breast cancer or osteoporosis include toremifene, GW5638, GW7604 (the active metab …
25 results