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Chemical Compound Review

SureCN1151787     3-[(Z)-1-[4-(2- dimethylaminoethoxy)phenyl]...

Synonyms: AC1NR4TW, ST51051233, I06-0595
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Disease relevance of Droloxifene

  • MATERIALS AND METHODS: Circulating NRP levels were determined in 94 patients who participated in a randomized trial of three different doses of the antiestrogen, droloxifene (DRO), as first-line HT for metastatic breast cancer [1].
  • However, tamoxifen has been shown to increase the risk of endometrial cancer which has stimulated research for new effective antiestrogens, such as droloxifene and toremifene [2].
  • The objective of this study was to determine the toxicity (and its reversibility) of droloxifene given at different doses to patients with advanced metastatic breast cancer refractory to conventional endocrine therapy and chemotherapy [3].
  • PURPOSE: This trial was designed to demonstrate equivalence between droloxifene 40 mg/d and tamoxifen 20 mg/d as first-line treatment in pre- and post-menopausal women with ER+ and/or PgR+ advanced breast cancer based on time to disease progression and tumor response [4].
  • Therefore, it can be assumed that Droloxifene may represent an important step forward in the treatment of mammary carcinomas in women through its better tolerability and increased efficacy compared with Tamoxifen [5].

High impact information on Droloxifene


Chemical compound and disease context of Droloxifene


Biological context of Droloxifene


Anatomical context of Droloxifene


Associations of Droloxifene with other chemical compounds


Gene context of Droloxifene

  • In patients in group 1, plasma lGF-I levels decreased by a mean value of 20% (P < 0.05) on treatment with droloxifene, while IGFBP-1 increased by a mean value of 45% (P > 0.1) [23].
  • Droloxifene increased SHBG and suppressed FSH at all dosages and suppressed LH at the 40 and 100 mg dosages [24].
  • Effects of droloxifene on apoptosis and Bax, Bcl-2 protein expression of luteal cells in pseudopregnant rats [25].
  • However, no obvious differences in the intensity or localization could be found during various days of the pseudopregnancy, while an increase in Bax and a decrease in Bcl-2 protein expression could be induced by droloxifene treatment [25].
  • We have confirmed this finding and also shown that the new anti-estrogen droloxifene inhibits the proliferation of epidermal growth factor (EGF) and insulin-like growth factor-I (IGF-I)-stimulated MCF-7 cells [26].

Analytical, diagnostic and therapeutic context of Droloxifene


  1. Prediction of response to antiestrogen therapy in advanced breast cancer patients by pretreatment circulating levels of extracellular domain of the HER-2/c-neu protein. Yamauchi, H., O'Neill, A., Gelman, R., Carney, W., Tenney, D.Y., Hösch, S., Hayes, D.F. J. Clin. Oncol. (1997) [Pubmed]
  2. Synthesis and reactivity of potential toxic metabolites of tamoxifen analogues: droloxifene and toremifene o-quinones. Yao, D., Zhang, F., Yu, L., Yang, Y., van Breemen, R.B., Bolton, J.L. Chem. Res. Toxicol. (2001) [Pubmed]
  3. Phase I trial of droloxifene in patients with metastatic breast cancer. Buzdar, A.U., Kau, S., Hortobagyi, G.N., Theriault, R.L., Booser, D., Holmes, F.A., Walters, R., Krakoff, I.H. Cancer Chemother. Pharmacol. (1994) [Pubmed]
  4. Phase III randomized trial of droloxifene and tamoxifen as first-line endocrine treatment of ER/PgR-positive advanced breast cancer. Buzdar, A., Hayes, D., El-Khoudary, A., Yan, S., Lønning, P., Lichinitser, M., Gopal, R., Falkson, G., Pritchard, K., Lipton, A., Wolter, K., Lee, A., Fly, K., Chew, R., Alderdice, M., Burke, K., Eisenber, P. Breast Cancer Res. Treat. (2002) [Pubmed]
  5. Preclinical data for Droloxifene. Hasmann, M., Rattel, B., Löser, R. Cancer Lett. (1994) [Pubmed]
  6. Estrogen and tamoxifen metabolites protect smooth muscle cell membrane phospholipids against peroxidation and inhibit cell growth. Dubey, R.K., Tyurina, Y.Y., Tyurin, V.A., Gillespie, D.G., Branch, R.A., Jackson, E.K., Kagan, V.E. Circ. Res. (1999) [Pubmed]
  7. Differential effects of E and droloxifene on C-reactive protein and other markers of inflammation in healthy postmenopausal women. Herrington, D.M., Brosnihan, K.B., Pusser, B.E., Seely, E.W., Ridker, P.M., Rifai, N., MacLean, D.B. J. Clin. Endocrinol. Metab. (2001) [Pubmed]
  8. The effect of droloxifene and estrogen on thyroid function in postmenopausal women. Marqusee, E., Braverman, L.E., Lawrence, J.E., Carroll, J.S., Seely, E.W. J. Clin. Endocrinol. Metab. (2000) [Pubmed]
  9. Cardiovascular effects of droloxifene, a new selective estrogen receptor modulator, in healthy postmenopausal women. Herrington, D.M., Pusser, B.E., Riley, W.A., Thuren, T.Y., Brosnihan, K.B., Brinton, E.A., MacLean, D.B. Arterioscler. Thromb. Vasc. Biol. (2000) [Pubmed]
  10. Common mechanism for the estrogen agonist and antagonist activities of droloxifene. Grasser, W.A., Pan, L.C., Thompson, D.D., Paralkar, V.M. J. Cell. Biochem. (1997) [Pubmed]
  11. Down-regulation of nitric oxide production by droloxifene and toremifene in human breast cancer cells. Martin, J.H., Symonds, A., Chohan, S. Oncol. Rep. (2003) [Pubmed]
  12. Influence of droloxifene on metastatic breast cancer as first-line endocrine treatment. Haarstad, H., Lønning, P.E., Gundersen, S., Wist, E., Raabe, N., Kvinnsland, S. Acta oncologica (Stockholm, Sweden) (1998) [Pubmed]
  13. Steroid hormone levels in patients with advanced breast cancer during therapy with droloxifene: a pilot study. Dalski, J., Görlich, M. Tumori. (1996) [Pubmed]
  14. Expression of functional estrogen receptors and galanin messenger ribonucleic acid in immortalized luteinizing hormone-releasing hormone neurons: estrogenic control of galanin gene expression. Shen, E.S., Meade, E.H., Pérez, M.C., Deecher, D.C., Negro-Vilar, A., López, F.J. Endocrinology (1998) [Pubmed]
  15. Apoptosis induced by droloxifene and c-myc, bax and bcl-2 mRNA expression in cultured luteal cells of rats. Leng, Y., Gu, Z.P., Cao, L. Eur. J. Pharmacol. (2000) [Pubmed]
  16. Effects of conjugated oestrogen and droloxifene on the renin-angiotensin system, blood pressure and renal blood flow in postmenopausal women. Seely, E.W., Brosnihan, K.B., Jeunemaitre, X., Okamura, K., Williams, G.H., Hollenberg, N.K., Herrington, D.M. Clin. Endocrinol. (Oxf) (2004) [Pubmed]
  17. Binding sites of droloxifene in the cytosol of 7,12-dimethylbenz[a]anthracene-induced rat mammary tumor cells. Kawamura, I., Lacey, E., Tanaka, Y., Nishigaki, F., Manda, T., Shimomura, K. Jpn. J. Cancer Res. (1994) [Pubmed]
  18. Estrogen-induced genes in the uterus of ovariectomized rats and their regulation by droloxifene and tamoxifen. Rivera-Gonzalez, R., Petersen, D.N., Tkalcevic, G., Thompson, D.D., Brown, T.A. J. Steroid Biochem. Mol. Biol. (1998) [Pubmed]
  19. Droloxifene (3-hydroxytamoxifen) has membrane antioxidant ability: potential relevance to its mechanism of therapeutic action in breast cancer. Wiseman, H., Smith, C., Halliwell, B., Cannon, M., Arnstein, H.R., Lennard, M.S. Cancer Lett. (1992) [Pubmed]
  20. In vitro efficacy of known P-glycoprotein modulators compared to droloxifene E and Z: studies on a human T-cell leukemia cell line and their resistant variants. Nüssler, V., Pelka-Fleisc, R., Gieseler, F., Hasmann, M., Löser, R., Gullis, E., Stötzer, O., Zwierzina, H., Wilmanns, W. Leuk. Lymphoma (1998) [Pubmed]
  21. Clastogenic and aneugenic effects of tamoxifen and some of its analogues in hepatocytes from dosed rats and in human lymphoblastoid cells transfected with human P450 cDNAs (MCL-5 cells). Styles, J.A., Davies, A., Davies, R., White, I.N., Smith, L.L. Carcinogenesis (1997) [Pubmed]
  22. Emerging selective estrogen receptor modulators: special focus on effects on coronary heart disease in postmenopausal women. Vogelvang, T.E., van der Mooren, M.J., Mijatovic, V., Kenemans, P. Drugs (2006) [Pubmed]
  23. Influence of droloxifene on plasma levels of insulin-like growth factor (IGF)-I, Pro-IGF-IIE, insulin-like growth factor binding protein (IGFBP)-1 and IGFBP-3 in breast cancer patients. Helle, S.I., Anker, G.B., Tally, M., Hall, K., Lønning, P.E. J. Steroid Biochem. Mol. Biol. (1996) [Pubmed]
  24. Droloxifene, a new antiestrogen: its role in metastatic breast cancer. Rauschning, W., Pritchard, K.I. Breast Cancer Res. Treat. (1994) [Pubmed]
  25. Effects of droloxifene on apoptosis and Bax, Bcl-2 protein expression of luteal cells in pseudopregnant rats. Leng, Y., Feng, Y., Cao, L., Gu, Z.P. Acta Pharmacol. Sin. (2001) [Pubmed]
  26. Inhibition of growth-factor-activated proliferation by anti-estrogens and effects on early gene expression of MCF-7 cells. Wosikowski, K., Küng, W., Hasmann, M., Löser, R., Eppenberger, U. Int. J. Cancer (1993) [Pubmed]
  27. Determination of droloxifene and two metabolites in serum by high-pressure liquid chromatography. Lien, E.A., Anker, G., Lønning, P.E., Ueland, P.M. Therapeutic drug monitoring. (1995) [Pubmed]
  28. Sensitive method for the quantitation of droloxifene in plasma and serum by high-performance liquid chromatography employing fluorimetric detection. Tess, D.A., Cole, R.O., Toler, S.M. J. Chromatogr. B, Biomed. Appl. (1995) [Pubmed]
  29. Intraperitoneal and intraportal administration of droloxifene to the Sprague-Dawley rat: assessing the first-pass effect. Nickerson, D.F., Toler, S.M. Xenobiotica (1997) [Pubmed]
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