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Chemical Compound Review

Arzoxifene     2-(4-methoxyphenyl)-3-[4-[2- (1...

Synonyms: CHEMBL226267, SureCN285277, DNC007422, AC1L4522, LY 353381, ...
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Disease relevance of Arzoxifene


High impact information on Arzoxifene


Chemical compound and disease context of Arzoxifene


Biological context of Arzoxifene


Anatomical context of Arzoxifene

  • Uteri wet weight from arzoxifene animals was 38-40% of sham compared with OVX rats, which were 29% of sham [3].
  • Histomorphometry of the PTM showed that arzoxifene prevented bone loss by reducing osteoclast number in OVX rats [3].
  • Compression testing of the vertebra and three-point bending testing of femoral shaft showed that strength and toughness were higher for arzoxifene-treated animals compared with OVX animals [3].
  • A new MCF-7 breast cancer cell line resistant to the arzoxifene metabolite desmethylarzoxifene [13].

Associations of Arzoxifene with other chemical compounds

  • PURPOSE: Arzoxifene, a new selective estrogen receptor modulator with strong breast antiestrogen activity and absence of uterine agonist activity, was explored as a potential chemoprevention agent [4].
  • Paclitaxel or 5-FU alone had minor effects to delay the appearance of xenografts whereas arzoxifene alone caused longer delay [7].

Gene context of Arzoxifene


Analytical, diagnostic and therapeutic context of Arzoxifene


  1. Phase II, randomized, double-blind study of two dose levels of arzoxifene in patients with locally advanced or metastatic breast cancer. Buzdar, A., O'Shaughnessy, J.A., Booser, D.J., Pippen, J.E., Jones, S.E., Munster, P.N., Peterson, P., Melemed, A.S., Winer, E., Hudis, C. J. Clin. Oncol. (2003) [Pubmed]
  2. Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer. Suh, N., Glasebrook, A.L., Palkowitz, A.D., Bryant, H.U., Burris, L.L., Starling, J.J., Pearce, H.L., Williams, C., Peer, C., Wang, Y., Sporn, M.B. Cancer Res. (2001) [Pubmed]
  3. Long-term dosing of arzoxifene lowers cholesterol, reduces bone turnover, and preserves bone quality in ovariectomized rats. Ma, Y.L., Bryant, H.U., Zeng, Q., Palkowitz, A., Jee, W.S., Turner, C.H., Sato, M. J. Bone Miner. Res. (2002) [Pubmed]
  4. Breast cancer chemoprevention phase I evaluation of biomarker modulation by arzoxifene, a third generation selective estrogen receptor modulator. Fabian, C.J., Kimler, B.F., Anderson, J., Tawfik, O.W., Mayo, M.S., Burak, W.E., O'Shaughnessy, J.A., Albain, K.S., Hyams, D.M., Budd, G.T., Ganz, P.A., Sauter, E.R., Beenken, S.W., Grizzle, W.E., Fruehauf, J.P., Arneson, D.W., Bacus, J.W., Lagios, M.D., Johnson, K.A., Browne, D. Clin. Cancer Res. (2004) [Pubmed]
  5. A phase II trial of arzoxifene, a selective estrogen response modulator, in patients with recurrent or advanced endometrial cancer. McMeekin, D.S., Gordon, A., Fowler, J., Melemed, A., Buller, R., Burke, T., Bloss, J., Sabbatini, P. Gynecol. Oncol. (2003) [Pubmed]
  6. The selective estrogen receptor modulator arzoxifene and the rexinoid LG100268 cooperate to promote transforming growth factor beta-dependent apoptosis in breast cancer. Rendi, M.H., Suh, N., Lamph, W.W., Krajewski, S., Reed, J.C., Heyman, R.A., Berchuck, A., Liby, K., Risingsong, R., Royce, D.B., Williams, C.R., Sporn, M.B. Cancer Res. (2004) [Pubmed]
  7. Effect of the selective estrogen receptor modulator arzoxifene on repopulation of hormone-responsive breast cancer xenografts between courses of chemotherapy. Wu, L., Tannock, I.F. Clin. Cancer Res. (2005) [Pubmed]
  8. Analysis of cross-resistance of the selective estrogen receptor modulators arzoxifene (LY353381) and LY117018 in tamoxifen-stimulated breast cancer xenografts. Schafer, J.M., Lee, E.S., Dardes, R.C., Bentrem, D., O'Regan, R.M., De Los Reyes, A., Jordan, V.C. Clin. Cancer Res. (2001) [Pubmed]
  9. Prevention and treatment of experimental breast cancer with the combination of a new selective estrogen receptor modulator, arzoxifene, and a new rexinoid, LG 100268. Suh, N., Lamph, W.W., Glasebrook, A.L., Grese, T.A., Palkowitz, A.D., Williams, C.R., Risingsong, R., Farris, M.R., Heyman, R.A., Sporn, M.B. Clin. Cancer Res. (2002) [Pubmed]
  10. Selective estrogen receptor modulators for the chemoprevention of prostate cancer. Steiner, M.S., Raghow, S., Neubauer, B.L. Urology (2001) [Pubmed]
  11. Effects of oral estrogen, raloxifene and arzoxifene on gene expression in serotonin neurons of macaques. Bethea, C.L., Mirkes, S.J., Su, A., Michelson, D. Psychoneuroendocrinology (2002) [Pubmed]
  12. Arzoxifene as therapy for endometrial cancer. Burke, T.W., Walker, C.L. Gynecol. Oncol. (2003) [Pubmed]
  13. A new MCF-7 breast cancer cell line resistant to the arzoxifene metabolite desmethylarzoxifene. Freddie, C.T., Christensen, G.L., Lykkesfeldt, A.E. Mol. Cell. Endocrinol. (2004) [Pubmed]
  14. Advances in breast cancer treatment and prevention: preclinical studies on aromatase inhibitors and new selective estrogen receptor modulators (SERMs). Schiff, R., Chamness, G.C., Brown, P.H. Breast Cancer Res. (2003) [Pubmed]
  15. The effect of the new SERM arzoxifene on growth and gene expression in MCF-7 breast cancer cells. Freddie, C.T., Larsen, S.S., Bartholomaeussen, M., Lykkesfeldt, A.E. Mol. Cell. Endocrinol. (2004) [Pubmed]
  16. Selective estrogen receptor modulators as inhibitors of repopulation of human breast cancer cell lines after chemotherapy. Licun, W., Tannock, I.F. Clin. Cancer Res. (2003) [Pubmed]
  17. Chemical modification modulates estrogenic activity, oxidative reactivity, and metabolic stability in 4'F-DMA, a new benzothiophene selective estrogen receptor modulator. Liu, H., Bolton, J.L., Thatcher, G.R. Chem. Res. Toxicol. (2006) [Pubmed]
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