Catalog No.S1776 Synonyms: NSC 613680
Molecular Weight(MW): 598.08
Toremifene Citrate is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.
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Choose Selective Estrogen/progestogen Receptor Inhibitors
|Description||Toremifene Citrate is an oral selective estrogen receptor modulator (SERM), used in the treatment of advanced breast cancer.|
Toremifene (7.5 mM) causes approximately 60% of the cells to exhibit morphologic characteristics typical of cells undergoing programmed death, or apoptosis in human breast cancer cells. Toremifene (5-10 mM) results in elevated levels of TRPM-2 and TGF beta 1 mRNAs in in vitro or in vivo grown tumor cells. Toremifene causes growth inhibition of estrogen-sensitive breast cancer cells by inducing some cells to undergo apoptosis and by inhibiting other cells from entering mitosis.  Toremifene induces a dose-dependent level of adducts that is lower than that observed for TAM. Toremifene significantly enhances endogenous DNA adduct formation.  Toremifene affects the cell turnover by inhibiting mitotic activity and modifying abundant spontaneous apoptosis in DMBA-induced rat mammary carcinoma. 
|In vivo||Toremifene, at the highest tested dose, increases the incidence of hepatocellular carcinomas in the DEN-initiated groups to a level one-third that observed with Tamoxifen administration to DEN-initiated rats. Toremifene increases the incidence of hypernephromas in previously DEN-initiated rats.  Toremifene results in aneuploidy in 50% of the cells examined and compared with the 85% level induced by Tamoxifen in female Sprague-Dawley rats. |
-  W鋜ri AM, et al. J Natl Cancer Inst, 1993, 85(17), 1412-1418.
-  Li D, et al. Cancer Res,1997, 57(8), 1438-1441.
-  Huovinen R, et al. Int J Cancer, 1993, 55(4), 685-691.
|In vitro||DMSO||100 mg/mL (167.2 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02506790||Recruiting||Breast Cancer||Petrov Research Institute of Oncology||July 2015||Phase 2|
|NCT02344940||Recruiting||Breast Cancer||Shanghai Jiao Tong University School of Medicine||December 2014||Phase 4|
|NCT02271282||Completed||Normal Healthy Volunteers||Mayo Clinic||December 2014||Phase 1|
|NCT02089854||Recruiting||Female Breast Cancer||Peking Union Medical College Hospital||November 2014||Phase 4|
|NCT02132390||Not yet recruiting||Breast Cancer|Chemotherapy Induced Amenorrhea|Ovarian Function Suppression||Peking Union Medical College Hospital||May 2014||Phase 3|
|NCT02132000||Recruiting||Breast Cancer Patients in Premenopausal|Estrogen and/or Progesterone Receptor Positive||Fengxi Su|Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University||April 2014||Phase 2|Phase 3|
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