tamoxifen

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tamoxifen

(təmŏk`sĭfĕn'), synthetic hormone used in the treatment of breast cancerbreast cancer,
cancer that originates in the breast. Breast cancer is the second leading cause of cancer death in women (following lung cancer). Although the vast majority of the cases occur in women, some men also get breast cancer.
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. Introduced in 1978, tamoxifen is used to prevent recurrences of cancer in women who have already undergone surgery to remove their tumors and to control metastatic breast cancer. In breast tissue, tamoxifen blocks the effect of estrogen on cancerous cells that need estrogen to grow; not all breast cancers are affected by tamoxifen and other selective estrogen receptor modulators. In postmenopausal women with breast cancer, aromatase inhibitors, which block the production of estrogen outside the ovaries, are typically used instead of tamoxifen. In 1998, a large study of healthy women at high risk for breast cancer showed that tamoxifen can also prevent first occurrence of the disease; women who took the drug had a 45% lower incidence of cancer that those who received a placebo, and tamoxifen is now also used to reduce the risk of breast cancer in high risk patients. Adverse effects include and increased risk of uterine and endometrial cancer, blood clots, stroke, and cataracts.
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To examine the effects of a number of therapeutic antiestrogens and other ligands on PI3K activation in ER[[alpha].sup.-]/[[beta].sup.-] Hec50 cells, we evaluated PH-RFP localization in cells treated with 4-hydroxytamoxifen, ICI182,780, the benzothiophene-based and recently FDA-approved SERM Raloxifene, the phytoestrogen genistein, and the widely used ER[alpha]-and ER[beta]-selective agonists propylpyrazoletriol (PPT) and diarylpropionitrile (DPN) (Figure 5(a)).
Another clinically active metabolite is 4-hydroxytamoxifen, which is formed by 4-hydroxylation, also at the para position of the phenyl ring of the parent drug.
TamoGel(tm)'s active ingredient, 4-hydroxytamoxifen, is the most active metabolite of the FDA-approved drug tamoxifen, a widely-prescribed adjuvant therapy for breast cancer.
TamoGel's active ingredient, 4-hydroxytamoxifen, is the most active metabolite of the FDA-approved drug tamoxifen, a widely-prescribed adjuvant therapy for breast cancer.
There is also "compelling evidence" that the drug's active metabolite in the body -- 4-hydroxytamoxifen -- stimulates the growth of human endometrial cancer cells grown in culture, notes Liam J.
Establishment of MCF-7(TamR) and T47d (TamR) cells: W + 5% media supplemented with [10.sup.-7] M 4-hydroxytamoxifen (Sigma-Aldrich, Egypt).
Afimoxifene is 4-hydroxytamoxifen, a highly potent metabolite of tamoxifen, in a proprietary hydroalcoholic gel.
Tamoxifen but not 4-hydroxytamoxifen initiates apoptosis in p53 (-) normal human mammary epithelial cells by inducing mitochondrial depolarization.
(Dallas, TX, USA); and 4-hydroxytamoxifen (OHT; CAS number 68392-35-8, purity 99%) from Zeneca (Macclesfield, UK).
17[beta]-Estradiol, genistein and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the G protein-coupled receptor GPR30.