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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In addition, isomerization of 4-hydroxytamoxifen is catalyzed by CYP1B1,2B6, and 2C19 (7).
At steady state, achieved after 2 weeks of therapy, mean plasma 4-hydroxytamoxifen levels were just 1/18 of those measured in 19 healthy controls taking 20 mg/day of oral tamoxifen.
The use of the innovative EHG(TM) technology as a delivery vehicle for 4-hydroxytamoxifen has enabled the clinical development of this promising, but previously undeveloped molecule, now in Phase II trials.
17[beta]-Estradiol, genistein, and 4-hydroxytamoxifen induce the proliferation of thyroid cancer cells through the G protein coupled-receptor GPR30.
Tamoxifen but not 4-hydroxytamoxifen initiates apoptosis in p53 (-) normal human mammary epithelial cells by inducing mitochondrial depolarization.
TamoGel(TM) is a percutaneously applied gel formulation of 4-Hydroxytamoxifen (4- OHT) that is currently under investigation in a variety of benign and malignant estrogen-dependent conditions by ASCEND Therapeutics.
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.