Tamoxifen mechanism of action

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    Tamoxifen mechanism of action


    Tamoxifen is both the most widely prescribed drug for breast cancer and preventative therapy worldwide. It is a synthetic derivative of triphenylethylene but was originally screened in a drug development program oriented toward discovering new post-coital contraceptive agents. In its testing, tamoxifen had proved effective in rats but not in women. It was only in 1997 that it was FDA approved for the clinical treatment of advanced breast cancer. That had followed animal studies demonstrating that it was incredibly effective in preventative action against the development of experimentally-induced breast cancer, caused by known carcinogens dimethylbenzanthracene and nitrosomethylurea. While Tamoxifen is commonly known as an anti-estrogen, this is not an accurate description of its clinical activity. In actual fact, Tamoxifen boasts both estrogenic and anti-estrogenic properties depending on the target tissue. In 2006, the large STAR clinical study concluded that raloxifene is equally effective in reducing the incidence of breast cancer, but after an average 4-year follow-up, although the difference was not statistically significant, there were 36% fewer uterine cancers and 29% fewer blood clots in women taking raloxifene than in women taking tamoxifen. Tamoxifen improves fertility in males with infertility by disinhibiting the hypothalamic–pituitary–gonadal axis (HPG axis) via ER antagonism and thereby increasing the secretion of luteinizing hormone (LH) and follicle-stimulating hormone (FSH) and increasing testicular testosterone production. It is taken as a preventative measure in small doses, or used at the onset of any symptoms such as nipple soreness or sensitivity. Other drugs are taken for similar purposes such as clomifene and the anti-aromatase drugs which are used in order to try to avoid the hormone-related adverse effects. Occasionally tamoxifen is used in treatment of the rare conditions of retroperitoneal fibrosis A report in September 2009 from Health and Human Services' Agency for Healthcare Research and Quality suggests that tamoxifen, raloxifene, and tibolone used to treat breast cancer significantly reduce invasive breast cancer in midlife and older women, but also increase the risk of adverse side effects. Some cases of lower-limb lymphedema have been associated with the use of tamoxifen, due to the blood clots and deep vein thrombosis (DVT) that can be caused by this medication. Resolution of the blood clots or DVT is needed before lymphedema treatment can be initiated.

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    OverviewMedical usesSide effectsInteractionsPharmacologyHistory Selective estrogen receptor modulator. Tamoxifen is a first-line hormonal treatment of ER-positive metastatic breast cancer. Mechanism of action. Tamoxifen action - A great assortment of prescription and non-prescription medications for diverse disorders Consider online pharmacy if you wish to get all the.

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    Tamoxifen mechanism of action

    Tamoxifen - YouTube, Selective estrogen receptor modulator - Wikipedia

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  6. For instance, estrogen is also important in bone growth, and blocking of estrogen action may lead to osteoporosis. Tamoxifen, however, is.

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    Understanding the molecular mechanism of tamoxifen-induced endometrial cancer. The tissue-dependent mode of action of tamoxifen may be explained by. MECHANISM OF ACTION Tamoxifen and several of its metabolites are thought to act as estrogen antagonists, by competitively binding to estrogen receptors on tumour and. Researchers have identified a new mechanism of action for tamoxifen, the most widely used drug for the treatment and prophylaxis of breast cancer Clin Cancer Res.

     
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