Tamoxifen mechanism

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  1. Mr. Wonderful XenForo Moderator

    Tamoxifen mechanism


    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. Tamoxifen ist ein selektiver Estrogenrezeptormodulator, der als Arzneistoff zur Therapie von Brustkrebs bei Frauen vor der Menopause eingesetzt wird. Tamoxifen wurde von ICI Pharmaceuticals (jetzt Astra Zeneca) entwickelt und bewirkt eine kompetitive Hemmung von Estrogenrezeptoren sowie eine Stimulation von Progesteronrezeptoren. Als „Vater“ der Brustkrebs-Behandlung mit Tamoxifen gilt V. Auch zur Therapie von fibrozystischen Brüsten wurde bei Frauen Tamoxifen angewendet, um Knoten, Schwellungen und Schmerzen zu reduzieren. Forscher der Universität San Diego sollen 2018 herausgefunden haben, dass Tamoxifen gegen die Amöbe Naegleria fowleri wirken soll. Diese löst bei Menschen die in bis zu 95 % der Fälle tödlich verlaufende Primäre Amöben-Meningoencephalitis aus. Als Hormonrezeptormodulator kann Tamoxifen potenziell die Wirkung anderer Hormonpräparate beeinflussen. Insbesondere bei gleichzeitiger Einnahme von Estrogenen mit Tamoxifen kann eine wechselseitige Wirkungsabschwächung beobachtet werden.

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    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. Tamoxifen is approved for this use regardless of menopausal status. Raloxifene is approved for use only in postmenopausal women. Two aromatase inhibitors — exemestane and anastrazole —have also been found to reduce the risk of breast cancer in postmenopausal women at increased risk of the disease. The oncostatic mechanism of the drug is believed to be through the reduction of oestrogen, but hydroxytamoxifen actually increases oestrogen.

    Hormones are substances that function as chemical messengers in the body. They affect the actions of cells and tissues at various locations in the body, often reaching their targets through the bloodstream. The hormones estrogen and progesterone are produced by the ovaries in premenopausal women and by some other tissues, including fat and skin, in both premenopausal and postmenopausal women and men. Estrogen promotes the development and maintenance of female sex characteristics and the growth of long bones. Progesterone plays a role in the menstrual cycle and pregnancy. Estrogen and progesterone also promote the growth of some breast cancers, which are called hormone-sensitive (or hormone-dependent) breast cancers. Hormone-sensitive breast cancer cells contain proteins called hormone receptors that become activated when hormones bind to them. One of the selective estrogen receptor modulators (SERM) with tissue-specific activities for the treatment and prevention of estrogen receptor positive breast cancer. Tamoxifen acts as an anti-estrogen (inhibiting agent) in the mammary tissue, but as an estrogen (stimulating agent) in cholesterol metabolism, bone density, and cell proliferation in the endometrium.

    Tamoxifen mechanism

    UpToDate, Hormone Therapy for Breast Cancer Fact Sheet - National.

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  7. Estradiol and tamoxifen. Estradiol, shown at the top, is a small carbon-rich steroid. Tamoxifen, shown at bottom, mimics the shape and chemical composition of estradiol. Tamoxifen, however, has an extra chain attached in the middle that is important for its antagonistic action.

    • The Molecular Perspective Tamoxifen and the Estrogen Receptor.
    • A new mechanism of action for tamoxifen - The Lancet Oncology.
    • Molecular mechanisms of tamoxifen-associated endometrial..

    The precise mechanism of its action is unknown, but one possibility is that it binds and blocks estrogen receptors on the surface of cells, preventing estrogens from binding and activating the cell. It is used in patients for treating and preventing breast cancer. When was tamoxifen Soltamox approved by the FDA? Uterine cancer. Here, we briefly explore all the molecular events related to tamoxifen resistance and focus on its mechanism of action as. UCSF oncologist Pamela Munster, MD, and her colleagues have discovered the molecular basis for tamoxifen resistance in women with breast.

     
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