tamoxifen

/teuh mok"seuh feuhn, -fen'/, n. Pharm.
an antineoplastic drug, C26H29NO, that blocks the estrogen receptors on cancer cells, used in the treatment of breast cancer.
[1970-75; perh. T(RANS)- + AM(INO)- + OXY-2 + PHEN(YL), with resp. of y and ph]

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Synthetic hormone, marketed as Nolvadex, that prevents the binding of estrogen to estrogen-sensitive breast cancer cells.

Initially used to prevent recurrences of breast cancer after successful treatment, it was later found to prevent first occurrences in women at high risk. The most serious side effect is an increased risk of thrombosis, which may require patients to take an anticoagulant as well. Studies on its effectiveness against breast and other cancers continue.

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drug
      synthetic hormone, used primarily in the prevention and treatment of breast cancer, that inhibits the growth-promoting actions of estrogen in breast cancer cells (cell).

      Tamoxifen was first synthesized in 1962 by scientists at the British pharmaceutical company Imperial Chemical Industries PLC (now AstraZeneca). The agent (then known as ICI 46474) was subsequently found to have contraceptive effects in rats and was believed to exert its effects solely through antiestrogen mechanisms. Thus, tamoxifen was initially investigated for potential use as a morning-after pill. However, in the early 1970s, when it was found that tamoxifen had the opposite effect in humans—it actually increased fertility by stimulating ovulation in women—research on the agent as a form of contraception was promptly abandoned.

      Several years later scientists recognized the potential application of tamoxifen as a therapy for hormone-dependent cancers (cancer) and began testing the agent in rats with breast cancer. It was found that tamoxifen exerted antiestrogen effects in breast cancers that expressed estrogen receptors but had no effect in breast cancers that did not express these receptors. Tamoxifen's complex actions, characterized by its inhibition of estrogen activity in breast tissue and its stimulation of estrogen activity in the endometrium, led to its reclassification—from antiestrogen to selective estrogen receptor modulator (SERM). In 1978, following a series of successful clinical trials in humans, the U.S. Food and Drug Administration (FDA) approved tamoxifen for the treatment of metastatic, estrogen receptor-positive breast cancer. In 1998 the FDA further approved the use of tamoxifen for the prevention of first occurrences of breast cancer in women at high risk.

      Tamoxifen is taken orally and works by competing with endogenous estrogens for receptor sites in breast tissue where the estrogens normally exert their actions. Under normal circumstances, estrogen enters a cell and binds to an estrogen receptor, which then diffuses into the cell nucleus. In the nucleus the estrogen–estrogen receptor complex binds to specific sequences of deoxyribonucleic acid ( DNA) to activate certain genes (gene). The estrogen–estrogen receptor complex typically activates genes that produce proteins (protein) capable of stimulating cell growth and cell division. However, in breast cells, when an estrogen receptor is bound to tamoxifen, its properties are altered in such a way that it can no longer activate genes. The result is a decrease in the growth of breast tissue and of breast cancer tissue. Tamoxifen is ineffective against recurrent breast cancer in about 25 to 35 percent of women. This resistance is believed to be the result of decreased levels of a protein involved in facilitating tamoxifen's inhibitory effects on gene activation.

      Today tamoxifen is the most widely used anticancer drug and is sometimes used to treat other conditions, such as gynecomastia in men undergoing antiandrogen therapy for prostate cancer and infertility in women affected by anovulatory disorders. The most common side effects of tamoxifen include nausea, vomiting, hot flashes, and irregular menstruation. High doses or long-term (more than two years) courses of tamoxifen can increase the risk of uterine cancer in some women. A serious side effect of treatment is an increased risk of thrombosis, which may require patients to take an anticoagulant as well.

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Universalium. 2010.

Look at other dictionaries:

  • Tamoxifen — Systematic (IUPAC) name (Z …   Wikipedia

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  • tamoxifen — [tə mäk′sə fen΄] n. a synthetic hormone, C32H37NO10, used as an estrogen blocking drug to inhibit the growth of certain types of tumors, esp. in cases of advanced breast cancer: in full tamoxifen citrate …   English World dictionary

  • Tamoxifen — Ta*mox i*fen (t[a^]*m[o^]k s[i^]*f[e^]n), n. a chemical compound ({C26H29NO}) which is non steroidal but physiogically active as an estrogen antagonist. It is used to treat postmenopausal breast cancer. Chemically it is 1 p… …   The Collaborative International Dictionary of English

  • Tamoxifen — Strukturformel Allgemeines Freiname Tamoxifen …   Deutsch Wikipedia

  • tamoxifen — A drug used to treat certain types of breast cancer in women and men. It is also used to prevent breast cancer in women who have had ductal carcinoma in situ (abnormal cells in the ducts of the breast) and are at a high risk of developing breast… …   English dictionary of cancer terms

  • tamoxifen — ta·mox·i·fen ta mäk si .fen n a selective estrogen receptor modulator that acts as an estrogen antagonist in breast tissue and is administered orally in the form of its citrate C26H29NO·C6H8O7 esp. to treat breast cancer see NOLVADEX * * * n. a… …   Medical dictionary

  • tamoxifen — [[t]təmɒ̱ksɪfen[/t]] N UNCOUNT Tamoxifen is a drug that is used for treating women who have breast cancer …   English dictionary

  • tamoxifen — n. a drug used in the treatment of breast cancer: it binds with hormone receptors in the tumour to inhibit the effect of oestrogens (see anti oestrogen, selective oestrogen receptor modulator). Tamoxifen is also used to treat female infertility… …   The new mediacal dictionary

  • tamoxifen — noun Etymology: probably by recombination & alteration of trans , oxy, and clomiphene Date: 1972 an estrogen antagonist C26H29NO used in the form of its citrate especially to treat postmenopausal breast cancer …   New Collegiate Dictionary


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