25 Facts About Tamoxifen

Tamoxifen, sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and treat breast cancer in women and men.

Tamoxifen is typically taken daily by mouth for five years for breast cancer.

Tamoxifen was initially made in 1962, by chemist Dora Richardson.

Tamoxifen has been used effectively to improve blood flow, reduce uterine contractility and pain in dysmenorrhea patients.

Tamoxifen is used for the treatment of both early and advanced estrogen receptor-positive breast cancer in pre- and postmenopausal women.

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Tamoxifen is used for ovulation induction to treat infertility in women with anovulatory disorders.

Tamoxifen improves fertility in males with infertility by disinhibiting the hypothalamic–pituitary–gonadal axis via ER antagonism and thereby increasing the secretion of luteinizing hormone and follicle-stimulating hormone and increasing testicular testosterone production.

Tamoxifen is useful in the treatment of peripheral precocious puberty, for instance due to McCune–Albright syndrome, in both girls and boys.

Tamoxifen has a number of contraindications, including known hypersensitivity to tamoxifen or other ingredients, individuals taking concomitant coumarin-type anticoagulant therapy, and women with a history of venous thromboembolism .

Tamoxifen has been associated with a number of cases of hepatotoxicity.

Tamoxifen seems to require a protein PAX2 for its full anticancer effect.

Tamoxifen is antigonadotropic in postmenopausal women and partially suppresses levels of the gonadotropins, luteinizing hormone and follicle-stimulating hormone in such women.

Tamoxifen is rapidly and extensively absorbed from the intestines with oral administration.

Tamoxifen is a prodrug and is metabolized in the liver by the cytochrome P450 isoforms CYP3A4, CYP2C9, and CYP2D6 into active metabolites such as endoxifen and afimoxifene .

Tamoxifen is excreted in bile and is eliminated in feces, while small amounts are eliminated in urine.

Tamoxifen is a nonsteroidal SERM of the triphenylethylene family and was structurally derived from diethylstilbestrol-like estrogens and antiestrogens such as chlorotrianisene and ethamoxytriphetol.

Tamoxifen is closely related structurally to other triphenylethylenes, such as clomifene, nafoxidine, ospemifene, toremifene, and numerous others.

Tamoxifen did eventually receive marketing approval as a fertility treatment, but the class of compounds never proved useful in human contraception.

Tamoxifen is one of three drugs in an anti-angiogenetic protocol developed by Dr Judah Folkman, a researcher at Children's Hospital at Harvard Medical School in Boston.

Tamoxifen was instrumental in funding V Craig Jordan to work on tamoxifen.

Two books, Estrogen Action, Selective Estrogen Receptor Modulators and Women's Health and Tamoxifen Pioneering Medicine in Breast Cancer tell this story.

Tamoxifen is marketed under the brand names Nolvadex and Soltamox, and a variety of other brand names throughout the world.

Tamoxifen has been seen to decrease rapid bone maturation which is the result of excessive estrogen and alter predicted adult height .

Tamoxifen has been studied in the treatment of the rare conditions of retroperitoneal fibrosis and idiopathic sclerosing mesenteritis.

Tamoxifen is used as a research tool to trigger tissue-specific gene expression in many conditional expression constructs in genetically modified animals including a version of the Cre-Lox recombination technique.

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