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In a 1970 clinical trial, tamoxifen, which went by the name Nolvadex, was given to 60 breast cancer patients. This anti-estrogen drug had significantly shrunk the tumors while causing minimal side effects. [6] In 1988, she published an article on the history of the development of Tamoxifen. [7] Richardson was named on several patents. [8]
Tamoxifen is a long-acting SERM, with a nuclear retention of the ER–tamoxifen (or metabolite) complex of greater than 48 hours. [ 71 ] [ 72 ] It has relatively little affinity for the ERs itself and instead acts as a prodrug of active metabolites such as endoxifen (4-hydroxy- N -desmethyltamoxifen) and afimoxifene (4-hydroxytamoxifen; 4-OHT ...
The Study of Tamoxifen and Raloxifene (STAR) is a clinical trial from the early 2000s designed determine how the drug raloxifene compares with the drug tamoxifen in reducing the incidence of breast cancer in women who are at increased risk of the disease.
Tamoxifen is a pure antiestrogenic trans-isomer and has differential actions at estrogen target tissues throughout the body. Tamoxifen is selectively antiestrogenic in the breast but estrogen-like in bones and endometrial cancer. [24] Tamoxifen undergo phase I metabolism in the liver by microsomal cytochrome P450 (CYP) enzymes.
Jordan, V.C. A current view of tamoxifen for the treatment and prevention of breast cancer (Gaddum Memorial Lecture)" British Journal of Pharmacology 110:507-517, 1993. (257 citations as of May 26, 2021). Jordan, V.C. and Morrow, M.M. Tamoxifen, raloxifene and the prevention of breast cancer. Endocrine Reviews 20:253-278, 1999.
Afimoxifene, also known as 4-hydroxytamoxifen (4-OHT) and by its tentative brand name TamoGel, is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite of tamoxifen. [1] [2] [3] The drug is under development under the tentative brand name TamoGel as a topical gel for the treatment of hyperplasia ...
Toremifene appears to be safer than tamoxifen. [15] It has a lower risk of venous thromboembolism (VTE) (e.g., pulmonary embolism), stroke, and cataracts. [15] The lower risk of VTE may be related to the fact tamoxifen decreases levels of the antithrombin III to a significantly greater extent than either 60 or 200 mg/day toremifene. [15]
Bazedoxifene, used as bazedoxifene acetate, is a medication for bone problems and possibly (pending more study) for cancer. [2] It is a third-generation selective estrogen receptor modulator (SERM). [3]