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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 ...
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]
Toremifene has been shown to be compatible with tamoxifen, and in 1996 it was approved for use in the treatment of breast cancer in postmenopausal women. [ 36 ] Raloxifene originally failed as a breast cancer drug due to its poor performance in comparison to tamoxifen in the laboratory [ 19 ] but the estrogenic effects of raloxifene on bone led ...
N-Desmethyltamoxifen (developmental code name ICI-55,548) is a major metabolite of tamoxifen, a selective estrogen receptor modulator (SERM). [1] [2] N-Desmethyltamoxifen is further metabolized into endoxifen (4-hydroxy-N-desmethyltamoxifen), which is thought to be the major active form of tamoxifen in the body.
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.
Raloxifene was approved for medical use in the United States in 1997. [6] It is available as a generic medication . [ 6 ] [ 8 ] In 2020, it was the 292nd most commonly prescribed medication in the United States, with more than 1 million prescriptions.
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 ...
Endoxifen is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). [3] [4] [5] The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce endoxifen and afimoxifene (4-hydroxytamoxifen). [6]
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