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Tamoxifen was initially made in 1962, by chemist Dora Richardson. [17] [18] It is on the World Health Organization's List of Essential Medicines. [19] Tamoxifen is available as a generic medication. [14] In 2020, it was the 317th most commonly prescribed medication in the United States, with more than 900 thousand prescriptions. [20] [21]
Estrogen deprivation therapy, also known as endocrine therapy, is a form of hormone therapy that is used in the treatment of breast cancer.Modalities include antiestrogens or estrogen blockers such as selective estrogen receptor modulators (SERMs) like tamoxifen, selective estrogen receptor degraders like fulvestrant, and aromatase inhibitors like anastrozole and ovariectomy.
Notes: Prevention of breast symptoms—specifically gynecomastia and breast pain—induced by 150 mg/day bicalutamide monotherapy with tamoxifen in 282 men with prostate cancer. Bicalutamide and tamoxifen were initiated at the same time (0 months). Estradiol levels were in the range of about 22 to 47 pg/mL in the treated group. [1] Sources: [2] [1]
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.
The drug is a synthetic androgen and anabolic steroid and hence is an agonist of the androgen receptor (AR), the biological target of androgens like testosterone and dihydrotestosterone (DHT). [ 3 ] [ 12 ] It has strong anabolic effects and weak androgenic effects, which give it a mild side effect profile and make it especially suitable for use ...
Sivifene (A-007) was initially thought to be a SERM due to its structural similarity to tamoxifen but it was subsequently found not to bind to the estrogen receptor (ER). [8] Tesmilifene (DPPE; YMB-1002, BMS-217380-01) is also structurally related to tamoxifen but similarly does not bind to the ER and is not a SERM. [9] [10]
Testosterone enanthate is used primarily in androgen replacement therapy. [4] [15] It is the most widely used form of testosterone in androgen replacement therapy. [4]The medication is specifically approved, in the United States, for the treatment of hypogonadism in men, delayed puberty in boys, and breast cancer in women. [16]
The drug was then successfully repurposed as a treatment for breast cancer where it was found to act as a full antagonist in breast tissue. [14] Somewhat unexpectedly, it was also discovered that tamoxifen preserves bone density [ 15 ] by acting as an agonist in bone resorbing osteoclasts . [ 16 ]