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[11] [7] Peak levels of tamoxifen after a single 40 mg oral dose were 65 ng/mL and steady state levels at 20 mg/day were 310 ng/mL. [5] Levels of tamoxifen show clear dose dependency across a dosage range of 1 to 20 mg/day. [5] [93] Endoxifen levels are approximately 5 to 10 times higher than afimoxifene levels, with large interindividual ...
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.
Tamoxifen is currently first-line treatment for nearly all pre-menopausal women with hormone receptor-positive breast cancer. [1] Raloxifene is another partial agonist SERM which does not seem to promote endometrial cancer , and is used primarily for chemoprevention of breast cancer in high-risk individuals, as well as to prevent osteoporosis ...
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 first SERM, tamoxifen, was originally developed as an anti-estrogen contraceptive. However, it was discovered it promoted ovulation in humans by acting as an agonist in ovaries. 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]
The side effects of toremifene are similar to those of tamoxifen. [5] The most common side effect is hot flashes. [5] Other side effects include sweating, nausea, vomiting, dizziness, vaginal discharge, and vaginal bleeding. [5] [7] In women with bone metastases, hypercalcemia may occur. [5] Toremifene has a small risk of thromboembolic events. [5]