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Exemestane is an irreversible, steroidal aromatase inactivator of type I, structurally related to the natural substrate 4-androstenedione. It acts as a false substrate for the aromatase enzyme, and is processed to an intermediate that binds irreversibly to the active site of the enzyme causing its inactivation, an effect also known as " suicide ...
Exemestane went through clinical trials in the 1990s and received FDA approval in 1999, marketed as Aromasin. Indication for exemestane is advanced breast cancer in postmenopausal women, where the cancer has progressed following tamoxifen therapy. Exemestane is the first oral aromatase inactivator. [5]
Ovarian stimulation with the aromatase inhibitor letrozole has been proposed for ovulation induction in order to treat unexplained female infertility. In a multi-center study funded by the National Institute of Child Health and Development, ovarian stimulation with letrozole resulted in a significantly lower frequency of multiple gestation (i.e., twins or triplets) but also a lower frequency ...
It takes 7 days of treatment to reach 90-95% of the steady-state serum concentration. [25] Anastrozole distributes completely around the body and only 40% of the drug is bound to plasma proteins. The elimination of anastrozole is slow and the elimination half-life is 40–50 hours.
Esterified estrogens/methyltestosterone (EEs/MT), sold under brand names such as Covaryx, Eemt, Essian, Estratest, Menogen, and Syntest, is a hormonal preparation that combines esterified estrogens (EEs) with methyltestosterone (MT) in one tablet and is used in menopausal hormone therapy. [2]
There were no obvious differences in effectiveness of raloxifene in the MORE trial for prevention of breast cancer at a dosage of 60 mg/m 2 /day relative to 120 mg/m 2 /day. [14] In the Study of Tamoxifen and Raloxifene (STAR) trial, 60 mg/day raloxifene was 78% as effective as 20 mg/day tamoxifen in preventing non-invasive breast cancer. [ 15 ]
Average number of moderate-to-severe hot flashes per week with placebo and different doses of oral estradiol in menopausal women [40] [41]. Estradiol is used in menopausal hormone therapy to prevent and treat moderate to severe menopausal symptoms such as hot flashes, vaginal dryness and atrophy, and osteoporosis (bone loss). [11]
Estradiol levels on the first day after single dose of 0.25 mg buccal estradiol or at steady state after the last dose with 0.25 mg buccal estradiol twice daily once every 12 hours (0.5 mg/day total) in 6 postmenopausal women. [142] Estradiol has been studied for use by buccal administration.