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Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, [1] [2] and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously. They may also be used for chemoprevention in women at high risk for breast cancer.
The drug is a nonsteroidal androgen receptor (AR) modulator with mixed agonistic and antagonistic (antiandrogenic) effects. [1] [5] It has been found to reduce the growth of androgen receptor-expressing MDA-MB-231 breast cancer cells in vitro.
An androgen prohormone, or proandrogen, is a prohormone (or prodrug) of an anabolic-androgenic steroid (AAS). They can be prohormones of testosterone or of synthetic AAS, for example, nandrolone (19-nortestosterone). Dehydroepiandrosterone (DHEA), DHEA sulfate (DHEA-S), and androstenedione may all be considered proandrogens of testosterone. [1]
The estrogen diethylstilbestrol (DES) is occasionally used to treat prostate cancer through suppression of testosterone production. It was previously used in the treatment of breast cancer, but has been replaced by more effective and less toxic agents. Estrace is an estrogen which was also formerly used for antiandrogen therapy of prostate ...
Enobosarm, also formerly known as ostarine and by the developmental code names GTx-024, MK-2866, and S-22, is a selective androgen receptor modulator (SARM) which is under development for the treatment of androgen receptor-positive breast cancer in women and for improvement of body composition (e.g., prevention of muscle loss) in people taking GLP-1 receptor agonists like semaglutide.
Vosilasarm has been assessed in clinical trials in women with breast cancer at doses ranging from 50 to 150 mg/day, with the maximum safe and tolerated dose being 100 mg/day. [ 10 ] [ 3 ] [ 2 ] The drug sold via black-market Internet suppliers and used non-medically has been reported to be taken at doses of 5 to 30 mg/day, with unknown adverse ...
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