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Testosterone, the major endogenous androgen and the target mediator of antiandrogens.. This is a list of antiandrogens, [1] or drugs that prevent the effects of androgens like testosterone and dihydrotestosterone (DHT). [2]
Antiestrogens (or so-called "estrogen blockers") like aromatase inhibitors (AIs) (e.g., anastrozole) or selective estrogen receptor modulators (SERMs) (e.g., tamoxifen) can be used to reduce the effects of high levels of endogenous estrogen (e.g., breast development, feminine fat distribution) in transgender men.
Atypical (dual estrogen and nitrogen mustard alkylating antineoplastic): Estramustine phosphate sodium (Emcyt) – 140 mg; Oral estradiol valerate (except in combination with dienogest as an oral contraceptive) is not available in the U.S. and is used primarily in Europe. [2]
Antiestrogens, also known as estrogen antagonists or estrogen blockers, are a class of drugs which prevent estrogens like estradiol from mediating their biological effects in the body. They act by blocking the estrogen receptor (ER) and/or inhibiting or suppressing estrogen production .
Triptorelin is used to treat prostate cancer as part of androgen deprivation therapy. [9]Another common use in the United Kingdom is for hormone replacement therapy to suppress testosterone or estrogen levels in transgender people (in conjunction with estradiol valerate for trans women or testosterone for trans men).
Neyman and colleagues in 2019 published a study on bicalutamide as a puberty blocker in adolescent transgender girls. [95] [101]: 477 It was employed both alone (n=17) and in combination with estrogen (n=6) at a dose of 50 mg/day in 23 transgender girls (mean age of 16 years, range 12 to 18.4 years) between 2013 and 2018.
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