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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. [1][2] Antiestrogens are one of three types of sex hormone ...
[8] [9] In men, they are being investigated in the treatment of benign prostatic hyperplasia [10] and also as potential contraceptive agents. [11] GnRH antagonists could be used as puberty blockers in transgender youth and to suppress sex hormone levels in transgender adolescents and adults, but have not been studied in this context. [12] [13 ...
Megestrol acetate is a weak partial agonist of the androgen receptor (AR). [121][122][123] It has been reported to bind to this receptor with 5% of the affinity of the anabolic steroid metribolone. [2][4][80] Despite its weak intrinsic activity at the androgen receptor, at clinical doses in humans, megestrol acetate appears to behave, for all ...
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.
Exemestane is an oral steroidal aromatase inhibitor that is used in ER-positive breast cancer in addition to surgery and/or radiation in post-menopausal women. The main source of estrogen is the ovaries in premenopausal women, while in post-menopausal women most of the body's estrogen is produced via the conversion of androgens into estrogen by ...
Enclomiphene is a selective estrogen receptor antagonist, antagonizing the estrogen receptors in the pituitary gland, disrupting the negative feedback loop by estrogen towards the hypothalamic-pituitary-gonadal axis, ultimately resulting in an increase in gonadotropin secretion. In men with secondary hypogonadotropic hypogonadism, this improves ...
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