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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 .
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 the aromatase enzyme in the peripheral tissues (i.e. adipose tissue like that of the breast) and a number of sites in the brain. Estrogen is produced locally ...
Enclomifene is the (E)-stereoisomer of clomifene, while zuclomifene is the (Z)-stereoisomer. [ 4 ] [ 5 ] Whereas zuclomifene is more estrogenic , enclomifene is more antiestrogenic . [ 3 ] In accordance, unlike enclomifene, zuclomifene is antigonadotropic due to activation of the ER and reduces testosterone levels in men. [ 3 ]
Tibolone is a synthetic steroid with weak estrogenic, progestogenic, and androgenic activity, and hence is an agonist of the estrogen, progesterone, and androgen receptors. [13] [1] [8] [6] It is a prodrug of several metabolites. [1] [13] [14] The estrogenic effects of tibolone may show tissue selectivity in their distribution. [13] [15] [14] [16]
Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonists/antagonists (ERAAs), [1] [2] are a class of drugs that act on estrogen receptors (ERs). [3] Compared to pure ER agonists – antagonists (e.g., full agonists and silent antagonists ), SERMs are more tissue-specific, allowing them to selectively inhibit or ...
Raloxifene is a selective estrogen receptor modulator (SERM) and therefore a mixed agonist–antagonist of the estrogen receptor (ER). [6] It has estrogenic effects in bone and antiestrogenic effects in the breasts and uterus. [6] Raloxifene was approved for medical use in the United States in 1997. [6] It is available as a generic medication.
"Baywatch" star Nicole Eggert shared the warning signs that she had overlooked before she was diagnosed with stage 2 cribriform carcinoma breast cancer in December 2023.
Steroidal aromatase inhibitors are a class of drugs that are mostly used for treating breast cancer in postmenopausal women. High levels of estrogen in breast tissue increases the risk of developing breast cancer and the enzyme aromatase is considered to be a good therapeutic target when treating breast cancer due to it being involved in the final step of estrogen biosynthetic pathway and also ...
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