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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 .
Fulvestrant is a SERD drug that acts by damaging and blocking estrogen receptors. [11] Fulvestrant is currently only approved by the FDA to treat cancer in postmenopausal women, but it is often prescribed off-label in combination with and LHRH agonist in premenopausal women to halt the functionality of the ovaries. [ 11 ]
ER- estrogen receptor, DHEA- dehydroepiandrosterone, 1- first generation NSAIs, 2- second generation NSAIs and 3- third generation NSAIs. Estrogen is a sex-hormone that plays a major role in women's body function. [20] Estrogen also plays a major role in stimulating breast cancer as it binds and activates the estrogen receptor (ER). When the ER ...
A nonsteroidal estrogen is an estrogen with a nonsteroidal chemical structure. [1] The most well-known example is the stilbestrol estrogen diethylstilbestrol (DES). [1] [2] Although nonsteroidal estrogens formerly had an important place in medicine, they have gradually fallen out of favor following the discovery of toxicities associated with high-dose DES starting in the early 1970s, and are ...
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 ...
Estradiol is a naturally occurring and bioidentical estrogen, or an agonist of the estrogen receptor, the biological target of estrogens like endogenous estradiol. [11] Due to its estrogenic activity, estradiol has antigonadotropic effects and can inhibit fertility and suppress sex hormone production in both women and men.