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Selective estrogen receptor modulator information


Selective estrogen receptor modulator
Drug class
Tamoxifen, a nonsteroidal triphenylethylene antiestrogen and a widely used drug in the treatment of breast cancer.
Class identifiers
SynonymsSERM; Estrogen receptor agonist/antagonist; ERAA
UseBreast cancer, infertility, osteoporosis, vaginal atrophy, dyspareunia, contraception, male hypogonadism, gynecomastia, breast pain, others
ATC codeG03XC
Biological targetEstrogen receptor
Legal status
In Wikidata

Selective estrogen receptor modulators (SERMs), also known as estrogen receptor agonist/antagonists (ERAAs),[1][2] are a class of drugs that act on the estrogen receptor (ER).[3] A characteristic that distinguishes these substances from pure ER agonists and antagonists (that is, full agonists and silent antagonists) is that their action is different in various tissues, thereby granting the possibility to selectively inhibit or stimulate estrogen-like action in various tissues.

  1. ^ Hirsch HD, Shih E, Thacker HL (June 2017). "ERAAs for menopause treatment: Welcome the 'designer estrogens'". Cleve Clin J Med. 84 (6): 463–470. doi:10.3949/ccjm.84a.15140. PMID 28628428.
  2. ^ Archer DF (August 2020). "Ospemifene: less venous thrombosis than other selective estrogen receptor modulators in postmenopausal women with vulvo vaginal atrophy". Menopause. 27 (8): 846–847. doi:10.1097/GME.0000000000001600. PMID 32576803. S2CID 220045301.
  3. ^ Riggs BL, Hartmann LC (Feb 2003). "Selective estrogen-receptor modulators -- mechanisms of action and application to clinical practice". The New England Journal of Medicine. 348 (7): 618–29. doi:10.1056/NEJMra022219. PMID 12584371.

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Estrogen receptor

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Tamoxifen

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sold under the brand name Nolvadex among others, is a selective estrogen receptor modulator used to prevent breast cancer in women and men. It is also...

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Raloxifene

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List of selective estrogen receptor modulators

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Enclomifene

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Ormeloxifene

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Antiestrogen

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include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader...

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Selective glucocorticoid receptor modulator

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Selective glucocorticoid receptor agonists. Selective receptor modulator Selective androgen receptor modulator Selective estrogen receptor modulator Selective...

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Clomifene

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unknown cause or who are pregnant. Clomifene is in the selective estrogen receptor modulator (SERM) family of medication and is a nonsteroidal medication...

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Selective receptor modulator

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Classes of selective receptor modulators include: Selective androgen receptor modulator (SARM) Selective estrogen receptor modulator (SERM) Selective glucocorticoid...

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Estrogen receptor alpha

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Phytoestrogens (e.g., coumestrol, daidzein, genistein, miroestrol) Selective estrogen receptor modulators (e.g., tamoxifen, clomifene, raloxifene) Antiestrogens (e...

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Receptor modulator

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A receptor modulator, or receptor ligand, is a general term for a substance, endogenous or exogenous, that binds to and regulates the activity of chemical...

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Ospemifene

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are post-menopausal. Ospemifene is a selective estrogen receptor modulator (SERM) acting similarly to an estrogen on the vaginal epithelium, building vaginal...

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Estrogen receptor beta

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Estrogen receptor beta (ERβ) also known as NR3A2 (nuclear receptor subfamily 3, group A, member 2) is one of two main types of estrogen receptor—a nuclear...

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Bazedoxifene

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(pending more study) for cancer. It is a third-generation selective estrogen receptor modulator (SERM). Since late 2013 it has had U.S. FDA approval for...

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Afimoxifene

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4-hydroxytamoxifen (4-OHT) and by its tentative brand name TamoGel, is a selective estrogen receptor modulator (SERM) of the triphenylethylene group and an active metabolite...

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Fertility medication

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estrogen, which include selective estrogen receptor modulators (SERM) and aromatase inhibitors. Clomiphene is a selective estrogen receptor modulator...

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Fulvestrant

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Fulvestrant is a selective estrogen receptor degrader (SERD) and was first-in-class to be approved. It works by binding to the estrogen receptor and destabilizing...

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Estrogen

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they bind to and activate estrogen receptors (ERs) which in turn modulate the expression of many genes. Additionally, estrogens bind to and activate rapid-signaling...

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Toremifene

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The medication is a selective estrogen receptor modulator (SERM) and hence is a mixed agonist–antagonist of the estrogen receptor (ER), the biological...

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Endoxifen

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known as 4-hydroxy-N-desmethyltamoxifen, is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group as well as a protein...

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Hormonal contraception

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are composed of steroid hormones, although in India one selective estrogen receptor modulator is marketed as a contraceptive. The original hormonal method—the...

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Hormone therapy

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cancer Estrogen deprivation therapy for women with estrogen receptor-positive breast cancer High-dose estrogen therapy for women with estrogen receptor-positive...

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Broparestrol

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β-diphenyl-β-p-ethylphenylethylene (BDPE), is a synthetic, nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group that has been used...

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Cyclofenil

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Cyclofenil, sold under the brand name Sexovid among others, is a selective estrogen receptor modulator (SERM) medication which is used as a gonadotropin stimulant...

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