| 词条 | Antiestrogen |
| 释义 |
| Image = Fulvestrant.svg | Alt = | Caption = Fulvestrant, a steroidal antiestrogen and a drug used in the treatment of breast cancer. | Width = 250px | Synonyms = Estrogen antagonists; Estrogen blockers; Estradiol antagonists | Use = Breast cancer; Infertility; Male hypogonadism; Gynecomastia; transgender men | ATC_prefix = L02BA | Biological_target = Estrogen receptor | Chemical_class = Steroidal; Nonsteroidal (triphenylethylene, others) | Drugs.com = | Consumer_Reports = | medicinenet = | rxlist = | MeshID = D020847 }}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 antagonists, the others being antiandrogens and antiprogestogens.[3] Types and examplesAntiestrogens include selective estrogen receptor modulators (SERMs) like tamoxifen, clomifene, and raloxifene, the ER silent antagonist and selective estrogen receptor degrader (SERD) fulvestrant,[4][5] aromatase inhibitors (AIs) like anastrozole, and antigonadotropins including androgens/anabolic steroids, progestogens, and GnRH analogues. Although aromatase inhibitors and antigonadotropins can be considered antiestrogens by some definitions, they are often treated as distinct classes.[6] Aromatase inhibitors and antigonadotropins reduce the production of estrogen, while the term "antiestrogen" is often reserved for agents reducing the response to estrogen.[7] Medical usesAntiestrogens are mainly used as a means of estrogen deprivation therapy in the treatment of ER-positive breast cancer. They are also used to treat infertility, male hypogonadism, and gynecomastia (breast development in men) and are used as a component of hormone replacement therapy for transgender men. Side effectsSide effects of antiestrogens include hot flashes, osteoporosis, breast atrophy, vaginal dryness, and vaginal atrophy. In addition, they may cause depression and reduced libido. HistoryEthamoxytriphetol (MER-25) was the first antagonist of the ER to be discovered,[8] followed by clomifene and tamoxifen.[9][10]References1. ^{{cite web |url=http://www.cancer.gov/dictionary/?CdrID=44813 |title=Definition of antiestrogen - NCI Dictionary of Cancer Terms, Definition of antiestrogen - NCI Dictionary of Cancer Terms |format= |work= |accessdate=}}, 2. ^{{DorlandsDict|one/000006027|antiestrogen}} 3. ^{{cite book|author=Judi Lindsley Nath|title=Using Medical Terminology: A Practical Approach|url=https://books.google.com/books?id=UEvTZg_5FBIC&pg=PA977|year=2006|publisher=Lippincott Williams & Wilkins|isbn=978-0-7817-4868-1|pages=977–}} 4. ^{{cite book|author1=Eckhard Ottow|author2=Hilmar Weinmann|title=Nuclear Receptors as Drug Targets|url=https://books.google.com/books?id=iATfLbPgRugC&pg=PA164|date=8 September 2008|publisher=John Wiley & Sons|isbn=978-3-527-62330-3|pages=164–165}} 5. ^{{cite book|author1=Bruce A. Chabner|author2=Dan L. Longo|title=Cancer Chemotherapy and Biotherapy: Principles and Practice|url=https://books.google.com/books?id=WL4arNFsQa8C&pg=PA660|date=8 November 2010|publisher=Lippincott Williams & Wilkins|isbn=978-1-60547-431-1|pages=660–}} 6. ^{{cite journal |vauthors=Riggins RB, Bouton AH, Liu MC, Clarke R |title=Antiestrogens, aromatase inhibitors, and apoptosis in breast cancer |journal=Vitam. Horm. |volume=71 |issue= |pages=201–37 |year=2005 |pmid=16112269 |doi=10.1016/S0083-6729(05)71007-4 |url=http://linkinghub.elsevier.com/retrieve/pii/S0083-6729(05)71007-4}} 7. ^{{cite journal|last1=Thiantanawat |last2=Long |last3=Brodie |first1=Apinya |first2=Brian |first3=Angela|title=Signaling Pathways of Apoptosis Activated by Aromatase Inhibitors and Antiestrogens|journal=The Journal of Cancer Research|date=2003-11-15|url=http://cancerres.aacrjournals.org/content/63/22/8037.full#ack-1|accessdate=2015-04-13}} 8. ^{{cite book|author1=Philipp Y. Maximov|author2=Russell E. McDaniel|author3=V. Craig Jordan|title=Tamoxifen: Pioneering Medicine in Breast Cancer|url=https://books.google.com/books?id=p-W5BAAAQBAJ&pg=PA7|date=23 July 2013|publisher=Springer Science & Business Media|isbn=978-3-0348-0664-0|pages=7–}} 9. ^{{cite book|author=V Craig Jordan|title=Estrogen Action, Selective Estrogen Receptor Modulators and Women's Health: Progress and Promise|url=https://books.google.com/books?id=ZM26CgAAQBAJ&pg=PA7|date=27 May 2013|publisher=World Scientific|isbn=978-1-84816-959-3|pages=7,112}} 10. ^{{cite book|author=Walter Sneader|title=Drug Discovery: A History|url=https://books.google.com/books?id=Cb6BOkj9fK4C&pg=PA198|date=23 June 2005|publisher=John Wiley & Sons|isbn=978-0-471-89979-2|pages=198–199}} External links{{NCI-cancer-dict}}{{Estrogens and antiestrogens}}{{Estrogen receptor modulators}} 4 : Antiestrogens|Hormonal antineoplastic drugs|Progonadotropins|Transgender and medicine |
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