An antiestrogen is a substance that blocks the production or utilization of estrogens,[1] or inhibits their effects.[2] Estrogens are the family of hormones that promote the development and maintenance of female sex characteristics.

Although aromatase inhibitors could be considered antiestrogens by some definitions, they are often considered to be a distinct class.[3] Aromatase inhibitors reduce the production of estrogen, while the term "antiestrogen" is usually reserved for agents reducing the response to estrogen.[4]

Hot flashes, osteoporosis, breast atrophy, and vaginal dryness can be side effects of antiestrogens.

Specific antiestrogens

Antiestrogens like tamoxifen can promote an invasive phenotype in estrogen receptor (ER)-positive breast cancer cells with deficient intercellular adhesion.

Ethamoxytriphetol (MER-25) was the first antiestrogen to be discovered,[5] followed by clomifene citrate and tamoxifen.[6][7] Fulvestrant is another antiestrogen, and is the only pure antiestrogen, or silent antagonist of the estrogen receptor, to have been introduced clinically.[8][9]

See also


  1. "Definition of antiestrogen - NCI Dictionary of Cancer Terms, Definition of antiestrogen - NCI Dictionary of Cancer Terms".,
  2. "antiestrogen" at Dorland's Medical Dictionary
  3. Riggins RB, Bouton AH, Liu MC, Clarke R (2005). "Antiestrogens, aromatase inhibitors, and apoptosis in breast cancer". Vitam. Horm. 71: 201–37. doi:10.1016/S0083-6729(05)71007-4. PMID 16112269.
  4. Thiantanawat, Apinya; Long, Brian; Brodie, Angela (2003-11-15). "Signaling Pathways of Apoptosis Activated by Aromatase Inhibitors and Antiestrogens". The Journal of Cancer Research. Retrieved 2015-04-13.
  5. Philipp Y. Maximov; Russell E. McDaniel; V. Craig Jordan (23 July 2013). Tamoxifen: Pioneering Medicine in Breast Cancer. Springer Science & Business Media. pp. 7–. ISBN 978-3-0348-0664-0.
  6. V Craig Jordan (27 May 2013). Estrogen Action, Selective Estrogen Receptor Modulators and Women's Health: Progress and Promise. World Scientific. pp. 7,112. ISBN 978-1-84816-959-3.
  7. Walter Sneader (23 June 2005). Drug Discovery: A History. John Wiley & Sons. pp. 198–199. ISBN 978-0-471-89979-2.
  8. Eckhard Ottow; Hilmar Weinmann (8 September 2008). Nuclear Receptors as Drug Targets. John Wiley & Sons. pp. 164–165. ISBN 978-3-527-62330-3.
  9. Bruce A. Chabner; Dan L. Longo (8 November 2010). Cancer Chemotherapy and Biotherapy: Principles and Practice. Lippincott Williams & Wilkins. pp. 660–. ISBN 978-1-60547-431-1.

External links

 This article incorporates public domain material from the U.S. National Cancer Institute document "Dictionary of Cancer Terms".

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