Nonsteroidal estrogen

Nonsteroidal estrogen
Drug class
Diethylstilbestrol, one of the most well-known nonsteroidal estrogens.
Class identifiers
SynonymsNonsteroidal estrogen receptor agonists
ATC codeG03C
Biological targetEstrogen receptors (ERα, ERβ, mERs (e.g., GPER, others))
Chemical classNonsteroidal
Legal status
In Wikidata

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 now almost never used.[2][3][4] On the other hand, virtually all selective estrogen receptor modulators (SERMs) are nonsteroidal, with triphenylethylenes like tamoxifen and clomifene having been derived from DES,[5] and these drugs remain widely used in medicine for the treatment of breast cancer among other indications.[6] In addition to pharmaceutical drugs, many xenoestrogens, including phytoestrogens, mycoestrogens, and synthetic endocrine disruptors like bisphenol A, are nonsteroidal substances with estrogenic activity.[7]

  1. ^ a b Hermkens PH, Kamp S, Lusher S, Veeneman GH (2006). "Non-steroidal steroid receptor modulators". IDrugs. 9 (7): 488–94. doi:10.2174/0929867053764671. PMID 16821162.
  2. ^ a b Scherr DS, Pitts WR (2003). "The nonsteroidal effects of diethylstilbestrol: the rationale for androgen deprivation therapy without estrogen deprivation in the treatment of prostate cancer". J. Urol. 170 (5): 1703–8. doi:10.1097/01.ju.0000077558.48257.3d. PMID 14532759.
  3. ^ Hammes B, Laitman CJ (2003). "Diethylstilbestrol (DES) update: recommendations for the identification and management of DES-exposed individuals". J Midwifery Womens Health. 48 (1): 19–29. doi:10.1016/s1526-9523(02)00370-7. PMID 12589302.
  4. ^ Schrager S, Potter BE (2004). "Diethylstilbestrol exposure". Am Fam Physician. 69 (10): 2395–400. PMID 15168959.
  5. ^ Philipp Y. Maximov; Russell E. McDaniel; V. Craig Jordan (23 July 2013). Tamoxifen: Pioneering Medicine in Breast Cancer. Springer Science & Business Media. pp. 4–. ISBN 978-3-0348-0664-0.
  6. ^ Edward P. Gelmann; Charles L. Sawyers; Frank J. Rauscher, III (19 December 2013). Molecular Oncology. Cambridge University Press. pp. 885–. ISBN 978-0-521-87662-9.
  7. ^ Witorsch RJ (2002). "Endocrine disruptors: can biological effects and environmental risks be predicted?". Regul. Toxicol. Pharmacol. 36 (1): 118–30. doi:10.1006/rtph.2002.1564. PMID 12383724.