Difference between revisions of "Selective estrogen receptor modulator"

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Selective estrogen receptor modulator (SERM) are a class of drugs that have tissue selective [[estrogen receptor]] [[agonist|agonism]] and [[antagonist|antagonism]]. For example, [[raloxifene]] acts as an estrogen in bone but an antiestrogen in breast and uterine tissue.<ref name="muchmore"/>
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Selective estrogen receptor modulators (SERMs) are a class of drugs that have tissue selective [[estrogen receptor]] [[agonist|agonism]] and [[antagonist|antagonism]]. For example, [[raloxifene]] acts as an estrogen in bone but an antiestrogen in breast and uterine tissue.<ref name="muchmore"/>
  
 
== Comparison ==
 
== Comparison ==

Revision as of 09:13, 4 December 2018

Selective estrogen receptor modulators (SERMs) are a class of drugs that have tissue selective estrogen receptor agonism and antagonism. For example, raloxifene acts as an estrogen in bone but an antiestrogen in breast and uterine tissue.[1]

Comparison

Tissue-specific ER activity
Drug Bone Uterus Breast Availability
Raloxifene agonist[1] antagonist[1] antagonist[1] currently available
Tamoxifen agonist agonist antagonist currently available
Afimoxifene agonist[2] N/Aa N/Aa phase III trials
Elacestrant agonist[3] degrader[3] degrader[3] phase II trials

a Afimoxifene has only been delivered topically to the breast. However, since afimoxifene is the active metabolite of tamoxifen,[2] it likely has the same effects as tamoxifen in bone and uterine tissue.

References

  1. 1.0 1.1 1.2 1.3 Muchmore DB (2000). "Raloxifene: A selective estrogen receptor modulator (SERM) with multiple target system effects". The oncologist. 5 (5): 388–392. https://dx.doi.org/10.1634/theoncologist.5-5-388
  2. 2.0 2.1 A Goyal, R Mansel, E Le Nestour and V Masini-Etévé. Topical tamoxifen gel (afimoxifene) is associated with low plasma levels of 4-OHT while achieving therapeutic local antiestrogenic effect in premenopausal women with cyclical mastalgia. Cancer Res January 15 2009 (69) (2 Supplement) 2154; https://dx.doi.org/10.1158/0008-5472.SABCS-2154
  3. 3.0 3.1 3.2 Fiona Garner, Maysoun Shomali, Dotty Paquin, C. Richard Lyttle, and Gary Hattersley. RAD1901: a novel, orally bioavailable selective estrogen receptor degrader that demonstrates antitumor activity in breast cancer xenograft models. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4560273/