Selective estrogen receptor modulator
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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.
See also
References
- ↑ 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
- ↑ 2.0 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
- ↑ 3.0 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/