Selective estrogen receptor modulator
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.
|Tissue-specific ER activity|
|Afimoxifene||agonist||N/Aa||N/Aa||phase III trials|
|Elacestrant||agonist||degrader||degrader||phase II trials|
a Afimoxifene has only been delivered topically to the breast. However, since afimoxifene is the active metabolite of tamoxifen, it likely has the same effects as tamoxifen in bone and uterine tissue.
- 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
- 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
- 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/