The Sound of Evolution
Raloxifene
Mechanism of action:
Raloxifene is a selective estrogen receptor modulator and belongs to the benzothiophene derivatives. Raloxifene can bind to estrogen receptor ERα and ERβ, but it induces receptor conformational changes that differ from those caused by estradiol, thereby producing different effects in different tissues. For example, it inhibits osteoclast activity, reduces bone resorption, and increases bone density; it suppresses estrogen receptor-mediated cell proliferation and lowers the risk of estrogen receptor-positive breast cancer; and it inhibits endometrial hyperplasia.
Reference(s):
1. Heringa M et al. (2003). Review on raloxifene: profile of a selective estrogen receptor modulator. Int J Clin Pharmacol Ther.
2. Cummings SR et al. (1999). The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. JAMA.
3. Bryant HU et al. (1999). An estrogen receptor basis for raloxifene action in bone. J Steroid Biochem Mol Biol.