The Sound of Evolution
Toremifene
Mechanism of action:
Toremifene is a selective estrogen receptor modulator and a triphenylethylene derivative. Toremifene antagonizes estrogen receptors ERalpha and ERbeta in breast cells, preventing endogenous estrogen from initiating transcription of genes related to cell proliferation and thereby inhibiting the growth and division of ER-positive breast cancer cells. In the endometrium, however, toremifene exerts mild agonistic effects on ERalpha and ERbeta, which may stimulate endometrial proliferation.
Reference(s):
1. Price N et al. (2005). Role of 5a-reductase inhibitors and selective estrogen receptor modulators as potential chemopreventive agents for prostate cancer. Clin Prostate Cancer.
2. Taneja SS et al. (2006). Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy. Expert Opin Investig Drugs.
3. Thompson IM et al. (2007). Chemoprevention of prostate cancer: agents and study designs. J Urol.