Toremifene Citrate Catalog Description (60mg/ml, 30ml)
Toremifene citrate (Fareston) is a SERM (selective estrogen receptor modulator), a compound with affinity for the estrogen receptor (ER) that typically behaves as an antagonist or otherwise limits the physiological effects of estrogen by binding to the receptor. Toremifene is approved for advanced metastatic breast cancer, and is succeeding in development as a prostate cancer chemopreventive. Off-label uses of toremifene include restoring testosterone or as an androgen substitute, as a fertility treatment for idiopathic oligospermia (low sperm content), and as a treatment for gynecomastia in males.
Toremifene is in the same class of SERMs as tamoxifen and clomiphene, the triphenethylenes. Like other SERMs, toremifene behaves as an estrogen receptor antagonist in most tissues, but sometimes behaves as an agonist. The agonist/antagonist profile of toremifene is similar to tamoxifen, with an antagonist effect in breast tissue and an agonist effect on lipids, bone, and the endometrium.
Tominaga et al (2010) examined a possible secondary benefit of SERMs. Through an agonistic effect, toremifene and tamoxifen positively impact the lipid profile in different ways:
Distinct differences between two selective estrogen receptor modulators on lipids were observed. Toremifene improved lipid profiles, particularly as an enhancer of high-density lipoprotein cholesterol. To a large extent, tamoxifen improved low-density lipoprotein cholesterol levels
According to the findings of Lewis et al (2010), toremifene and tamoxifen are roughly equally effective in treating breast cancer, and are both appropriate. The authors concluded that while the two SERMs are equivalent in many ways, toremifene may have an edge in overall therapeutic efficacy:
toremifene as compared with tamoxifen given as adjuvant therapy for early stage breast cancer would result in equivalent survival with an improved side effect profile, therefore, providing superior therapeutic efficacy
Tsourdi et al (2009) compared the effects of equivalent dosages of once daily toremifene (60mg), tamoxifen (20mg), and raloxifene (60mg), concluded that in treating idiopathic oligozoospermia, tamoxifen and toremifene are roughly equally effective in restoring gonadotropin secretion (which leads to improved fertility), while raloxifene was less effective. The mechanism by which SERMs increase gonadotropin levels is an anti-estrogenic effect at the level of the hypothalamus.
Farmakiotis et al (2007) evaluated the effect of toremifene on three main sperm parameters:
Toremifene administration for a period of 3 months in men with idiopathic oligozoospermia is associated with significant improvements of sperm count, motility, and morphology, mediated by increased gonadotropin secretion and possibly a direct beneficial effect of toremifene on the testes.
Toremifene has also "shown promise in reducing fracture risk in [androgen deprivation therapy]."
Fujimura T, Takahashi S, Kume H, Urano T, Takayama K, Yamada Y, Suzuki M, Fukuhara H, Nakagawa T, Inoue S, Homma Y. Toremifene, a selective estrogen receptor modulator, significantly improved biochemical recurrence in bone metastatic prostate cancer: a randomized controlled phase II a trial. BMC Cancer. 2015 Nov 2;15:836.
Haskell SG. Selective estrogen receptor modulators. South Med J. 2003 May;96(5):469-76.
Tominaga T, Kimijima I, Kimura M, Takatsuka Y, Takashima S, Nomura Y, Kasumi F, Yamaguchi A, Masuda N, Noguchi S, Eshima N. Effects of Toremifene and Tamoxifen on Lipid Profiles in Post-menopausal Patients with Early Breast Cancer: Interim Results from a Japanese Phase III Trial. Jpn J Clin Oncol. 2010 Apr 8.
Lewis JD, Chagpar AB, Shaughnessy EA, Nurko J, McMasters K, Edwards MJ. Excellent outcomes with adjuvant toremifene or tamoxifen in early stage breast cancer. Cancer. 2010 May 15;116(10):2307-15.
Tsourdi E, Kourtis A, Farmakiotis D, Katsikis I, Salmas M, Panidis D. The effect of selective estrogen receptor modulator administration on the hypothalamic-pituitary-testicular axis in men with idiopathic oligozoospermia. Fertil Steril. 2009 Apr;91(4 Suppl):1427-30.
Farmakiotis D, Farmakis C, Rousso D, Kourtis A, Katsikis I, Panidis D. The beneficial effects of toremifene administration on the hypothalamic-pituitary-testicular axis and sperm parameters in men with idiopathic oligozoospermia. Fertil Steril. 2007 Oct;88(4):847-53
Taneja SS, Smith MR, Dalton JT, Raghow S, Barnette G, Steiner M, Veverka KA. Toremifene--a promising therapy for the prevention of prostate cancer and complications of androgen deprivation therapy. Expert Opin Investig Drugs. 2006 Mar;15(3):293-305.