TOREMIFEN CITRATE 60MG / ML | 60ML

Toremifene belongs to the group of class non-steroidal selective estrogen receptor modulator (SERM). It is a chlorinated derivative of tamoxifen and shows equal efficacy in treating breast cancer. It exhibits estrogenic activity in bones and antiestrogenic action in breast tissues. As an FDA-approved drug, it is primarily indicated for the treatment of estrogen receptor-positive breast cancer and cancer of unknown receptor status in postmenopausal women. Furthermore, research indicates that it exerts a positive effect on osteoporosis and promotes fat loss. Currently, it is being studied for its effect on prostate cancer in men. At Pinnacle Peptides, toremifene for sale is exclusively available for research and experimentation.

From Pubchem

IUPAC Name: 2-[4-[(Z)-4-chloro-1,2-diphenylbut-1-enyl]phenoxy]-N,N-dimethylethanamine
Synonyms: Acapodene, Farestone, Z-Toremifene
Molecular Formula: C26H28ClNO
Molecular Weight: 406.0 g/mol
CAS number: 89778-26-7
PubChem CID: 3005573

Toremifene is a synthetic derivative of tamoxifen and exhibits a similar mechanism of action. It shows antagonist action at estrogen receptors in breast tissues. It competes with estrogen and reversibly binds to the receptor, thus preventing ER from activating estrogen-response element on DNA. This, in turn, suppresses the proliferation of breast cancer cells. On the contrary, it exhibits agonism and mimics the action of endogenous estrogen in bone tissues, thus preventing bone resorption.

1. Bone Mineral Density

Research demonstrates that toremifene can enhance bone mineral density and reduce the risk of fractures. A randomized phase III clinical trial found that toremifene treatment resulted in a significant increase in bone mineral density at the hip and spine in prostate cancer patients undergoing androgen deprivation therapy[1]. In another study, the drug’s use was associated with a 79.5% reduction in the risk of new vertebral fractures in men under 80 years of age, accompanied by a 7% decrease in bone loss and an increase in bone mineral density across various sites [2].

Additionally, a comparative study was designed to investigate the effects of tamoxifen and toremifene on bone biochemistry and bone mineral density in postmenopausal women. Participants were randomized to receive either 20mg of tamoxifen or 40mg of toremifene for a year. The study concluded that tamoxifen significantly increases bone mineral density. Interestingly, toremifene did not exhibit a similar influence on bone mineral density in postmenopausal women [3].

2. Dyslipidemia

Toremifene has also been investigated for its effect on dyslipidemia, characterized by abnormal lipid levels in the blood. Research shows that dyslipidemia is prevalent among postmenopausal women, making them susceptible to cardiovascular diseases. The literature demonstrates that toremifene might improve serum lipid levels. One study found that toremifene significantly decreased LDL cholesterol (bad cholesterol) and increased HDL-C (good cholesterol) levels [4].

Similarly, androgen deprivation therapy raises serum lipid levels and increases the risk of coronary artery disease and myocardial infarction. Research conducted on men with prostate cancer undergoing antiandrogen treatment found that toremifene decreased total cholesterol, triglycerides and LDL-C levels [5].

3. Comparison with Tamoxifen

Research shows that toremifene and tamoxifen exhibit equivalent efficacy for the treatment of breast cancer in postmenopausal women. Analysis of nine phase III randomized trials indicates that toremifene has the same effect as tamoxifen. However, it exhibits a slightly better side effect profile and is less likely to cause uterine neoplasm [6].

The pharmacokinetic characteristics (absorption, distribution, metabolism and elimination) of both drugs vary as a result of slight differences in structure. Tamoxifen is a prodrug that is converted into its active metabolite through transformation by CYP2D6. On the other hand, toremifene doesn’t need such enzymes for its therapeutic action. These findings suggest that toremifene might serve as an alternative option for patients with CPY2D6 polymorphism [7].

4. Prevention of Prostate Cancer

Research shows that toremifene can prevent prostate cancer in men who are at high risk. One study found a decrease in the incidence of prostate cancer in men with prostatic intraepithelial neoplasia (PIN) who were treated with toremifene. Prostatic intraepithelial neoplasia is characterized by pathological changes in the cell lining of the prostate gland ducts, representing precursors to prostate cancer. [8].

Toremifene is a non-steroidal selective estrogen receptor modulator (SERM). It is used for the treatment of hormone-sensitive breast cancer in postmenopausal women. Furthermore, research suggests that it can improve serum lipid profile. Improve bone mineral density and lower the risk of prostate cancer. At Pinnacle Peptides, toremifene purchase is only available for research and educational institutions. Only buy toremifene if you are an authorized researcher.

1. Smith, M.R., et al., Toremifene increases bone mineral density in men receiving androgen deprivation therapy for prostate cancer: interim analysis of a multicenter phase 3 clinical study. J Urol, 2008. 179(1): p. 152-5.
2. Smith, M.R., et al., Toremifene Decreases Vertebral Fractures in Men Younger Than 80 Years Receiving Androgen Deprivation Therapy for Prostate Cancer. The Journal of Urology, 2011. 186(6): p. 2239-2244.
3. Marttunen, M.B., P.i. Hietanen, A. Tiitinen, and O. Ylikorkala, Comparison of Effects of Tamoxifen and Toremifene on Bone Biochemistry and Bone Mineral Density in Postmenopausal Breast Cancer Patients. The Journal of Clinical Endocrinology & Metabolism, 1998. 83(4): p. 1158-1162.
4. Tominaga, T., et al., Effects of Toremifene and Tamoxifen on Lipid Profiles in Post-menopausal Patients with Early Breast Cancer: Interim Results from a Japanese Phase III Trial. Japanese Journal of Clinical Oncology, 2010. 40(7): p. 627-633.
5. Smith, M.R., et al., Toremifene improves lipid profiles in men receiving androgen-deprivation therapy for prostate cancer: interim analysis of a multicenter phase III study. J Clin Oncol, 2008. 26(11): p. 1824-9.
6. Mustonen, M.V., S. Pyrhönen, and P.L. Kellokumpu-Lehtinen, Toremifene in the treatment of breast cancer. World J Clin Oncol, 2014. 5(3): p. 393-405.
7. Li, X., et al., Toremifene, an Alternative Adjuvant Endocrine Therapy, Is Better than Tamoxifen in Breast Cancer Patients with CYP2D6*10 Mutant Genotypes. Cancer research and treatment, 2023.
8. Price, D., et al., Toremifene for the Prevention of Prostate Cancer in Men With High Grade Prostatic Intraepithelial Neoplasia: Results of a Double-Blind, Placebo Controlled, Phase IIB Clinical Trial. The Journal of Urology, 2006. 176(3): p. 965-971.