Tamoxifen

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Tamoxifen is a SERM (selective estrogen receptor modifier). It acts as an estrogen receptor (ER) antagonist in some tissue (in this case, breasts) and an ER agonist in other tissue (in this case, bone and uterus). It is often used for breast cancer treatment for this reason, as it prevents osteoporosis and the spread of estrogen-sensitive cancer in the breasts and can be combined with GnRH blockers (either GnRH antagonists or agonists) for treatment.

In other words, tamoxifen acts as an anti estrogen in the breasts but as estrogen in bones and skin.^{[citation needed]}

This medication would likely be effective in halting breast growth (as it would prevent estrogen from acting in the breasts), and is already used for the treatment of fibrocystic breasts and breast cancer due to lack of side effects compared to other medications like danazol. It is sometimes used in treatment of gynecomastia.

It can possibly lower levels of IGF-1 (insulin growth factor 1), but also can lead to higher levels of estrogen in the uterus, which could lead to uterine cancer (though the risks are small).

Unlike tamoxifen, raloxifene is an ER antagonist in uterine tissue (lowering the risk for uterine cancer), and has a greater ER affinity in bone.

Tamoxifen has been proven to lower fibroglandular and breast volume/density in premenopausal women, and it and other SERMS have been proven to move fat distribution from the butt and central region to the legs. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005955/

Some medications may interfere with tamoxifen! They include paroxetine (Paxil), fluoxetine (Prozac), and bupropion (Wellbutrin) which inhibit metabolization of tamoxifen to a form the body can use. (https://www.health.harvard.edu/newsletter_article/antidepressants-and-tamoxifen)

Side effects

Tamoxifen can cause cognitive dysfunction^[1], increase the risk of stroke and pulmonary embolism,^[2], and increase the risk of endometrial cancer and cataracts.^[3]

References

↑ Paganini-Hill, A. & Clark, L.J. Breast Cancer Res Treat (2000) 64: 165. doi:10.1023/A:1006426132338
↑ Fisher, Bernard, et al. (16 September 1998). "Tamoxifen for Prevention of Breast Cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study". JNCI: Journal of the National Cancer Institute. 90 (18): 1371–1388. doi:10.1093/jnci/90.18.1371.
↑ Darlene K. Taylor et al (2012). "Treatment for uterine fibroids: Searching for effective drug therapies". Drug Discovery Today: Therapeutic Strategies. 9 (1): e41–e49. doi:10.1016/j.ddstr.2012.06.001. PMC 3525705. PMID 23264802. ISSN 17406773.

Jeon-Hor Chen, M.D., Yeun-Chung Chang, M.D., Daniel Chang, et. al, Reduction of Breast Density Following Tamoxifen Treatment Evaluated by 3-D MRI: Preliminary Study. Available from: https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3005955/
Sporn MB, Lippman SM. Agents for Chemoprevention and Their Mechanism of Action. In: Kufe DW, Pollock RE, Weichselbaum RR, et al., editors. Holland-Frei Cancer Medicine. 6th edition. Hamilton (ON): BC Decker; 2003. Available from: https://www.ncbi.nlm.nih.gov/books/NBK12522/
DrugBank. Tamoxifen. https://www.drugbank.ca/drugs/DB00675
Harvard Health. “Antidepressants and tamoxifen.” June 2010. https://www.health.harvard.edu/newsletter_article/antidepressants-and-tamoxifen

[1] Paganini-Hill, A. & Clark, L.J. Breast Cancer Res Treat (2000) 64: 165. doi:10.1023/A:1006426132338

[Fisher1998-2] Fisher, Bernard, et al. (16 September 1998). "Tamoxifen for Prevention of Breast Cancer: Report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study". JNCI: Journal of the National Cancer Institute. 90 (18): 1371–1388. doi:10.1093/jnci/90.18.1371.

[TaylorLeppert2012-3] Darlene K. Taylor et al (2012). "Treatment for uterine fibroids: Searching for effective drug therapies". Drug Discovery Today: Therapeutic Strategies. 9 (1): e41–e49. doi:10.1016/j.ddstr.2012.06.001. PMC 3525705. PMID 23264802. ISSN 17406773.

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