View source for Selective Estrogen Receptor Modulators

== Other Names ==

SERMs

* tamoxifen, raloxifene, toremifene, bazedoxifene, ospemifene, and lasofoxifene
* clomiphene, enclomiphene 

== General ==

* SERMs are primarily used in the treatment and prevention of breast cancer, osteoporosis, and ovulatory dysfunction, with tissue-specific agonist or antagonist effects on estrogen receptors in various organs.
* SERMs are frequently used off-label with anecdotal claims of boosting endogenous testosterone levels. While there are no official guidelines supporting their use for this purpose, they are commonly employed as standalone agents or as part of post-cycle therapy (PCT) protocols to aid in recovery of the hypothalamic-pituitary-gonadal axis.<ref>Wu YC, Sung WW. ''Clomiphene Citrate Treatment as an Alternative Therapeutic Approach for Male Hypogonadism: Mechanisms and Clinical Implications''. Pharmaceuticals (Basel). 2024;17(9):1233. doi:10.3390/ph17091233.</ref>
* SERMs are frequently used off-label to counteract or prevent gynecomastia in individuals using anabolic steroids, especially as part of PCT<ref>Hanavadi S, Banerjee D, Monypenny IJ, Mansel RE. The Role of Tamoxifen in the Management of Gynaecomastia. ''Breast (Edinb).'' 2006;15(2):276–80. doi:10.1016/j.breast.2005.04.007</ref>

== Performance Enhancing Effects ==

* SERM administration leads to increased LH and testosterone levels, however there is no evidence that SERMs directly enhance muscle strength, endurance, or other athletic performance<ref>Shelly W, Draper MW, Krishnan V, Wong M, Jaffe RB. Selective Estrogen Receptor Modulators: An Update on Recent Clinical Findings. ''Obstet Gynecol Surv.'' 2008;63(3):163–81. doi:10.1097/OGX.0b013e31816400d7</ref>

== Medical Indications ==

* hormone receptor-positive breast cancer
* postmenopausal osteoporosis 
* anovulation
* gynecomastia

== Adverse Effects ==

* Most common symptoms include hot flushes, dizziness, and gastrointestinal symptoms (such as nausea and abdominal discomfort) and venous thromboembolism (VTE) <ref>Ellis AJ, Hendrick VM, Williams R, Komm BS. Selective Estrogen Receptor Modulators in Clinical Practice: A Safety Overview. Expert Opin Drug Saf. 2015;14(6):921–34. doi:10.1517/14740338.2015.1014799</ref>
* Tamoxifen is associated with a small but significant risk of stroke and endometrial cancer in women

== Mechanism ==

* In post cycle therapy, SERMs are used to block estrogenic negative feedback at the hypothalamus and pituitary, thereby increasing secretion of gonadotropin-releasing hormone (GnRH), which in turn stimulates luteinizing hormone (LH) and follicle-stimulating hormone (FSH) release, ultimately promoting endogenous testosterone production.<ref>Goldstein SR, Siddhanti S, Ciaccia AV, Plouffe L. A Pharmacological Review of Selective Oestrogen Receptor Modulators. ''Hum Reprod Update.'' 2000 May-Jun;6(3):212–24. doi:10.1093/humupd/6.3.212</ref>

== WADA Considerations ==

* banned by WADA

== See Also == 

== References ==