Raloxifene
Raloxifene is selective estrogen receptor modulator (SERM). This means it has the same effect as estrogen in most of the body, but has the opposite effect in some places, including the breasts.
Trans people (especially non-binary people) sometimes take raloxifene with the aim of inducing feminization without breast development (Aly, 2019). This is usually done instead of- or along with estrogen and/or testosterone blockers.
Raloxifene regimens are experimental, and there is only minimal data available on whether they work well, or are safe in the long term. No prescriber guidelines currently recommend their use, although this was also once true of all other transgender hormone regimens.
Unlike estrogen, raloxifene does not lower testosterone production. Instead, it significantly increases testosterone levels in people who were assigned male at birth. This means that raloxifene may cause unwanted masculinization if It is not combined with testosterone blockers or surgery. (Duschek, Gooren, & Netelenbos, 2004).
Key points
- Experimentally used for feminization without breast development
- Works like estrogen in most of the body, but has the opposite effect in the breasts
- Minimal information on efficacy and safety
- No standardized regimens
- Combining with calcium, vitamin D, exercise, and general healthy lifestyle may reduce risks
- Combining with testosterone-blocking treatment necessary to avoid unwanted masculinization
- Possibly safer when taken as 120 mg instead of 60 mg
- Sometimes used by people who self-medicate, only rarely prescribed
Dosing
Raloxifene is a pill that is swallowed. It is most commonly used at a dose of 60 mg once daily (Lilly, 2018), but different dosages are sometimes used, particularly by people who self-medicate.
Extremely limited data suggests that a dose of 120 mg could possibly be more protective for long-term cognition than 60 mg (Yaffe et al., 2005).
Risks & management
Raloxifene may increase the risk of blood clots and stroke. This is especially important to remember when combining it with other drugs that also increase this risk, such as cyproterone acetate and oral estrogen pills (Adomaityte, Farooq, & Qayyum, 2008).
Raloxifene significantly increases testosterone production in people who are assigned male at birth. This could cause unwanted masculinization if not offset using other medications, and it is therefore advisable to monitor testosterone levels when taking raloxifene (Duschek, Gooren & Netelenbos, 2004).
Regimens that involve raloxifene may increase the risk of developing problems with low bone density. The risk of this could be reduced with the use of calcium and vitamin D supplements, as well as regular exercise, and the avoidance of smoking and excessive alcohol consumption (Lilly, 2018).
In the short-term, hormone regimens involving raloxifene are likely relatively safe, though they may cause menopausal symptoms such as hot flashes. In the long term, their safety is unstudied, with concerns long-term use could carry significant negative health effects. There is little concrete data available on this (Xu et al., 2021).
Interactions
Raloxifene has relatively few known interactions. The manufacturer advises avoiding cholestyramine, and exercising caution with several other drugs including warfarin, diazepam, and lidocaine. The manufacturer also advises that the safety of using raloxifene in combination with estrogen has not been established (Lilly, 2018).
Other information
Raloxifene is rarely prescribed in formal healthcare settings due to limited data and lack of prescriber guidelines. Most people who use raloxifene are self-medicating.
Raloxifene is also called "Evista", "Raloxiheal", "Raloxo", or simply "ralox".
See also
References
- Adomaityte, J., Farooq, M., & Qayyum, R. (2008). Effect of raloxifene therapy on venous thromboembolism in postmenopausal women. A meta-analysis. Thrombosis and haemostasis, 99(2), 338–342. [DOI:10.1160/TH07-07-0468]
- Aly. (2019). An Exploration of Possibilities for Hormone Therapy in Non-Binary Transfeminine People. Transfeminine Science. [URL]
- Duschek, E. J., Gooren, L. J., & Netelenbos, C. (2004). Effects of raloxifene on gonadotrophins, sex hormones, bone turnover and lipids in healthy elderly men. European journal of endocrinology, 150(4), 539–546. [DOI:10.1530/eje.0.1500539]
- Lilly. (2018). Evista: Highlights of prescribing information. [PDF]
- Xu, J. Y., O'Connell, M. A., Notini, L., Cheung, A. S., Zwickl, S., & Pang, K. C. (2021). Selective Estrogen Receptor Modulators: A Potential Option For Non-Binary Gender-Affirming Hormonal Care?. Frontiers in endocrinology, 12, 701364. [DOI:10.3389/fendo.2021.701364]
- Yaffe, K., Krueger, K., Cummings, S. R., Blackwell, T., Henderson, V. W., Sarkar, S., Ensrud, K., & Grady, D. (2005). Effect of raloxifene on prevention of dementia and cognitive impairment in older women: the Multiple Outcomes of Raloxifene Evaluation (MORE) randomized trial. The American journal of psychiatry, 162(4), 683–690. [DOI:10.1176/appi.ajp.162.4.683]