AN UPDATE ON SERMs (SELECTIVE ESTROGEN RECEPTOR MODULATORS)
Dr Steven R. Goldstein MD is a past President of the International Menopause Society, a past President of The Menopause Society, and a Certified Menopause Practitioner. In private practice for over 35 years as a Menopause Specialist in NYC, Dr Goldstein has helped thousands of patients combat the symptoms of Menopause and Perimenopause.
Dr Goldstein is also a HRT Specialist NYC who uses hormone replacement therapy to help women in the Menopause stage of life. Dr Goldstein writes the below article on SERMs (a form of hormone replacement therapy) for your edification. It does not constitute medical advice.
A SERM (selective estrogen receptor modulator) is a molecule that combines to the estrogen receptor and produces estrogenic effects in
some tissues like bone, vagina, sometimes uterus, while being an estrogen blocker in other tissues – breast, sometimes uterus. There are a number of SERMs, many of which you have heard of and some which you have not.
The original SERM was tamoxifen. Most of you have heard of this as a breast cancer drug. It binds to estrogen receptors in the breast and acts as an anti-estrogen. What is not well known is that it is a very good bone drug – it acts like estrogen in bone metabolism. One of the problems with tamoxifen is that a very small number of women will develop endometrial cancers and precancers. More women will develop benign endometrial polyps. Any bleeding whatsoever in a patient on tamoxifen has to be reported immediately and must be evaluated.
The next SERM was raloxifene originally marketed as Evista but is now generic. I did all of the uterine safety studies for raloxifene. It is a cousin of tamoxifen without the baggage in the uterus. It acts as an antiestrogen in breast and estrogenic in bone. In 1997, it was approved for prevention and treatment of osteoporosis. And although then we knew that it would be of tremendous value in reducing breast cancer risk, it was not until 2009 that the FDA added that to the label. So, raloxifene, also known as Evista, is approved for prevention and treatment of osteoporosis and breast cancer prevention. What is also little known is that on average, it will lower cholesterol approximately 20%. It is neutral in the uterus unlike tamoxifen, but it does not improve vaginal dryness or atrophy which are often the causes of painful intercourse in menopause.
Still another SERM is called ospemifene and marketed under the name Osphena. This is estrogenic in the vagina and is approved by the FDA to
treat dryness and atrophy of the vagina which results in painful intercourse and discomfort in menopausal women, which simply gets worse the further into menopause a patient gets. Osphena, because of a class activity of SERMs, would have some benefit in bone and breast but the magnitude of that benefit is unstudied. In addition, because it is unstudied, it is not carried in the label. Very, very few healthcare providers are aware that Osphena has any benefit in bone and breast.
I have had many primary care doctors who have told my Osphena patients that they are crazy to take an oral pill for their vagina. The question arises, why not simply insert a cream or tablet into the vagina? Thus, the utilization of Osphena, in my opinion, is markedly less than it should be, and I have discussed this with many patients who are appropriate candidates for it.
The final SERM to talk about is bazedoxifene. This is yet another SERM which gives the best protective effect in the uterus. Pfizer produces a hormone replacement product called Duavee which combines their estrogen Premarin with the SERM bazedoxifene. The bazedoxifene is given for uterine protection. Thus, this is hormone replacement which is progestogen-free.
If you are a woman in the Menopause stage of life or are postmenopausal and need help coping with Menopause, then a consultation with Dr Steven R. Goldstein, a Menopause Specialist in NYC and a HRT Specialist NYC may be in order.