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New class of estrogen agents show promise in menopause treatment
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A new class of agents combining selective estrogen receptor modulators with estrogen compounds in tissue-selective estrogen complexes may prove more effective in treating postmenopausal women with uteruses vs. selective estrogen receptor modulators alone, unopposed estrogens or estrogens with progestogens, according to a recent review.
In the overview of current therapeutic approaches to menopausal symptoms, the researchers used PubMed to search for studies using keywords such as estrogen deficiency, menopause, hormone therapy and estrogen-only therapy. They culled various pivotal or recent randomized controlled trials, large observational studies, comprehensive meta-analyses and therapeutic guidelines.
The researchers discussed the utility of systemic estrogens in relieving menopause symptoms in postmenopausal women who underwent a hysterectomy, but they cited the increased risk for endometrial hyperplasia and endometrial cancer in women with intact uteruses. These risks have shifted the preferred treatment for these women toward estrogens with progestogens. However, the combination of progestogens with conjugated estrogens has been found to increase the risks for breast cancer and heart disease vs. placebo. This increased knowledge of estrogen’s pharmacological effects has given rise to new approaches and combinations, including selective estrogen receptor modulators (SERMS) and tissue selective estrogen complexes (TSECS). Although SERMs have been found to offset some symptoms of estrogen deficiency, they have been linked to increased rates of venous thromboembolism and vasomotor symptoms, thus detracting from their favorability as a treatment. It has been suggested that combining a SERM with a TSEC can yield unique, positive changes in estrogen receptor activity compared with that of each constituent used alone. Combinations of different SERMS with different TSECs have demonstrated distinct mechanisms and effects. The TSEC that has been most frequently studied to date, combining bazedoxifene (Duavee, Wyeth Pharmaceuticals) with conjugated estrogens, has shown promise in the tissue-specific treatment of menopausal women.
“The selective pairing of a SERM with an estrogen compound in a TSEC based on the unique spectrum of [estrogen receptor] activity identified for each component has resulted in a new class of agents that have thus far demonstrated more favorable profiles or [estrogen receptor] activity in postmenopausal women with a uterus than SERMS alone, [estrogens] or [estrogens with progestogens],” the researchers wrote.
Disclosure: Medical writing support was provided by Precise Publications and funded by Pfizer.
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