Use of SERMs for treatment in postmenopausal women

Area of Science:

• Endocrinology
• Pharmacology
• Women's Health

Background:

• Selective estrogen receptor modulators (SERMs) are non-steroidal agents with variable estrogenic and anti-estrogenic effects across different tissues.
• These differential effects are attributed to SERM binding-induced conformational changes in the estrogen receptor, influencing gene transcription.
• Clinical trials evaluate SERMs for postmenopausal women, focusing on effects on breast, bone, cardiovascular health, endometrium, vagina, and vasomotor symptoms.

Purpose of the Study:

• To describe the clinical differences in selected target tissues of approved, discontinued, and investigational SERMs.
• To highlight the tissue-selective actions of SERMs, alone or in combination with estrogens, for individualized postmenopausal therapy.
• To review the role of SERMs in managing menopausal symptoms and associated health risks.

Main Methods:

• Review of FDA-approved, discontinued, and investigational SERMs.
• Analysis of clinical trial data on SERM effects in postmenopausal women.
• Description of the first tissue-selective estrogen complex (TSEC) pairing.

Main Results:

• FDA-approved SERMs include tamoxifen, toremifene (breast cancer), raloxifene (osteoporosis, breast cancer), and ospemifene (vaginal atrophy).
• The first TSEC combines conjugated equine estrogens with bazedoxifene, reducing endometrial hyperplasia risk and offering estrogenic benefits without uterine or breast stimulation.
• SERMs allow for individualized treatment of postmenopausal women by providing targeted tissue effects.

Conclusions:

• SERMs offer a versatile therapeutic approach for postmenopausal women, addressing diverse health needs.
• Tissue-selective actions of SERMs and TSEC enable personalized treatment strategies.
• The development and application of SERMs continue to advance women's health during menopause.