ERAAs for menopause treatment: Welcome the ‘designer estrogens’

Cleveland Clinic Journal of Medicine.

Release date: June 1, 2017

Heather D. Hirsch, MD, MS, NCMP
Assistant Professor, Clinical Internal Medicine, Division of General Internal Medicine, The Ohio State University, Columbus, and Center for Women’s Health, The Ohio State University Wexner Medical Center, Upper Arlington, OH

Elim Shih, MD, NCMP
Department of Obstetrics and Gynecology, Women’s Health Institute, Cleveland Clinic

Holly L. Thacker, MD, NCMP
Director of Center for Specialized Women’s Health, Department of Obstetrics and Gynecology, Women’s Health Institute, Cleveland Clinic; Professor, Cleveland Clinic Lerner College of Medicine of Case Western Reserve University, Cleveland, OH

ABSTRACT

Estrogen receptor agonist-antagonists (ERAAs) selectively inhibit or stimulate estrogen-like action in targeted tissues. This review summarizes how ERAAs can be used in combination with an estrogen or alone to treat menopausal symptoms (vasomotor symptoms, genitourinary syndrome of menopause), breast cancer or the risk of breast cancer, osteopenia, osteoporosis, and other female midlife concerns.

KEY POINTS

  • Tamoxifen is approved to prevent and treat breast cancer. It may also have beneficial effects on bone and on cardiovascular risk factors, but these are not approved uses.
  • Raloxifene, a second-generation ERAA, was initially approved for preventing and treating osteoporosis and later received approval to reduce the risk of invasive estrogen receptor-positive breast cancer in postmenopausal women.
  • Ospemifene is approved for treatment of genitourinary syndrome of menopause.
  • The combination of conjugated estrogen and bazedoxifene is approved for treating moderate to severe vasomotor symptoms associated with menopause and also for preventing postmenopausal osteoporosis in women with an intact uterus.

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