Safety and efficacy of ospemifene for the treatment of dyspareunia associated with vulvar and vaginal atrophy due to menopause

Gregory T. Wurz, Chiao Jung Kao, Michael W. DeGregorio

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

During the menopausal transition, women experience a number of symptoms due to declining estrogen levels, including vasomotor symptoms and vulvar and vaginal atrophy (VVA). Unlike vasomotor symptoms, vaginal dryness and dyspareunia, the main symptoms of VVA, typically worsen without treatment and can significantly impact the quality of life. Up to 60% of postmenopausal women may be affected by VVA, but many women unfortunately do not seek treatment due to embarrassment or other factors. After 20+ years in development, ospemifene (Osphena™) was approved by the US Food and Drug Administration in 2013 for treatment of moderate-to-severe dyspareunia associated with VVA due to menopause. As the first non-hormonal alternative to estrogen-based products for this indication, the approval of ospemifene represents a significant milestone in postmenopausal women's health. Ospemifene is a non-steroidal estrogen receptor agonist/antagonist, also known as a selective estrogen receptor modulator (SERM), from the same chemical class as the breast cancer drugs tamoxifen and toremifene. Unlike other selective estrogen receptor modulators, ospemifene exerts a strong, nearly full estrogen agonist effect in the vaginal epithelium, making it well suited for the treatment of dyspareunia in postmenopausal women. Results of Phase III clinical trials showed that ospemifene significantly improved the vaginal maturation index (decreased parabasal cells and increased superficial cells), decreased vaginal pH, and decreased severity of the self-identified most bothersome symptom (dyspareunia or vaginal dryness) compared to placebo. Long-term safety studies revealed that 60 mg ospemifene given daily for 52 weeks was well tolerated and was not associated with any endometrium or breast-related safety concerns. This review discusses the preclinical and clinical data supporting the use of ospemifene for the treatment of dyspareunia associated with VVA due to menopause and provides an overview of its clinical safety.

Original languageEnglish (US)
Pages (from-to)1939-1950
Number of pages12
JournalClinical Interventions in Aging
Volume9
DOIs
StatePublished - Nov 13 2014

Fingerprint

Dyspareunia
Menopause
Atrophy
Safety
Estrogens
Selective Estrogen Receptor Modulators
Non-Steroidal Estrogens
Toremifene
Consumer Product Safety
Therapeutics
Phase III Clinical Trials
Ospemifene
Women's Health
United States Food and Drug Administration
Tamoxifen
Endometrium
Breast
Epithelium
Placebos
Quality of Life

Keywords

  • Genitourinary syndrome of menopause
  • SERM
  • Sexual dysfunction

ASJC Scopus subject areas

  • Geriatrics and Gerontology

Cite this

Safety and efficacy of ospemifene for the treatment of dyspareunia associated with vulvar and vaginal atrophy due to menopause. / Wurz, Gregory T.; Kao, Chiao Jung; DeGregorio, Michael W.

In: Clinical Interventions in Aging, Vol. 9, 13.11.2014, p. 1939-1950.

Research output: Contribution to journalArticle

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