Ospemifene for the treatment of menopausal vaginal dryness, a symptom of the genitourinary syndrome of menopause

ABSTRACT

Introduction: Vulvovaginal atrophy (VVA), a component of the genitourinary syndrome of menopause, is a progressive condition due to decline in estrogen leading to vaginal and vulvar epithelial changes. Accompanying symptoms of dryness, irritation, burning, dysuria, and/or dyspareunia have a negative impact on quality of life. Ospemifene is a selective estrogen receptor modulator (SERM) approved by the FDA for moderate to severe dyspareunia and vaginal dryness due to postmenopausal VVA.

Areas covered: PubMed was searched from inception to March 2019 with keywords ospemifene and vulvar vaginal atrophy to review preclinical and clinical data describing the safety and efficacy of ospemifene for vaginal dryness and dyspareunia due to VVA. Covered topics include efficacy of ospemifene on vaginal cell populations, vaginal pH, and most bothersome VVA symptoms; imaging studies of vulvar and vaginal tissues; effects on sexual function; and safety of ospemifene on endometrium, cardiovascular system, and breast.

Expert opinion: Ospemifene is significantly more effective than placebo in all efficacy analyses studied, working through estrogen receptors and possibly androgen receptors. Safety as assessed by adverse events was generally comparable to that with placebo and to other SERMs, and/or adverse events were not clinically meaningful. No cases of endometrial or breast cancer were reported.

KEYWORDS:

• Genitourinary syndrome of menopause
• menopause
• ospemifene
• vaginal dryness
• vulvovaginal atrophy

Article Highlights

• Ospemifene is approved for the treatment of moderate to severe dyspareunia and/or vaginal dryness as a symptom of VVA due to menopause (in the US) and of moderate to severe symptomatic VVA in postmenopausal women not candidates for local vaginal estrogen therapy (in Europe)

• Objective and subjective measures, including vulvar-vestibular photography, show improvements in vaginal dryness and overall vulvar and vaginal health in postmenopausal women

• Safety (assessed by adverse events) was generally comparable to that with placebo and other SERMs

• No cases of endometrial or breast cancer were reported

• Longer-term data on the use of ospemifene will help create a better understanding of the best way to counsel women on using ospemifene as a VVA/GSM treatment

Acknowledgments

The authors thank Laura J. Ninger, ELS and Kathleen Ohleth, PhD, CMPP for medical writing assistance supported by Duchesnay.

Declaration of interest

DF Archer consults for AbbVie, Actavis, Agile Therapeutics, Bayer Healthcare, Endoceutics, Exeltis, InnovaGyn, Merck, Pfizer, Radius Health, Sermonix, Shionogi, Teva Women’s Healthcare, and TherapeuticsMD; and has received research support from Actavis, Bayer Healthcare, Endoceutics, Glenmark, Merck, Radius Health, Shionogi, and TherapeuticsMD. JA Simon has served (within the past year, or current) as a consultant/advisor to AbbVie, Allergan plc, AMAG, Amgen, Ascend Therapeutics, Bayer Healthcare, CEEK Enterprises, Covance, Dare Bioscience, Duchesnay, Hologic, KaNDy/NeRRe Therapeutics, Mitsubishi Tanage, ObsEva SA, Palatin Technologies, Sanofi SA, Shionogi, Sprout, and TherapeuticsMD; has received (within the past year, or current) grant/research support from AbbVie, Agile Therapeutics, Allergan plc, Bayer Healthcare, Endoceutics, GTx, Ipsen, Myovant Sciences, New England Research Institute, ObsEva SA, Palatin Technologies, Symbio Research, TherapeuticsMD, and Viveve Medical; has also served (within the past year, or current) on the speaker’s bureaus of AbbVie, AMAG, Duchesnay, Novo Nordisk, Shionogi, and TherapeuticsMD; and is a stockholder (direct purchase) in Sermonix Pharmaceuticals. DJ Portman consults for Duchesnay, Agile Therapeutics, ITF Research Pharma, Sebela, Endoceutics, and AMAG; has received research support from Palatin, Endoceutics, Shionogi, TherapeuticsMD, and Population Council; is on the speaker’s bureau for AMAG and TherapeuticsMD; and is currently Chief Executive Officer of Sermonix with stock/stock options. SR Goldstein is on the advisory board of AbbVie, AMAG, and TherapeuticsMD; consults for Cook ObGyn, Cooper Surgical, and IBSA; and has served on the speaker’s bureau of AMAG, Duchesnay, and TherapeuticsMD. I Goldstein has received research support from AMAG, Endoceutics, Ipsen, and Strategic Science & Technologies; serves as consultant/advisor to Duchesnay, Ipsen, Shionogi, Strategic Science & Technologies; and is on the speaker’s bureau for AMAG. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

Duchesnay provided support for the medical writing assistance provided by Laura J. Ninger, ELS and Kathleen Ohleth, PhD, CMPP (Precise Publications, LLC).