Effect of raloxifene on the vaginal epithelium of postmenopausal women

Delmanto, Armando; Nahás, Eliana Aguiar Petri; Oliveira, Maria Luiza Cotrim Sartor de; Fernandes, César Eduardo; Traiman, Paulo

doi:10.1016/j.ejogrb.2008.01.017

Cited by 13 publications

(11 citation statements)

References 24 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…It is possible for a suitable compound to have positive effects in vaginal tissue with neutral or minimal effects on estrogen-dependent tissues such as the endometrium and breast. Existing estrogen agonists/antagonists 32,34,35 such as tamoxifen, raloxifene, bazedoxifene and lasofoxifene are not indicated for the treatment of VVA.…”

Section: Discussionmentioning

confidence: 99%

“…Consistent with other published data 26 , there were clear statistically significant effects of ospemifene 60 mg/day treatment compared with placebo on physiological vaginal parameters (increased proportion of superficial cells, decreased proportion of parabasal cells, reduced vaginal pH and improved visual evaluation), which were sustained throughout the study 26,28 . SERMs such as tamoxifen and raloxifene have not demonstrated similar favorable agonist effects of ospemifene on vaginal tissue 34,45 .…”

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Ospemifene 12-month safety and efficacy in postmenopausal women with vulvar and vaginal atrophy

et al. 2013

View full text Add to dashboard Cite

Objective Assessment of 12-month safety of ospemifene 60 mg/day for treatment of postmenopausal women with vulvar and vaginal atrophy (VVA).Methods In this 52-week, randomized, double-blind, placebo-controlled, parallel-group study, women 40–80 years with VVA and an intact uterus were randomized 6 : 1 to ospemifene 60 mg/day or placebo. The primary objective was 12-month safety, particularly endometrial; 12-week efficacy was assessed. Safety assessments included endometrial histology and thickness, and breast and gynecological examinations. Efficacy evaluations included changes from baseline to week 12 in percentage of superficial and parabasal cells and vaginal pH.Results Of 426 randomized subjects, 81.9% (n = 349) completed the study with adverse events the most common reason for discontinuation (ospemifene 9.5%; placebo 3.9%). Most (88%) treatment-emergent adverse events with ospemifene were considered mild or moderate. Three cases (1.0%) of active proliferation were observed in the ospemifene group. For one, active proliferation was seen at end of study week 52, and diagnosed as simple hyperplasia without atypia on follow-up biopsy 3 months after the last dose. This subsequently resolved with progestogen treatment and dilatation and curettage. In six subjects (five ospemifene (1.4%), one placebo (1.6%)) endometrial polyps were found (histopathology); however, only one (ospemifene) was confirmed as a true polyp during additional expert review. Endometrial histology showed no evidence of carcinoma. Statistically significant improvements were seen for all primary and secondary efficacy measures and were sustained through week 52 with ospemifene vs. placebo.Conclusions The findings of this 52-week study confirm the tolerance and efficacy of oral ospemifene previously reported in short- and long-term studies.

show abstract

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Ospemifene 12-month safety and efficacy in postmenopausal women with vulvar and vaginal atrophy

et al. 2013

View full text Add to dashboard Cite

show abstract

“…Briefly, tamoxifen has demonstrated an agonist and antagonist activity in the vaginal epithelium,53 as well as gynecological adverse effects such as dyspareunia and vaginal dryness 50,52. The evidence available for raloxifene does not show any effect on postmenopausal monotherapy-treated women’s urogenital epithelium,48,50 or in combination with vaginal estrogens as it provides no additional benefit in relieving genitourinary atrophy signs and symptoms 53–55. Data on bazedoxifene, although limited, conclude that it could only be a safe and effective option in combination with conjugated estrogens as it improves VVA measures56,57 and reduces the incidence of dyspareunia, among other moderate-to-severe VVA symptoms 58…”

Section: Treatment Optionsmentioning

confidence: 99%

“…However, tamoxifen, raloxifene, and bazedoxifene as monotherapy are not currently indicated in VVA treatment 48–52. Briefly, tamoxifen has demonstrated an agonist and antagonist activity in the vaginal epithelium,53 as well as gynecological adverse effects such as dyspareunia and vaginal dryness 50,52.…”

Section: Treatment Optionsmentioning

confidence: 99%

Clinical update on the use of ospemifene in the treatment of severe symptomatic vulvar and vaginal atrophy

Palacios

Cancelo

2016

IJWH

View full text Add to dashboard Cite

The physiological decrease in vaginal estrogens is accountable for the emergence of vulvar and vaginal atrophy (VVA) and its related symptoms such as vaginal dryness, dyspareunia, vaginal and/or vulvar irritation or itching, and dysuria. The repercussion of these symptoms on quality of life often makes it necessary to initiate treatment. Up until now, the treatments available included vaginal moisturizers and lubricants, local estrogens, and hormonal therapy. However, therapeutic options have now been increased with the approval of 60 mg ospemifene, the first nonhormonal oral treatment with an agonist effect on the vaginal epithelium and an endometrial and breast safety profile which makes it unique. This is the first selective estrogen receptor modulator indicated in women with moderate-to-severe vaginal atrophy not eligible for local estrogen treatment. Considering that “local estrogen noneligible women” are those in whom such treatment cannot be administered either because it is contraindicated or due to skill issues, who are averse to the mode and convenience of vaginal products’ administration or to their use on account of potential systemic absorption, or those who demonstrate dissatisfaction in terms of efficacy and safety, it is clear that there is a significant unmet medical need in VVA management. In fact, a great number of women show lack of adherence, dropping out of at least one VVA treatment, including nonhormonal moisturizers and lubricants, which they consider to be ineffective and uncomfortable. If they could choose, many of them may opt for oral treatment. In Phase III studies, ospemifene demonstrated efficacy in vaginal dryness and dyspareunia, regenerating vaginal cells, improving lubrication, and reducing pain during sexual intercourse. Symptoms improved in the first 4 weeks and endured for up to 1 year. Additionally, it demonstrated a good endometrial, cardiovascular system, and breast safety profile.

show abstract

“…Tamoxifen and raloxifene are FDA‐approved SERMs; however, neither is appropriate for systemic treatment of vaginal atrophy. Raloxifene does not have a significant positive effect on the vagina, 3 , 4 , 5 and, although tamoxifen has modest and variable estrogen‐like effects on the vagina, 6 , 7 , 8 , 9 , 10 its long‐term adverse uterine effects (e.g., endometrial cancer) would raise concerns over the risk–benefit ratio if used to treat vaginal atrophy alone. However, there are two newer SERMs in clinical development that may be candidates for the treatment of vaginal atrophy.…”

Section: Compounds With Positive Clinical Data But Not Approved For Vmentioning

confidence: 99%

Progress and Prospects in Treating Postmenopausal Vaginal Atrophy

Winneker¹,

Harris

2010

Clin Pharmacol Ther

View full text Add to dashboard Cite

Anatomically described as a “potential space,” the vagina is a highly estrogen-responsive organ, and its biology changes dramatically at menopause. After menopause, many women experience vaginal dryness and/or dyspareunia, which are caused primarily by regression of the vaginal epithelium.Unlike vasomotor symptoms, which typically resolve overtime, vaginal atrophy remains a persistent consequence of the menopausal transition. This article discusses current trends and potential future treatments that may improve choices for menopausal and postmenopausal women.

show abstract

Effect of raloxifene on the vaginal epithelium of postmenopausal women

Cited by 13 publications

References 24 publications

Ospemifene 12-month safety and efficacy in postmenopausal women with vulvar and vaginal atrophy

Ospemifene 12-month safety and efficacy in postmenopausal women with vulvar and vaginal atrophy

Clinical update on the use of ospemifene in the treatment of severe symptomatic vulvar and vaginal atrophy

Progress and Prospects in Treating Postmenopausal Vaginal Atrophy

Contact Info

Product

Resources

About