Tissue selectivity of ospemifene: Pharmacologic profile and clinical implications

Kangas, Lauri; Unkila, Mikko

doi:10.1016/j.steroids.2013.09.003

Cited by 37 publications

(57 citation statements)

References 32 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

Section: Animal Studiesmentioning

confidence: 76%

“…26 After 1 year, all doses of ospemifene prevented the loss of proximal femur BMC, which was observed in untreated OVX animals, maintaining the baseline mean proximal femur BMC values. 26 Long-term ospemifene treatment also dose-dependently reduced the loss of trabecular BMD after ovariectomy. 26 Animals treated with 1, 5, or 25 mg/kg ospemifene had significantly higher levels of trabecular BMD at the proximal tibia and distal femur relative to OVX controls (P < 0.01 for all).…”

Section: Animal Studiesmentioning

confidence: 76%

“…26 Long-term ospemifene treatment also dose-dependently reduced the loss of trabecular BMD after ovariectomy. 26 Animals treated with 1, 5, or 25 mg/kg ospemifene had significantly higher levels of trabecular BMD at the proximal tibia and distal femur relative to OVX controls (P < 0.01 for all). 26 Lack of any statistically significant difference in trabecular BMD levels at the tibia between ospemifene-treated (25 mg/kg) and sham groups indicated full protection was achieved with ospemifene.…”

Section: Animal Studiesmentioning

confidence: 93%

“…25 A separate 4-week study noted similar improvement in ash weight. 26 An OVX-induced reduction in bone ash weight was prevented after 52 weeks of ospemifene 1 mg/kg, with significant improvement being noted for lumbar vertebra (LV) 3 (P < 0.05), but not for the left tibia. 26 Bone mineral content and density…”

Section: Animal Studiesmentioning

confidence: 94%

“…Two preclinical studies have characterized the short-and long-term effects of ospemifene on bone health and turnover in OVX rats. 25,26 Ash weight Initial measures of ospemifene's effect on bone content were of ash weight. After 4 weeks, ospemifene 1 mg/kg significantly increased the epiphyseal ash weight (P < 0.05 relative to OVX control), but not total ash weight.…”

Section: Animal Studiesmentioning

confidence: 99%

See 4 more Smart Citations

Effects of ospemifene on bone parameters including clinical biomarkers in postmenopausal women

Constantine¹,

Kagan

Miller

2016

Menopause

View full text Add to dashboard Cite

Ospemifene 60 mg/d may have a protective effect on the bone health of women being treated for dyspareunia. The initial clinical data for ospemifene follows a trend similar to raloxifene and bazedoxifene, suggesting that ospemifene may have bone-protective effects in postmenopausal women. However, additional rigorous clinical trials are necessary to confirm any positive effects ospemifene may have on vertebral fractures and bone mineral density in healthy and osteoporotic women.

show abstract

Section: Animal Studiesmentioning

confidence: 76%

Section: Animal Studiesmentioning

confidence: 76%

Section: Animal Studiesmentioning

confidence: 93%

Section: Animal Studiesmentioning

confidence: 94%

Section: Animal Studiesmentioning

confidence: 99%

See 3 more Smart Citations

Effects of ospemifene on bone parameters including clinical biomarkers in postmenopausal women

Constantine¹,

Kagan

Miller

2016

Menopause

View full text Add to dashboard Cite

show abstract

Ospemifene for the Treatment of Vulvovaginal Atrophy and Dyspareunia in Postmenopausal Women

2014

View full text Add to dashboard Cite

Vulvovaginal atrophy (VVA) and dyspareunia are common problems experienced by postmenopausal women, although few seek treatment. Symptom-based therapies include nonhormonal vaginal lubricants, vaginal moisturizers, low-dose vaginal estrogen, and systemic estrogen. The 2013 United States Food and Drug Administration approval of ospemifene, an estrogen agonist/antagonist for the treatment of moderate-to-severe dyspareunia associated with VVA, increased options available to women. Several studies have evaluated the effects of ospemifene on VVA and dyspareunia and indicate an improvement in subjective findings. Objective findings such as a decrease in pH and recovery of a premenopausal vaginal maturation index have been reported. Beneficial effects have also been demonstrated in bone. Evaluations of breast health support the safety of ospemifene, although data are limited to 1 year. Short-term risks appear to be limited and include the development of hot flushes. Until additional comparative studies of ospemifene and estrogens have been performed, ospemifene should be recommended for women with symptoms of VVA and dyspareunia who are unable to tolerate or unwilling to take local or systemic estrogens. In this review, current evidence for the safety and efficacy of ospemifene in the treatment of moderate-to-severe VVA and dyspareunia are evaluated.

show abstract

New potential selective estrogen receptor modulators in traditional Chinese medicine for treating menopausal syndrome

Song,

Shen,

Contreras

et al. 2024

Phytotherapy Research

View full text Add to dashboard Cite

Women go through several predictable conditions and symptoms during menopause that are caused by age, changes in sex hormone levels, and other factors. Conventional menopause hormone therapy has raised serious concerns about the increased risks of cancers, blood clots, depression, etc. Selective estrogen receptor modulators (SERMs) that can be both agonists and antagonists of estrogen receptors in a tissue‐specific manner are being developed to reduce the health concerns associated with menopause hormone therapy. Here, we have searched the Chinese national traditional Chinese medicine (TCM) patent database to identify potential SERM‐like compounds with reduced health risks. TCM has been widely used for treating complex symptoms associated with menopause syndrome and thus can be a particularly rich source for pharmaceutical alternatives with SERM properties. After extensive literature review and molecular simulation, we conclude that protopanaxatriol, paeoniflorin, astragalin, catalpol, and hyperoside among others may be particularly promising as SERM‐like compounds in treating the menopausal syndrome. Compounds in TCM hold promise in yielding comparable outcomes to hormone therapy but with reduced associated risks, thus presenting promising avenues for their clinical applications.

show abstract

Tissue selectivity of ospemifene: Pharmacologic profile and clinical implications

Cited by 37 publications

References 32 publications

Effects of ospemifene on bone parameters including clinical biomarkers in postmenopausal women

Effects of ospemifene on bone parameters including clinical biomarkers in postmenopausal women

Ospemifene for the Treatment of Vulvovaginal Atrophy and Dyspareunia in Postmenopausal Women

New potential selective estrogen receptor modulators in traditional Chinese medicine for treating menopausal syndrome

Contact Info

Product

Resources

About