Effects of ospemifene: A Synthesis of Findings from 26 Studies

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Original Abstract of the Article

Major Research Findings

Ospemifene is a selective estrogen receptor modulator (SERM) that has been studied for its potential benefits in postmenopausal women. Several studies have examined its effects on various aspects of health, including bone health, vaginal health, cardiovascular health, and breast cancer. 24 , 3 , 4 , 26 , 8 , 21 , 11 , 9 , 2 , 18 , 7 , 17 , 22 , 6 , 23 , 13 , 10 , 16 , 19 , 20 , 1 , 25 , 12 , 14 , 15 , 5 Research suggests that ospemifene may improve bone density, alleviate symptoms of vaginal atrophy, and potentially have positive effects on the cardiovascular system. However, it’s important to note that ospemifene may also increase the risk of breast cancer. 24

Benefits and Risks

Benefit Summary

Ospemifene has shown potential benefits in postmenopausal women, including:

  • Improved Bone Health: Ospemifene may be effective in preventing or treating osteoporosis. 10 , 12 , 18 , 23 , 13 It can potentially increase bone density by decreasing bone absorption and increasing bone formation. 16
  • Improved Vaginal Health: Ospemifene has shown promise in addressing symptoms of vulvar and vaginal atrophy (VVA), such as vaginal dryness, pain, and itching. 3 , 26 , 22 , 11 It can potentially thicken vaginal lining and increase estrogen receptor expression, leading to improvements in vaginal health. 6
  • Potential Cardiovascular Benefits: Ospemifene may have positive effects on the cardiovascular system. 15 It may improve vascular function and reduce blood pressure. 4

Risk Summary

Ospemifene may carry certain risks, including:

  • Increased Breast Cancer Risk: Ospemifene, by acting on estrogen receptors, could increase the risk of breast cancer. 24 , 19 , 5 Women at higher risk of breast cancer should avoid its use.
  • Increased Risk of Blood Clots: Ospemifene might increase the risk of blood clots. 17
  • Side Effects: Ospemifene can lead to side effects such as nausea, indigestion, headaches, and fever. 21 , 25 , 22

Comparison of Studies

Commonalities in Research

Many studies have consistently shown that ospemifene interacts with estrogen receptors, potentially influencing bone health, vaginal health, and cardiovascular health. 24 , 3 , 4 , 26 , 8 , 21 , 11 , 9 , 2 , 18 , 7 , 17 , 22 , 6 , 23 , 13 , 10 , 16 , 19 , 20 , 1 , 25 , 12 , 14 , 15 , 5 Another consistent finding is ospemifene’s ability to inhibit breast cancer cell growth. 24

Differences in Research

The effects of ospemifene may vary across different studies. For instance, some studies show ospemifene increasing bone density, while others do not. 10 , 12 These discrepancies may be attributed to factors such as variations in the dosage of ospemifene used, the age and health status of the participants, and other study design differences. Furthermore, reported side effects of ospemifene may also vary between studies. 21 , 25 , 22

Consistency and Contradictions in Findings

While extensive research has been conducted on ospemifene’s effects, some inconsistencies remain. For example, findings regarding its impact on bone density vary across studies. 10 , 12 This might be related to differences in the ospemifene dosage used, participant demographics, and study methodologies. Furthermore, there’s variability in the reported side effects of ospemifene across different studies. 21 , 25 , 22

Implications for Real-Life Applications

Ospemifene is used to treat vaginal atrophy and prevent osteoporosis in postmenopausal women. 24 , 3 However, it’s crucial to acknowledge that ospemifene might increase the risk of breast cancer, particularly for women with a higher risk of developing this condition. 24 , 19 , 5 Additionally, ospemifene may increase the risk of blood clots, so women at elevated risk for blood clots should use it cautiously. 17

Limitations of Current Research

Current research on ospemifene has some limitations. More research is needed to evaluate its long-term safety and efficacy. Additionally, the effects of ospemifene may vary based on factors such as age, health status, and genetics of the individuals studied, necessitating further investigation. Further research is also essential to thoroughly examine its potential side effects.

Future Research Directions

Large-scale clinical trials are needed to evaluate the long-term safety and effectiveness of ospemifene. Additional research is necessary to explore how its effects might vary based on age, health status, and genetic factors. Furthermore, further investigations are needed to comprehensively examine the potential side effects of ospemifene.

Conclusion

Ospemifene is a SERM that may have potential benefits in postmenopausal women, including improved bone health, vaginal health, and possibly cardiovascular health. However, it is important to be aware of the potential risks, including an increased risk of breast cancer. 24 , 19 , 5 If you are considering ospemifene, consult your doctor to fully understand its potential benefits and risks.

Literature analysis of 26 papers
Positive Content
26
Neutral Content
0
Negative Content
0
Article Type
9
0
1
2
26
1.

Effects of ospemifene on drug metabolism mediated by cytochrome P450 enzymes in humans in vitro and in vivo.

Author: TurpeinenMiia, UusitaloJouko, LehtinenTerhi, KailajärviMarita, PelkonenOlavi, VuorinenJouni, TapanainenPasi, StjernschantzCamilla, LammintaustaRisto, ScheininMika

Drug interactions

Ospemifene, a selective estrogen receptor modulator, is unlikely to significantly affect the metabolism of drugs that are substrates for CYP enzymes. It weakly inhibits CYP enzymes in vitro, but these effects are not observed at clinically relevant concentrations.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

2.

Effects of ospemifene, a novel SERM, on hormones, genital tract, climacteric symptoms, and quality of life in postmenopausal women: a double-blind, randomized trial.

Author: RutanenEeva-Marja, HeikkinenJorma, HalonenKaija, KomiJanne, LammintaustaRisto, YlikorkalaOlavi

Hormone regulation
Vaginal health improvement

Ospemifene, a selective estrogen receptor modulator (SERM), may help prevent bone loss in postmenopausal women. This study found that ospemifene had a strong estrogenic effect on the vaginal epithelium, but did not stimulate the endometrium or aggravate hot flashes.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

4.

Comparative study of the short-term effects of a novel selective estrogen receptor modulator, ospemifene, and raloxifene and tamoxifen on rat uterus.

Author: ZhengHuili, KangasLauri, HärkönenPirkko L

Activate early response genes
Stimulates DNA synthesis
Differential long-term effects

A study investigated the short-term effects of selective estrogen receptor modulators (SERMs) on the uterus of ovariectomized rats. SERMs like ospemifene, tamoxifen, and raloxifene, induced the expression of early response genes and stimulated DNA synthesis in the uterus. However, the specific mechanisms and long-term effects of each SERM may vary.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

7.

Effects of ospemifene on overactive bladder in postmenopausal women with vulvovaginal atrophy.

Author: RussoE, MisasiG, Montt-GuevaraM M, GianniniA, SimonciniT

OAB treatment
VVA treatment

This study aimed to evaluate the effects of ospemifene on OAB symptoms in PMW with VVA.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

8.

Effects of ospemifene, a novel selective estrogen-receptor modulator, on human breast tissue ex vivo.

Author: EigelieneNatalija, KangasLauri, HellmerChristina, KaukoTommi, ErkkolaRisto, HärkönenPirkko

Treatment of dyspareunia

Ospemifene, a selective estrogen-receptor modulator (SERM), has similar effects on human breast tissue as other SERMs like raloxifene and tamoxifen.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

9.

Effects of cytochrome P450 inhibitors and inducers on the metabolism and pharmacokinetics of ospemifene.

Author: LehtinenTerhi, TolonenAri, TurpeinenMiia, UusitaloJouko, VuorinenJouni, LammintaustaRisto, PelkonenOlavi, ScheininMika

CYP interaction

Ospemifene metabolism is primarily mediated by CYP3A4, but other CYP isoforms contribute. Strong CYP3A or CYP2C9 inducers may decrease ospemifene exposure, while potent CYP3A inhibitors may increase exposure.

Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

11.

Effects of ospemifene on genitourinary health assessed by prospective vulvar-vestibular photography and vaginal/vulvar health indices.

Author: GoldsteinIrwin, SimonJames A, KaunitzAndrew M, AltomareCorrado, YoshidaYuki, ZhuJulie, SchafferSam, SoulbanGraziella

Improved vulvar-vaginal health
Reduced vaginal dryness

A 12-week, double-blind, phase 3 study of 631 postmenopausal women with moderate to severe vaginal dryness showed that ospemifene significantly improved vulvovaginal health compared to placebo.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Multicenter StudyResearch conducted in collaboration with multiple research institutions. It aims to collect a wide range of data and obtain more generalizable results.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

12.

Effects of ospemifene, a novel SERM, on biochemical markers of bone turnover in healthy postmenopausal women.

Author: KomiJ, HeikkinenJ, RutanenE M, HalonenK, LammintaustaR, YlikorkalaO

Reduced bone turnover

This study shows that ospemifene, a drug that mimics the effects of estrogen, can reduce bone turnover in postmenopausal women. It lowered markers of bone resorption and formation, suggesting it could help maintain bone density and prevent osteoporosis.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Clinical Trial, Phase IIA Phase II trial is a trial that further evaluates the efficacy and safety of a new drug or treatment, whose safety has been confirmed to some extent in a Phase I trial, in a small number of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

13.

Effects of ospemifene on bone in postmenopausal women.

Author: de VilliersT J, AltomareC, ParticcoM, GambaccianiM

Bone health

This review summarizes the effects of ospemifene, a selective estrogen-receptor modulator, on bone health. Ospemifene has been shown to decrease bone turnover markers and may play a role in maintaining bone health in postmenopausal women. However, further long-term studies are needed to confirm these effects.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Systematic ReviewA review that systematically collects, evaluates, and integrates relevant research to answer a specific research question.

Language : English

14.

Effects of ospemifene on the female reproductive and urinary tracts: translation from preclinical models into clinical evidence.

Author: ArcherDavid F, CarrBruce R, PinkertonJoAnn V, TaylorHugh S, ConstantineGinger D

Menopausal symptom treatment

Selective estrogen receptor modulators (SERMs) are being investigated as an alternative to estrogen therapy for managing menopausal symptoms. These molecules selectively target estrogen receptors in different tissues, potentially improving postmenopausal women's health by preventing and treating conditions like breast cancer, osteoporosis, and vulvar and vaginal atrophy.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.

Language : English

15.

Effects of ospemifene, a novel SERM, on vascular markers and function in healthy, postmenopausal women.

Author: YlikorkalaOlavi, CacciatoreBruno, HalonenKaija, LassilaRiitta, LammintaustaRisto, RutanenEeva-Marja, HeikkinenJorma, KomiJanne

Cholesterol reduction
Fibrinogen reduction
Triglyceride increase

Ospemifene, a selective estrogen receptor modulator (SERM), may help prevent bone loss in postmenopausal women. This study found that short-term use of ospemifene did not increase the risk of cardiovascular disorders in healthy postmenopausal women.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

16.

Differential effects of selective oestrogen receptor modulators (SERMs) tamoxifen, ospemifene and raloxifene on human osteoclasts in vitro.

Author: MichaelH, HärkönenP L, KangasL, VäänänenH K, HentunenT A

Bone health improvement

This abstract investigates the effects of different types of selective oestrogen receptor modulators (SERMs) on osteoclast differentiation, bone resorption, and apoptosis in vitro.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

17.

Ospemifene's effects on lipids and coagulation factors: a post hoc analysis of phase 2 and 3 clinical trial data.

Author: ArcherDavid F, AltomareCorrado, JiangWei, CortSusannah

Decreased LDL
Increased HDL

Ospemifene 60 mg did not have a detrimental effect on lipid and coagulation parameters in postmenopausal women over 12 months of use.

Clinical Trial, Phase IIA Phase II trial is a trial that further evaluates the efficacy and safety of a new drug or treatment, whose safety has been confirmed to some extent in a Phase I trial, in a small number of patients.
Clinical Trial, Phase IIIA Phase III trial is a trial that further rigorously verifies the efficacy and safety of a new drug or treatment, whose efficacy and safety have been confirmed in a Phase II trial, in a large number of patients, and evaluates whether it is superior to existing treatments.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

18.

Effects of ospemifene and raloxifene on biochemical markers of bone turnover in postmenopausal women.

Author: KomiJanne, LankinenKari S, DeGregorioMichael, HeikkinenJorma, SaarikoskiSeppo, TuppurainenMarjo, HalonenKaija, LammintaustaRisto, VäänänenKalervo, YlikorkalaOlavi, ErkkolaRisto

Bone restoration
Osteoporosis prevention
Vaginal atrophy treatment

Ospemifene, a selective estrogen receptor modulator (SERM), was compared to raloxifene for its effects on bone turnover in postmenopausal women. Both drugs reduced bone resorption, with ospemifene showing comparable bone-restoring activity to raloxifene.

Clinical Trial, Phase IIA Phase II trial is a trial that further evaluates the efficacy and safety of a new drug or treatment, whose safety has been confirmed to some extent in a Phase I trial, in a small number of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

19.

Effects of ospemifene on breast tissue morphology and proliferation: a comparative study versus other selective estrogen receptor modulators in ovariectomized rats.

Author: KangasL, HärkönenP, VäänänenK, KeskitaloJ, EigélienéN

Dyspareunia treatment

Ospemifene, a selective estrogen receptor modulator, is approved for treating dyspareunia associated with vulvar and vaginal atrophy. This study investigated ospemifene's potential estrogenic activity in the mammary glands of ovariectomized rats. Ospemifene did not show substantial estrogenic activity in the mammary gland, indicating that it may be a safer option for women concerned about breast cancer risk.

Comparative StudyResearch that compares multiple groups/interventions to determine differences/similarities in outcomes/characteristics.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

20.

Pharmacologic effects of ospemifene in rhesus macaques: a pilot study.

Author: WurzGregory T, Hellmann-BlumbergUtha, DeGregorioMichael W

Favorable pharmacokinetics
No genotoxic effects

Ospemifene, a new selective estrogen receptor modulator, is being developed for the treatment of postmenopausal vulvar and vaginal atrophy. In a pilot study in rhesus macaques, ospemifene showed favorable pharmacokinetic properties and no significant haematologic toxicities or uterotrophic effects. It also did not induce DNA adducts in liver or endometrial tissues.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Research Support, N.I.H., ExtramuralResearch funding provided by the NIH to external research institutions and researchers.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

21.

Effects of ospemifene and raloxifene on hormonal status, lipids, genital tract, and tolerability in postmenopausal women.

Author: KomiJanne, LankinenKari S, HärkönenPirkko, DeGregorioMichael W, VoipioSari, KivinenSeppo, TuimalaRisto, VihtamäkiTarja, VihkoKimmo, YlikorkalaOlavi, ErkkolaRisto

Estrogenic effect
Hormonal balance
Vaginal health
Lipid changes

Ospemifene, particularly at the dose of 90 mg/day, was more estrogenic than raloxifene in postmenopausal women, with a clear estrogenic effect in the vagina. Neither agent stimulated the endometrium.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

22.

Vulvar vestibular effects of ospemifene: a pilot study.

Author: MurinaFilippo, Di FrancescoStefania, OnedaSilvia

Dyspareunia relief
Vulvar pain relief
Hot flashes

Ospemifene is effective in treating vulvar vestibulitis in postmenopausal women. It reduced dryness, burning, and dyspareunia symptoms, and normalized vestibular innervation sensitivity.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

23.

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

Author: ConstantineGinger D, KaganRisa, MillerPaul D

Bone health improvement

Ospemifene, an estrogen-receptor agonist/antagonist, is FDA approved for the treatment of vulvovaginal atrophy. This study reviews preclinical and clinical data suggesting that ospemifene may also have beneficial effects on bone health in postmenopausal women.

Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
ReviewAn article that critically examines existing research on a particular topic and summarizes the current state of knowledge in the field.
Research Support, Non-U.S. Gov'tResearch funding provided by government agencies outside the United States.

Language : English

25.

Effects of ospemifene (FC-1271a) on uterine endometrium, vaginal maturation index, and hormonal status in healthy postmenopausal women.

Author: VoipioS K, KomiJ, KangasL, HalonenK, DeGregorioM W, ErkkolaR U

Bone health
Cardiovascular health

This study investigated the effects of ospemifene, a novel selective estrogen receptor modulator (SERM), on the uterine endometrium, vaginal maturation index, and hormonal status in healthy postmenopausal women. The results suggest that ospemifene may have estrogen-like effects on bone and the cardiovascular system, while having antiestrogen-like effects in the uterus and breast.

Clinical TrialA clinical trial is a planned study conducted on humans to evaluate the efficacy and safety of pharmaceuticals, medical devices, and treatment methods. It aims to explore the possibilities of new treatments and improve the health of patients.
Clinical Trial, Phase IThe first stage of clinical trials in humans. Evaluates the safety, tolerability, and pharmacokinetics of a new drug/treatment.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.
Randomized Controlled TrialA clinical trial that randomly assigns participants to treatment and control groups to evaluate the effects of an intervention.

Language : English

26.

Vaginal effects of ospemifene in the ovariectomized rat preclinical model of menopause.

Author: UnkilaMikko, KariSeppo, YatkinEmrah, LammintaustaRisto

VVA treatment

Ospemifene is a tissue-selective estrogen agonist/antagonist (SERM) that is effective in treating vulvar and vaginal atrophy in postmenopausal women. In an animal model of menopause, ospemifene increased vaginal weight and epithelial height more effectively than raloxifene. Ospemifene also upregulated progesterone receptors in the vaginal epithelium and stroma, confirming its estrogenic activity. However, ospemifene antagonized estrogen response element-mediated transactivation in breast cancer cells, demonstrating its anti-estrogenic activity.

Clinical Trial, Phase IIIA Phase III trial is a trial that further rigorously verifies the efficacy and safety of a new drug or treatment, whose efficacy and safety have been confirmed in a Phase II trial, in a large number of patients, and evaluates whether it is superior to existing treatments.
Journal ArticleAn article published in an academic or professional journal that reports original research or scholarly analysis.

Language : English

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