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Cited by 45Menopause: Health Impacts and TreatmentsEstrogen and related hormone effectsPhytoestrogen effects and research

The DOI matches its Crossref record; 40 of the 40 references it cites were found in a registry or an index.

Pharmacodynamic effects of the fetal estrogen estetrol in postmenopausal women: results from a multiple-rising-dose study

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Coelingh Bennink, Herjan J.T., Verhoeven, Carole, Zimmerman, Yvette, Visser, Monique, Foidart, Jean-Michel, Gemzell-Danielsson, Kristina·2017·Menopause
DOI 10.1097/gme.0000000000000823
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Abstract

OBJECTIVE: Estetrol (E4) is an estrogen produced exclusively by the human fetal liver during pregnancy. In this study the pharmacodynamic effects of escalating doses of E4 in postmenopausal women were investigated. METHODS: This was a partly randomized, open-label, multiple-rising-dose study in 49 postmenopausal women. Participants were randomized to receive either 2 mg E4 or 2 mg estradiol-valerate (E2 V) for 28 days. Subsequent dose-escalation groups were (non-randomized): 10, 20 and 40 mg E4. Blood samples were collected regularly for measuring endocrine and hemostasis variables, lipids and lipoproteins, fasting glucose and bone turnover markers. RESULTS: Estetrol treatment resulted in a decrease of follicle-stimulating hormone and luteinizing hormone and an increase of sex-hormone binding globulin. Changes in hemostasis variables were small. A lowering effect on low-density lipoprotein cholesterol was accompanied with an increase in high-density lipoprotein cholesterol and no or minimal changes in triglycerides. The considerable decrease in osteocalcin levels in the three highest E4 dose groups and the small decrease in C-telopeptide levels were comparable to the E2 V control group and suggest a preventive effect on bone loss. All changes observed were dose-dependent. CONCLUSIONS: In this study, estetrol treatment showed dose-dependent estrogenic effects on endocrine parameters, bone turnover markers, and lipids and lipoproteins. The effect on triglycerides was small as were the effects on hemostatic variables. These results support the further investigation of estetrol as a candidate for hormone therapy. Quantitatively, the effects of 10 mg estetrol were similar to the study comparator 2 mg estradiol valerate.

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Metadata

Authors
Coelingh Bennink, H. J. T., Verhoeven, C., Zimmerman, Y., Visser, M., Foidart, J.-M., & Gemzell-Danielsson, K.
Affiliations
  • Pantarhei Bioscience BV, Zeist, The Netherlands
  • Pantarhei Bioscience (Netherlands) (NL)
  • University of Liège (BE)
  • Department of Women's and Children's Health, Karolinska Institutet and Karolinska University Hospital, Stockholm, Sweden.
ORCID
Venue
Menopause
Publisher
Ovid Technologies (Wolters Kluwer Health)
Published
2017-06
Volume
24
Issue
6
Pages
677-685
ISSN
  • 1072-3714 (ISSN-L)
  • 1530-0374
DOI
10.1097/gme.0000000000000823
OpenAlex
W2588950891
Cited by
45
References
40
Citations by year
2026: 2 · 2025: 5 · 2024: 5 · 2023: 3 · 2022: 7 · 2021: 7 · 2020: 6 · 2019: 4 · 2018: 2 · 2017: 3
FWCI
3.24
Type
journal article
Language
en
Open access
Licence
Locations
  • Menopause The Journal of The North American Menopause Society (publishedVersion, cc-by-nc-nd)
  • PubMed (publishedVersion)
Topics
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Menopause: Health Impacts and Treatments
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Endocrinology › Estrogen and related hormone effects
  • Health Sciences › Nursing › Nutrition and Dietetics › Phytoestrogen effects and research
Keywords
estetrol, postmenopausal women, hormone therapy, estradiol valerate, follicle-stimulating hormone, luteinizing hormone, sex hormone-binding globulin, lipoproteins, LDL cholesterol, HDL cholesterol, triglycerides, bone turnover markers, osteocalcin, C-terminal telopeptide, bone loss prevention, dose-dependent effects, hemostasis
MeSH terms
Aged, Cholesterol, Dose-Response Relationship, Drug, Estetrol, Estradiol, Female, Follicle Stimulating Hormone, Humans, Luteinizing Hormone, Cholesterol, HDL, Cholesterol, LDL, Middle Aged, Peptides, Sex Hormone-Binding Globulin, Osteoporosis, Postmenopausal, Osteocalcin, Postmenopause, Collagen Type I

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