Cited by 56Reproductive Health and ContraceptionEstrogen and related hormone effectsMenopause: Health Impacts and Treatments

An overview of the development of combined oral contraceptives containing estradiol: focus on estradiol valerate/dienogest

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Fruzzetti, Franca, Trémollieres, Florence, Bitzer, Johannes·2012·Gynecological Endocrinology

Abstract

Natural estrogens such as estradiol (E(2)) or its valerate ester (E(2)V) offer an alternative to ethinyl estradiol (EE). E(2)-containing combined oral contraceptives (COCs) have demonstrated sufficient ovulation inhibition and acceptable contraceptive efficacy. However, earlier formulations were generally associated with unacceptable bleeding profiles. Two E(2)V-containing preparations have been approved to date for contraceptive use: E(2)V/cyproterone acetate (CPA) (Femilar(®); only approved in Finland and only in women >40 years or women aged 35-40 years in whom a COC containing EE is not appropriate) and E(2)V/dienogest (DNG; Qlaira(®)/Natazia(®)). The objective of the current review is to provide an overview of the development of COCs containing natural estrogen, highlighting past issues and challenges faced by earlier formulations, as well as the current status and future directions. The majority of information to date pertains to the development of E(2)V/DNG.

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Authors
Fruzzetti, F., Trémollieres, F., & Bitzer, J.
Affiliations
University Hospital of Basel (CH)
Corresponding author
Fruzzetti, Franca
Venue
Gynecological Endocrinology
Published
2012-04-02
Volume
28
Issue
5
Pages
400-408
ISSN
  • 0951-3590 (ISSN-L)
  • 1473-0766
OpenAlex
W2150882666
Cited by
56
References
52
Citations by year
2026: 3 · 2025: 2 · 2024: 3 · 2023: 2 · 2022: 3 · 2021: 10 · 2020: 3 · 2019: 3 · 2018: 3 · 2017: 2 · 2016: 5 · 2015: 4 · 2014: 7 · 2013: 5 · 2012: 1
FWCI
0.85
Type
journal article
Language
en
Open access
Locations
  • Gynecological Endocrinology (publishedVersion)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
Funders
Bayer HealthCare
Topics
  • Health Sciences › Medicine › Public Health, Environmental and Occupational Health › Reproductive Health and Contraception
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
  • Health Sciences › Medicine › Endocrinology, Diabetes and Metabolism › Menopause: Health Impacts and Treatments
Keywords
estradiol valerate, dienogest, combined oral contraceptives, natural estrogens, cyproterone acetate, bleeding profile, ovulation inhibition, contraceptive efficacy, drug development history
MeSH terms
Contraceptives, Oral, Combined, Estradiol, Female, Humans, Nandrolone, History, 20th Century

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