2012/04/02 by Franca Fruzzetti, Florence Trémollières, Johannes Bitzer · 2 citations
Medicine · #Reproductive Health and Contraception #Ovarian function and disorders #Menopause: Health Impacts and Treatments
paper · pdf · doi:10.3109/09513590.2012.662547
openalex publication_date 2012/04/02 · openalex created_date 2025/10/10 · openalex updated_date 2026/08/04
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.