Comparison of the pharmacologic and clinical profiles of new combined oral contraceptives containing estradiol

Jeffrey T. Jensen, Johannes Bitzer, Marco Serrani
In: Open Access Journal of Contraception · 2013 · pp. 39 · doi:10.2147/oajc.s50693 · W1971661444
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⚙ AI-generated summary by claude@2026-06, 2026-06-07 ⓘ

This review compared three estradiol-containing oral contraceptives, finding them all effective but noting potential bleeding profile advantages for estradiol valerate/dienogest and estradiol/nomegestrol acetate.

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-07 · read from full text ⓘ

This paper reviews published information on three estradiol-containing combined oral contraceptives (estradiol valerate/cyproterone acetate, estradiol valerate/dienogest, and estradiol/nomegestrol acetate), aiming to compare their pharmacologic and clinical profiles using an Ovid-based literature search. The authors report that all three formulations are effective oral contraceptives, and while direct head-to-head comparisons are lacking, indirect evidence indicates E2V/DNG and E2/NOMAC may produce better bleeding profiles than E2V/CPA. They further state that E2V/DNG and E2/NOMAC have minimal effects on hemostatic, lipid, and carbohydrate metabolism parameters compared with ethinylestradiol-based pills, but note that the clinical meaning of surrogate markers is debated and requires large post-marketing prospective Phase IV studies. This paper does not explicitly discuss endometriosis or adenomyosis; it was included in the corpus via a keyword match in the upstream search index.

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Abstract

Abstract: Three estradiol (E 2 )-containing oral contraceptives, estradiol valerate/cyproterone acetate (E 2 V/CPA, Femilar ® ), estradiol valerate/dienogest (E 2 V/DNG, Qlaira ® /Natazia™), and estradiol/nomegestrol acetate (E 2 /NOMAC; Zoely ® ), have received approval for use in general practice. Only Finnish women currently have access to all three E 2 -based formulations. E 2 /NOMAC is currently approved only in Europe, while E 2 V/DNG is approved globally. To assist clinicians counseling women considering use of one of these formulations, we conducted a review of the published information about the current E 2 -containing oral contraceptives. A literature search was conducted using the Ovid interface and a combination of free search terms relevant to estradiol and oral contraception to identify suitable articles for inclusion in this review. The available data show that E 2 V/DNG, E 2 /NOMAC, and E 2 V/CPA are all effective oral contraceptives. While direct comparisons are lacking, indirect evidence suggests that E 2 V/DNG and E 2 /NOMAC may have better bleeding profiles than E 2 V/CPA. E 2 V/DNG is also approved for the treatment of heavy menstrual bleeding. Both E 2 V/DNG and E 2 /NOMAC have minimal influence on hemostatic, lipid, and carbohydrate metabolism parameters, or induce less change in these parameters relative to ethinylestradiol-based oral contraceptives. However, the predictive value of these surrogate parameters is a matter of debate, and whether these differences can be translated into meaningful clinical outcomes needs to be established in large-scale, post-marketing, prospective, Phase IV cohort studies. Future studies are required to determine whether E 2 -based oral contraceptives confer additional benefits compared with those of ethinylestradiol-based COCs. Keywords: estradiol valerate, dienogest, nomegestrol acetate, cyproterone acetate
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Abstract

Three estradiol (E2)-containing oral contraceptives, estradiol valerate/cyproterone acetate (E2V/CPA, Femilar®), estradiol valerate/dienogest (E2V/DNG, Qlaira®/Natazia™), and estradiol/nomegestrol acetate (E2/NOMAC; Zoely®), have received approval for use in general practice. Only Finnish women currently have access to all three E2-based formulations. E2/NOMAC is currently approved only in Europe, while E2V/DNG is approved globally. To assist clinicians counseling women considering use of one of these formulations, we conducted a review of the published information about the current E2-containing oral contraceptives. A literature search was conducted using the Ovid interface and a combination of free search terms relevant to estradiol and oral contraception to identify suitable articles for inclusion in this review. The available data show that E2V/DNG, E2/NOMAC, and E2V/CPA are all effective oral contraceptives. While direct comparisons are lacking, indirect evidence suggests that E2V/DNG and E2/NOMAC may have better bleeding profiles than E2V/CPA. E2V/DNG is also approved for the treatment of heavy menstrual bleeding. Both E2V/DNG and E2/NOMAC have minimal influence on hemostatic, lipid, and carbohydrate metabolism parameters, or induce less change in these parameters relative to ethinylestradiol-based oral contraceptives. However, the predictive value of these surrogate parameters is a matter of debate, and whether these differences can be translated into meaningful clinical outcomes needs to be established in large-scale, post-marketing, prospective, Phase IV cohort studies. Future studies are required to determine whether E2-based oral contraceptives confer additional benefits compared with those of ethinylestradiol-based COCs.

Keywords

estradiol valerate, dienogest, nomegestrol acetate, cyproterone acetate © 2013 The Author(s). This work is published and licensed by Dove Medical Press Limited. The full terms of this license are available at https://www.dovepress.com/terms and incorporate the Creative Commons Attribution - Non Commercial (unported, 3.0) License. By accessing the work you hereby accept the Terms. Non-commercial uses of the work are permitted without any further permission from Dove Medical Press Limited, provided the work is properly attributed. For permission for commercial use of this work, please see paragraphs 4.2 and 5 of our Terms.

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