Profile of estetrol, a promising native estrogen for oral contraception and the relief of climacteric symptoms of menopause
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| Názov: | Profile of estetrol, a promising native estrogen for oral contraception and the relief of climacteric symptoms of menopause |
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| Autori: | Gérard, Céline, Arnal, Jean-François, Jost, Maud, Douxfils, Jonathan, Lenfant, Françoise, Fontaine, Coralie, Houtman, René, Archer, David, F, Reid, Robert, L, Lobo, Rogerio, A, Gaspard, Ulysse, Coelingh Bennink, Herjan, J T, Creinin, Mitchell, D, Foidart, Jean-Michel |
| Prispievatelia: | Mithra Pharmaceuticals, Institut des Maladies Métaboliques et Casdiovasculaires (UPS/Inserm U1297 - I2MC), Université Toulouse III - Paul Sabatier (UT3), Université de Toulouse (UT)-Université de Toulouse (UT)-Institut National de la Santé et de la Recherche Médicale (INSERM), Centre Hospitalier Universitaire de Toulouse (CHU Toulouse), Université de Namur Namur (UNamur), Qualiblood, Precision Medicine Lab, Eastern Virginia Medical School Norfolk (EVMS), Old Dominion University Norfolk (ODU), Queen's University Kingston, Canada, Columbia University College of Physicians and Surgeons, Université de Liège = University of Liège = Universiteit van Luik = Universität Lüttich (ULiège), Pantarhei Oncology, University of California (UC) |
| Zdroj: | ISSN: 1751-2433. |
| Informácie o vydavateľovi: | CCSD Informa Plc |
| Rok vydania: | 2022 |
| Zbierka: | Université Toulouse III - Paul Sabatier: HAL-UPS |
| Predmety: | Combined oral contraception, E4, contraception, estetrol, estrogen, estrogen receptor, hemostasis, menopause, venous thrombosis, Combined oral contraception contraception estetrol E4 estrogen estrogen receptor hemostasis menopause venous thrombosis, MESH: Contraception, MESH: Contraceptives, Oral, Combined, MESH: Estetrol, MESH: Estrogens, MESH: Female, MESH: Humans, MESH: Menopause, [SDV.MHEP.CSC]Life Sciences [q-bio]/Human health and pathology/Cardiology and cardiovascular system |
| Popis: | International audience ; IntroductionEstrogens used in women’s healthcare have been associated with increased risks of venous thromboembolism (VTE) and breast cancer. Estetrol (E4), an estrogen produced by the human fetal liver, has recently been approved for the first time as a new estrogenic component of a novel combined oral contraceptive (E4/drospirenone [DRSP]) for over a decade. In phase 3 studies, E4/DRSP showed good contraceptive efficacy, a predictable bleeding pattern, and a favorable safety and tolerability profile.Areas coveredThis narrative review discusses E4ʹs pharmacological characteristics, mode of action, and the results of preclinical and clinical studies for contraception, as well as for menopause and oncology.Expert opinionExtensive studies have elucidated the properties of E4 that underlie its favorable safety profile. While classical estrogens (such as estradiol) exert their actions via both activation of nuclear and membrane estrogen receptor α (ERα), E4 presents a specific profile of ERα activation: E4 binds and activates nuclear ERα but does not induce the activation of membrane ERα signaling pathways in specific tissues. E4 has a small effect on normal breast tissue proliferation and minimally affects hepatic parameters. This distinct profile of ERα activation, uncoupling nuclear and membrane activation, is unique. |
| Druh dokumentu: | article in journal/newspaper |
| Jazyk: | English |
| Relation: | info:eu-repo/semantics/altIdentifier/pmid/35306927; PUBMED: 35306927 |
| DOI: | 10.1080/17512433.2022.2054413 |
| Dostupnosť: | https://ut3-toulouseinp.hal.science/hal-04848204 https://ut3-toulouseinp.hal.science/hal-04848204v1/document https://ut3-toulouseinp.hal.science/hal-04848204v1/file/G%C3%A9rard_2022.pdf https://doi.org/10.1080/17512433.2022.2054413 |
| Rights: | http://creativecommons.org/licenses/by-nc-nd/ ; info:eu-repo/semantics/OpenAccess |
| Prístupové číslo: | edsbas.19DD5D6E |
| Databáza: | BASE |
Nájsť tento článok vo Web of Science | Abstrakt: | International audience ; IntroductionEstrogens used in women’s healthcare have been associated with increased risks of venous thromboembolism (VTE) and breast cancer. Estetrol (E4), an estrogen produced by the human fetal liver, has recently been approved for the first time as a new estrogenic component of a novel combined oral contraceptive (E4/drospirenone [DRSP]) for over a decade. In phase 3 studies, E4/DRSP showed good contraceptive efficacy, a predictable bleeding pattern, and a favorable safety and tolerability profile.Areas coveredThis narrative review discusses E4ʹs pharmacological characteristics, mode of action, and the results of preclinical and clinical studies for contraception, as well as for menopause and oncology.Expert opinionExtensive studies have elucidated the properties of E4 that underlie its favorable safety profile. While classical estrogens (such as estradiol) exert their actions via both activation of nuclear and membrane estrogen receptor α (ERα), E4 presents a specific profile of ERα activation: E4 binds and activates nuclear ERα but does not induce the activation of membrane ERα signaling pathways in specific tissues. E4 has a small effect on normal breast tissue proliferation and minimally affects hepatic parameters. This distinct profile of ERα activation, uncoupling nuclear and membrane activation, is unique. |
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| DOI: | 10.1080/17512433.2022.2054413 |