No full text
Contribution to collective works (Parts of books)
Unique Vascular Benefits of Estetrol, a Native Fetal Estrogen with Specific Actions in Tissues (NEST)
Foidart, Jean-Michel; GASPARD, Ulysse; Pequeux, Christel et al.
2019In Diaz Brinton, Roberta; Genazzani, Andrea; Simoncini, Tommaso et al. (Eds.) Sex Steroids' Effects on Brain, Heart and Vessels: Volume 6: Frontiers in Gynecological Endocrinology
Peer reviewed
 

Files


Full Text
No document available.

Send to



Details



Abstract :
[en] Estrogens (E), in combination with oral contraceptives (COCs) and hormone replacement therapy (HRT) drugs used for the relief of climacteric symptoms of menopause, increase the synthesis of clotting factors, decrease the levels of coagulation inhibitors, and increase the risk of venous thromboembolic events (VTE). Ischemic stroke incidence in postmenopausal women during HRT use is also increased and is probably due to a thrombotic event. This suggests that a safer estrogen may reduce stroke and VTE incidence, with lower impact on hemostasis. Estetrol (E4) is a relatively recently described new human-specific E produced exclusively by the fetal liver during pregnancy. This Native (human and natural) E has Selective actions in Tissues (NEST). Nest activities of E4 are the consequence of its unique dual role. It activates the nuclear estrogen receptor alpha (ERα) but antagonizes the membrane ERα in contrast to other E, which activate both types of receptors. Most beneficial effects of E on the vascular system have been ascribed to the activation of the membrane ERα of vascular endothelial cells, including enhancement of nitric oxide (NO) production, vasodilation, and prevention of atherosclerosis, of neointimal proliferation, and of hypertension. In a series of papers reviewed here, the INSERM team in Toulouse has demonstrated, by the combined use of pharmacological tools and of transgenic mice lacking either the nuclear ERα, the membrane ERα, or both, that the nuclear ERα plays a major role in controlling E activities in vessels. E4 is able to elicit the important vasculoprotective actions mediated by estradiol (E2). Furthermore, phase 1 and 2 clinical studies of E4 in a contraceptive indication (in combination with drospirenone) or in postmenopausal women for the relief of climacteric complaints demonstrate that E4 has a minimal impact on hemostasis, coagulation factors, coagulation inhibitors, fibrinolysis, angiotensinogen, triglycerides, and cholesterol. Altogether, preclinical studies and phase 1 and 2 clinical data indicate that E4 could be a new E with a better safety/efficacy profile than other E for women’s healthcare.
Disciplines :
Cardiovascular & respiratory systems
Author, co-author :
Foidart, Jean-Michel ;  Université de Liège - ULiège > Département des sciences cliniques > Département des sciences cliniques
GASPARD, Ulysse ;  Centre Hospitalier Universitaire de Liège - CHU > Département de gynécologie-obstétrique > Service de gynécologie-obstétrique
Pequeux, Christel  ;  Université de Liège - ULiège > Département des sciences biomédicales et précliniques > Département des sciences biomédicales et précliniques
Jost, Maud
Gordenne, Valérie
Tskitishvili, Ekaterine  ;  Université de Liège - ULiège > Cancer-Tumours and development biology
Gallez, Anne ;  Université de Liège - ULiège > Cancer-Tumours and development biology
Valera, Marie-C.;  I2MC, Institut National de la Santé et de la Recherche Médicale (INSERM) U 1048, University of Toulouse 3, Toulouse, France
Gourdy, Pierre;  I2MC, Institut National de la Santé et de la Recherche Médicale (INSERM) U 1048, University of Toulouse 3, Toulouse, France
Fontaine, Coralie;  I2MC, Institut National de la Santé et de la Recherche Médicale (INSERM) U 1048, University of Toulouse 3, Toulouse, France
Henrion, Daniel
Genazzani, Andrea R.;  University of Pisa
Lenfant, Françoise;  I2MC, Institut National de la Santé et de la Recherche Médicale (INSERM) U 1048, University of Toulouse 3, Toulouse, France
Arnal, Jean-François;  I2MC, Institut National de la Santé et de la Recherche Médicale (INSERM) U 1048, University of Toulouse 3, Toulouse, France
More authors (4 more) Less
Language :
English
Title :
Unique Vascular Benefits of Estetrol, a Native Fetal Estrogen with Specific Actions in Tissues (NEST)
Publication date :
2019
Main work title :
Sex Steroids' Effects on Brain, Heart and Vessels: Volume 6: Frontiers in Gynecological Endocrinology
Author, co-author :
Diaz Brinton, Roberta
Genazzani, Andrea
Simoncini, Tommaso
Stevenson, John
Publisher :
Springer Nature, Cham, Switzerland
ISBN/EAN :
978-3-030-11354-4
Collection name :
ISGE Series, International Society of Gynecological Endocrinology
Peer reviewed :
Peer reviewed
Available on ORBi :
since 21 February 2020

Statistics


Number of views
259 (10 by ULiège)
Number of downloads
0 (0 by ULiège)

OpenCitations
 
0

Bibliography


Similar publications



Contact ORBi