Estetrol is a natural compound that is produced by the fetus during fetal life and circulates in the unborn child and the mother. It is an estrogenic compound. In this study the safety and tolerability of 28 days of the oral administration of estetrol in healthy postmenopausal women are investigated. In addition, the pharmacokinetics and some pharmacodynamic parameters are studied. The lowest dose of 2 mg estetrol is directly compared with 2 mg estradiol.
This is a partly randomized open-label study in healthy postmenopausal women. Groups are treated in the following sequence: first a 2 mg estetrol group together with a 2 mg estradiol group. When the dose of 2 mg estetrol is safe and the tolerability is good, a next higher dose group of estetrol will start, possibly followed by two next higher dose groups if the previous dose group is safe and the tolerability is good. The primary objective of this study is to investigate the safety and tolerability of estetrol during multiple dosing for 28 days. Furthermore steady state pharmacokinetics and some pharmacodynamic parameters of estetrol will be investigated. In addition, the pharmacokinetics and pharmacodynamic effects of the 2 mg estetrol group will be compared with those of the 2 mg estradiol group. In each group 5 postmenopausal women will be included with \> 50 hot flushes per week and 5 postmenopausal women with \< 10 hot flushes per week. These criteria are set to get a more homologous composition in each group.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
TREATMENT
Masking
NONE
Enrollment
49
Kendle Clinical Pharmacology Unit
Utrecht, Utrecht, Netherlands
safety of estetrol
tolerability of estetrol
steady state pharmacokinetics of estetrol
pharmacodynamic effects of estetrol
to compare the pharmacokinetics and pharmacodynamic effects of 2 mg estetrol with 2 mg estradiol
to investigate the effect on the number of hot flushes and sweating of 2 mg estetrol compared with 2 mg estradiol
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