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Moxestrol is a synthetic estrogen and a potent agonist of the estrogen receptor, particularly with higher selectivity for the estrogen receptor alpha (ERα) over ERβ. It is the 11β-methoxy derivative of ethinylestradiol and exhibits an estimated potency 10 to 100 times greater than estradiol and about five times more potent than ethinylestradiol. Moxestrol has minimal plasma protein binding, is metabolized in the liver primarily by hydroxylation, and has a biological half-life of approximately 8.2 hours. It was used in Europe for treating menopausal symptoms and menstrual disorders, as well as studied for postmenopausal disturbances[1][3][4][6]. Its high affinity for ERα underlies its strong estrogenic effects on target tissues such as breast and endometrium[1][6].
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