Under conditions associated with reduced estrogen synthesis in humans (aromatase deficiency, placental sulfatase deficiency, fetal anencephaly), estrogen production and concentrations may be reduced by 80-90%.
Estrone sulfate partially blocked the inactivation of the enzyme by the compound, indicating that the compound inactivated sulfatase at the active site.
However, a recent report indicated that estrone may be released during the inactivation of sulfatase by estrone-3-O-sulfamate and rendered the inhibitor to be estrogenic.
Routes of administration and dosages of commonly used estrogens Estrogen Route Dosage Natural and equine estrogens Conjugated equine estrogens Oral 0.3-2.5 mg/day Intramuscular 25 mg/day Intravenous 25 mg/day Vaginal 2-4 g/day Piperazine estrone sulfate Oral 0.625-2.5 mg/day Vaginal 2-4 g/day Estradiol Patch 0.05-0.1 mg every 3-4 days Vaginal 1-4 g/day Micronized, valerate Oral 1-2 mg/day Valerate Intramuscular 10 mg/month Cypionate Intramuscular 1-5 mg/month Synthetic estrogens Ethinylestradiol Oral 20-50 µg/day Mestranol Oral 50-100 µg/day Diethylstilbestrol Oral 1-5 mg/day Quinestrol Oral 0.1 mg/day Table 17.
Several research groups have reported the development of estrone sulfatase inhibitors, and estrone-3-O-sulfamate has been shown to be the most potent sulfatase inhibitor.