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estradiols

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Definitions of estradiols in various dictionaries:

noun - the most powerful female hormone that occurs naturally

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Estradiols might refer to
Estradiol sulfamate (E2MATE; developmental code names J995, PGL-2, PGL-2001, ZK-190628, others), or estradiol-3-O-sulfamate, is a steroid sulfatase (STS) inhibitor which is under development for the treatment of endometriosis. It is the C3 sulfamate ester of estradiol, and was originally thought to be a prodrug of estradiol. The drug shows profoundly reduced susceptibility to first-pass metabolism relative to estradiol, and was believed to be the first "potent" estradiol prodrug to be discovered. It was clinically investigated for possible use as an estrogen for indications like hormonal contraception and menopausal hormone therapy. However, it showed no estrogenic effects in women. This was found to be due to STS inhibition, which blocked the conversion of E2MATE into estradiol and thereby abolished its estrogenicity in humans. Following this, E2MATE was repurposed as a STS inhibitor for the treatment of estrogen-dependent conditions like endometriosis. As of 2017, E2MATE is in phase II clinical trials for endometriosis.Unlike estradiol and other estradiol esters, due to its unique sulfamate ester, E2MATE is not hydrolyzed during the first pass with oral administration, and instead can only be cleaved into estradiol systemically. E2MATE itself shows no affinity for the estrogen receptor or estrogenic activity in vitro, requiring hydrolysis into estradiol for estrogenicity. In accordance, the systemic potency of oral E2MATE as an estrogen in rodents was found to be increased approximately 100-fold relative to that of oral estradiol, whereas its hepatotropic activity is increased only marginally, by about 2- to 3-fold. As such, E2MATE has virtually absent effects on estrogen-modulated liver functions with oral administration at typical dosages equivalent to those of estradiol and behaves much like parenterally or transdermally administered estradiol, thereby combining the advantages of transdermal estradiol with the convenience of oral administration. It has been determined that this is due to binding of E2MATE to carbonic anhydrase II in erythrocytes (red blood cells), which results in E2MATE being rapidly taken up into erythrocytes from the blood of the hepatic portal vein and bypassing the liver during the first pass with oral administration. Following this, E2MATE is slowly released from erythrocytes into the circulation.However, it has been found that E2MATE, without being hydrolyzed first, can be converted by 17β-hydroxysteroid dehydrogenase into estrone sulfamate (EMATE), analogously to the conversion of estradiol into estrone. Moreover, EMATE is the dominant fraction found in the circulation, and EMATE is an extremely potent STS inhibitor. As a result, EMATE prevents the bioactivation of itself and E2MATE into estrone and estradiol, respectively, which effectively abolishes their estrogenic activity in humans. In relation to these findings, according to Elger and colleagues, "In spite of high levels of [E2MATE] and EMATE in the ...

Estradiols might refer to

Estradiol sulfamate (E2MATE; developmental code names J995, PGL-2, PGL-2001, ZK-190628, others), or estradiol-3-O-sulfamate, is a steroid sulfatase (STS) inhibitor which is under development for the treatment of endometriosis. It is the C3 sulfamate ester of estradiol, and was originally thought to be a prodrug of estradiol. The drug shows profoundly reduced susceptibility to first-pass metabolism relative to estradiol, and was believed to be the first "potent" estradiol prodrug to be discovered. It was clinically investigated for possible use as an estrogen for indications like hormonal contraception and menopausal hormone therapy. However, it showed no estrogenic effects in women. This was found to be due to STS inhibition, which blocked the conversion of E2MATE into estradiol and thereby abolished its estrogenicity in humans. Following this, E2MATE was repurposed as a STS inhibitor for the treatment of estrogen-dependent conditions like endometriosis. As of 2017, E2MATE is in phase II clinical trials for endometriosis.Unlike estradiol and other estradiol esters, due to its unique sulfamate ester, E2MATE is not hydrolyzed during the first pass with oral administration, and instead can only be cleaved into estradiol systemically. E2MATE itself shows no affinity for the estrogen receptor or estrogenic activity in vitro, requiring hydrolysis into estradiol for estrogenicity. In accordance, the systemic potency of oral E2MATE as an estrogen in rodents was found to be increased approximately 100-fold relative to that of oral estradiol, whereas its hepatotropic activity is increased only marginally, by about 2- to 3-fold. As such, E2MATE has virtually absent effects on estrogen-modulated liver functions with oral administration at typical dosages equivalent to those of estradiol and behaves much like parenterally or transdermally administered estradiol, thereby combining the advantages of transdermal estradiol with the convenience of oral administration. It has been determined that this is due to binding of E2MATE to carbonic anhydrase II in erythrocytes (red blood cells), which results in E2MATE being rapidly taken up into erythrocytes from the blood of the hepatic portal vein and bypassing the liver during the first pass with oral administration. Following this, E2MATE is slowly released from erythrocytes into the circulation.However, it has been found that E2MATE, without being hydrolyzed first, can be converted by 17β-hydroxysteroid dehydrogenase into estrone sulfamate (EMATE), analogously to the conversion of estradiol into estrone. Moreover, EMATE is the dominant fraction found in the circulation, and EMATE is an extremely potent STS inhibitor. As a result, EMATE prevents the bioactivation of itself and E2MATE into estrone and estradiol, respectively, which effectively abolishes their estrogenic activity in humans. In relation to these findings, according to Elger and colleagues, "In spite of high levels of [E2MATE] and EMATE in the ...

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