Estradiol 3-saccharinylmethyl Ether
Estradiol 3-saccharinylmethyl ether (E2SME), also known as 3-''O''-(saccharinylmethyl)-17β-estradiol, is a synthetic compound, synthetic estrogen (medication), estrogen and estrogen ether – specifically, the C3 saccharine, saccharinylmethyl group, methyl ether of estradiol (medication), estradiol – which was described in the mid-1990s and was never marketed. It is a prodrug of estradiol (medication), estradiol and appears to be partially protected from first-pass metabolism in the liver and intestines with oral administration, showing greatly improved oral potency compared to estradiol. E2SME has been found to be 9-fold as potency (pharmacology), potent as estradiol by the oral administration, oral route in rats. Similarly, its bioavailability (16%) was 5-fold greater than that of estradiol via the oral route in rats, and the elimination half-life of released estradiol was 5- to 7-fold longer than that of regular estradiol. Conversely, when E2SME and estradiol were given intr ...
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