Drug intelligence / Profile preview

17α-dihydroequilin sulfate

Development stage
Unknown
Lead developer
Pfizer
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular
01

Overview

17α-dihydroequilin sulfate is the sulfate ester sodium salt form of 17α-dihydroequilin, a naturally occurring equine estrogen. It is one of the principal components of conjugated estrogens (such as those found in the pharmaceutical mixture Premarin), where it constitutes approximately 13.8% of the active mixture. This compound functions as a synthetic, water-soluble estrogen, exerting its activity primarily via binding and activation of the estrogen receptor. Its biological effects are similar to endogenous estrogens, influencing reproductive tissue growth, cholesterol metabolism, and bone density. The sulfate conjugated form is more water-soluble and amenable to pharmaceutical formulation. It is not available as a stand-alone drug product but is included as a constituent of conjugated estrogen mixtures used for menopausal hormone therapy, osteoporosis prevention, and certain estrogen-responsive cancers[1][3][4][5][9].

Other names
17α-Dihydroequilin Sodium Sulfate17α-Dihydro Equilin 3-Sulfateα-Equilol Sodium Sulfate(17α)-Estra-1,3,5(10),7-tetraene-3,17-diol 3-(hydrogen sulfate) sodium salt7-dehydro-17α-estradiolestra-1,3,5(10),7-tetraene-3,17α-diol 3-sulfate sodium salt
02

Targets

ESR2 (ERβ)ESR1 (ERα)

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