Estradiol stearate
Estradiol stearate (brand name Depofollan), or estradiol octadecanoate, is a naturally occurring steroidal estrogen and an estrogen ester – specifically, the C17β stearate ester of estradiol. It occurs in the body as a very long-lasting metabolite and prohormone of estradiol. In addition, estradiol stearate is or has been available as a pharmaceutical drug for use via depot intramuscular injection. The drug was introduced in 1941 as Depofollan and was the first long-acting estrogen, although it has never been widely used. It has been reported in at least one source to have a duration of at least one month.
Pharmacokinetics of estradiol
In contrast to estradiol, estrone has very low activity as an estrogen. The affinities of estrone for the human ERs and its estrogenic activity have been reported to be approximately 3 to 4% of those of estradiol. In addition, unlike estradiol and estriol, estrone is not accumulated in target tissues. Because estrone can be transformed into estradiol, most of its activity "in vivo" is actually due to conversion into estradiol. In accordance, dosages of oral and transdermal estradiol that achieve similar levels of estradiol have been found, in spite of markedly elevated levels of estrone with oral estradiol but not with transdermal estradiol, to possess equivalent and non-significantly different potency in terms of clinical measures including suppression of LH and FSH levels, inhibition of bone resorption, and relief of menopausal symptoms such as hot flashes. In addition, estradiol levels were found to correlate with these effects, while estrone levels did not. These findings suggest that estrone contributes very little or not at all to the estrogenic potency of estradiol, while also not antagonizing the estrogenic activity of estradiol. This contradicts some "in vitro" research suggesting that estrone might be able to partially antagonize the actions of estradiol.