Estradiol valerate
In addition to single-drug formulations, oral estradiol valerate is available in combination with the progestin dienogest as a combined oral contraceptive and intramuscular estradiol valerate is marketed in combination with the progestins hydroxyprogesterone caproate and norethisterone enantate as combined injectable contraceptives. Intramuscular estradiol valerate has also been marketed in combination with testosterone enantate, but this formulation has been discontinued. The availability of estradiol valerate-containing products varies throughout the world.
Estriol
Although estriol is an efficacious agonist of the ERs, it is reported to have mixed agonist–antagonist (partial agonist) activity at the ER; on its own, it is weakly estrogenic, but in the presence estradiol, it is antiestrogenic. Given by subcutaneous injection in mice, estradiol is about 10-fold more potent than estrone and about 100-fold more potent than estriol. It is notable that unlike estriol, estrone can be metabolized into estradiol, and most of its potency "in vivo" is in fact actually due to conversion into estradiol.