Estradiol (medication)
, estradiol is available in the United States in the following forms:Oral estradiol valerate (Progynova) and other esters of estradiol that are used by injection like estradiol benzoate, estradiol enantate, and estradiol undecylate all are not marketed in the U.S. Polyestradiol phosphate (Estradurin) was marketed in the U.S. previously but is no longer available.
Estradiol (medication)
Estradiol was first isolated in 1935. It was also originally known as "dihydroxyestrin" or "alpha-estradiol". It was first marketed, as estradiol benzoate, in 1936. Estradiol was also marketed in the 1930s under brand names such as Progynon-DH, Ovocylin, and Dimenformon. Micronized estradiol, via the oral route, was first evaluated in 1972, and this was followed by the evaluation of vaginal and intranasal micronized estradiol in 1977. Oral micronized estradiol was first approved in the United States under the brand name Estrace in 1975.
In 1931, Butenandt found that the benzoic acid ester of estrone had a prolonged duration of action. Subsequently, Schwenk and Hildebrant synthesized estradiol benzoate from estradiol in 1933, and estradiol benzoate was introduced by Schering-Kahlbaum for medical use via intramuscular injection under the brand name Progynon-B in 1936. It was the first estrogen ester to be marketed, and has since been followed by many additional esters, for instance estradiol valerate and estradiol cypionate in the 1950s. Ethinylestradiol was synthesized from estradiol by Inhoffen and Hohlweg in 1938 and was introduced for oral use by Schering in the United States under the brand name Estinyl in 1943. It remains widely used in combined oral contraceptives.