Estradiol enantate
Estradiol enantate, sold under the brand names Perlutal and Topasel among others, is an estrogen medication which is used in hormonal birth control. It is formulated in combination with dihydroxyprogesterone acetophenide (DHPA; algestone acetophenide), a progestin, and is used as a combined injectable contraceptive. Estradiol enantate is not available alone. The medication is given by injection into muscle once a month.
Side effects of estradiol enantate include breast tenderness, breast enlargement, nausea, headache, and fluid retention. The drug is a synthetic estrogen and hence is an agonist of the estrogen receptor (ER), the biological target of estrogens like estradiol. Estradiol enantate is an estrogen ester and a long-lasting prodrug of estradiol in the body. Because of this, it is considered to be a natural and bioidentical form of estrogen.
Estradiol enantate was first described by 1954, and was first studied in combination with DHPA as a combined injectable contraceptive in 1964. The combination was introduced for clinical use by the mid-1970s. Estradiol enantate is not available as a standalone medication (i.e., by itself without DHPA). The combination is available in Latin America and Hong Kong, and was also previously marketed in Spain and Portugal.
Estetrol (medication)
Estetrol was discovered in 1965 by Egon Diczfalusy and coworkers at the Karolinska Institute in Stockholm, Sweden, via isolation from the urine of pregnant women. Basic research on estetrol was conducted from 1965 to 1984. It was established that estetrol is exclusively synthesized in the fetal liver and hence that it is a fetal estrogen. By 1984, estetrol was regarded as a weak estrogen; interest fell, and research was virtually abandoned. Subsequently a project at Pantarhei Bioscience was started to investigate estetrol with state-of-the-art technologies in 2001, with the sole reasoning that estetrol must have some biological role or function of importance as it would not be produced in such high quantities in the fetus otherwise. By 2008, estetrol was of major interest for potential clinical use, and development was in-progress. As of 2018, it is in mid- to late-stage clinical development for a variety of indications.https://adisinsight.springer.com/drugs/800034634 It was initially developed by Pantarhei Bioscience and Estetra SA (subsequently renamed Estetra SPRL), and is now being developed by Mithra Pharmaceuticals.