This is a list of estrogen esters, or ester prodrugs of estrogens. It includes esters, as well as ethers, of steroidal estrogens like estradiol, estrone, and estriol and of nonsteroidal estrogens like the stilbestrols diethylstilbestrol and hexestrol.
Esters of steroidal estrogens
Estradiol esters
Marketed Many esters of estradiol have been marketed, including the following major esters:
Estradiol acetate (Femring, Femtrace, Menoring) Estradiol benzoate (Agofollin Depot, Progynon-B; Duogynon, Primosiston, Sistocyclin) Estradiol cypionate (Depo-Estradiol, Depofemin, Estradep; Cyclofem, Lunelle) Estradiol dipropionate (Agofollin, Di-Ovocyclin, Progynon-DP; EP Hormone Depot) Estradiol enanthate (Perlutal, Topasel, Unalmes, Yectames) Estradiol undecylate (Delestrec, Progynon Depot) Estradiol valerate (Delestrogen, Progynon Depot, Progynova; Gravibinon, Mesigyna, Mesygest; Neofollin) Polyestradiol phosphate (Estradurin) (an estradiol ester in polymeric form) And the following less commonly used esters:
Cloxestradiol acetate (Genovul; diacetate ester of cloxestradiol, or estradiol 17β-chloral hemiacetal ether) Estradiol benzoate butyrate (Redimen, Soluna, Unijab, Unimens) Estradiol butyrylacetate (Follikoside) Estradiol dibutyrate (Triormon Depositum) Estradiol dienantate (Climacteron, Lactimex, Lactostat) Estradiol diundecylate (Estrolent; Trioestrine Retard) Estradiol diundecylenate (Etrosteron) Estradiol furoate (Di-Folliculine) Estradiol hemisuccinate (Eutocol; Hosterona) Estradiol hemihydrate (Estrofem) Estradiol hexahydrobenzoate (Benzo-Ginoestril A.P., BenzoGynoestryl Retard, Ginestryl-15-Depot, Menodin, Tardoginestryl) Estradiol palmitate (Esmopal) Estradiol phenylpropionate (Dimenformon Prolongatum; Estandron Prolongatum, Lynandron Prolongatum, Mixogen) Estradiol pivalate (Estrotate; Estrotate with Progesterone) Estradiol propionate (estradiol 17β-propionate) (Acrofollin, Akrofollin, Follhormon) Estradiol propoxyphenylpropionate (Durovex) Estradiol stearate (Depofollan) Estradiol sulfate (a minor constituent of conjugated estrogens (Premarin)) The following nitrogen mustard ester of estradiol is a cytostatic antineoplastic agent and has been marketed:
Estramustine phosphate (Emcyt, Estracyt; estradiol 3-normustine 17β-phosphate)
Never marketed A number of other estradiol esters which have not been marketed include:
Estradiol 3-furoate Estradiol 3-propionate (not to be confused with estradiol monopropionate (estradiol 17β-propionate)) Estradiol 17β-(1-(4-(aminosulfonyl)benzoyl)-L-proline) (EC508) Estradiol acetate benzoate Estradiol 17β-acetate Estradiol 17β-benzoate Estradiol acetylsalicylate (estradiol 3-acetylsalicylate) Estradiol anthranilate (estradiol 3-anthranilate) Estradiol arachidonate Estradiol benzoate cyclooctenyl ether (estradiol 3-benzoate 17β-cyclooctenyl ether; EBCO) Estradiol caprylate (estradiol octanoate) Estradiol cyclooctyl acetate (E2CoA) Estradiol decanoate (estradiol 17β-decanoate) Estradiol diacetate Estradiol dibenzoate Estradiol dicypionate Estradiol dioleate Estradiol dipalmitate Estradiol distearate Estradiol disulfate Estradiol glucuronide Estradiol sulfate glucuronide Estradiol linoleate Estradiol oleate Estradiol phosphate Estradiol salicylate (estradiol 3-salicylate) Estradiol sulfamate (E2MATE; J995, PGL-2, PGL-2001, ZK-190628; estradiol-3-O-sulfamate) Estradiol undecylenate (SH-368) Estrapronicate (estradiol 3-propionate 17β-nicotinate; Trophobolene, Trophoboline) Orestrate (estradiol 3-propionate 17β-(1-cyclohexenyl) ether) The following cytostatic antineoplastic nitrogen mustard esters of estradiol have not been marketed:
Alestramustine (estradiol 3-(bis(2-chloroethyl)carbamate), 17-ester with L-alanine) Atrimustine (KM-2210; bestrabucil, busramustine) Estradiol mustard (NSC-112259; chlorphenacyl estradiol diester) Estramustine (Leo 275; Ro 21-8837) Estromustine (Leo 271 f; estrone 17β-3-N-bis(2-chloroethyl)carbamate, estrone–cytostatic complex)
Estrone esters
Marketed Esters of estrone that have been marketed include:
Estrone acetate (Hovigal) Estrone sulfate (as the primary component of conjugated estrogens (Premarin)) Estropipate (Ogen, Ortho-Est) (a salt of estrone sulfate and piperazine) Estrone tetraacetylglucoside (Glucovex, Glycovex)
Never marketed Other estrone esters which are notable but have not been marketed include:
Estrone benzoate Estrone cyanate Estrone enanthate Estrone enanthate benzilic acid hydrazone Estrone glucuronide Estrone phosphate Estrone propionate Estrone sulfamate (EMATE; J994; estrone-3-O-sulfamate) Estrone oleate
Estriol esters
Marketed Esters of estriol that have been marketed include:
Estriol 3-glucuronide (as a component of conjugated estriol (Emmenin, Progynon)) Estriol acetate benzoate (Holin-Depot) Estriol glucuronide (as a component of conjugated estriol (Emmenin, Progynon)) Estriol succinate (Sinapause, Styptanon, Synapause) Estriol sodium succinate (Pausan, Styptanon) Estriol sulfate (as a component of conjugated estriol (Emmenin, Progynon)) Estriol sulfate glucuronide (as a component of conjugated estriol (Emmenin, Progynon)) Estriol tripropionate (Estriel) Polyestriol phosphate (Gynäsan, Klimadurin, Triodurin) (an estriol ester in polymeric form)
Never marketed The following ester of estriol was never marketed:
Estriol dihexanoate Estriol dipropionate Estriol phosphate (E3P) Estriol sulfamate (E3MATE; J1034; estriol-3-O-sulfamate) Estriol triacetate
Ethinylestradiol esters
Marketed The following esters of ethinylestradiol exist and have been marketed:
Ethinylestradiol sulfonate (Turisteron; ethinylestradiol 3-isopropylsulfonate)
Never marketed Ethinylestradiol benzoate – the 3-benzoate ester of ethinylestradiol Ethinylestradiol N,N-diethylsulfamate (J271) – the 3-(N,N-diethyl)sulfamate ester of ethinylestradiol Ethinylestradiol pyrrolidinosulfonate (J272) – the 3-pyrrolidinosulfonate ester of ethinylestradiol Ethinylestradiol sulfamate (J1028) – the 3-sulfamate ester of ethinylestradiol Ethinylestradiol sulfate
Esters of other steroidal estrogens
Marketed The following esters of other estrogens exist and have been marketed:
Hydroxyestrone diacetate (Colpoginon, Colpormon, Hormobion, Hormocervix) – the 3,16α-diacetate ester of 16α-hydroxyestrone
Ethers of steroidal estrogens
Marketed A number of estrogen ethers also exist and have been marketed, including:
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