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Prodrug
List of estrogen esters
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    List of estrogen esters

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    Estradiol, the base estrogen of most estrogen esters.

    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:

    And the following less commonly used esters:

    The following nitrogen mustard ester of estradiol is a cytostatic antineoplastic agent and has been marketed:

    Never marketed

    A number of other estradiol esters which have not been marketed include:

    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:

    Never marketed

    Other estrone esters which are notable but have not been marketed include:

    Estriol esters

    Marketed

    Esters of estriol that have been marketed include:

    Never marketed

    The following ester of estriol was never marketed:

    Ethinylestradiol esters

    Marketed

    The following esters of ethinylestradiol exist and have been marketed:

    Never marketed

    Esters of other steroidal estrogens

    Marketed

    The following esters of other estrogens exist and have been marketed:

    Ethers of steroidal estrogens

    Marketed

    A number of estrogen ethers also exist and have been marketed, including:

    Never marketed

    A few other estrogen ethers which are notable but have not been marketed include:

    Esters of nonsteroidal estrogens

    Diethylstilbestrol esters

    Marketed

    Major esters of diethylstilbestrol include:

    • Diethylstilbestrol dipropionate (Agostilben, Biokeral, Clinestrol, Cyclen, Estilbin, Estril, Neobenzoestrol, Orestol, Oroestrol, Ostregenin, Prostilbene, Stilbestriol DP, Stilboestrolum Dipropionicum, Stilboestrol, Synestrin, Willestrol)
    • Fosfestrol (diethylstilbestrol diphosphate) (Honvan, Difostilben, Fosfostilben, Fostrolin, Stilbol, Stilphostrol, Vagestrol)

    Less commonly used esters of diethylstilbestrol include:

    Never marketed

    As well as the following nitrogen mustard ester:

    • ICI-85966 (Stilbostat; diethylstilbestrol bis(di(2-chloroethyl)carbamate))

    Hexestrol esters

    Marketed

    Never marketed

    The following nitrogen mustard ester of hexestrol was never marketed:

    • Phenestrol (fenestrol; hexestrol bis[4-[bis(2-chloroethyl)amino]phenylacetate)

    Esters of other nonsteroidal estrogens

    Marketed

    Ethers of nonsteroidal estrogens

    Diethylstilbestrol

    Marketed

    • Diethylstilbestrol monobenzyl ether (benzelstilbestrol) (Monozol, Hypantin, Pituitrope)
    • Dimestrol (dianisylhexene, diethylstilbestrol dimethyl ether, dimethoxydiethylstilbestrol) (Depot-Ostromon, Synthila)
    • Mestilbol (diethylstilbestrol monomethyl ether) (Monomestro or Monomestrol)

    See also



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