List of 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.

Estradiol, the base estrogen of most estrogen esters.

Esters of steroidal estrogens

Marketed

Many esters of estradiol have been marketed, including the following major esters:[1][2]

And the following less commonly used esters:[1][2]

The following nitrogen mustard ester of estradiol is a cytostatic antineoplastic agent and has been marketed:[1][2]

Never marketed

A few other estradiol esters which are notable but have not been marketed include:[2]

The following cytostatic antineoplastic nitrogen mustard esters of estradiol have not been marketed:[2]

  • 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)

Marketed

Esters of estrone that have been marketed include:[1][2]

Never marketed

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

Marketed

Esters of estriol that have been marketed include:[1][2]

Never marketed

The following ester of estriol was never marketed:

Marketed

The following esters of ethinylestradiol exist and have been marketed:[1][2]

Never marketed

Marketed

The following esters of other estrogens exist and have been marketed:[1]

Ethers of steroidal estrogens

Marketed

A number of estrogen ethers also exist and have been marketed, including:[22][1]

  • Clomestrone (Arterolo, Atheran, Colesterel, Iposclerone, Liprotene, Persclerol) – the 3-methyl ether of 16α-chloroestrone
  • Cloxestradiol acetate (Genovul) – the O,O-diacetate ester of cloxestradiol (estradiol 17β-chloral hemiacetal ether)
  • Mestranol (Devocin, Ovastol, Tranel) (component of Enovid, Enavid, Ortho-Novin, Femigen, Norbiogest) – the 3-methyl ether of ethinylestradiol
  • Moxestrol (Surestryl) – the 11β-methoxy derivative of ethinylestradiol (and hence the 11β-methyl ether of the 11β-hydroxyl derivative of ethinylestradiol)
  • Nilestriol (Wei Ni An) – the 3-cyclopentyl ether of ethinylestriol
  • Promestriene (Colpotrofin, Colpotrophine, Delipoderm) – the 3-propyl and 17β-methyl diether of estradiol
  • Quinestradol (Colpovis, Colpovister, Pentovis) – the 3-cyclopentyl ether of estriol
  • Quinestrol (Agalacto-Quilea, Basaquines, Eston, Estrovis, Estrovister, Plestrovis, Qui-lea) – the 3-cyclopentyl ether of ethinylestradiol

Never marketed

A few other estrogen ethers which are notable but have not been marketed include:[22]

Esters of nonsteroidal estrogens

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))

Marketed

Never marketed

The following nitrogen mustard ester of hexestrol was never marketed:

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

Marketed

Ethers of nonsteroidal estrogens

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

References
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