From Wikipedia, the free encyclopedia
A sex-hormonal agent, also known as a sex-hormone receptor modulator, is a type of
hormonal agent which specifically modulates the effects of
sex hormones and of their
biological targets, the
sex hormone receptors. The sex hormones include
androgens such as
testosterone,
estrogens such as
estradiol, and
progestogens such as
progesterone.
[1] Sex-hormonal agents may be either
steroidal or
nonsteroidal in
chemical structure and may serve to either
enhance,
inhibit, or have
mixed effects on the function of the sex hormone systems.
[2]
Sex-hormonal agents are used in
medicine for a variety of purposes including
hormone therapy (e.g.,
menopausal hormone therapy,
androgen replacement therapy,
transgender hormone therapy),
antihormone therapy (e.g.,
androgen deprivation therapy,
estrogen deprivation therapy), and
hormonal contraception, among others.
Types and examples
Androgen receptor (AR) modulators
Estrogen receptor (ER) modulators
Progesterone receptor (PR) modulators
Indirect sex-hormonal agents
Drugs that indirectly influence sex hormone systems, such as
antigonadotropins like
GnRH analogues and
prolactin releasers (e.g.,
D2 receptor antagonists),
progonadotropins like
GnRH agonists, and
steroidogenesis inhibitors like
aromatase inhibitors and
androgen synthesis inhibitors, are also sex-hormonal agents.
See also
References
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Androgens (incl.
AASTooltip anabolic–androgenic steroid) | |
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Antiandrogens |
ARTooltip Androgen receptor
antagonists | |
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Steroidogenesis inhibitors | |
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Antigonadotropins |
-
D2 receptor
antagonists (
prolactin releasers) (e.g.,
domperidone,
metoclopramide,
risperidone,
haloperidol,
chlorpromazine,
sulpiride)
-
Estrogens (e.g.,
bifluranol,
diethylstilbestrol,
estradiol,
estradiol esters,
ethinylestradiol,
ethinylestradiol sulfonate,
paroxypropione)
-
GnRH agonists (e.g.,
leuprorelin)
-
GnRH antagonists (e.g.,
cetrorelix)
-
Progestogens (incl.,
chlormadinone acetate,
cyproterone acetate,
hydroxyprogesterone caproate,
gestonorone caproate,
medroxyprogesterone acetate,
megestrol acetate)
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Others | |
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Estrogens |
ERTooltip Estrogen receptor agonists |
- Steroidal:
Alfatradiol
- Certain
androgens/
anabolic steroids (e.g.,
testosterone,
testosterone esters,
methyltestosterone,
metandienone,
nandrolone esters) (via estrogenic metabolites)
- Certain
progestins (e.g.,
norethisterone,
noretynodrel,
etynodiol diacetate,
tibolone)
-
Clomestrone
-
Cloxestradiol acetate
-
Conjugated estriol
-
Conjugated estrogens
-
Epiestriol
-
Epimestrol
-
Esterified estrogens
-
Estetrol†
-
Estradiol
-
Estradiol esters (e.g.,
estradiol acetate,
estradiol benzoate,
estradiol cypionate,
estradiol enanthate,
estradiol undecylate,
estradiol valerate,
polyestradiol phosphate,
estradiol ester mixtures (
Climacteron))
-
Estramustine phosphate
-
Estriol
-
Estriol esters (e.g.,
estriol succinate,
polyestriol phosphate)
-
Estrogenic substances
-
Estrone
-
Estrone esters
-
Ethinylestradiol#
-
Hydroxyestrone diacetate
-
Mestranol
-
Methylestradiol
-
Moxestrol
-
Nilestriol
-
Prasterone (dehydroepiandrosterone; DHEA)
-
Promestriene
-
Quinestradol
-
Quinestrol
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Progonadotropins | |
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Antiestrogens |
ERTooltip Estrogen receptor antagonists (incl.
SERMsTooltip selective estrogen receptor modulators/
SERDsTooltip selective estrogen receptor downregulators) | |
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Aromatase inhibitors | |
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Antigonadotropins |
-
Androgens/
anabolic steroids (e.g.,
testosterone,
testosterone esters,
nandrolone esters,
oxandrolone,
fluoxymesterone)
-
D2 receptor
antagonists (
prolactin releasers) (e.g.,
domperidone,
metoclopramide,
risperidone,
haloperidol,
chlorpromazine,
sulpiride)
-
GnRH agonists (e.g.,
leuprorelin,
goserelin)
-
GnRH antagonists (e.g.,
cetrorelix,
elagolix)
-
Progestogens (e.g.,
chlormadinone acetate,
cyproterone acetate,
gestonorone caproate,
hydroxyprogesterone caproate,
medroxyprogesterone acetate,
megestrol acetate)
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Others | |
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ARTooltip Androgen receptor | Agonists | |
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SARMsTooltip Selective androgen receptor modulator | |
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Antagonists | |
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GPRC6A | |
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ERTooltip Estrogen receptor | Agonists |
- Steroidal:
2-Hydroxyestradiol
-
2-Hydroxyestrone
-
3-Methyl-19-methyleneandrosta-3,5-dien-17β-ol
-
3α-Androstanediol
-
3α,5α-Dihydrolevonorgestrel
-
3β,5α-Dihydrolevonorgestrel
-
3α-Hydroxytibolone
-
3β-Hydroxytibolone
-
3β-Androstanediol
-
4-Androstenediol
-
4-Androstenedione
-
4-Fluoroestradiol
-
4-Hydroxyestradiol
-
4-Hydroxyestrone
-
4-Methoxyestradiol
-
4-Methoxyestrone
-
5-Androstenediol
-
7-Oxo-DHEA
-
7α-Hydroxy-DHEA
-
7α-Methylestradiol
-
7β-Hydroxyepiandrosterone
-
8,9-Dehydroestradiol
-
8,9-Dehydroestrone
-
8β-VE2
-
10β,17β-Dihydroxyestra-1,4-dien-3-one (DHED)
-
11β-Chloromethylestradiol
-
11β-Methoxyestradiol
-
15α-Hydroxyestradiol
-
16-Ketoestradiol
-
16-Ketoestrone
-
16α-Fluoroestradiol
-
16α-Hydroxy-DHEA
-
16α-Hydroxyestrone
-
16α-Iodoestradiol
-
16α-LE2
-
16β-Hydroxyestrone
-
16β,17α-Epiestriol (16β-hydroxy-17α-estradiol)
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17α-Estradiol (
alfatradiol)
-
17α-Dihydroequilenin
-
17α-Dihydroequilin
-
17α-Epiestriol (16α-hydroxy-17α-estradiol)
-
17α-Ethynyl-3α-androstanediol
-
17α-Ethynyl-3β-androstanediol
-
17β-Dihydroequilenin
-
17β-Dihydroequilin
-
17β-Methyl-17α-dihydroequilenin
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Abiraterone
-
Abiraterone acetate
-
Alestramustine
-
Almestrone
-
Anabolic steroids (e.g.,
testosterone and
esters,
methyltestosterone,
metandienone (methandrostenolone),
nandrolone and
esters, many others; via estrogenic metabolites)
-
Atrimustine
-
Bolandiol
-
Bolandiol dipropionate
-
Butolame
-
Clomestrone
-
Cloxestradiol
-
Conjugated estriol
-
Conjugated estrogens
-
Cyclodiol
-
Cyclotriol
-
DHEA
-
DHEA-S
-
ent-Estradiol
-
Epiestriol (16β-epiestriol, 16β-hydroxy-17β-estradiol)
-
Epimestrol
-
Equilenin
-
Equilin
-
ERA-63 (ORG-37663)
-
Esterified estrogens
-
Estetrol
-
Estradiol
-
Estramustine
-
Estramustine phosphate
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Estrapronicate
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Estrazinol
-
Estriol
-
Estrofurate
-
Estrogenic substances
-
Estromustine
-
Estrone
-
Etamestrol (eptamestrol)
-
Ethinylandrostenediol
-
Ethinylestradiol
-
Ethinylestriol
-
Ethylestradiol
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Etynodiol
-
Etynodiol diacetate
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Hexolame
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Hippulin
-
Hydroxyestrone diacetate
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Lynestrenol
-
Lynestrenol phenylpropionate
-
Mestranol
-
Methylestradiol
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Moxestrol
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Mytatrienediol
-
Nilestriol
-
Norethisterone
-
Noretynodrel
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Orestrate
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Pentolame
-
Prodiame
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Prolame
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Promestriene
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RU-16117
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Quinestradol
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Quinestrol
-
Tibolone
- Xenoestrogens:
Anise-related (e.g.,
anethole,
anol,
dianethole,
dianol,
photoanethole)
-
Chalconoids (e.g.,
isoliquiritigenin,
phloretin,
phlorizin (phloridzin),
wedelolactone)
-
Coumestans (e.g.,
coumestrol,
psoralidin)
-
Flavonoids (incl.
7,8-DHF,
8-prenylnaringenin,
apigenin,
baicalein,
baicalin,
biochanin A,
calycosin,
catechin,
daidzein,
daidzin,
ECG,
EGCG,
epicatechin,
equol,
formononetin,
glabrene,
glabridin,
genistein,
genistin,
glycitein,
kaempferol,
liquiritigenin,
mirificin,
myricetin,
naringenin,
penduletin,
pinocembrin,
prunetin,
puerarin,
quercetin,
tectoridin,
tectorigenin)
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Lavender oil
-
Lignans (e.g.,
enterodiol,
enterolactone,
nyasol (cis-hinokiresinol))
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Metalloestrogens (e.g.,
cadmium)
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Pesticides (e.g.,
alternariol,
dieldrin,
endosulfan,
fenarimol,
HPTE,
methiocarb,
methoxychlor,
triclocarban,
triclosan)
-
Phytosteroids (e.g.,
digitoxin (
digitalis),
diosgenin,
guggulsterone)
-
Phytosterols (e.g.,
β-sitosterol,
campesterol,
stigmasterol)
-
Resorcylic acid lactones (e.g.,
zearalanone,
α-zearalenol,
β-zearalenol,
zearalenone,
zeranol (α-zearalanol),
taleranol (teranol, β-zearalanol))
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Steroid-like (e.g.,
deoxymiroestrol,
miroestrol)
-
Stilbenoids (e.g.,
resveratrol,
rhaponticin)
-
Synthetic xenoestrogens (e.g.,
alkylphenols,
bisphenols (e.g.,
BPA,
BPF,
BPS),
DDT,
parabens,
PBBs,
PHBA,
phthalates,
PCBs)
- Others (e.g.,
agnuside,
rotundifuran)
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Mixed (
SERMsTooltip Selective estrogen receptor modulators) | |
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Antagonists |
- Coregulator-binding modulators:
ERX-11
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GPERTooltip G protein-coupled estrogen receptor | Agonists | |
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Antagonists | |
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Unknown | |
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PRTooltip Progesterone receptor | Agonists |
- Testosterone derivatives: Progestins:
6,6-Difluoronorethisterone
-
6,6-Difluoronorethisterone acetate
-
17α-Allyl-19-nortestosterone
-
Allylestrenol
-
Altrenogest
-
Chloroethynylnorgestrel
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Cingestol
-
Danazol
-
Desogestrel
-
Dienogest
-
Ethinylandrostenediol
-
Ethisterone
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Ethynerone
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Etonogestrel
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Etynodiol
-
Etynodiol diacetate
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Gestodene
-
Gestrinone
-
Levonorgestrel
-
Levonorgestrel esters (e.g.,
levonorgestrel butanoate)
-
Lynestrenol
-
Lynestrenol phenylpropionate
-
Metynodiol
-
Metynodiol diacetate
-
Norelgestromin
-
Norethisterone (norethindrone)
-
Norethisterone esters (e.g.,
norethisterone acetate,
norethisterone enanthate)
-
Noretynodrel
-
Norgesterone
-
Norgestimate
-
Norgestrel
-
Norgestrienone
-
Norvinisterone
-
Oxendolone
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Quingestanol
-
Quingestanol acetate
-
Tibolone
-
Tigestol
-
Tosagestin; Anabolic–androgenic steroids:
11β-Methyl-19-nortestosterone
-
11β-Methyl-19-nortestosterone dodecylcarbonate
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19-Nor-5-androstenediol
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19-Nor-5-androstenedione
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19-Nordehydroepiandrosterone
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Bolandiol
-
Bolandiol dipropionate
-
Bolandione
-
Dimethisterone
-
Dienedione
-
Dienolone
-
Dimethandrolone
-
Dimethandrolone buciclate
-
Dimethandrolone dodecylcarbonate
-
Dimethandrolone undecanoate
-
Dimethyldienolone
-
Dimethyltrienolone
-
Ethyldienolone
-
Ethylestrenol (ethylnandrol)
-
Methyldienolone
-
Metribolone (R-1881)
-
Methoxydienone (methoxygonadiene)
-
Mibolerone
-
Nandrolone
-
Nandrolone esters (e.g.,
nandrolone decanoate,
nandrolone phenylpropionate)
-
Norethandrolone
-
Normethandrone (methylestrenolone, normethandrolone, normethisterone)
-
RU-2309
-
Tetrahydrogestrinone
-
Trenbolone (trienolone)
-
Trenbolone esters (e.g.,
trenbolone acetate,
trenbolone enanthate)
-
Trendione
-
Trestolone
-
Trestolone acetate
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Mixed (
SPRMsTooltip Selective progesterone receptor modulators) | |
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Antagonists | |
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mPRTooltip Membrane progesterone receptor (
PAQRTooltip Progestin and adipoQ receptor) | |
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