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.
Androgen receptor (AR) modulators
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Estrogen receptor (ER) modulators
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Progesterone receptor (PR) modulators
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Indirect sex-hormonal agents
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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.
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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)
- 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
- 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
- Estrapronicate
- Estrazinol
- Estriol
- Estrofurate
- Estrogenic substances
- Estromustine
- Estrone
- Etamestrol (eptamestrol)
- Ethinylandrostenediol
- Ethinylestradiol
- Ethinylestriol
- Ethylestradiol
- Etynodiol
- Etynodiol diacetate
- Hexolame
- Hippulin
- Hydroxyestrone diacetate
- Lynestrenol
- Lynestrenol phenylpropionate
- Mestranol
- Methylestradiol
- Moxestrol
- Mytatrienediol
- Nilestriol
- Norethisterone
- Noretynodrel
- Orestrate
- Pentolame
- Prodiame
- Prolame
- Promestriene
- RU-16117
- Quinestradol
- 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)
- Lavender oil
- Lignans (e.g., enterodiol, enterolactone, nyasol (cis-hinokiresinol))
- Metalloestrogens (e.g., cadmium)
- 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))
- 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
- Cingestol
- Danazol
- Desogestrel
- Dienogest
- Ethinylandrostenediol
- Ethisterone
- Ethynerone
- Etonogestrel
- Etynodiol
- Etynodiol diacetate
- 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
- Quingestanol
- Quingestanol acetate
- Tibolone
- Tigestol
- Tosagestin; Anabolic–androgenic steroids: 11β-Methyl-19-nortestosterone
- 11β-Methyl-19-nortestosterone dodecylcarbonate
- 19-Nor-5-androstenediol
- 19-Nor-5-androstenedione
- 19-Nordehydroepiandrosterone
- 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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