Antiestrogen

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An antiestrogen is a substance that blocks the production or utilization of estrogens,^[1] or inhibits their effects.^[2] (Estrogens are the family of hormones that promote the development and maintenance of female sex characteristics.)

Antiestrogens like tamoxifen can promote an invasive phenotype in estrogen receptor (ER)-positive breast cancer cells with deficient intercellular adhesion.

Although aromatase inhibitors could be considered antiestrogens by some definitions, they are often considered to be a distinct class.^[3] Aromatase inhibitors reduce the production of estrogen, while the term "antiestrogen" is usually reserved for agents reducing the response to estrogen.

References

^ "Definition of antiestrogen - NCI Dictionary of Cancer Terms, Definition of antiestrogen - NCI Dictionary of Cancer Terms". http://www.cancer.gov/dictionary/?CdrID=44813. ,
^ "antiestrogen" at Dorland's Medical Dictionary
^ Riggins RB, Bouton AH, Liu MC, Clarke R (2005). "Antiestrogens, aromatase inhibitors, and apoptosis in breast cancer". Vitam. Horm. 71: 201–37. doi:10.1016/S0083-6729(05)71007-4. PMID 16112269. http://linkinghub.elsevier.com/retrieve/pii/S0083-6729(05)71007-4.

External links

This article incorporates public domain material from the U.S. National Cancer Institute document "Dictionary of Cancer Terms".

Estrogens and progestogens (G03C-D, L02)

Progestogens/
progestins
(progesterone)

Agonist

1st	Norpregnene Norethisterone^#/Norethisterone acetate Ethynodiol diacetate

2nd	Norpregnene Levonorgestrel^#/Norgestrel/Norelgestromin

3rd	19-nortestosterone Desogestrel/Etonogestrel Gestodene Norgestimate

4th	Androstene Drospirenone 19-norprogesterone Nomegestrol Promegestone Trimegestone 19-nortestosterone Dienogest

17-OH	Chlormadinone Cyproterone Medroxyprogesterone/Medroxyprogesterone 17-acetate^# Megestrol

Other/ ungrouped	Pregnenedione Gestonorone Pregnene Ethisterone Pregnadiene Medrogestone Melengestrol Norpregnane Norgestrienone Lynestrenol Norethynodrel Tibolone Dydrogesterone Quingestanol

Antiprogestin/
SPRM

antagonists
- Aglepristone
- Mifepristone

Estrogens

Agonist

Steroidal	Diosgenin Estetrol Estradiol Estradiol benzoate Estradiol cypionate^# Estradiol dipropionate Estradiol enanthate Estradiol undecylate Estradiol valerate Polyestradiol phosphate Estrone Estrone sulfate Estriol Ethinylestradiol^# Mestranol Promestriene Equilenin Equilin

Nonsteroidal	Chlorotrianisene Dienestrol Fosfestrol Diethylstilbestrol Zeranol

Antiestrogen/
SERM

pure antagonist: Fulvestrant

Aromatase inhibitors

nonselective: Aminoglutethimide; Testolactone

selective: Anastrozole; Atamestane; Exemestane; Fadrozole; Formestane; Letrozole; Minamestane; Plomestane; Vorozole

^#WHO-EM
^‡Withdrawn from market
Clinical trials:
- ^†Phase III
- ^§Never to phase III

M: ♀ FRS

anat/phys/devp

noco/cong/npls, sysi/epon

proc/asst, drug (G1/G2B/G3CD)

Estrogenics

Receptor

ER (α, β)	Agonists: 16α-Hydroxyestrone Alestramustine Almestrone Benzestrol Bifluranol Broparestrol Carbestrol Chlorotrianisene Cloxestradiol Dienestrol Diethylstilbestrol Diethylstilbestrol diphosphate Diosgenin Doisynoestrol DPN Epiestriol Epimestrol Eptamestrol/Etamestrol ERB-041 Equilenin Equilin Estetrol Estradiol Estradiol benzoate Estradiol butyrylacetate Estradiol cypionate Estradiol dienanthate Estradiol dipropionate Estradiol diundecylate Estradiol diundecylenate Estradiol enanthate Estradiol fluroate Estradiol hemisuccinate Estradiol hexahydrobenzoate Estradiol monopropionate Estradiol palmitate Estradiol pivalate Estradiol propoxyphenylpropionate Estradiol stearate Estradiol succinate Estradiol undecylate Estradiol valerate Estramustine Estramustine phosphate Estrapronicate Estrazinol Estriol Estriol succinate Estriol tripropionate Estrofurate Estromustine Estrone Estrone acetate Estrone cyanate Estrone sulfate Estrone tetraacetylglucoside Estropipate Etamestrol Ethinylestradiol Ethinylestradiol 3-isopropylsulfonate FERb 033 Fenestrel Fosfestrol Furostilbestrol Hexestrol Hexestrol diacetate Hexestrol dicaprylate Hexestrol diphosphate Hexestrol dipropionate Hydroxyestrone diacetate Mestranol Methallenestril Methestrol Methestrol dipropionate Moxestrol Nilestriol Orestrate Polyestradiol phosphate PPT Promestriene Promethoestrol Quinestradol Quinestrol β-Sitosterol WAY-200,070 Note: Though not listed here, many anabolic steroids can also be estrogenic as they can be aromatized into estrogen-like metabolites that possess estrogenic activity. Mixed (SERMs): 2-Hydroxyestrone Acolbifene Afimoxifene Arzoxifene Bazedoxifene Clomifene Clomifenoxide Cyclofenil Droloxifene Enclomifene Endoxifen Epimestrol Femarelle Fispemifene GW5638 Idoxifene Lasofoxifene Levormeloxifene Menerba Mepitiostane Miproxifene Nafoxidine Nitromifene Ormeloxifene Ospemifene Panomifene Pipendoxifene Prinaberel Raloxifene SS1010 Sivifene Tamoxifen TAS-108 Tesmilifene Tibolone Toremifene Trioxifene Y-134 Zindoxifene Zuclomifene Antagonists: Acefluranol Clometerone Delmadinone Dimepregnen Epitiostanol Fulvestrant Gestrinone ICI-164,384 Mepitiostane MPP PHTPP RU-58,668 SS1020 ZK-164,015 ZK-191,703 Note: Xenoestrogens (e.g., phytoestrogens and mycoestrogens) are not included here. For a full list of xenoestrogens, see here.

GPER	Agonists: Estradiol Fulvestrant G-1 Genistein Quercetin Tamoxifen Antagonists: G-15

Enzyme
(inhibitors)

20,22-Desmolase	22-ABC 3,3′-Dimethoxybenzidine 3-Methoxybenzidine Aminoglutethimide Cyanoketone Danazol Etomidate Mitotane Trilostane

17α-Hydroxylase, 17,20-Lyase	22-ABC 22-Oxime Abiraterone Bifonazole Clotrimazole Cyanoketone Cyproterone Danazol Desogestrel Econazole Galeterone Gestrinone Isoconazole Ketoconazole L-39 Levonorgestrel Liarozole LY-207,320 MDL-27,302 Miconazole Mifepristone Norethisterone Orteronel Pioglitazone Rosiglitazone Spironolactone Stanozolol SU-10,603 Tioconazole TGF-β Troglitazone VN/87-1 YM116

3β-HSD	4-MA Azastene Cyanoketone Danazol Desogestrel Epostane Genistein Gestrinone Levonorgestrel Medroxyprogesterone Medroxyprogesterone acetate Metyrapone Norethisterone Oxymetholone Pioglitazone Rosiglitazone Trilostane Troglitazone

17β-HSD	Danazol Simvastatin

Aromatase	1,4,6-Androstatriene-3,17-dione 4-Androstene-3,6,17-trione 4-Cyclohexylaniline 4-Hydroxytestosterone 5α-DHNET Abyssinone II Aminoglutethimide Anastrozole Ascorbic acid (Vitamin C) Atamestane Bifonazole CGP-45,688 CGS-47,645 Clotrimazole DHT Difeconazole Econazole Exemestane Fadrozole Fenarimol Finrozole Formestane Imazalil Isoconazole Ketoconazole Letrozole Liarozole MEN-11066 Miconazole Minamestane Nimorazole NKS01 Norethindrone ORG-33,201 Penconazole Plomestane Prochloraz Propioconazole Pyridoglutethimide Rogletimide Rotenone Talarozole Testolactone Tioconazole Triadimefon Triadimenol Troglitazone Vorozole YM511 Zinc Note: 5α-reductase and 21-hydroxylase inhibitors may also affect estrogen levels as they prevent metabolism of estrogen steroid precursors.

Other

Precursors	Cholesterol 22R-Hydroxycholesterol 20α,22R-Dihydroxycholesterol Pregnenolone 17-Hydroxypregnenolone Progesterone 17-Hydroxyprogesterone Cortodoxone DHEA DHEA sulfate Androstenediol Androstenedione Testosterone

Indirect	Androgens/Antiandrogens (see here) Calcitriol (a form of Vitamin D) GnRH agonists/antagonists (see here) Gonadotropins (see here) Plasma proteins (SHBG, ABP, Albumin) Progestogens/Antiprogestins (see here) Prolactin

Procedures	Adrenalectomy Hypophysectomy Oophorectomy Orchiectomy

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