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Trioxifene (LY-133,314) was a selective estrogen receptor modulator (SERM) with competitive binding activity against estradiol for estrogen receptor-alpha (ERα) and antagonistic activity against ERα-mediated gene expression, that was under preclinical and clinical development by Eli Lilly and Company for breast cancer and prostate cancer,[1] but was abandoned.[2]:11
References
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Receptor
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Agonists
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- (R)-DPN
- (S)-DPN
- (R,R)-THC
- (S,S)-THC
- 2,8-DHHHC
- 3α-Androstanediol
- 3β-Androstanediol
- 3α-Hydroxytibolone
- 3β-Hydroxytibolone
- 7-Oxo-DHEA
- 7α-Hydroxy-DHEA
- 7β-Hydroxyepiandrosterone
- 8β-VE2
- 16α-Hydroxy-DHEA
- 16α-Hydroxyestrone
- 16α-IE2
- 16α-LE2 (Cpd1471)
- Δ4-Androstenedione
- Δ5-Androstenediol
- 17α-Estradiol (alfatradiol)
- 17β-Estradiol (estradiol)
- Alestramustine
- Almestrone
- Anabolic steroids (prodrugs; e.g., testosterone, metandienone (methandrostenolone), others)
- Anethole
- Anol
- Atrimustine
- Benzestrol
- Bifluranol
- Bisdehydrodoisynolic acid
- Cadmium
- Carbestrol
- Chalconoids (e.g., isoliquiritigenin, phloretin, phlorizin (phloridzin), wedelolactone)
- Cloxestradiol
- Conjugated equine estrogens (e.g., sodium equilin sulfate, sodium equilenin sulfate)
- Coumestans (e.g., coumestrol, psoralidin)
- DHEA
- DHEA-S
- Deoxymiroestrol
- Dianethole
- Dianol
- Diarylpropionitrile
- Dieldrin
- Dienestrol
- Dienestrol acetate
- Diethylstilbestrol
- Diethylstilbestrol dipropionate
- Diosgenin
- Doisynoestrol (fenocycline)
- Doisynolic acid
- DY-131 (GSK-9089)
- Endosulfan
- Epiestriol
- Epimestrol
- ERB-196 (WAY-202196)
- Esterified estrogens (e.g., estrone sulfate, equilin sulfate, equilenin sulfate)
- Estetrol
- Estradiol benzoate
- Estradiol butyrylacetate
- Estradiol cypionate
- Estradiol dienanthate
- Estradiol dipropionate
- Estradiol diundecylate
- Estradiol diundecylenate
- Estradiol enanthate
- Estradiol furoate
- Estradiol hemihydrate
- 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
- Estrobin (DBE)
- Estrofurate
- Estromustine
- Estrone
- Estrone acetate
- Estrone cyanate
- Estrone sulfate
- Estrone tetraacetylglucoside
- Estropipate
- Estropronicate
- Etamestrol (eptamestrol)
- Ethinyl estradiol
- Ethinyl estradiol 3-isopropylsulfonate
- Etynodiol diacetate
- Fenarimol
- Fenestrel
- FERb 033
- Flavonoids (incl. 7,8-DHF, 8-prenylnaringenin, apigenin, baicalein, baicalin, calycosin, catechin, daidzein, daidzin, ECG, EGCG, epicatechin, equol, formononetin, glabrene, glabridin, genistein, genistin, glycitein, kaempferol, liquiritigenin, mirificin, myricetin, naringenin, pinocembrin, prunetin, puerarin, quercetin, tectoridin, tectorigenin)
- Fosfestrol
- Furostilbestrol
- GSK-4716
- Hexestrol
- Hexestrol diacetate
- Hexestrol dicaprylate
- Hexestrol diphosphate
- Hexestrol dipropionate
- Hydroxyestrone diacetate
- Lavender oil
- Lignans (e.g., enterodiol, enterolactone)
- Mestranol
- Metalloestrogens (e.g., cadmium)
- Methallenestril
- Methestrol
- Methestrol dipropionate
- Methiocarb
- Methylestradiol
- Miroestrol
- Moxestrol
- Nilestriol
- Noretynodrel
- Orestrate
- Paroxypropione
- Phytosterols (e.g., β-sitosterol, campesterol, stigmasterol)
- Polyestradiol phosphate
- Prinaberel (ERB-041, WAY-202041)
- Propylpyrazoletriol
- Promestriene
- Resorcylic acid lactones (e.g., zearalanone, zearalenol, zearalenone, zeranal (zearalanol))
- Quadrosilan
- Quinestradol
- Quinestrol
- SKF-82,958
- Stilbenoids (e.g., resveratrol)
- Synthetic xenoestrogens (e.g., alkylphenols, bisphenols (e.g., BPA, BPF, BPS), DDT, parabens, PBBs, PHBA, phthalates, PCBs)
- WAY-166818
- WAY-200070
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Antagonists
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| Enzyme |
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| Others |
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Precursors
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Indirect
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- Antigonadotropins (e.g., androgens, estrogens, progestogens, prolactin)
- Calcitriol (vitamin D)
- GnRH agonists (e,g, GnRH, leuprorelin)
- GnRH antagonists (e.g., cetrorelix)
- Gonadotropins (e.g., FSH, hCG, LH)
- Kisspeptin
- Plasma proteins (ABP, albumin, SHBG)
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- ↑ Lua error in package.lua at line 80: module 'strict' not found.
- ↑ Philipp Y. Maximov, Russell E. McDaniel, V. Craig Jordan. Tamoxifen: Pioneering Medicine in Breast Cancer. Milestones in Drug Therapy. Springer Science & Business Media, 2013. ISBN 9783034806640
