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Polyestriol phosphate is a synthetic, steroidal estrogen and an estrogen ester – specifically, the 3-(dihydrogen phosphate) ester of polyestriol – which is used in medicine. It is a long-acting and water-soluble form of polyestriol.
As a phosphate ester of polyestriol, polyestriol phosphate is a prodrug of polyestriol that is stored in the body and is slowly hydrolyzed into polyestriol, which is the active form. The medication has a very long duration of action when given by intramuscular injection, and a single dose has a duration of about one month.
Polyestriol phosphate is used in the treatment of menopausal symptoms and osteoporosis in women. It has also been used to treat prostate cancer in men.
Side effects of polyestriol phosphate are similar to those of other estrogens and include breast tenderness, breast enlargement, nausea, headache, and fluid retention.
Following an intramuscular injection of polyestriol phosphate, the medication is slowly absorbed into the bloodstream and is then slowly hydrolyzed into polyestriol, which is the active form.
Polyestriol phosphate was first described in the literature in 1957 and was introduced for medical use by 1960.
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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
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- 16α-Hydroxy-DHEA
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- 16α-Iodoestradiol
- 16α-LE2
- 16β-Hydroxyestrone
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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
- 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
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- Cyclotriol
- DHEA
- DHEA-S
- ent-Estradiol
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- 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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- Coregulator-binding modulators: ERX-11
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Natural estrogens | |
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Estrogens |
ER
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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Antiestrogens |
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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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