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ESTRADIOL Drug Record

  • Summary
  • Interactions
  • Claims
  • ESTRADIOL chembl:CHEMBL135 Approved

    Alternate Names:

    EVOREL 100
    CLIMARA
    ESTRADERM MX 100
    DERMESTRIL 25
    ESTROGEL
    GYNERGON
    E-CYPIONATE
    ELLESTE SOLO MX 80
    ADGYN ESTRO
    DEPO-ESTRADIOL
    VAGIFEM 18
    ELESTRIM
    AGOFOLLIN
    ESTRADERM MX 50
    VAGIFEM
    FEMSEVEN 50
    ESTRING
    DIHYDROTHEELIN
    ELLESTE SOLO MX 40
    VAGIFEM 8
    INNOFEM
    EVOREL 50
    GVNODIOL
    IMVEXXY
    DERMESTRIL SEPTEM 25
    ELESTRIN
    MENOREST 75
    VIVELLE-DOT
    MINIVELLE
    GYNOESTRYL
    FEMATRIX 80
    VIVELLE
    ESTRADERM TTS 100
    EVOREL 25
    GYNOGEN
    ESTRADERM TTS 25
    ESTRADIOL
    WC3011
    DERMESTRIL SEPTEM 50
    ESTRADERM MX 25
    ESTRADERM MX 75
    ESTRASORB
    DESTRADIOL
    ZUMENON
    FEMATRIX 40
    ESTRADERM TTS 50
    MENOREST 37.5
    MENORING 50
    AQUAGEN
    FEMPATCH
    ALFATRADIOL
    GYNODIOL
    CLIMARA PRO
    EVAMIST
    ESTRADIOL HEMIHYDRATE
    EVOREL 75
    DERMESTRIL 50
    ELLESTE SOLO
    ALORA
    ESTRADERM
    NSC-20293
    WC-3011
    BEDOL
    FEMSEVEN 75
    MENOREST 50
    DERMESTRIL SEPTEM 75
    DIHYDROXYESTRIN
    MENOSTAR
    OESTRADIOL
    ESCLIM
    DERMESTRIL 100
    DIVIGEL
    FEMSEVEN 100
    NSC-9895
    ESTRACE
    PROGYNOVA TS
    SANDRENA
    COMPUDOSE
    ESTRADERM TTS
    B-ESTRADIOL
    SYNDIOL
    17B-ESTRADIOL
    DIHYDROFOLLICULAR HORMONE
    DELTA-OESTRADIOL
    ESTRADIOL-17-BETA
    PRIMOFOL
    (17BETA)-ESTRA-1,3,5(10)-TRIENE-3,17-DIOL
    ESTROGEN
    (1S,10R,11S,14S,15S)-15-METHYLTETRACYCLO[8.7.0.0^{2,7}.0^{11,15}]HEPTADECA-2,4,6-TRIENE-5,14-DIOL
    DIOGYN
    ESTROCLIM
    CLIMADERM
    MACRODIOL
    OESCLIM
    17BETA-OESTRADIOL
    OVAHORMON
    FEMESTRAL
    OVOCYCLIN
    17BETA-ESTRA-1,3,5(10)-TRIENE-3,17-DIOL
    FEMOGEN
    EVOREL
    OESTROGEL
    CIS-ESTRADIOL
    AERODIOL
    DIHYDROFOLLICULIN
    OVASTEVOL
    ESTRADOT
    DIOGYNETS
    17Β-ESTRA-1,3,5(10)-TRIENE-3,17-DIOL
    ESTROVITE
    AQUADIOL
    3,17B-DIHYDROXYESTRA-1,3,5(10)-TRIENE
    ESTRA-1,3,5(10)-TRIENE-3,17B-DIOL
    PROGYNON DH
    DIMENFORMON
    ESTRADIOLUM
    GINOSEDOL
    EPIESTRIOL 50
    (8R,9S,13S,14S,17S)-13-METHYL-6,7,8,9,11,12,14,15,16,17-DECAHYDROCYCLOPENTA[A]PHENANTHRENE-3,17-DIOL
    OVASTEROL
    SANDRENA 1
    3,17B-ESTRADIOL
    BARDIOL
    LAMDIOL
    (+)-3,17B-ESTRADIOL
    PROFOLIOL
    PERLATANOL
    ESTRALDINE
    DIHYDRO-THEELIN
    NORDICOL
    OESTERGON
    3,17-EPIDIHYDROXYESTRATRIENE
    OVOCYLIN
    D-ESTRADIOL
    DERMESTRIL
    GELESTRA
    OESTROGEN
    ESTRING VAGINAL RING
    OESTRODIOL
    DELTA-ESTRADIOL
    ESTRADIOL-17BETA
    D-OESTRADIOL
    ALTRAD
    OESTRA-1,3,5(10)-TRIENE-3,17B-DIOL
    BETA-ESTRADIOL
    OESTROGLANDOL
    17BETA-ESTRADIOL
    E2
    DIHYDROMENFORMON
    17Β-OESTRADIOL
    CORPAGEN
    17BETA OESTRADIOL
    ESTROGEL HBF
    13B-METHYL-1,3,5(10)-GONATRIENE-3,17B-OL
    (17Β)-ESTRA-1,3,5(10)-TRIENE-3,17-DIOL
    AMNESTROGEN
    17B-OESTRADIOL
    PROGYNON
    FOLLICYCLIN
    ESTROCLIM 50
    PROFOLIOL B
    ENCORE
    SYSTEN
    MENOREST
    chemidplus:50-28-2
    pubchem.compound:5757
    drugbank:00783
    chembl:CHEMBL135

    Drug Info:

    Drug Class hormone replacement agents
    Year of Approval approved before 1982
    Drug Class Small molecule
    Drug Indications for treatment of menopausal symptoms
    Drug Indications contraceptive
    Drug Indications hormone replacement
    FDA Approval approved
    Drug Class Small Molecule
    Drug Indications hormone replacement,treatment for menopause
    (4 More Sources)

    Publications:

    Sasson, 1991, Equilibrium binding analysis of estrogen agonists and antagonists: relation to the activation of the estrogen receptor., Pathol. Biol.
    Lehnes et al., 2007, The effect of estradiol on in vivo tumorigenesis is modulated by the human epidermal growth factor receptor 2/phosphatidylinositol 3-kinase/Akt1 pathway., Endocrinology
    Brama et al., 2007, Cadmium induces mitogenic signaling in breast cancer cell by an ERalpha-dependent mechanism., Mol. Cell. Endocrinol.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Jain D et al., 2010, A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements., Bioorg Med Chem Lett
    Maximov PY et al., 2010, Structure-function relationships of estrogenic triphenylethylenes related to endoxifen and 4-hydroxytamoxifen., J Med Chem
    Chang FR et al., 2005, The transgenic Arabidopsis plant system, pER8-GFP, as a powerful tool in searching for natural product estrogen-agonists/antagonists., J Nat Prod
    Bologa et al., 2006, Virtual and biomolecular screening converge on a selective agonist for GPR30., Nat. Chem. Biol.
    Renner S et al., 2009, Bioactivity-guided mapping and navigation of chemical space., Nat Chem Biol
    Lai A et al., 2015, Identification of GDC-0810 (ARN-810), an Orally Bioavailable Selective Estrogen Receptor Degrader (SERD) that Demonstrates Robust Activity in Tamoxifen-Resistant Breast Cancer Xenografts., J Med Chem
    Maximov PY et al., 2014, Influence of the length and positioning of the antiestrogenic side chain of endoxifen and 4-hydroxytamoxifen on gene activation and growth of estrogen receptor positive cancer cells., J Med Chem
    Banerjee M et al., 2013, Modulation of xenobiotic receptors by steroids., Molecules
    Paterni I et al., 2014, Estrogen receptors alpha (ERα) and beta (ERβ): subtype-selective ligands and clinical potential., Steroids
    Jiang XR et al., 2013, Synthesis of novel estrogen receptor antagonists using metal-catalyzed coupling reactions and characterization of their biological activity., J Med Chem
    Hixon et al., 1987, Effects of a luteolytic dose of oestradiol benzoate on uterine oxytocin receptor concentrations, phosphoinositide turnover and prostaglandin F-2 alpha secretion in sheep., J. Reprod. Fertil.
    Daehlin, 1985, On the effects of oestrogen in the male. Some effects of different oestrogenic substances in rats and men with prostatic carcinoma., Scand J Urol Nephrol Suppl
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Vijayanathan et al., 2007, Effects of estradiol and 4-hydroxytamoxifen on the conformation, thermal stability, and DNA recognition of estrogen receptor beta., Biochem. Cell Biol.
    Jiang Y et al., 2013, Mechanisms enforcing the estrogen receptor β selectivity of botanical estrogens., FASEB J
    Richette et al., 2007, Oestrogens inhibit interleukin 1beta-mediated nitric oxide synthase expression in articular chondrocytes through nuclear factor-kappa B impairment., Ann. Rheum. Dis.
    Reinhart et al., 1999, Xeno-oestrogens and phyto-oestrogens induce the synthesis of leukaemia inhibitory factor by human and bovine oviduct cells., Mol. Hum. Reprod.
    Schreiber et al., 1980, Dopaminergic modulation of the adenohypophyseal reaction to oestradiol: interaction of perphenazine with the thyroid hormones., Physiol Bohemoslov
    Thomas P et al., 2006, Binding and activation of the seven-transmembrane estrogen receptor GPR30 by environmental estrogens: a potential novel mechanism of endocrine disruption., J Steroid Biochem Mol Biol
    Prossnitz ER et al., 2007, GPR30: A G protein-coupled receptor for estrogen., Mol Cell Endocrinol
    Levenson et al., 1998, Oestradiol regulation of the components of the plasminogen-plasmin system in MDA-MB-231 human breast cancer cells stably expressing the oestrogen receptor., Br. J. Cancer
    Harlow et al., 2007, Oestrogen formation and connective tissue growth factor expression in rat granulosa cells., J. Endocrinol.
    Kurokawa et al., 2008, Acute effects of oestrogen on the guinea pig and human IKr channels and drug-induced prolongation of cardiac repolarization., J. Physiol. (Lond.)
    Gupta et al., 2003, Effects of cortisol and oestradiol on hepatic 11beta-hydroxysteroid dehydrogenase type 1 and glucocorticoid receptor proteins in late-gestation sheep fetus., J. Endocrinol.
    Ordóñez et al., 2007, Insulin sensitivity in streptozotocin-induced diabetic rats treated with different doses of 17beta-oestradiol or progesterone., Exp. Physiol.
    Robertson et al., 1998, Tamoxifen up-regulates oestrogen receptor-alpha, c-fos and glyceraldehyde 3-phosphate-dehydrogenase mRNAs in ovine endometrium., J. Steroid Biochem. Mol. Biol.
    Jönsson et al., 2007, Demonstration of mitochondrial oestrogen receptor beta and oestrogen-induced attenuation of cytochrome c oxidase subunit I expression in human periodontal ligament cells., Arch. Oral Biol.
    Wahab et al., 1999, The distribution of endometrial leukocytes and their proliferation markers in trimegestone-treated postmenopausal women compared to the endometrium of the natural cycle: a dose-ranging study., Hum. Reprod.
  • ESTRADIOL   GPER1

    Interaction Score: 8.24

    Interaction Types & Directionality:
    binder

    Interaction Info:

    PMIDs:
    16520733 17088055 17222505


    Sources:
    DTC

  • ESTRADIOL   MT-CO1

    Interaction Score: 2.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17223066


    Sources:
    NCI

  • ESTRADIOL   PZP

    Interaction Score: 1.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    3868029


    Sources:
    NCI

  • ESTRADIOL   ESRRA

    Interaction Score: 1.03

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    23448346


    Sources:
    DTC

  • ESTRADIOL   LIF

    Interaction Score: 0.37

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10508216


    Sources:
    NCI

  • ESTRADIOL   PTPRC

    Interaction Score: 0.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10325261


    Sources:
    NCI

  • ESTRADIOL   PROS1

    Interaction Score: 0.34

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Combination therapy Estradiol,Progesterone

    PMIDs:
    None found


    Sources:
    FDA

  • ESTRADIOL   ESR2

    Interaction Score: 0.34

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Trial Name Bio-E-Gel, estradiol,Elestrin
    Novel drug target Established target
    Trial Name drospirenone plus estradiol,Angeliq

    PMIDs:
    16520733 19561619 20659801 17464340 2011412 23882126 24971815


    Sources:
    DTC TdgClinicalTrial TEND

  • ESTRADIOL   OXTR

    Interaction Score: 0.32

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    3033233


    Sources:
    NCI

  • ESTRADIOL   CP

    Interaction Score: 0.29

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    6446099


    Sources:
    NCI

  • ESTRADIOL   GAPDH

    Interaction Score: 0.27

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9883985


    Sources:
    NCI

  • ESTRADIOL   PROC

    Interaction Score: 0.26

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Combination therapy Estradiol,Progesterone

    PMIDs:
    None found


    Sources:
    FDA

  • ESTRADIOL   CCN2

    Interaction Score: 0.22

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17210741


    Sources:
    NCI

  • ESTRADIOL   NOS2

    Interaction Score: 0.2

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17068060


    Sources:
    NCI

  • ESTRADIOL   ESR1

    Interaction Score: 0.19

    Interaction Types & Directionality:
    agonist (activating)

    Interaction Info:
    Direct Interaction yes
    Mechanism of Interaction Estrogen receptor alpha agonist
    Trial Name transdermal estradiol,Divigel

    PMIDs:
    2011412 17138652 17125913 11752352 20659801 20334368 16038533 16520733 19561619 25879485 24805199 23884115 24971815


    Sources:
    DTC TdgClinicalTrial ChemblInteractions TEND TTD

  • ESTRADIOL   PLAU

    Interaction Score: 0.16

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    9662256


    Sources:
    NCI

  • ESTRADIOL   SLC2A4

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    17068109


    Sources:
    NCI

  • ESTRADIOL   SERPINC1

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Combination therapy Estradiol,Progesterone

    PMIDs:
    None found


    Sources:
    FDA

  • ESTRADIOL   NR3C1

    Interaction Score: 0.05

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    12553866


    Sources:
    DTC NCI

  • ESTRADIOL   RORC

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ESTRADIOL   PPARG

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ESTRADIOL   KCNH2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    18440994


    Sources:
    NCI

  • ESTRADIOL   RECQL

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ESTRADIOL   CYP2C9

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ESTRADIOL   CYP2C19

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ESTRADIOL   CYP1A2

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ESTRADIOL   CYP2D6

    Interaction Score: 0.01

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ESTRADIOL   CYP3A4

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    22931300


    Sources:
    DTC

  • ESTRADIOL   AR

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • ESTRADIOL   EHMT2

    Interaction Score: 0.0

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    DTC

  • TEND: ESTRADIOL

    • Version: 01-August-2011

    Alternate Names:
    ESTRADIOL Primary Drug Name

    Drug Info:
    Year of Approval approved before 1982
    Drug Class hormone replacement agents

    Publications:

  • TdgClinicalTrial: ESTRADIOL

    • Version: January-2014

    Alternate Names:

    Drug Info:
    Drug Indications hormone replacement,treatment for menopause
    Drug Class Small Molecule
    FDA Approval approved

    Publications:

  • NCI: OESTRADIOL

    • Version: 14-September-2017

    Alternate Names:
    C478 NCI drug code

    Drug Info:

    Publications:
    Hixon et al., 1987, Effects of a luteolytic dose of oestradiol benzoate on uterine oxytocin receptor concentrations, phosphoinositide turnover and prostaglandin F-2 alpha secretion in sheep., J. Reprod. Fertil.
    Reinhart et al., 1999, Xeno-oestrogens and phyto-oestrogens induce the synthesis of leukaemia inhibitory factor by human and bovine oviduct cells., Mol. Hum. Reprod.
    Schreiber et al., 1980, Dopaminergic modulation of the adenohypophyseal reaction to oestradiol: interaction of perphenazine with the thyroid hormones., Physiol Bohemoslov

  • DTC: ESTRADIOL

    • Version: 02-September-2020

    Alternate Names:
    CHEMBL135 ChEMBL Drug ID

    Drug Info:

    Publications:
    Sakatis MZ et al., 2012, Preclinical strategy to reduce clinical hepatotoxicity using in vitro bioactivation data for >200 compounds., Chem Res Toxicol
    Jain D et al., 2010, A mutant selective anti-estrogen is a pure antagonist on EREs and AP-1 response elements., Bioorg Med Chem Lett
    Bologa et al., 2006, Virtual and biomolecular screening converge on a selective agonist for GPR30., Nat. Chem. Biol.

  • TTD: Estradiol

    • Version: 2020.06.01

    Alternate Names:
    D08QMX TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL135

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL135

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • FDA: Estradiol

    • Version: 04-September-2020

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21