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Identification
NameEstradiol
Accession NumberDB00783  (APRD00311)
TypeSmall Molecule
GroupsApproved, Investigational, Vet Approved
DescriptionGenerally refers to the 17-beta-isomer of estradiol, an aromatized C18 steroid with hydroxyl group at 3-beta- and 17-beta-position. Estradiol-17-beta is the most potent form of mammalian estrogenic steroids. In humans, it is produced primarily by the cyclic ovaries and the placenta. It is also produced by the adipose tissue of men and postmenopausal women. The 17-alpha-isomer of estradiol binds weakly to estrogen receptors (receptors, estrogen) and exhibits little estrogenic activity in estrogen-responsive tissues. Various isomers can be synthesized. [PubChem]
Structure
Thumb
Synonyms
(17beta)-Estra-1,3,5(10)-triene-3,17-diol
17beta Oestradiol
17beta-Estra-1,3,5(10)-triene-3,17-diol
17beta-Oestradiol
Benzhormovarine
beta-Estradiol
cis-Estradiol
Dihydrofollicular hormone
Dihydrofolliculin
Dihydrotheelin
Dihydroxyestrin
Estradiol
Estradiol
Estradiol
Estradiol-17beta
Estradiolum
Femestral
Lio-Oid
External Identifiers
  • E3A
  • NSC 17590
  • SQ 16150
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Alorapatch.05 mg/dtransdermalActavis Pharma, Inc.1996-12-20Not applicableUs
Alorapatch.075 mg/dtransdermalActavis Pharma, Inc.1996-12-20Not applicableUs
Alorapatch.1 mg/dtransdermalActavis Pharma, Inc.1996-12-20Not applicableUs
Alorapatch.025 mg/dtransdermalActavis Pharma, Inc.2002-04-05Not applicableUs
Climarapatch.025 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.1999-03-05Not applicableUs
Climarapatch.05 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.1994-12-22Not applicableUs
Climarapatch.1 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.1994-12-22Not applicableUs
Climarapatch.0375 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.2003-05-27Not applicableUs
Climarapatch.075 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.1998-03-23Not applicableUs
Climarapatch.06 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.2008-01-03Not applicableUs
Climara 100patch7.6 mgtransdermalBayer Inc1997-12-01Not applicableCanada
Climara 25patch2 mgtransdermalBayer Inc2004-03-12Not applicableCanada
Climara 50patch3.8 mgtransdermalBayer Inc1997-12-01Not applicableCanada
Climara 75patch5.7 mgtransdermalBayer Inc2004-03-12Not applicableCanada
Delestrogeninjection10 mg/mLintramuscularPar Pharmaceutical Inc.2007-11-01Not applicableUs
Delestrogeninjection20 mg/mLintramuscularPar Pharmaceutical Inc.2007-11-01Not applicableUs
Delestrogeninjection40 mg/mLintramuscularPar Pharmaceutical Inc.2007-11-01Not applicableUs
Delestrogen Inj 10mg/mlliquid10 mgintramuscularTheramed Corporation1955-12-312008-03-03Canada
Divigelgel.25 mg/gtopicalVertical Pharmaceuticals, LLC2014-10-27Not applicableUs
Divigelgel0.1 %transdermalTeva Canada Limited2015-04-13Not applicableCanada
Divigelgel.25 mg/gtopicalUpsher Smith Laboratories, Inc.2011-02-28Not applicableUs
Divigelgel0.1 %transdermalTeva Canada Limited2012-09-272015-04-23Canada
Divigelgel.5 mg/gtopicalVertical Pharmaceuticals, LLC2014-10-27Not applicableUs
Divigelgel.5 mg/gtopicalUpsher Smith Laboratories, Inc.2011-02-28Not applicableUs
Divigelgel0.1 %transdermalTeva Canada Limited2015-04-13Not applicableCanada
Divigelgel1 mg/gtopicalVertical Pharmaceuticals, LLC2014-10-27Not applicableUs
Divigelgel1 mg/gtopicalPhysicians Total Care, Inc.2009-08-04Not applicableUs
Divigelgel1 mg/gtopicalUpsher Smith Laboratories, Inc.2011-02-28Not applicableUs
Divigelgel0.1 %transdermalTeva Canada Limited2015-04-13Not applicableCanada
Elestringel, metered.52 mg/gtopicalMEDA Pharmaceuticals2014-06-02Not applicableUs
Elestringel, metered.52 mg/gtopicalMEDA Pharmaceuticals2014-06-02Not applicableUs
Elestringel.6 mg/gtransdermalJazz Pharmaceuticals Commercial Corp.2007-06-01Not applicableUs
Elestringel.6 mg/gtransdermalJazz Pharmaceuticals Commercial Corp.2007-06-01Not applicableUs
Estracetablet0.5 mgoralAcerus Pharmaceuticals Corporation1997-07-10Not applicableCanada
Estracetablet2 mgoralAcerus Pharmaceuticals Corporation1995-12-31Not applicableCanada
Estracetablet1 mgoralAcerus Pharmaceuticals Corporation1995-12-31Not applicableCanada
Estrace Tab 1mgtablet1 mgoralBristol Labs Division Of Bristol Myers Squibb1976-12-311999-01-07Canada
Estrace Tab 2mgtablet2 mgoralBristol Labs Division Of Bristol Myers Squibb1976-12-311998-04-07Canada
Estraderm-100patch (extended release)8 mgtransdermalNovartis Pharmaceuticals Canada Inc1987-12-312013-01-08Canada
Estraderm-25patch (extended release)2 mgtransdermalNovartis Pharmaceuticals Canada Inc1987-12-312012-10-25Canada
Estraderm-50patch (extended release)4 mgtransdermalNovartis Pharmaceuticals Canada Inc1987-12-312010-05-10Canada
Estradiolpatch, extended release.0375 mg/dtransdermalSandoz Inc2014-12-22Not applicableUs
Estradioltablet2 mgoralAcerus Pharmaceuticals CorporationNot applicableNot applicableCanada
Estradiolpatch, extended release.05 mg/dtransdermalSandoz Inc2014-12-22Not applicableUs
Estradioltablet0.5 mgoralAcerus Pharmaceuticals CorporationNot applicableNot applicableCanada
Estradiolpatch, extended release.075 mg/dtransdermalSandoz Inc2014-12-22Not applicableUs
Estradioltablet1 mgoralAcerus Pharmaceuticals CorporationNot applicableNot applicableCanada
Estradiolpatch, extended release.1 mg/dtransdermalSandoz Inc2014-12-22Not applicableUs
Estradiolpatch, extended release.025 mg/dtransdermalSandoz Inc2014-12-22Not applicableUs
Estradiol Transdermal Systempatch.05 mg/dtransdermalAlvogen, Inc.2011-12-20Not applicableUs
Estradiol Transdermal Systempatch.06 mg/dtransdermalAlvogen, Inc.2011-12-20Not applicableUs
Estradiol Transdermal Systempatch.075 mg/dtransdermalAlvogen, Inc.2011-12-20Not applicableUs
Estradiol Transdermal Systempatch.025 mg/dtransdermalAlvogen, Inc.2011-12-20Not applicableUs
Estradiol Transdermal Systempatch.1 mg/dtransdermalAlvogen, Inc.2011-12-19Not applicableUs
Estradiol Transdermal Systempatch.0375 mg/dtransdermalAlvogen, Inc.2011-12-20Not applicableUs
Estradiol Valerateinjection20 mg/mLintramuscularJHP Pharmaceuticals, LLC2012-06-01Not applicableUs
Estradiol Valerateinjection40 mg/mLintramuscularJHP Pharmaceuticals, LLC2012-06-01Not applicableUs
Estradiol Valerateinjection10 mg/mLintramuscularJHP Pharmaceuticals, LLC2012-06-01Not applicableUs
Estradot 100patch1.56 mgtransdermalNovartis Pharmaceuticals Canada Inc2001-09-05Not applicableCanada
Estradot 25patch0.39 mgtransdermalNovartis Pharmaceuticals Canada Inc2002-10-03Not applicableCanada
Estradot 37.5patch0.585 mgtransdermalNovartis Pharmaceuticals Canada Inc2001-09-05Not applicableCanada
Estradot 50patch0.780 mgtransdermalNovartis Pharmaceuticals Canada Inc2001-09-05Not applicableCanada
Estradot 75patch1.17 mgtransdermalNovartis Pharmaceuticals Canada Inc2001-09-05Not applicableCanada
Estringring2 mg/1vaginalPhysicians Total Care, Inc.2006-02-27Not applicableUs
Estringring (slow-release)2 mgvaginalPfizer Canada Inc1995-12-31Not applicableCanada
Estringring2 mg/1vaginalPharmacia And Upjohn Company Llc1996-04-26Not applicableUs
Estringring2 mg/1vaginalU.S. Pharmaceuticals1996-04-26Not applicableUs
Estrogelgel0.06 %transdermalMerck Canada Inc1998-11-16Not applicableCanada
Estrogelgel, metered.75 mg/1.25gtransdermalASCEND Therapeutics US, LLC2004-02-09Not applicableUs
Estrogelgel, metered.75 mg/1.25gtransdermalASCEND Therapeutics US, LLC2004-02-09Not applicableUs
Evamistspray, metered1.53 mg/1transdermalPhysicians Total Care, Inc.2010-08-23Not applicableUs
Evamistspray1.53 mg/1transdermalPaddock Laboratories, LLC2015-04-11Not applicableUs
Evamistspray, metered1.53 mg/1transdermalTher Rx Corporation2009-07-08Not applicableUs
Femringring.05 mg/dvaginalWarner Chilcott (US), LLC2003-07-01Not applicableUs
Femringring.1 mg/dvaginalWarner Chilcott (US), LLC2003-07-01Not applicableUs
Femringring.1 mg/24[USP'U]vaginalPhysicians Total Care, Inc.2009-05-04Not applicableUs
Lupin-estradioltablet2 mgoralLupin Pharma Canada Limited2016-02-29Not applicableCanada
Lupin-estradioltablet0.5 mgoralLupin Pharma Canada Limited2016-02-29Not applicableCanada
Lupin-estradioltablet1 mgoralLupin Pharma Canada Limited2016-02-29Not applicableCanada
Menostarpatch14 ug/dtransdermalBayer Health Care Pharmaceuticals Inc.2004-06-08Not applicableUs
Minivellefilm, extended release.025 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not applicableUs
Minivellefilm, extended release.0375 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not applicableUs
Minivellefilm, extended release.05 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not applicableUs
Minivellefilm, extended release.075 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not applicableUs
Minivellefilm, extended release.1 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not applicableUs
Neo-diol Inj 20mg/mlliquid20 mgintramuscularNeolab Inc1982-12-312003-07-29Canada
Oesclimpatch15 mgtransdermalSearchlight Pharma Inc2015-05-29Not applicableCanada
Oesclimpatch5 mgtransdermalSearchlight Pharma Inc2002-03-22Not applicableCanada
Oesclimpatch20 mgtransdermalSearchlight Pharma Inc2015-05-29Not applicableCanada
Oesclimpatch5 mgtransdermalFournier Pharma Inc1998-09-292002-07-12Canada
Oesclimpatch7.5 mgtransdermalSearchlight Pharma Inc2015-05-29Not applicableCanada
Oesclimpatch10 mgtransdermalFournier Pharma Inc1998-09-292002-07-12Canada
Oesclimpatch10 mgtransdermalSearchlight Pharma Inc2002-03-21Not applicableCanada
PMS-estradiol Valerate Inj 10mg/mlliquid10 mgintramuscularPharmascience Inc1989-12-31Not applicableCanada
Sandoz Estradiol Derm 100patch8 mgtransdermalSandoz Canada Incorporated2003-04-24Not applicableCanada
Sandoz Estradiol Derm 50patch4 mgtransdermalSandoz Canada Incorporated2003-04-24Not applicableCanada
Sandoz Estradiol Derm 75patch6 mgtransdermalSandoz Canada Incorporated2003-04-24Not applicableCanada
Vagifemtablet, film coated10 ug/1vaginalNovo Nordisk2010-01-11Not applicableUs
Vagifemtablet, film coated10 ug/1vaginalPhysicians Total Care, Inc.2010-09-24Not applicableUs
Vagifemvaginal tablet25 mcgvaginalNovo Nordisk Canada Inc2002-05-082014-07-28Canada
Vagifem 10vaginal tablet10 mcgvaginalNovo Nordisk Canada Inc2010-04-28Not applicableCanada
Vivelle 100mcgpatch8.66 mgtransdermalNovartis Pharmaceuticals Canada Inc1996-12-312003-12-03Canada
Vivelle 37.5mcgpatch3.28 mgtransdermalNovartis Pharmaceuticals Canada Inc1996-12-312003-12-03Canada
Vivelle 50mcgpatch4.33 mgtransdermalNovartis Pharmaceuticals Canada Inc1996-12-312008-11-21Canada
Vivelle 75mcgpatch6.56 mgtransdermalNovartis Pharmaceuticals Canada Inc1996-12-312003-12-03Canada
Vivelle Dotpatch, extended release.05 mg/dtransdermalPhysicians Total Care, Inc.2003-06-10Not applicableUs
Vivelle Dotpatch, extended release.075 mg/dtransdermalPhysicians Total Care, Inc.2003-06-10Not applicableUs
Vivelle Dotpatch, extended release.1 mg/dtransdermalPhysicians Total Care, Inc.2003-06-10Not applicableUs
Vivelle Dotpatch, extended release.0375 mg/dtransdermalPhysicians Total Care, Inc.2003-09-23Not applicableUs
Vivelle-dotpatch, extended release.075 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not applicableUs
Vivelle-dotpatch, extended release.1 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not applicableUs
Vivelle-dotpatch, extended release.0375 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not applicableUs
Vivelle-dotpatch, extended release.025 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not applicableUs
Vivelle-dotpatch, extended release.05 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not applicableUs
Approved Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Depo-estradiolinjection5 mg/mLintramuscularPharmacia and Upjohn Company1979-08-15Not applicableUs
Depo-estradiolinjection5 mg/mLintramuscularPhysicians Total Care, Inc.1998-10-16Not applicableUs
Estracecream.1 mg/gvaginalWarner Chilcott (US), LLC2001-07-01Not applicableUs
Estracetablet.5 mg/1oralWarner Chilcott (US), LLC2011-12-26Not applicableUs
Estracetablet1 mg/1oralWarner Chilcott (US), LLC2011-12-26Not applicableUs
Estracetablet2 mg/1oralWarner Chilcott (US), LLC2011-12-26Not applicableUs
Estradiolpatch.97 mg/48[USP'U]transdermalPhysicians Total Care, Inc.2003-06-14Not applicableUs
Estradioltablet.5 mg/1oralbryant ranch prepack1996-03-14Not applicableUs
Estradioltablet2 mg/1oralMylan Pharmaceuticals Inc.1999-06-17Not applicableUs
Estradioltablet.5 mg/1oralHeritage Pharmaceuticals Inc2010-11-05Not applicableUs
Estradioltablet.5 mg/1oralAv Pak2014-02-12Not applicableUs
Estradioltablet2 mg/1oralGolden State Medical Supply, Inc.2014-11-26Not applicableUs
Estradiolpatch.075 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not applicableUs
Estradioltablet.5 mg/1oralWatson Laboratories, Inc.1996-03-14Not applicableUs
Estradioltablet.5 mg/1oralPd Rx Pharmaceuticals, Inc.1996-03-14Not applicableUs
Estradioltablet.5 mg/1oralPd Rx Pharmaceuticals, Inc.2009-12-17Not applicableUs
Estradioltablet1 mg/1oralPreferred Pharmaceuticals, Inc.2014-12-04Not applicableUs
Estradiolpatch.1 mg/dtransdermalMylan Pharmaceuticals Inc.2000-02-24Not applicableUs
Estradioltablet2 mg/1oralAidarex Pharmaceuticals LLC1997-10-28Not applicableUs
Estradioltablet1 mg/1oralPhysicians Total Care, Inc.2000-09-18Not applicableUs
Estradioltablet.5 mg/1oralbryant ranch prepack1996-03-14Not applicableUs
Estradioltablet.5 mg/1oralKAISER FOUNDATION HOSPITALS2015-10-14Not applicableUs
Estradioltablet1 mg/1oralSTAT Rx USA LLC1996-03-14Not applicableUs
Estradiolpatch1.46 mg/48[USP'U]transdermalPhysicians Total Care, Inc.2003-06-09Not applicableUs
Estradioltablet1 mg/1oralReady Meds1996-03-14Not applicableUs
Estradioltablet1 mg/1oralBarr Laboratories Inc.1997-10-28Not applicableUs
Estradiolpatch.025 mg/dtransdermalMylan Pharmaceuticals Inc.2005-03-28Not applicableUs
Estradioltablet1 mg/1oralHeritage Pharmaceuticals Inc2010-11-05Not applicableUs
Estradioltablet1 mg/1oralAv Pak2014-02-12Not applicableUs
Estradioltablet.5 mg/1oralDIRECT RX2015-11-25Not applicableUs
Estradiolpatch.05 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not applicableUs
Estradioltablet.5 mg/1oralKAISER FOUNDATION HOSPITALS2010-10-07Not applicableUs
Estradioltablet1 mg/1oralBlenheim Pharmacal, Inc.2012-02-14Not applicableUs
Estradioltablet1 mg/1oralPd Rx Pharmaceuticals, Inc.2009-12-17Not applicableUs
Estradioltablet1 mg/1oralPreferred Pharmaceuticals, Inc.2012-02-13Not applicableUs
Estradiolpatch.0375 mg/dtransdermalMylan Pharmaceuticals Inc.2006-08-10Not applicableUs
Estradioltablet2 mg/1oralPd Rx Pharmaceuticals, Inc.1996-03-14Not applicableUs
Estradioltablet2 mg/1oralPhysicians Total Care, Inc.2003-05-07Not applicableUs
Estradioltablet1 mg/1oralbryant ranch prepack1996-03-14Not applicableUs
Estradioltablet.5 mg/1oralMylan Pharmaceuticals Inc.1999-06-17Not applicableUs
Estradioltablet1 mg/1oralRebel Distributors Corp1996-03-14Not applicableUs
Estradiolpatch1.94 mg/48[USP'U]transdermalPhysicians Total Care, Inc.2008-12-11Not applicableUs
Estradioltablet2 mg/1oralReady Meds1996-03-14Not applicableUs
Estradioltablet2 mg/1oralBarr Laboratories Inc.1997-10-28Not applicableUs
Estradiolpatch.05 mg/dtransdermalMylan Pharmaceuticals Inc.2000-02-24Not applicableUs
Estradioltablet2 mg/1oralHeritage Pharmaceuticals Inc2010-11-05Not applicableUs
Estradioltablet2 mg/1oralAv Pak2014-02-12Not applicableUs
Estradioltablet1 mg/1oralDIRECT RX2015-01-01Not applicableUs
Estradiolpatch.0375 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not applicableUs
Estradioltablet1 mg/1oralKAISER FOUNDATION HOSPITALS2010-10-20Not applicableUs
Estradioltablet2 mg/1oralBlenheim Pharmacal, Inc.2012-03-05Not applicableUs
Estradioltablet1 mg/1oralWatson Laboratories, Inc.1996-03-14Not applicableUs
Estradiolpatch.06 mg/dtransdermalMylan Pharmaceuticals Inc.2006-08-10Not applicableUs
Estradioltablet1 mg/1oralPd Rx Pharmaceuticals, Inc.1996-03-14Not applicableUs
Estradioltablet.5 mg/1oralGolden State Medical Supply, Inc.2014-11-26Not applicableUs
Estradioltablet1 mg/1oralAvera Mc Kennan Hospital2015-06-23Not applicableUs
Estradioltablet2 mg/1oralbryant ranch prepack1996-03-14Not applicableUs
Estradioltablet1 mg/1oralMylan Pharmaceuticals Inc.1999-06-17Not applicableUs
Estradioltablet2 mg/1oralRebel Distributors Corp1996-03-14Not applicableUs
Estradioltablet.5 mg/1oralPhysicians Total Care, Inc.2003-06-09Not applicableUs
Estradioltablet1 mg/1oralCardinal Health2009-12-17Not applicableUs
Estradioltablet10 ug/1vaginalAmneal Pharmaceuticals of New York, LLC2015-06-07Not applicableUs
Estradioltablet.5 mg/1oralBarr Laboratories Inc.1997-10-28Not applicableUs
Estradiolpatch.075 mg/dtransdermalMylan Pharmaceuticals Inc.2005-03-28Not applicableUs
Estradioltablet1 mg/1oralAidarex Pharmaceuticals LLC1997-10-28Not applicableUs
Estradioltablet1 mg/1oralProficient Rx LP1996-03-14Not applicableUs
Estradiolpatch.025 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not applicableUs
Estradioltablet1 mg/1oralKAISER FOUNDATION HOSPITALS2012-09-12Not applicableUs
Estradioltablet.5 mg/1oralStat Rx USA1997-10-22Not applicableUs
Estradioltablet1 mg/1oralGolden State Medical Supply, Inc.2014-11-26Not applicableUs
Estradioltablet1 mg/1oralAvera Mc Kennan Hospital2015-07-14Not applicableUs
Estradioltablet2 mg/1oralWatson Laboratories, Inc.1996-03-14Not applicableUs
Estradiolpatch.1 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not applicableUs
Estradioltablet1 mg/1oralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-12Not applicableUs
Estradiol Valerateinjection, solution20 mg/mLintramuscularPerrigo Company2010-03-31Not applicableUs
Estradiol Valerateinjection, solution40 mg/mLintramuscularPerrigo Company2010-03-31Not applicableUs
Approved Over the Counter ProductsNot Available
Unapproved/Other Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Estradiolpellet25 mg/1oralQualgen Llc2015-09-01Not applicableUs
Estradiolpellet6 mg/1oralQualgen Llc2015-09-01Not applicableUs
Estradiolpellet18 mg/1oralQualgen Llc2015-09-01Not applicableUs
Estradiolpellet10 mg/1oralQualgen Llc2015-09-01Not applicableUs
Estradiolpellet20 mg/1oralQualgen Llc2015-09-01Not applicableUs
Estradiolpellet12.5 mg/1oralQualgen Llc2015-09-01Not applicableUs
Estradiolpellet22 mg/1oralQualgen Llc2015-09-01Not applicableUs
Estradiolpellet15 mg/1oralQualgen Llc2015-09-01Not applicableUs
International Brands
NameCompany
Estraderm MXNovartis
Estraderm TTSNovartis
EstrasorbMedicis
EstrofemNovo Nordisk
FemtraceWarner Chilcott
InnofemNovo Nordisk
VivelleNovartis
Brand mixtures
NameLabellerIngredients
ActivellaNovo Nordisk
ActivelleNovo Nordisk Canada Inc
Activelle LdNovo Nordisk Canada Inc
AngeliqBayer Health Care Pharmaceuticals Inc.
Climara ProBayer Health Care Pharmaceuticals Inc.
CombipatchNovartis Pharmaceuticals Corporation
Combipatch (estradiol/norethindrone Acetate Transdermal System)NOVEN THERAPEUTICS, LLC
Estalis 140/50 McgNovartis Pharmaceuticals Canada Inc
Estalis 250/50 McgNovartis Pharmaceuticals Canada Inc
Estalis SequiNovartis Pharmaceuticals Canada Inc
EstracombNovartis Pharmaceuticals Canada Inc
Estradiol / Norethindrone AcetateBreckenridge Pharmaceutical, Inc.
Estrogel PropakMerck Canada Inc
LopreezaAmneal Pharmaceuticals of New York, LLC
MimveyTeva Pharmaceuticals USA Inc
Mimvey LoTeva Pharmaceuticals USA Inc
NataziaBayer Inc
Neo Pause InjectionNeolab Inc
PrefestaSearchlight Pharma Inc
Salts
Name/CASStructureProperties
Estradiol acetate
Thumb
  • InChI Key: FHXBMXJMKMWVRG-SLHNCBLASA-N
  • Monoisotopic Mass: 314.188194698
  • Average Mass: 314.4186
DBSALT000065
Estradiol benzoate
Thumb
  • InChI Key: UYIFTLBWAOGQBI-BZDYCCQFSA-N
  • Monoisotopic Mass: 376.203844762
  • Average Mass: 376.488
DBSALT000066
Estradiol cypionate
Thumb
  • InChI Key: UOACKFBJUYNSLK-XRKIENNPSA-N
  • Monoisotopic Mass: 396.266445018
  • Average Mass: 396.5622
DBSALT000067
Estradiol hemihydrate
ThumbNot applicableDBSALT001383
Estradiol valerate
Thumb
  • InChI Key: RSEPBGGWRJCQGY-RBRWEJTLSA-N
  • Monoisotopic Mass: 356.23514489
  • Average Mass: 356.4984
DBSALT000068
Categories
UNII4TI98Z838E
CAS number50-28-2
WeightAverage: 272.382
Monoisotopic: 272.177630012
Chemical FormulaC18H24O2
InChI KeyInChIKey=VOXZDWNPVJITMN-ZBRFXRBCSA-N
InChI
InChI=1S/C18H24O2/c1-18-9-8-14-13-5-3-12(19)10-11(13)2-4-15(14)16(18)6-7-17(18)20/h3,5,10,14-17,19-20H,2,4,6-9H2,1H3/t14-,15-,16+,17+,18+/m1/s1
IUPAC Name
(1S,10R,11S,14S,15S)-15-methyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-2(7),3,5-triene-5,14-diol
SMILES
[H][C@@]12CC[[email protected]](O)[C@@]1(C)CC[C@]1([H])C3=C(CC[C@@]21[H])C=C(O)C=C3
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as estrogens and derivatives. These are steroids with a structure containing a 3-hydroxylated estrane.
KingdomOrganic compounds
Super ClassLipids and lipid-like molecules
ClassSteroids and steroid derivatives
Sub ClassEstrane steroids
Direct ParentEstrogens and derivatives
Alternative Parents
Substituents
  • Estrogen-skeleton
  • 17-hydroxysteroid
  • Hydroxysteroid
  • 3-hydroxysteroid
  • Phenanthrene
  • Tetralin
  • Benzenoid
  • Cyclic alcohol
  • Secondary alcohol
  • Hydrocarbon derivative
  • Organooxygen compound
  • Alcohol
  • Aromatic homopolycyclic compound
Molecular FrameworkAromatic homopolycyclic compounds
External Descriptors
Pharmacology
IndicationFor the treatment of urogenital symptoms associated with post-menopausal atrophy of the vagina (such as dryness, burning, pruritus and dyspareunia) and/or the lower urinary tract (urinary urgency and dysuria).
PharmacodynamicsEstradiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level.
Mechanism of actionEstradiol enters target cells freely (e.g., female organs, breasts, hypothalamus, pituitary) and interacts with a target cell receptor. When the estrogen receptor has bound its ligand it can enter the nucleus of the target cell, and regulate gene transcription which leads to formation of messenger RNA. The mRNA interacts with ribosomes to produce specific proteins that express the effect of estradiol upon the target cell. Estrogens increase the hepatic synthesis of sex hormone binding globulin (SHBG), thyroid-binding globulin (TBG), and other serum proteins and suppress follicle-stimulating hormone (FSH) from the anterior pituitary.
Related Articles
Absorption43%
Volume of distributionNot Available
Protein binding>95%
Metabolism

Exogenous estrogens are metabolized using the same mechanism as endogenous estrogens. Estrogens are partially metabolized by cytochrome P450.

SubstrateEnzymesProduct
Estradiol
2-hydroxyestradiolDetails
Estradiol
4-hydroxystradiolDetails
Estradiol
Not Available
Estradiol-17beta 3-sulfateDetails
Estradiol
Not Available
2-Methoxyestrone 3-glucuronideDetails
Estradiol
Not Available
17-beta-Estradiol-3-glucuronideDetails
Estradiol
Not Available
2-Methoxy-estradiol-17b 3-glucuronideDetails
Estradiol
Not Available
17-beta-Estradiol glucuronideDetails
Estradiol
Not Available
3,17-Androstanediol glucuronideDetails
Estradiol
Not Available
17-alpha-Estradiol-3-glucuronideDetails
Estradiol
Not Available
Estradiol-17alpha 3-D-glucuronosideDetails
Estradiol
Not Available
17-beta-estradiol 3-sulfate-17-(beta-D-glucuronide)Details
Estradiol
Not Available
17-Beta-Estradiol-3,17-beta-sulfateDetails
Route of eliminationEstradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates.
Half life36 hours
ClearanceNot Available
ToxicityCan cause nausea and vomiting, and withdrawal bleeding may occur in females.
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategorySMPDB ID
Aromatase deficiencyDiseaseSMP00565
17-Beta Hydroxysteroid Dehydrogenase III DeficiencyDiseaseSMP00356
Androgen and Estrogen MetabolismMetabolicSMP00068
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8917
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.7058
P-glycoprotein inhibitor INon-inhibitor0.9147
P-glycoprotein inhibitor IINon-inhibitor0.9403
Renal organic cation transporterNon-inhibitor0.8008
CYP450 2C9 substrateNon-substrate0.727
CYP450 2D6 substrateNon-substrate0.801
CYP450 3A4 substrateSubstrate0.7132
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorNon-inhibitor0.939
CYP450 2D6 inhibitorNon-inhibitor0.9574
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7887
Ames testNon AMES toxic0.9198
CarcinogenicityNon-carcinogens0.8829
BiodegradationNot ready biodegradable0.9746
Rat acute toxicity2.2272 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8647
hERG inhibition (predictor II)Inhibitor0.6624
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Warner chilcott inc
  • Watson laboratories inc
  • Bayer healthcare pharmaceuticals inc
  • Women first healthcare inc
  • Novartis pharmaceuticals corp
  • Mylan technologies inc
  • Ortho mcneil pharmaceutical inc
  • Parke davis pharmaceutical research div warner lambert co
  • Azur pharma international ii ltd
  • Ascend therapeutics inc
  • Upsher smith laboratories inc
  • Pharmacia and upjohn co
  • Kv pharmaceutical co
  • Bristol myers squibb co
  • Bristol myers squibb co pharmaceutical research institute
  • Aai pharma inc
  • Barr laboratories inc
  • Heritage pharmaceuticals inc
  • Mylan pharmaceuticals inc
  • Usl pharma inc
  • Duramed pharmaceuticals inc sub barr laboratories inc
  • Novo nordisk inc
  • Galen ltd
  • Graceway pharmaceuticals llc
  • Jhp pharmaceuticals llc
  • Pharmaforce inc
  • Sandoz canada inc
  • Private formulations inc
  • Monarch pharmaceuticals inc
  • Wyeth ayerst laboratories
Packagers
Dosage forms
FormRouteStrength
Patchtransdermal7.6 mg
Patchtransdermal2 mg
Patchtransdermal3.8 mg
Patchtransdermal5.7 mg
Patchtransdermal
Patch, extended releasetransdermal
Injectionintramuscular10 mg/mL
Injectionintramuscular20 mg/mL
Injectionintramuscular40 mg/mL
Injectionintramuscular5 mg/mL
Geltopical.25 mg/g
Geltopical.5 mg/g
Geltopical1 mg/g
Geltransdermal0.1 %
Geltransdermal.6 mg/g
Gel, meteredtopical.52 mg/g
Creamvaginal.1 mg/g
Tabletoral0.5 mg
Tabletoral1 mg
Tabletoral2 mg
Patch (extended release)transdermal8 mg
Patch (extended release)transdermal2 mg
Patch (extended release)transdermal4 mg
Patchtransdermal.025 mg/d
Patchtransdermal.0375 mg/d
Patchtransdermal.05 mg/d
Patchtransdermal.06 mg/d
Patchtransdermal.075 mg/d
Patchtransdermal.1 mg/d
Patchtransdermal.97 mg/48[USP'U]
Patchtransdermal1.46 mg/48[USP'U]
Patchtransdermal1.94 mg/48[USP'U]
Pelletoral10 mg/1
Pelletoral12.5 mg/1
Pelletoral15 mg/1
Pelletoral18 mg/1
Pelletoral20 mg/1
Pelletoral22 mg/1
Pelletoral25 mg/1
Pelletoral6 mg/1
Tabletoral.5 mg/1
Tabletoral1 mg/1
Tabletoral2 mg/1
Tabletvaginal10 ug/1
Injection, solutionintramuscular20 mg/mL
Injection, solutionintramuscular40 mg/mL
Patchtransdermal1.56 mg
Patchtransdermal0.39 mg
Patchtransdermal0.585 mg
Patchtransdermal0.780 mg
Patchtransdermal1.17 mg
Ringvaginal2 mg/1
Ring (slow-release)vaginal2 mg
Geltransdermal0.06 %
Gel, meteredtransdermal.75 mg/1.25g
Metered-dose pump; capsuleoral; transdermal
Spraytransdermal1.53 mg/1
Spray, meteredtransdermal1.53 mg/1
Ringvaginal.05 mg/d
Ringvaginal.1 mg/d
Ringvaginal.1 mg/24[USP'U]
Patchtransdermal14 ug/d
Tablet, film coatedoral
Tabletoral
Film, extended releasetransdermal.025 mg/d
Film, extended releasetransdermal.0375 mg/d
Film, extended releasetransdermal.05 mg/d
Film, extended releasetransdermal.075 mg/d
Film, extended releasetransdermal.1 mg/d
Solutionintramuscular
Liquidintramuscular20 mg
Patchtransdermal10 mg
Patchtransdermal15 mg
Patchtransdermal20 mg
Patchtransdermal5 mg
Patchtransdermal7.5 mg
Liquidintramuscular10 mg
Patchtransdermal8 mg
Patchtransdermal4 mg
Patchtransdermal6 mg
Tablet, film coatedvaginal10 ug/1
Vaginal tabletvaginal25 mcg
Vaginal tabletvaginal10 mcg
Patchtransdermal8.66 mg
Patchtransdermal3.28 mg
Patchtransdermal4.33 mg
Patchtransdermal6.56 mg
Patch, extended releasetransdermal.025 mg/d
Patch, extended releasetransdermal.0375 mg/d
Patch, extended releasetransdermal.05 mg/d
Patch, extended releasetransdermal.075 mg/d
Patch, extended releasetransdermal.1 mg/d
Prices
Unit descriptionCostUnit
Femring 0.1 mg/24hr Ring218.6USD ring
Estring 2 mg Ring Box210.39USD box
Femring 0.10 mg vaginal ring210.19USD ring
Femring 0.05 mg/24hr Ring205.15USD ring
Estring 2 mg vaginal ring202.3USD ring
Femring 0.05 mg vaginal ring197.26USD ring
Elestrin 0.52 mg/0.87 gm(0.06%) Gel 144 gm Bottle162.06USD bottle
Ethinyl estradiol powder140.0USD g
Vagifem 18 25 mcg tablet Box139.78USD box
Estrace 0.1 mg/gm Cream 42.5 gm Tube133.27USD tube
Estradiol cypionate powder88.74USD g
Delestrogen 10 mg/ml Oil 5ml Vial88.04USD vial
Evamist 1.53 mg/spray Solution 8.1ml Bottle87.18USD bottle
Divigel 1 mg/gm Gel Box Of 30 gm85.53USD box
Estrogel 0.75 mg/1.25 gm(0.06%) Gel 50 gm Bottle84.24USD bottle
Divigel 30 0.25 mg/0.25 gm Gel 30 Patches/box81.24USD box
Climara 4 0.025 mg/24hr Patches Box75.58USD box
Climara 4 0.05 mg/24hr Patches Box75.58USD box
Climara 4 0.1 mg/24hr Patches Box75.58USD box
Menostar 4 14 mcg/24hr Patches Box73.18USD box
Divigel 0.5 mg/0.5 gm Gel Box72.99USD box
Estraderm 8 0.1 mg/24hr Patches Box72.47USD box
Vivelle-Dot 8 0.1 mg/24hr Patches Box72.46USD box
Vivelle-Dot 8 0.025 mg/24hr Patches Box70.69USD box
Climara 4 0.075 mg/24hr Patches Box69.04USD box
Climara Pro 4 0.045-0.015 mg/day Patches Box69.04USD box
Vivelle-Dot 8 0.0375 mg/24hr Patches Box68.84USD box
Vivelle-Dot 8 0.075 mg/24hr Patches Box66.89USD box
CombiPatch 8 0.05-0.25 mg/day Patches Box66.45USD box
Estraderm 8 0.05 mg/24hr Patches Box66.35USD box
Vivelle-Dot 8 0.05 mg/24hr Patches Box65.99USD box
Estring 2 mg Slow-Release Ring65.39USD ring
Alora 8 0.1 mg/24hr Patches Box62.99USD box
Alora 8 0.05 mg/24hr Patches Box60.99USD box
Alora 8 0.075 mg/24hr Patches Box58.27USD box
Vagifem 8 25 mcg tablet Box58.23USD box
Vagifem 8 10 mcg tablet Box54.99USD box
Vivelle 8 0.05 mg/24hr Patches Box49.99USD box
Estradiol benzoate powder42.0USD g
Estradiol 4 0.025 mg/24hr Patches Box40.92USD box
Estradiol 4 0.05 mg/24hr Patches Box40.92USD box
Estradiol 4 0.075 mg/24hr Patches Box40.92USD box
Estradiol 4 0.1 mg/24hr Patches Box40.92USD box
Estradiol 4 0.06 mg/24hr Patches Box39.99USD box
Delestrogen 40 mg/ml Oil39.52USD ml
Estradiol 4 0.0375 mg/24hr Patches Box39.35USD box
Delestrogen 40 mg/ml vial38.0USD ml
Estradiol valerate 40 mg/ml vial35.62USD ml
Estradiol valerate powder32.13USD g
Delestrogen 20 mg/ml Oil23.82USD ml
Delestrogen 20 mg/ml vial22.91USD ml
Estradiol valerate 20 mg/ml vial21.25USD ml
Estradiol 0.1 mg/day patch20.55USD patch
Estradiol powder17.86USD g
Climara 0.0375 mg/24hr Patches17.26USD patch
Climara 0.06 mg/24hr Patches17.26USD patch
Estradiol 0.05 mg/day patch16.91USD patch
Delestrogen 10 mg/ml vial16.25USD ml
Climara 0.025 mg/day patch15.77USD patch
Climara 0.0375 mg/day patch15.77USD patch
Climara 0.05 mg/day patch15.77USD patch
Climara 0.06/mg day patch15.77USD patch
Climara 0.075 mg/day patch15.77USD patch
Climara 0.1 mg/day patch15.77USD patch
Climara pro patch15.77USD patch
Estradiol valerate 10 mg/ml vial15.24USD ml
Evamist 1.53 mg/spray10.43USD ml
Estradiol tds 0.025 mg/day9.84USD each
Estradiol tds 0.0375 mg/day9.84USD each
Estradiol tds 0.06 mg/day9.84USD each
Estradiol tds 0.075 mg/day9.84USD each
Depo-Estradiol 5 mg/ml Oil9.66USD ml
Estraderm 0.1 mg patch8.66USD patch
CombiPatch 0.05-0.14 mg/day Patches8.65USD patch
Vivelle-dot 0.075 mg patch8.49USD patch
Estraderm 0.05 mg patch8.07USD patch
Combipatch 0.05-0.14 mg ptch7.92USD patch
Combipatch 0.05-0.25 mg ptch7.91USD patch
Depo-estradiol 5 mg/ml vial7.89USD ml
Vivelle-dot 0.1 mg patch7.89USD patch
Vivelle-dot 0.05 mg patch7.61USD patch
Vivelle-dot 0.0375 mg patch7.54USD patch
Vivelle-dot 0.025 mg patch7.53USD patch
Alora 0.1 mg patch7.16USD patch
Alora 0.075 mg patch7.0USD patch
Alora 0.05 mg patch6.86USD patch
Vagifem 10 mcg vaginal tab6.78USD each
Vagifem 25 mcg vaginal tab6.78USD each
Climara 100 (7.8 Mg/Pth) 100 mcg/day Patch6.67USD patch
Climara 75 (5.7 Mg/Pth) 75 mcg/day Patch6.31USD patch
Alora 0.025 mg patch6.26USD patch
Vivelle 0.1 mg patch5.94USD patch
Climara 50 (3.9 Mg/Pth) 50 mcg/day Patch5.91USD patch
Vivelle 0.05 mg patch5.74USD patch
Climara 25 (2 Mg/Pth) 25 mcg/day Patch5.54USD patch
Estraderm-100 (8.0 Mg/Pth) 100 mcg/day Patch4.52USD patch
Estraderm-25 (2 Mg/Pth) 25 mcg/day Patch3.74USD patch
Estradot 100 (1.56 Mg/Pth) 100 mcg/day Patch3.49USD patch
Estradot 75 (1.17 Mg/Pth) 75 mcg/day Patch3.3USD patch
Vagifem 25 mcg Tablet3.21USD tablet
Estradot 50 (0.78 Mg/Pth) 50 mcg/day Patch3.07USD patch
Oesclim 50 (10 Mg/Pth) 50 mcg/day Patch3.06USD patch
Estrace 0.01% cream3.05USD g
Estrace 2 mg tablet2.98USD tablet
Estradot 37.5 (0.585 Mg/Pth) 37.5 mcg/day Patch2.88USD patch
Estradot 25 (0.39 Mg/Pth) 25 mcg/day Patch2.86USD patch
Estrasorb 4.35 mg/1.74 gm Emulsion 1.74 gm Packet2.83USD packet
Oesclim 25 (5 Mg/Pth) 25 mcg/day Patch2.83USD patch
Divigel 0.25 mg gel packet2.74USD each
Divigel 0.5 mg gel packet2.74USD each
Divigel 1 mg gel packet2.74USD g
Sandoz Estradiol Derm 100 (8 Mg/Pth) 100 mcg/day Patch2.64USD patch
Menest 2.5 mg tablet2.6USD tablet
Femtrace 1.8 mg tablet2.59USD tablet
Sandoz Estradiol Derm 75 (6 Mg/Pth) 75 mcg/day Patch2.5USD patch
Sandoz Estradiol Derm 50 (4 Mg/Pth) 50 mcg/day Patch2.34USD patch
Estrace 0.5 mg tablet2.29USD tablet
Femtrace 0.45 mg tablet2.02USD tablet
Femtrace 0.9 mg tablet2.02USD tablet
Estrace 1 mg tablet1.93USD tablet
Estrogel 0.06% gel1.63USD g
Menest 1.25 mg tablet1.56USD tablet
Menest 0.625 mg tablet1.41USD tablet
Estrasorb packet1.21USD g
Elestrin 0.06% gel0.94USD g
Menest 0.3 mg tablet0.89USD tablet
Gynodiol 1.5 mg tablet0.5USD tablet
Estradiol 2 mg tablet0.49USD tablet
Estrace 2 mg Tablet0.44USD tablet
Estradiol 1 mg tablet0.42USD tablet
Estradiol 0.5 mg tablet0.36USD tablet
Estrogel 0.06 % Gel0.31USD g
Estrace 1 mg Tablet0.25USD tablet
Estrace 0.5 mg Tablet0.13USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
CA1338660 No1996-10-222013-10-22Canada
CA2306881 No2008-09-022018-11-19Canada
US5223261 No1993-06-292010-06-29Us
US5855906 No1995-12-192015-12-19Us
US5860946 No1997-07-012017-07-01Us
US5891868 No1997-11-212017-11-21Us
US6133251 No1996-10-252016-10-25Us
US6299900 No1997-02-192017-02-19Us
US6692763 No1997-11-212017-11-21Us
US6747019 No2000-03-202020-03-20Us
US6818226 No1997-02-192017-02-19Us
US6841716 No2000-04-272020-04-27Us
US6884793 No1996-10-252016-10-25Us
US6923983 No1997-02-192017-02-19Us
US6933395 No1997-08-112017-08-11Us
US6962908 No2001-12-212021-12-21Us
US6978945 No2002-07-312022-07-31Us
US7018992 No2002-09-172022-09-17Us
US7198801 No2002-06-252022-06-25Us
US7320970 No2000-03-302020-03-30Us
US7470433 No2001-08-032021-08-03Us
US7572779 No2005-10-022025-10-02Us
US7799771 No2001-12-212021-12-21Us
US8071577 No2006-05-132026-05-13Us
US8153616 No2008-01-302028-01-30Us
US8231906 No2010-07-042030-07-04Us
US8906890 No2011-10-222031-10-22Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
melting point151-152Ott, A.C.; US. Patent 2.61 1,773; September 23,1952; assigned to The Upjohn Company.
water solubility3.6 mg/L (at 27 °C)YALKOWSKY,SH & DANNENFELSER,RM (1992)
logP4.01HANSCH,C ET AL. (1995)
Caco2 permeability-4.77ADME Research, USCD
Predicted Properties
PropertyValueSource
Water Solubility0.0213 mg/mLALOGPS
logP3.57ALOGPS
logP3.75ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)10.33ChemAxon
pKa (Strongest Basic)-0.88ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area40.46 Å2ChemAxon
Rotatable Bond Count0ChemAxon
Refractivity79.9 m3·mol-1ChemAxon
Polarizability32.13 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Download (9.34 KB)
Spectra
Spectrum TypeDescriptionSplash Key
GC-MSGC-MS Spectrum - GC-MS (2 TMS)splash10-017r-1791100000-7b16254894cdcb8ee86dView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 10V, Positive (Annotated)splash10-05fr-0590000000-1dd83cbcb3d21edfbdbdView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 25V, Positive (Annotated)splash10-0a4i-2900000000-f3279d6cdab9cf3800fdView in MoNA
LC-MS/MSLC-MS/MS Spectrum - Quattro_QQQ 40V, Positive (Annotated)splash10-0a4i-8900000000-0efe28378f612aab8c3dView in MoNA
LC-MS/MSLC-MS/MS Spectrum - EI-B (JEOL JMS-01-SG-2) , Positivesplash10-00di-1980000000-b2dec84718861de189ecView in MoNA
LC-MS/MSLC-MS/MS Spectrum - EI-B (HITACHI RMU-6E) , Positivesplash10-00di-3940000000-f3692a81f624f15d3e0bView in MoNA
LC-MS/MSLC-MS/MS Spectrum - EI-B (HITACHI M-52) , Positivesplash10-00di-0960000000-be4e96105398cb805cd9View in MoNA
LC-MS/MSLC-MS/MS Spectrum - EI-B (HITACHI M-80) , Positivesplash10-00di-0790000000-5c83456da6e28375ad51View in MoNA
MSMass Spectrum (Electron Ionization)splash10-075a-2920000000-10218bfa5b56f829853eView in MoNA
1D NMR1H NMR SpectrumNot Available
2D NMR[1H,13C] 2D NMR SpectrumNot Available
References
Synthesis Reference

Akira Nakagawa, Munehiko Hirano, Miyuki Shinmura, “Estradiol percutaneous administration preparations.” U.S. Patent US5248676, issued November, 1980.

US5248676
General References
  1. Pentikainen V, Erkkila K, Suomalainen L, Parvinen M, Dunkel L: Estradiol acts as a germ cell survival factor in the human testis in vitro. J Clin Endocrinol Metab. 2000 May;85(5):2057-67. [PubMed:10843196 ]
  2. Sharpe RM, Skakkebaek NE: Are oestrogens involved in falling sperm counts and disorders of the male reproductive tract? Lancet. 1993 May 29;341(8857):1392-5. [PubMed:8098802 ]
  3. Raman JD, Schlegel PN: Aromatase inhibitors for male infertility. J Urol. 2002 Feb;167(2 Pt 1):624-9. [PubMed:11792932 ]
  4. Carani C, Qin K, Simoni M, Faustini-Fustini M, Serpente S, Boyd J, Korach KS, Simpson ER: Effect of testosterone and estradiol in a man with aromatase deficiency. N Engl J Med. 1997 Jul 10;337(2):91-5. [PubMed:9211678 ]
  5. Behl C, Widmann M, Trapp T, Holsboer F: 17-beta estradiol protects neurons from oxidative stress-induced cell death in vitro. Biochem Biophys Res Commun. 1995 Nov 13;216(2):473-82. [PubMed:7488136 ]
  6. Schmidt JW, Wollner D, Curcio J, Riedlinger J, Kim LS: Hormone replacement therapy in menopausal women: Past problems and future possibilities. Gynecol Endocrinol. 2006 Oct;22(10):564-77. [PubMed:17135036 ]
  7. Foresta C, Zuccarello D, Biagioli A, De Toni L, Prana E, Nicoletti V, Ambrosini G, Ferlin A: Oestrogen stimulates endothelial progenitor cells via oestrogen receptor-alpha. Clin Endocrinol (Oxf). 2007 Oct;67(4):520-5. Epub 2007 Jun 15. [PubMed:17573901 ]
  8. Garcia-Segura LM, Sanz A, Mendez P: Cross-talk between IGF-I and estradiol in the brain: focus on neuroprotection. Neuroendocrinology. 2006;84(4):275-9. Epub 2006 Nov 23. [PubMed:17124377 ]
External Links
ATC CodesG03FA11G03FA16G03FA17G03FA12G03FB12G03FB09G03FA05G03EA03G03FA08G03FB01G03AB08G03FA14G03AA14G03EA02G03CA53G03FA07G03FB07G03FB04G03HB01G03FB11G03FB05G03FB02G03CA03G03FA15G03FB10G03EA01G03FA06G03FA09G03FA13G03FA04G03FA10G03FB08G03FA01G03FB06G02BB01G03FA03G03FA02G03FB03
AHFS Codes
  • 68:16.04
PDB EntriesNot Available
FDA labelDownload (89.1 KB)
MSDSDownload (73.8 KB)
Interactions
Drug Interactions
Drug
4-AndrostenedioneThe serum concentration of 4-Androstenedione can be increased when it is combined with Estradiol.
AbciximabEstradiol may decrease the anticoagulant activities of Abciximab.
AbirateroneThe serum concentration of Estradiol can be increased when it is combined with Abiraterone.
AcarboseThe therapeutic efficacy of Acarbose can be decreased when used in combination with Estradiol.
AcenocoumarolEstradiol may decrease the anticoagulant activities of Acenocoumarol.
AcetaminophenThe serum concentration of Estradiol can be increased when it is combined with Acetaminophen.
AcetohexamideThe therapeutic efficacy of Acetohexamide can be decreased when used in combination with Estradiol.
AfatinibThe serum concentration of Estradiol can be increased when it is combined with Afatinib.
AicarThe therapeutic efficacy of Aicar can be decreased when used in combination with Estradiol.
AlbendazoleThe serum concentration of Estradiol can be increased when it is combined with Albendazole.
AlclometasoneThe serum concentration of Alclometasone can be increased when it is combined with Estradiol.
AldosteroneThe serum concentration of Aldosterone can be increased when it is combined with Estradiol.
AldosteroneThe serum concentration of Estradiol can be decreased when it is combined with Aldosterone.
AlectinibThe serum concentration of Estradiol can be increased when it is combined with Alectinib.
AlfentanilThe serum concentration of Estradiol can be increased when it is combined with Alfentanil.
AlogliptinThe therapeutic efficacy of Alogliptin can be decreased when used in combination with Estradiol.
AmantadineThe serum concentration of Estradiol can be increased when it is combined with Amantadine.
AmcinonideThe serum concentration of Amcinonide can be increased when it is combined with Estradiol.
Aminohippuric acidThe serum concentration of Estradiol can be increased when it is combined with Aminohippuric acid.
AminophyllineThe serum concentration of Aminophylline can be increased when it is combined with Estradiol.
AmiodaroneThe serum concentration of Estradiol can be decreased when it is combined with Amiodarone.
AmitriptylineThe serum concentration of Estradiol can be increased when it is combined with Amitriptyline.
AmlodipineThe serum concentration of Estradiol can be increased when it is combined with Amlodipine.
AmprenavirThe serum concentration of Estradiol can be decreased when it is combined with Amprenavir.
AmsacrineThe serum concentration of Estradiol can be increased when it is combined with Amsacrine.
AnastrozoleThe therapeutic efficacy of Anastrozole can be decreased when used in combination with Estradiol.
AncrodEstradiol may decrease the anticoagulant activities of Ancrod.
Anthrax immune globulin humanEstradiol may increase the thrombogenic activities of Anthrax immune globulin human.
Antithrombin III humanEstradiol may decrease the anticoagulant activities of Antithrombin III human.
ApixabanEstradiol may decrease the anticoagulant activities of Apixaban.
AprepitantThe serum concentration of Estradiol can be increased when it is combined with Aprepitant.
ArdeparinEstradiol may decrease the anticoagulant activities of Ardeparin.
ArgatrobanEstradiol may decrease the anticoagulant activities of Argatroban.
ArmodafinilThe metabolism of Estradiol can be decreased when combined with Armodafinil.
AstemizoleThe serum concentration of Estradiol can be increased when it is combined with Astemizole.
AtazanavirThe serum concentration of Estradiol can be increased when it is combined with Atazanavir.
AtenololThe serum concentration of Estradiol can be increased when it is combined with Atenolol.
AtomoxetineThe metabolism of Estradiol can be decreased when combined with Atomoxetine.
AtorvastatinThe serum concentration of Estradiol can be increased when it is combined with Atorvastatin.
AzelastineThe serum concentration of Estradiol can be increased when it is combined with Azelastine.
AzithromycinThe serum concentration of Estradiol can be increased when it is combined with Azithromycin.
BecaplerminEstradiol may decrease the anticoagulant activities of Becaplermin.
Beclomethasone dipropionateThe serum concentration of Beclomethasone dipropionate can be increased when it is combined with Estradiol.
BenzocaineThe serum concentration of Estradiol can be increased when it is combined with Benzocaine.
BepridilThe serum concentration of Estradiol can be increased when it is combined with Bepridil.
BetamethasoneThe serum concentration of Betamethasone can be increased when it is combined with Estradiol.
BexaroteneThe serum concentration of Estradiol can be decreased when it is combined with Bexarotene.
BiperidenThe serum concentration of Estradiol can be increased when it is combined with Biperiden.
BivalirudinEstradiol may decrease the anticoagulant activities of Bivalirudin.
BoceprevirThe metabolism of Estradiol can be decreased when combined with Boceprevir.
BortezomibThe metabolism of Estradiol can be decreased when combined with Bortezomib.
BosentanThe serum concentration of Estradiol can be decreased when it is combined with Bosentan.
BosutinibThe serum concentration of Estradiol can be increased when it is combined with Bosutinib.
BromocriptineThe serum concentration of Estradiol can be increased when it is combined with Bromocriptine.
BudesonideThe serum concentration of Budesonide can be increased when it is combined with Estradiol.
BuforminThe therapeutic efficacy of Buformin can be decreased when used in combination with Estradiol.
BuprenorphineThe serum concentration of Estradiol can be increased when it is combined with Buprenorphine.
BuspironeThe serum concentration of Estradiol can be increased when it is combined with Buspirone.
C1 Esterase Inhibitor (Human)Estradiol may increase the thrombogenic activities of C1 Esterase Inhibitor (Human).
C1 Esterase Inhibitor (Recombinant)Estradiol may increase the thrombogenic activities of C1 Esterase Inhibitor (Recombinant).
CabazitaxelThe serum concentration of Estradiol can be increased when it is combined with Cabazitaxel.
CaffeineThe serum concentration of Estradiol can be increased when it is combined with Caffeine.
CanagliflozinThe therapeutic efficacy of Canagliflozin can be decreased when used in combination with Estradiol.
CanagliflozinThe serum concentration of Estradiol can be increased when it is combined with Canagliflozin.
CandesartanThe serum concentration of Estradiol can be increased when it is combined with Candesartan.
CapecitabineThe metabolism of Estradiol can be decreased when combined with Capecitabine.
CaptoprilThe serum concentration of Estradiol can be increased when it is combined with Captopril.
CarbamazepineThe serum concentration of Estradiol can be decreased when it is combined with Carbamazepine.
CarvedilolThe serum concentration of Estradiol can be increased when it is combined with Carvedilol.
CaspofunginThe serum concentration of Estradiol can be increased when it is combined with Caspofungin.
CastanospermineThe therapeutic efficacy of Castanospermine can be decreased when used in combination with Estradiol.
CelecoxibThe metabolism of Estradiol can be decreased when combined with Celecoxib.
CeritinibThe serum concentration of Estradiol can be increased when it is combined with Ceritinib.
CertoparinEstradiol may decrease the anticoagulant activities of Certoparin.
Chenodeoxycholic acidThe therapeutic efficacy of Chenodeoxycholic acid can be decreased when used in combination with Estradiol.
ChloramphenicolThe metabolism of Estradiol can be decreased when combined with Chloramphenicol.
ChloroquineThe serum concentration of Estradiol can be increased when it is combined with Chloroquine.
ChlorpromazineThe serum concentration of Estradiol can be increased when it is combined with Chlorpromazine.
ChlorpropamideThe therapeutic efficacy of Chlorpropamide can be decreased when used in combination with Estradiol.
ChlorpropamideThe serum concentration of Estradiol can be increased when it is combined with Chlorpropamide.
ChlorprothixeneThe serum concentration of Estradiol can be increased when it is combined with Chlorprothixene.
CholecalciferolThe metabolism of Estradiol can be decreased when combined with Cholecalciferol.
CholesterolThe serum concentration of Estradiol can be increased when it is combined with Cholesterol.
Cholic AcidThe serum concentration of Estradiol can be decreased when it is combined with Cholic Acid.
Choline C 11The therapeutic efficacy of Choline C 11 can be decreased when used in combination with Estradiol.
CiclesonideThe serum concentration of Ciclesonide can be increased when it is combined with Estradiol.
CiglitazoneThe therapeutic efficacy of Ciglitazone can be decreased when used in combination with Estradiol.
CilazaprilThe serum concentration of Estradiol can be increased when it is combined with Cilazapril.
CimetidineThe serum concentration of Estradiol can be decreased when it is combined with Cimetidine.
CiprofloxacinThe serum concentration of Estradiol can be increased when it is combined with Ciprofloxacin.
CitalopramThe serum concentration of Estradiol can be increased when it is combined with Citalopram.
Citric AcidEstradiol may decrease the anticoagulant activities of Citric Acid.
ClarithromycinThe serum concentration of Estradiol can be increased when it is combined with Clarithromycin.
ClemastineThe metabolism of Estradiol can be decreased when combined with Clemastine.
Clobetasol propionateThe serum concentration of Clobetasol propionate can be increased when it is combined with Estradiol.
ClocortoloneThe serum concentration of Clocortolone can be increased when it is combined with Estradiol.
ClofazimineThe serum concentration of Estradiol can be increased when it is combined with Clofazimine.
ClomipramineThe serum concentration of Estradiol can be increased when it is combined with Clomipramine.
ClopidogrelThe metabolism of Estradiol can be decreased when combined with Clopidogrel.
ClotrimazoleThe metabolism of Estradiol can be decreased when combined with Clotrimazole.
CobicistatThe serum concentration of Estradiol can be increased when it is combined with Cobicistat.
ColchicineThe serum concentration of Estradiol can be increased when it is combined with Colchicine.
ColforsinThe serum concentration of Estradiol can be increased when it is combined with Colforsin.
ConivaptanThe serum concentration of Estradiol can be increased when it is combined with Conivaptan.
Cortisone acetateThe serum concentration of Cortisone acetate can be increased when it is combined with Estradiol.
CrizotinibThe metabolism of Estradiol can be decreased when combined with Crizotinib.
CyclophosphamideThe serum concentration of Estradiol can be increased when it is combined with Cyclophosphamide.
CyclosporineThe metabolism of Estradiol can be decreased when combined with Cyclosporine.
Cyproterone acetateThe serum concentration of Estradiol can be decreased when it is combined with Cyproterone acetate.
Dabigatran etexilateEstradiol may decrease the anticoagulant activities of Dabigatran etexilate.
DabrafenibThe serum concentration of Estradiol can be decreased when it is combined with Dabrafenib.
DaclatasvirThe serum concentration of Estradiol can be increased when it is combined with Daclatasvir.
DactinomycinThe serum concentration of Estradiol can be increased when it is combined with Dactinomycin.
DalteparinEstradiol may decrease the anticoagulant activities of Dalteparin.
DanaparoidEstradiol may decrease the anticoagulant activities of Danaparoid.
DarunavirThe metabolism of Estradiol can be decreased when combined with Darunavir.
DasatinibThe serum concentration of Estradiol can be increased when it is combined with Dasatinib.
DaunorubicinThe serum concentration of Estradiol can be decreased when it is combined with Daunorubicin.
DeferasiroxThe serum concentration of Estradiol can be decreased when it is combined with Deferasirox.
DehydroepiandrosteroneThe risk or severity of adverse effects can be increased when Dehydroepiandrosterone is combined with Estradiol.
DehydroepiandrosteroneThe serum concentration of Dehydroepiandrosterone can be increased when it is combined with Estradiol.
dehydroepiandrosterone sulfateThe serum concentration of dehydroepiandrosterone sulfate can be increased when it is combined with Estradiol.
DelavirdineThe metabolism of Estradiol can be decreased when combined with Delavirdine.
DesipramineThe serum concentration of Estradiol can be increased when it is combined with Desipramine.
DesirudinEstradiol may decrease the anticoagulant activities of Desirudin.
DesloratadineThe serum concentration of Estradiol can be increased when it is combined with Desloratadine.
DesoximetasoneThe serum concentration of Desoximetasone can be increased when it is combined with Estradiol.
Desoxycorticosterone acetateThe serum concentration of Desoxycorticosterone acetate can be increased when it is combined with Estradiol.
DexamethasoneThe serum concentration of Dexamethasone can be increased when it is combined with Estradiol.
DexamethasoneThe serum concentration of Estradiol can be decreased when it is combined with Dexamethasone.
Dexamethasone isonicotinateThe serum concentration of Dexamethasone isonicotinate can be increased when it is combined with Estradiol.
DextranEstradiol may decrease the anticoagulant activities of Dextran.
Dextran 40Estradiol may decrease the anticoagulant activities of Dextran 40.
Dextran 70Estradiol may decrease the anticoagulant activities of Dextran 70.
Dextran 75Estradiol may decrease the anticoagulant activities of Dextran 75.
DextromethorphanThe serum concentration of Estradiol can be increased when it is combined with Dextromethorphan.
DiclofenacThe serum concentration of Estradiol can be increased when it is combined with Diclofenac.
DicoumarolEstradiol may decrease the anticoagulant activities of Dicoumarol.
DiflorasoneThe serum concentration of Diflorasone can be increased when it is combined with Estradiol.
DifluocortoloneThe serum concentration of Difluocortolone can be increased when it is combined with Estradiol.
DifluprednateThe serum concentration of Difluprednate can be increased when it is combined with Estradiol.
DigoxinThe serum concentration of Estradiol can be decreased when it is combined with Digoxin.
DihydroergotamineThe metabolism of Estradiol can be decreased when combined with Dihydroergotamine.
DiltiazemThe metabolism of Estradiol can be decreased when combined with Diltiazem.
DipyridamoleThe serum concentration of Estradiol can be increased when it is combined with Dipyridamole.
DoxazosinThe serum concentration of Estradiol can be increased when it is combined with Doxazosin.
DoxepinThe serum concentration of Estradiol can be increased when it is combined with Doxepin.
DoxorubicinThe serum concentration of Estradiol can be decreased when it is combined with Doxorubicin.
DoxycyclineThe metabolism of Estradiol can be decreased when combined with Doxycycline.
DronabinolThe serum concentration of Estradiol can be increased when it is combined with Dronabinol.
DronedaroneThe metabolism of Estradiol can be decreased when combined with Dronedarone.
DulaglutideThe therapeutic efficacy of Dulaglutide can be decreased when used in combination with Estradiol.
DyphyllineThe serum concentration of Dyphylline can be increased when it is combined with Estradiol.
Edetic AcidEstradiol may decrease the anticoagulant activities of Edetic Acid.
EdoxabanEstradiol may decrease the anticoagulant activities of Edoxaban.
EfavirenzThe serum concentration of Estradiol can be decreased when it is combined with Efavirenz.
ElbasvirThe serum concentration of Estradiol can be increased when it is combined with Elbasvir.
EmpagliflozinThe therapeutic efficacy of Empagliflozin can be decreased when used in combination with Estradiol.
EnalaprilThe serum concentration of Estradiol can be increased when it is combined with Enalapril.
EnoxaparinEstradiol may decrease the anticoagulant activities of Enoxaparin.
EnzalutamideThe serum concentration of Estradiol can be increased when it is combined with Enzalutamide.
EquileninThe serum concentration of Equilenin can be increased when it is combined with Estradiol.
EquilinThe serum concentration of Equilin can be increased when it is combined with Estradiol.
ErgonovineThe serum concentration of Estradiol can be increased when it is combined with Ergonovine.
ErgotamineThe serum concentration of Estradiol can be increased when it is combined with Ergotamine.
ErythromycinThe metabolism of Estradiol can be decreased when combined with Erythromycin.
Eslicarbazepine acetateThe serum concentration of Estradiol can be decreased when it is combined with Eslicarbazepine acetate.
EsomeprazoleThe metabolism of Estradiol can be decreased when combined with Esomeprazole.
EstramustineThe serum concentration of Estradiol can be increased when it is combined with Estramustine.
EstriolThe serum concentration of Estradiol can be decreased when it is combined with Estriol.
EstroneThe serum concentration of Estrone can be increased when it is combined with Estradiol.
EstroneThe serum concentration of Estradiol can be decreased when it is combined with Estrone.
Ethyl biscoumacetateEstradiol may decrease the anticoagulant activities of Ethyl biscoumacetate.
EtoposideThe serum concentration of Estradiol can be increased when it is combined with Etoposide.
EtravirineThe serum concentration of Estradiol can be decreased when it is combined with Etravirine.
ExemestaneThe therapeutic efficacy of Exemestane can be decreased when used in combination with Estradiol.
ExenatideThe therapeutic efficacy of Exenatide can be decreased when used in combination with Estradiol.
FelodipineThe serum concentration of Estradiol can be increased when it is combined with Felodipine.
FentanylThe serum concentration of Estradiol can be increased when it is combined with Fentanyl.
FexofenadineThe serum concentration of Estradiol can be increased when it is combined with Fexofenadine.
FidaxomicinThe serum concentration of Estradiol can be increased when it is combined with Fidaxomicin.
FloxuridineThe metabolism of Estradiol can be decreased when combined with Floxuridine.
FluconazoleThe metabolism of Estradiol can be decreased when combined with Fluconazole.
FludrocortisoneThe serum concentration of Fludrocortisone can be increased when it is combined with Estradiol.
FlumethasoneThe serum concentration of Flumethasone can be increased when it is combined with Estradiol.
FlunisolideThe serum concentration of Flunisolide can be increased when it is combined with Estradiol.
Fluocinolone AcetonideThe serum concentration of Fluocinolone Acetonide can be increased when it is combined with Estradiol.
FluocinonideThe serum concentration of Fluocinonide can be increased when it is combined with Estradiol.
FluocortoloneThe serum concentration of Fluocortolone can be increased when it is combined with Estradiol.
FluorometholoneThe serum concentration of Fluorometholone can be increased when it is combined with Estradiol.
FluorouracilThe metabolism of Estradiol can be decreased when combined with Fluorouracil.
FluoxetineThe serum concentration of Estradiol can be increased when it is combined with Fluoxetine.
FlupentixolThe serum concentration of Estradiol can be increased when it is combined with Flupentixol.
FluphenazineThe serum concentration of Estradiol can be increased when it is combined with Fluphenazine.
FluprednideneThe serum concentration of Fluprednidene can be increased when it is combined with Estradiol.
FluprednisoloneThe serum concentration of Fluprednisolone can be increased when it is combined with Estradiol.
FlurandrenolideThe serum concentration of Flurandrenolide can be increased when it is combined with Estradiol.
FlurazepamThe serum concentration of Estradiol can be increased when it is combined with Flurazepam.
Fluticasone furoateThe serum concentration of Fluticasone furoate can be increased when it is combined with Estradiol.
Fluticasone PropionateThe serum concentration of Fluticasone Propionate can be increased when it is combined with Estradiol.
FluvastatinThe metabolism of Estradiol can be decreased when combined with Fluvastatin.
FluvoxamineThe metabolism of Estradiol can be decreased when combined with Fluvoxamine.
Fondaparinux sodiumEstradiol may decrease the anticoagulant activities of Fondaparinux sodium.
FosamprenavirThe metabolism of Estradiol can be decreased when combined with Fosamprenavir.
FosaprepitantThe serum concentration of Estradiol can be increased when it is combined with Fosaprepitant.
FosphenytoinThe metabolism of Estradiol can be increased when combined with Fosphenytoin.
Fusidic AcidThe serum concentration of Estradiol can be increased when it is combined with Fusidic Acid.
GefitinibThe serum concentration of Estradiol can be increased when it is combined with Gefitinib.
GemfibrozilThe metabolism of Estradiol can be decreased when combined with Gemfibrozil.
GenisteinThe serum concentration of Estradiol can be increased when it is combined with Genistein.
GlibornurideThe therapeutic efficacy of Glibornuride can be decreased when used in combination with Estradiol.
GliclazideThe therapeutic efficacy of Gliclazide can be decreased when used in combination with Estradiol.
GlimepirideThe therapeutic efficacy of Glimepiride can be decreased when used in combination with Estradiol.
GlipizideThe therapeutic efficacy of Glipizide can be decreased when used in combination with Estradiol.
GliquidoneThe therapeutic efficacy of Gliquidone can be decreased when used in combination with Estradiol.
GlyburideThe therapeutic efficacy of Glyburide can be decreased when used in combination with Estradiol.
GlyburideThe serum concentration of Estradiol can be increased when it is combined with Glyburide.
GlycerolThe serum concentration of Estradiol can be increased when it is combined with Glycerol.
Gramicidin DThe serum concentration of Estradiol can be increased when it is combined with Gramicidin D.
GrepafloxacinThe serum concentration of Estradiol can be increased when it is combined with Grepafloxacin.
HaloperidolThe serum concentration of Estradiol can be increased when it is combined with Haloperidol.
HeparinEstradiol may decrease the anticoagulant activities of Heparin.
HirulogEstradiol may decrease the anticoagulant activities of Hirulog.
HyaluronidaseThe therapeutic efficacy of Hyaluronidase can be decreased when used in combination with Estradiol.
HydrocodoneThe serum concentration of Hydrocodone can be decreased when it is combined with Estradiol.
HydrocortisoneThe serum concentration of Hydrocortisone can be increased when it is combined with Estradiol.
IdelalisibThe serum concentration of Estradiol can be increased when it is combined with Idelalisib.
ImatinibThe metabolism of Estradiol can be decreased when combined with Imatinib.
ImipramineThe serum concentration of Estradiol can be increased when it is combined with Imipramine.
IndinavirThe serum concentration of Estradiol can be decreased when it is combined with Indinavir.
IndomethacinThe serum concentration of Estradiol can be increased when it is combined with Indomethacin.
Insulin AspartThe therapeutic efficacy of Insulin Aspart can be decreased when used in combination with Estradiol.
Insulin DetemirThe therapeutic efficacy of Insulin Detemir can be decreased when used in combination with Estradiol.
Insulin GlargineThe therapeutic efficacy of Insulin Glargine can be decreased when used in combination with Estradiol.
Insulin GlulisineThe therapeutic efficacy of Insulin Glulisine can be decreased when used in combination with Estradiol.
Insulin LisproThe therapeutic efficacy of Insulin Lispro can be decreased when used in combination with Estradiol.
Insulin PorkThe therapeutic efficacy of Insulin Pork can be decreased when used in combination with Estradiol.
IrbesartanThe metabolism of Estradiol can be decreased when combined with Irbesartan.
IsavuconazoniumThe metabolism of Estradiol can be decreased when combined with Isavuconazonium.
IsoniazidThe metabolism of Estradiol can be decreased when combined with Isoniazid.
IsradipineThe metabolism of Estradiol can be decreased when combined with Isradipine.
ItraconazoleThe serum concentration of Estradiol can be increased when it is combined with Itraconazole.
IvacaftorThe serum concentration of Estradiol can be increased when it is combined with Ivacaftor.
IvermectinThe serum concentration of Estradiol can be increased when it is combined with Ivermectin.
KetamineThe serum concentration of Estradiol can be increased when it is combined with Ketamine.
KetoconazoleThe serum concentration of Estradiol can be increased when it is combined with Ketoconazole.
LansoprazoleThe serum concentration of Estradiol can be increased when it is combined with Lansoprazole.
LapatinibThe serum concentration of Estradiol can be increased when it is combined with Lapatinib.
LeflunomideThe metabolism of Estradiol can be decreased when combined with Leflunomide.
LenalidomideEstradiol may increase the thrombogenic activities of Lenalidomide.
LepirudinEstradiol may decrease the anticoagulant activities of Lepirudin.
LevofloxacinThe serum concentration of Estradiol can be increased when it is combined with Levofloxacin.
LevothyroxineThe therapeutic efficacy of Levothyroxine can be decreased when used in combination with Estradiol.
LevothyroxineThe serum concentration of Estradiol can be decreased when it is combined with Levothyroxine.
LidocaineThe serum concentration of Estradiol can be increased when it is combined with Lidocaine.
LinagliptinThe therapeutic efficacy of Linagliptin can be decreased when used in combination with Estradiol.
LiothyronineThe therapeutic efficacy of Liothyronine can be decreased when used in combination with Estradiol.
LiothyronineThe serum concentration of Estradiol can be decreased when it is combined with Liothyronine.
LiotrixThe therapeutic efficacy of Liotrix can be decreased when used in combination with Estradiol.
LiotrixThe serum concentration of Estradiol can be decreased when it is combined with Liotrix.
LiraglutideThe therapeutic efficacy of Liraglutide can be decreased when used in combination with Estradiol.
LisinoprilThe serum concentration of Estradiol can be increased when it is combined with Lisinopril.
LomitapideThe serum concentration of Estradiol can be increased when it is combined with Lomitapide.
LoperamideThe serum concentration of Estradiol can be increased when it is combined with Loperamide.
LopinavirThe serum concentration of Estradiol can be increased when it is combined with Lopinavir.
LoratadineThe serum concentration of Estradiol can be increased when it is combined with Loratadine.
LosartanThe serum concentration of Estradiol can be increased when it is combined with Losartan.
LovastatinThe metabolism of Estradiol can be decreased when combined with Lovastatin.
LuliconazoleThe serum concentration of Estradiol can be increased when it is combined with Luliconazole.
LumacaftorThe serum concentration of Estradiol can be decreased when it is combined with Lumacaftor.
MaprotilineThe serum concentration of Estradiol can be increased when it is combined with Maprotiline.
MebendazoleThe serum concentration of Estradiol can be increased when it is combined with Mebendazole.
MedrysoneThe serum concentration of Medrysone can be increased when it is combined with Estradiol.
MefloquineThe serum concentration of Estradiol can be increased when it is combined with Mefloquine.
Megestrol acetateThe serum concentration of Estradiol can be increased when it is combined with Megestrol acetate.
MelengestrolThe serum concentration of Melengestrol can be increased when it is combined with Estradiol.
MeprobamateThe serum concentration of Estradiol can be increased when it is combined with Meprobamate.
MetforminThe therapeutic efficacy of Metformin can be decreased when used in combination with Estradiol.
MethadoneThe serum concentration of Estradiol can be increased when it is combined with Methadone.
MethylprednisoloneThe serum concentration of Methylprednisolone can be increased when it is combined with Estradiol.
MetoprololThe serum concentration of Estradiol can be increased when it is combined with Metoprolol.
MexiletineThe metabolism of Estradiol can be decreased when combined with Mexiletine.
MibefradilThe serum concentration of Estradiol can be increased when it is combined with Mibefradil.
MiconazoleThe serum concentration of Estradiol can be increased when it is combined with Miconazole.
MidazolamThe serum concentration of Estradiol can be decreased when it is combined with Midazolam.
MifepristoneThe metabolism of Estradiol can be decreased when combined with Mifepristone.
MiglitolThe therapeutic efficacy of Miglitol can be decreased when used in combination with Estradiol.
MiglustatThe therapeutic efficacy of Miglustat can be decreased when used in combination with Estradiol.
MitiglinideThe therapeutic efficacy of Mitiglinide can be decreased when used in combination with Estradiol.
MitomycinThe serum concentration of Estradiol can be increased when it is combined with Mitomycin.
MitotaneThe serum concentration of Estradiol can be decreased when it is combined with Mitotane.
MitoxantroneThe serum concentration of Estradiol can be decreased when it is combined with Mitoxantrone.
MoclobemideThe metabolism of Estradiol can be decreased when combined with Moclobemide.
ModafinilThe serum concentration of Estradiol can be decreased when it is combined with Modafinil.
MometasoneThe serum concentration of Mometasone can be increased when it is combined with Estradiol.
MorphineThe serum concentration of Estradiol can be increased when it is combined with Morphine.
NadroparinEstradiol may decrease the anticoagulant activities of Nadroparin.
NafcillinThe serum concentration of Estradiol can be decreased when it is combined with Nafcillin.
NaltrexoneThe serum concentration of Estradiol can be increased when it is combined with Naltrexone.
NaringeninThe serum concentration of Estradiol can be increased when it is combined with Naringenin.
NateglinideThe therapeutic efficacy of Nateglinide can be decreased when used in combination with Estradiol.
NefazodoneThe serum concentration of Estradiol can be decreased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Estradiol can be decreased when it is combined with Nelfinavir.
NeostigmineThe serum concentration of Estradiol can be increased when it is combined with Neostigmine.
NetupitantThe serum concentration of Estradiol can be increased when it is combined with Netupitant.
NevirapineThe metabolism of Estradiol can be decreased when combined with Nevirapine.
NicardipineThe serum concentration of Estradiol can be increased when it is combined with Nicardipine.
NifedipineThe serum concentration of Estradiol can be decreased when it is combined with Nifedipine.
NilotinibThe metabolism of Estradiol can be decreased when combined with Nilotinib.
NimodipineThe serum concentration of Nimodipine can be decreased when it is combined with Estradiol.
NisoldipineThe serum concentration of Estradiol can be increased when it is combined with Nisoldipine.
NitrazepamThe serum concentration of Estradiol can be increased when it is combined with Nitrazepam.
NitrendipineThe serum concentration of Estradiol can be increased when it is combined with Nitrendipine.
NorethisteroneThe serum concentration of Estradiol can be decreased when it is combined with Norethisterone.
OlaparibThe metabolism of Estradiol can be decreased when combined with Olaparib.
OmeprazoleThe serum concentration of Estradiol can be increased when it is combined with Omeprazole.
OsimertinibThe serum concentration of Estradiol can be increased when it is combined with Osimertinib.
OspemifeneThe risk or severity of adverse effects can be increased when Estradiol is combined with Ospemifene.
OtamixabanEstradiol may decrease the anticoagulant activities of Otamixaban.
P-NitrophenolThe serum concentration of Estradiol can be increased when it is combined with P-Nitrophenol.
PaclitaxelThe serum concentration of Estradiol can be increased when it is combined with Paclitaxel.
PalbociclibThe serum concentration of Estradiol can be increased when it is combined with Palbociclib.
Palmitic AcidThe serum concentration of Estradiol can be increased when it is combined with Palmitic Acid.
PantoprazoleThe serum concentration of Estradiol can be increased when it is combined with Pantoprazole.
ParamethasoneThe serum concentration of Paramethasone can be increased when it is combined with Estradiol.
ParoxetineThe serum concentration of Estradiol can be increased when it is combined with Paroxetine.
PazopanibThe serum concentration of Pazopanib can be increased when it is combined with Estradiol.
Peginterferon alfa-2bThe serum concentration of Estradiol can be increased when it is combined with Peginterferon alfa-2b.
PentobarbitalThe metabolism of Estradiol can be increased when combined with Pentobarbital.
Pentosan PolysulfateEstradiol may decrease the anticoagulant activities of Pentosan Polysulfate.
PerindoprilThe serum concentration of Estradiol can be increased when it is combined with Perindopril.
PhenforminThe therapeutic efficacy of Phenformin can be decreased when used in combination with Estradiol.
PhenindioneEstradiol may decrease the anticoagulant activities of Phenindione.
PhenobarbitalThe serum concentration of Estradiol can be decreased when it is combined with Phenobarbital.
PhenprocoumonEstradiol may decrease the anticoagulant activities of Phenprocoumon.
PhenytoinThe metabolism of Estradiol can be increased when combined with Phenytoin.
PimozideThe serum concentration of Estradiol can be increased when it is combined with Pimozide.
PioglitazoneThe therapeutic efficacy of Pioglitazone can be decreased when used in combination with Estradiol.
PioglitazoneThe metabolism of Estradiol can be decreased when combined with Pioglitazone.
Platelet Activating FactorThe serum concentration of Estradiol can be decreased when it is combined with Platelet Activating Factor.
PonatinibThe serum concentration of Estradiol can be increased when it is combined with Ponatinib.
PosaconazoleThe serum concentration of Estradiol can be increased when it is combined with Posaconazole.
PramlintideThe therapeutic efficacy of Pramlintide can be decreased when used in combination with Estradiol.
PravastatinThe serum concentration of Estradiol can be increased when it is combined with Pravastatin.
PrazosinThe serum concentration of Estradiol can be increased when it is combined with Prazosin.
PrednicarbateThe serum concentration of Prednicarbate can be increased when it is combined with Estradiol.
PrednisoloneThe serum concentration of Prednisolone can be increased when it is combined with Estradiol.
PrednisoneThe serum concentration of Prednisone can be increased when it is combined with Estradiol.
PregnenoloneThe serum concentration of Pregnenolone can be increased when it is combined with Estradiol.
PrimidoneThe metabolism of Estradiol can be increased when combined with Primidone.
ProbenecidThe serum concentration of Estradiol can be increased when it is combined with Probenecid.
ProgesteroneThe serum concentration of Estradiol can be decreased when it is combined with Progesterone.
PromethazineThe serum concentration of Estradiol can be increased when it is combined with Promethazine.
PropafenoneThe serum concentration of Estradiol can be increased when it is combined with Propafenone.
PropranololThe serum concentration of Estradiol can be increased when it is combined with Propranolol.
Protein CEstradiol may decrease the anticoagulant activities of Protein C.
ProtocatechualdehydeEstradiol may decrease the anticoagulant activities of Protocatechualdehyde.
ProtriptylineThe serum concentration of Estradiol can be increased when it is combined with Protriptyline.
PyrimethamineThe metabolism of Estradiol can be decreased when combined with Pyrimethamine.
QuercetinThe serum concentration of Estradiol can be increased when it is combined with Quercetin.
QuinacrineThe serum concentration of Estradiol can be increased when it is combined with Quinacrine.
QuinidineThe serum concentration of Estradiol can be increased when it is combined with Quinidine.
QuinineThe serum concentration of Estradiol can be increased when it is combined with Quinine.
RabeprazoleThe metabolism of Estradiol can be decreased when combined with Rabeprazole.
RanitidineThe serum concentration of Estradiol can be increased when it is combined with Ranitidine.
RanolazineThe serum concentration of Estradiol can be increased when it is combined with Ranolazine.
ReboxetineThe serum concentration of Estradiol can be increased when it is combined with Reboxetine.
RegorafenibThe serum concentration of Estradiol can be increased when it is combined with Regorafenib.
RepaglinideThe therapeutic efficacy of Repaglinide can be decreased when used in combination with Estradiol.
ReserpineThe serum concentration of Estradiol can be decreased when it is combined with Reserpine.
ReviparinEstradiol may decrease the anticoagulant activities of Reviparin.
RifabutinThe metabolism of Estradiol can be increased when combined with Rifabutin.
RifampicinThe serum concentration of Estradiol can be decreased when it is combined with Rifampicin.
RifapentineThe metabolism of Estradiol can be increased when combined with Rifapentine.
RilpivirineThe serum concentration of Estradiol can be increased when it is combined with Rilpivirine.
RimexoloneThe serum concentration of Rimexolone can be increased when it is combined with Estradiol.
RitonavirThe serum concentration of Estradiol can be decreased when it is combined with Ritonavir.
RivaroxabanEstradiol may decrease the anticoagulant activities of Rivaroxaban.
RolapitantThe serum concentration of Estradiol can be increased when it is combined with Rolapitant.
RopiniroleThe serum concentration of Ropinirole can be increased when it is combined with Estradiol.
RopiniroleThe metabolism of Estradiol can be decreased when combined with Ropinirole.
RosiglitazoneThe therapeutic efficacy of Rosiglitazone can be decreased when used in combination with Estradiol.
RosiglitazoneThe metabolism of Estradiol can be decreased when combined with Rosiglitazone.
SaquinavirThe serum concentration of Estradiol can be decreased when it is combined with Saquinavir.
SaxagliptinThe therapeutic efficacy of Saxagliptin can be decreased when used in combination with Estradiol.
ScopolamineThe serum concentration of Estradiol can be increased when it is combined with Scopolamine.
SecobarbitalThe metabolism of Estradiol can be increased when combined with Secobarbital.
SelegilineThe serum concentration of Estradiol can be increased when it is combined with Selegiline.
SertralineThe serum concentration of Estradiol can be increased when it is combined with Sertraline.
SildenafilThe metabolism of Estradiol can be decreased when combined with Sildenafil.
SiltuximabThe serum concentration of Estradiol can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Estradiol can be increased when it is combined with Simeprevir.
SimvastatinThe serum concentration of Estradiol can be increased when it is combined with Simvastatin.
SirolimusThe serum concentration of Estradiol can be decreased when it is combined with Sirolimus.
SitagliptinThe therapeutic efficacy of Sitagliptin can be decreased when used in combination with Estradiol.
Somatropin recombinantThe therapeutic efficacy of Somatropin recombinant can be decreased when used in combination with Estradiol.
SorafenibThe serum concentration of Estradiol can be increased when it is combined with Sorafenib.
SpironolactoneThe serum concentration of Estradiol can be increased when it is combined with Spironolactone.
St. John's WortThe serum concentration of Estradiol can be decreased when it is combined with St. John's Wort.
StaurosporineThe serum concentration of Estradiol can be increased when it is combined with Staurosporine.
StiripentolThe serum concentration of Estradiol can be increased when it is combined with Stiripentol.
StreptozocinThe serum concentration of Estradiol can be decreased when it is combined with Streptozocin.
SulfadiazineThe metabolism of Estradiol can be decreased when combined with Sulfadiazine.
SulfamethoxazoleThe metabolism of Estradiol can be decreased when combined with Sulfamethoxazole.
SulfinpyrazoneThe serum concentration of Estradiol can be increased when it is combined with Sulfinpyrazone.
SulfisoxazoleThe metabolism of Estradiol can be decreased when combined with Sulfisoxazole.
SulodexideThe therapeutic efficacy of Sulodexide can be decreased when used in combination with Estradiol.
SumatriptanThe serum concentration of Estradiol can be increased when it is combined with Sumatriptan.
SunitinibThe serum concentration of Estradiol can be increased when it is combined with Sunitinib.
TacrineThe serum concentration of Estradiol can be increased when it is combined with Tacrine.
TacrolimusThe serum concentration of Estradiol can be decreased when it is combined with Tacrolimus.
TamoxifenThe serum concentration of Estradiol can be decreased when it is combined with Tamoxifen.
Taurocholic AcidThe serum concentration of Estradiol can be increased when it is combined with Taurocholic Acid.
TelaprevirThe metabolism of Estradiol can be decreased when combined with Telaprevir.
TelithromycinThe metabolism of Estradiol can be decreased when combined with Telithromycin.
TelmisartanThe serum concentration of Estradiol can be increased when it is combined with Telmisartan.
TemsirolimusThe serum concentration of Estradiol can be increased when it is combined with Temsirolimus.
TenofovirThe metabolism of Estradiol can be decreased when combined with Tenofovir.
TerazosinThe serum concentration of Estradiol can be increased when it is combined with Terazosin.
TerfenadineThe serum concentration of Estradiol can be increased when it is combined with Terfenadine.
TeriflunomideThe serum concentration of Estradiol can be decreased when it is combined with Teriflunomide.
TesmilifeneThe serum concentration of Estradiol can be decreased when it is combined with Tesmilifene.
TestosteroneThe serum concentration of Estradiol can be increased when it is combined with Testosterone.
ThalidomideEstradiol may increase the thrombogenic activities of Thalidomide.
TheophyllineThe serum concentration of Theophylline can be increased when it is combined with Estradiol.
TheophyllineThe metabolism of Estradiol can be decreased when combined with Theophylline.
Thyroid, porcineThe therapeutic efficacy of Thyroid, porcine can be decreased when used in combination with Estradiol.
TicagrelorThe serum concentration of Estradiol can be increased when it is combined with Ticagrelor.
TiclopidineThe metabolism of Estradiol can be decreased when combined with Ticlopidine.
TipranavirEstradiol may increase the dermatologic adverse activities of Tipranavir.
TixocortolThe serum concentration of Tixocortol can be increased when it is combined with Estradiol.
TocilizumabThe serum concentration of Estradiol can be decreased when it is combined with Tocilizumab.
TolazamideThe therapeutic efficacy of Tolazamide can be decreased when used in combination with Estradiol.
TolbutamideThe therapeutic efficacy of Tolbutamide can be decreased when used in combination with Estradiol.
TolbutamideThe metabolism of Estradiol can be decreased when combined with Tolbutamide.
TolvaptanThe serum concentration of Estradiol can be increased when it is combined with Tolvaptan.
TopiramateThe metabolism of Estradiol can be decreased when combined with Topiramate.
TopotecanThe serum concentration of Topotecan can be increased when it is combined with Estradiol.
TranylcypromineThe metabolism of Estradiol can be decreased when combined with Tranylcypromine.
TrazodoneThe serum concentration of Estradiol can be decreased when it is combined with Trazodone.
TriamcinoloneThe serum concentration of Triamcinolone can be increased when it is combined with Estradiol.
TrifluoperazineThe serum concentration of Estradiol can be increased when it is combined with Trifluoperazine.
TriflupromazineThe serum concentration of Estradiol can be increased when it is combined with Triflupromazine.
TrimethoprimThe serum concentration of Estradiol can be decreased when it is combined with Trimethoprim.
TrimipramineThe serum concentration of Estradiol can be increased when it is combined with Trimipramine.
TroglitazoneThe therapeutic efficacy of Troglitazone can be decreased when used in combination with Estradiol.
TroleandomycinThe serum concentration of Estradiol can be increased when it is combined with Troleandomycin.
Ursodeoxycholic acidThe therapeutic efficacy of Ursodeoxycholic acid can be decreased when used in combination with Estradiol.
Valproic AcidThe metabolism of Estradiol can be decreased when combined with Valproic Acid.
ValsartanThe metabolism of Estradiol can be decreased when combined with Valsartan.
VemurafenibThe serum concentration of Estradiol can be increased when it is combined with Vemurafenib.
VenlafaxineThe metabolism of Estradiol can be decreased when combined with Venlafaxine.
VerapamilThe metabolism of Estradiol can be decreased when combined with Verapamil.
VildagliptinThe therapeutic efficacy of Vildagliptin can be decreased when used in combination with Estradiol.
VinblastineThe serum concentration of Estradiol can be decreased when it is combined with Vinblastine.
VincristineThe serum concentration of Estradiol can be decreased when it is combined with Vincristine.
VinorelbineThe serum concentration of Estradiol can be increased when it is combined with Vinorelbine.
Vitamin CThe serum concentration of Estradiol can be increased when it is combined with Vitamin C.
VogliboseThe therapeutic efficacy of Voglibose can be decreased when used in combination with Estradiol.
VoriconazoleThe metabolism of Estradiol can be decreased when combined with Voriconazole.
WarfarinEstradiol may decrease the anticoagulant activities of Warfarin.
XimelagatranEstradiol may decrease the anticoagulant activities of Ximelagatran.
ZafirlukastThe metabolism of Estradiol can be decreased when combined with Zafirlukast.
ZimelidineThe serum concentration of Estradiol can be increased when it is combined with Zimelidine.
ZiprasidoneThe metabolism of Estradiol can be decreased when combined with Ziprasidone.
Food Interactions
  • Take with food to decrease nausea.

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Ligand-dependent nuclear transactivation involves either direct homodimer binding to a palindromic estrogen response element (ERE) sequence or association with other DNA-binding transcription fact...
Gene Name:
ESR1
Uniprot ID:
P03372
Molecular Weight:
66215.45 Da
References
  1. Brama M, Gnessi L, Basciani S, Cerulli N, Politi L, Spera G, Mariani S, Cherubini S, Scotto d'Abusco A, Scandurra R, Migliaccio S: Cadmium induces mitogenic signaling in breast cancer cell by an ERalpha-dependent mechanism. Mol Cell Endocrinol. 2007 Jan 29;264(1-2):102-8. Epub 2006 Nov 27. [PubMed:17125913 ]
  2. Lehnes K, Winder AD, Alfonso C, Kasid N, Simoneaux M, Summe H, Morgan E, Iann MC, Duncan J, Eagan M, Tavaluc R, Evans CH Jr, Russell R, Wang A, Hu F, Stoica A: The effect of estradiol on in vivo tumorigenesis is modulated by the human epidermal growth factor receptor 2/phosphatidylinositol 3-kinase/Akt1 pathway. Endocrinology. 2007 Mar;148(3):1171-80. Epub 2006 Nov 30. [PubMed:17138652 ]
  3. Sasson S: Equilibrium binding analysis of estrogen agonists and antagonists: relation to the activation of the estrogen receptor. Pathol Biol (Paris). 1991 Jan;39(1):59-69. [PubMed:2011412 ]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Zinc ion binding
Specific Function:
Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent manner (PubMed:20074560). Isoform beta-cx lacks ligand binding ability and has no or only very low ere binding activity resulting in the loss of ligand-dependent transactivation ability. DNA-binding by...
Gene Name:
ESR2
Uniprot ID:
Q92731
Molecular Weight:
59215.765 Da
References
  1. Vijayanathan V, Greenfield NJ, Thomas TJ, Ivanova MM, Tyulmenkov VV, Klinge CM, Gallo MA, Thomas T: Effects of estradiol and 4-hydroxytamoxifen on the conformation, thermal stability, and DNA recognition of estrogen receptor beta. Biochem Cell Biol. 2007 Feb;85(1):1-10. [PubMed:17464340 ]
  2. Sasson S: Equilibrium binding analysis of estrogen agonists and antagonists: relation to the activation of the estrogen receptor. Pathol Biol (Paris). 1991 Jan;39(1):59-69. [PubMed:2011412 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Zinc ion binding
Specific Function:
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and is...
Gene Name:
NR1I2
Uniprot ID:
O75469
Molecular Weight:
49761.245 Da
References
  1. Xue Y, Moore LB, Orans J, Peng L, Bencharit S, Kliewer SA, Redinbo MR: Crystal structure of the pregnane X receptor-estradiol complex provides insights into endobiotic recognition. Mol Endocrinol. 2007 May;21(5):1028-38. Epub 2007 Feb 27. [PubMed:17327420 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Lee AJ, Cai MX, Thomas PE, Conney AH, Zhu BT: Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98. [PubMed:12865317 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N...
Gene Name:
CYP1A2
Uniprot ID:
P05177
Molecular Weight:
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Lee AJ, Cai MX, Thomas PE, Conney AH, Zhu BT: Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98. [PubMed:12865317 ]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A5
Uniprot ID:
P20815
Molecular Weight:
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP3A7
Uniprot ID:
P24462
Molecular Weight:
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid binding
Specific Function:
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the IX-alpha-C8 and IX-alpha-C12 monoconjugates and diconjugate. Is also able to catalyze the glucuronidation of 17beta-estradiol, 17alpha-ethinylestradiol, 1-hydroxypyrene, 4-methylumbelliferone, 1-naph...
Gene Name:
UGT1A1
Uniprot ID:
P22309
Molecular Weight:
59590.91 Da
References
  1. Hanioka N, Tanabe N, Jinno H, Tanaka-Kagawa T, Nagaoka K, Naito S, Koeda A, Narimatsu S: Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8. doi: 10.1016/j.lfs.2010.07.001. Epub 2010 Jul 8. [PubMed:20620155 ]
  2. Guillemette C, Belanger A, Lepine J: Metabolic inactivation of estrogens in breast tissue by UDP-glucuronosyltransferase enzymes: an overview. Breast Cancer Res. 2004;6(6):246-54. Epub 2004 Sep 27. [PubMed:15535854 ]
  3. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d 24-hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
Gene Name:
CYP1A1
Uniprot ID:
P04798
Molecular Weight:
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Oxygen binding
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, retinoid and xenobiotics. Preferentially oxidizes 17beta-estradiol to the carcinogenic 4-hydroxy derivative, and a variety of procarcinogenic compou...
Gene Name:
CYP1B1
Uniprot ID:
Q16678
Molecular Weight:
60845.33 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme...
Gene Name:
CYP2C8
Uniprot ID:
P10632
Molecular Weight:
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
  2. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]

Carriers

Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Androgen binding
Specific Function:
Functions as an androgen transport protein, but may also be involved in receptor mediated processes. Each dimer binds one molecule of steroid. Specific for 5-alpha-dihydrotestosterone, testosterone, and 17-beta-estradiol. Regulates the plasma metabolic clearance rate of steroid hormones by controlling their plasma concentration.
Gene Name:
SHBG
Uniprot ID:
P04278
Molecular Weight:
43778.755 Da
References
  1. Campusano M C, Brusco G F, Campino J C, Rodriguez P L, Arteaga U E: [Assessment of androgenic decline in the elderly]. Rev Med Chil. 2006 Sep;134(9):1123-8. Epub 2006 Dec 12. [PubMed:17171213 ]
  2. Kuba R, Pohanka M, Zakopcan J, Novotna I, Rektor I: Sexual dysfunctions and blood hormonal profile in men with focal epilepsy. Epilepsia. 2006 Dec;47(12):2135-40. [PubMed:17201714 ]
  3. Bendlova B, Zavadilova J, Vankova M, Vejrazkova D, Lukasova P, Vcelak J, Hill M, Cibula D, Vondra K, Starka L, Vrbikova J: Role of D327N sex hormone-binding globulin gene polymorphism in the pathogenesis of polycystic ovary syndrome. J Steroid Biochem Mol Biol. 2007 Apr;104(1-2):68-74. Epub 2007 Jan 26. [PubMed:17258903 ]
  4. Sablik Z, Samborska-Sablik A, Bolinska-Soltysiak H, Goch JH, Kula K: [Hyperandrogenism as a risk factor of coronary artery disease in young women]. Pol Arch Med Wewn. 2006 Feb;115(2):118-24. [PubMed:17274467 ]
  5. Mohamad MJ, Mohammad MA, Karayyem M, Hairi A, Hader AA: Serum levels of sex hormones in men with acute myocardial infarction. Neuro Endocrinol Lett. 2007 Apr;28(2):182-6. [PubMed:17435665 ]
  6. O'Connell MB: Pharmacokinetic and pharmacologic variation between different estrogen products. J Clin Pharmacol. 1995 Sep;35(9 Suppl):18S-24S. [PubMed:8530713 ]
  7. Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. [PubMed:3521955 ]
Kind
Protein
Organism
Human
Pharmacological action
no
General Function:
Toxic substance binding
Specific Function:
Serum albumin, the main protein of plasma, has a good binding capacity for water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs. Its main function is the regulation of the colloidal osmotic pressure of blood. Major zinc transporter in plasma, typically binds about 80% of all plasma zinc.
Gene Name:
ALB
Uniprot ID:
P02768
Molecular Weight:
69365.94 Da
References
  1. O'Connell MB: Pharmacokinetic and pharmacologic variation between different estrogen products. J Clin Pharmacol. 1995 Sep;35(9 Suppl):18S-24S. [PubMed:8530713 ]
Kind
Protein
Organism
Human
Pharmacological action
no
General Function:
Transporter activity
Specific Function:
FABP are thought to play a role in the intracellular transport of long-chain fatty acids and their acyl-CoA esters. FABP2 is probably involved in triglyceride-rich lipoprotein synthesis. Binds saturated long-chain fatty acids with a high affinity, but binds with a lower affinity to unsaturated long-chain fatty acids. FABP2 may also help maintain energy homeostasis by functioning as a lipid sensor.
Gene Name:
FABP2
Uniprot ID:
P12104
Molecular Weight:
15207.165 Da
References
  1. Rowland A, Knights KM, Mackenzie PI, Miners JO: Characterization of the binding of drugs to human intestinal fatty acid binding protein (IFABP): potential role of IFABP as an alternative to albumin for in vitro-in vivo extrapolation of drug kinetic parameters. Drug Metab Dispos. 2009 Jul;37(7):1395-403. doi: 10.1124/dmd.109.027656. Epub 2009 Apr 27. [PubMed:19398502 ]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Quaternary ammonium group transmembrane transporter activity
Specific Function:
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creatinine, amantadine, memantine, acriflavine, 4-[4-(dimethylamino)-styryl]-N-methylpyridinium ASP, amiloride, metformin, N-1-methylnicotinamide (NMN), tetraethylammonium (TEA), 1-methyl-4-phenylpyridiniu...
Gene Name:
SLC22A2
Uniprot ID:
O15244
Molecular Weight:
62579.99 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Secondary active organic cation transmembrane transporter activity
Specific Function:
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnicotinamide (NMN), 4-(4-(dimethylamino)styryl)-N-methylpyridinium (ASP), the endogenous compounds choline, guanidine, histamine, epinephrine, adrenaline, noradrenaline and dopamine, and the drugs quinine...
Gene Name:
SLC22A1
Uniprot ID:
O15245
Molecular Weight:
61153.345 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Toxin transporter activity
Specific Function:
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name:
SLC22A3
Uniprot ID:
O75751
Molecular Weight:
61279.485 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607 ]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name:
SLCO2B1
Uniprot ID:
O94956
Molecular Weight:
76709.98 Da
References
  1. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A: Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res. 2001 Sep;18(9):1262-9. [PubMed:11683238 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibited by the grapefruit juice component naringin.
Gene Name:
SLCO1A2
Uniprot ID:
P46721
Molecular Weight:
74144.105 Da
References
  1. Kanai N, Lu R, Bao Y, Wolkoff AW, Vore M, Schuster VL: Estradiol 17 beta-D-glucuronide is a high-affinity substrate for oatp organic anion transporter. Am J Physiol. 1996 Feb;270(2 Pt 2):F326-31. [PubMed:8779894 ]
  2. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [PubMed:8786566 ]
  3. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Atpase activity, coupled to transmembrane movement of substances
Specific Function:
ATP-dependent transporter probably involved in cellular detoxification through lipophilic anion extrusion.
Gene Name:
ABCC10
Uniprot ID:
Q5T3U5
Molecular Weight:
161627.375 Da
References
  1. Chen ZS, Hopper-Borge E, Belinsky MG, Shchaveleva I, Kotova E, Kruh GD: Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10). Mol Pharmacol. 2003 Feb;63(2):351-8. [PubMed:12527806 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name:
SLC22A11
Uniprot ID:
Q9NSA0
Molecular Weight:
59970.945 Da
References
  1. Cha SH, Sekine T, Kusuhara H, Yu E, Kim JY, Kim DK, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. J Biol Chem. 2000 Feb 11;275(6):4507-12. [PubMed:10660625 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both from mitochondria to cytosol and from cytosol to extracellular space, and cellular export of hemin, and heme. Xenobiotic transporter that may play an important role in the exclusion of xenobiotics from t...
Gene Name:
ABCG2
Uniprot ID:
Q9UNQ0
Molecular Weight:
72313.47 Da
References
  1. Imai Y, Asada S, Tsukahara S, Ishikawa E, Tsuruo T, Sugimoto Y: Breast cancer resistance protein exports sulfated estrogens but not free estrogens. Mol Pharmacol. 2003 Sep;64(3):610-8. [PubMed:12920197 ]
  2. Imai Y, Tsukahara S, Ishikawa E, Tsuruo T, Sugimoto Y: Estrone and 17beta-estradiol reverse breast cancer resistance protein-mediated multidrug resistance. Jpn J Cancer Res. 2002 Mar;93(3):231-5. [PubMed:11927002 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
inhibitor
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostaglandin E2, thromboxane B2, leukotriene C3, leukotriene E4, thyroxine and triiodothyronine. Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B1
Uniprot ID:
Q9Y6L6
Molecular Weight:
76447.99 Da
References
  1. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A: Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res. 2001 Sep;18(9):1262-9. [PubMed:11683238 ]
  2. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Xenobiotic-transporting atpase activity
Specific Function:
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name:
ABCB1
Uniprot ID:
P08183
Molecular Weight:
141477.255 Da
References
  1. Rao US, Fine RL, Scarborough GA: Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. [PubMed:7914405 ]
  2. Kim WY, Benet LZ: P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm Res. 2004 Jul;21(7):1284-93. [PubMed:15290871 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenadine. Transports benzylpenicillin (PCG), estrone-3-sulfate (E1S), cimetidine (CMD), 2,4-dichloro-phenoxyacetate (2,4-D), p-amino-hippurate (PAH), acyclovir (ACV) and ochratoxin (OTA).
Gene Name:
SLC22A8
Uniprot ID:
Q8TCC7
Molecular Weight:
59855.585 Da
References
  1. Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. [PubMed:11306713 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Sodium-independent organic anion transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotrexate and sulfobromophthalein (BSP). Involved in the clearance of bile acids and organic anions from the liver.
Gene Name:
SLCO1B3
Uniprot ID:
Q9NPD5
Molecular Weight:
77402.175 Da
References
  1. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Thyroid hormone transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent high affinity transport of organic anions such as the thyroid hormones thyroxine (T4) and rT3. Other potential substrates, such as triiodothyronine (T3), 17-beta-glucuronosyl estradiol, estrone-3-sulfate and sulfobromophthalein (BSP) are transported with much lower efficiency. May play a signifiant role in regulating T4 flux into and out of the brain (By similarity).
Gene Name:
SLCO1C1
Uniprot ID:
Q9NYB5
Molecular Weight:
78695.625 Da
References
  1. Pizzagalli F, Hagenbuch B, Stieger B, Klenk U, Folkers G, Meier PJ: Identification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter. Mol Endocrinol. 2002 Oct;16(10):2283-96. [PubMed:12351693 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
General Function:
Thyroid hormone transmembrane transporter activity
Specific Function:
Mediates the Na(+)-independent transport of organic anions such as the thyroid hormones T3 (triiodo-L-thyronine), T4 (thyroxine) and rT3, and of estrone-3-sulfate and taurocholate.
Gene Name:
SLCO4A1
Uniprot ID:
Q96BD0
Molecular Weight:
77192.505 Da
References
  1. Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595 ]
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Drug created on June 13, 2005 07:24 / Updated on September 29, 2016 02:27