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Identification
NameEstradiol
Accession NumberDB00783  (APRD00311)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Generally 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
SynonymLanguageCode
(17beta)-Estra-1,3,5(10)-triene-3,17-diolNot AvailableNot Available
17beta OestradiolNot AvailableNot Available
17beta-Estra-1,3,5(10)-triene-3,17-diolNot AvailableNot Available
17beta-OestradiolNot AvailableNot Available
BenzhormovarineNot AvailableIS
beta-EstradiolNot AvailableNot Available
cis-EstradiolNot AvailableNot Available
Dihydrofollicular hormoneNot AvailableIS
DihydrofolliculinNot AvailableIS
DihydrotheelinNot AvailableIS
DihydroxyestrinNot AvailableIS
EstradiolGermanINN
EstradiolFrenchINN
EstradiolSpanishINN
Estradiol-17betaNot AvailableNot Available
EstradiolumLatinINN
FemestralNot AvailableIS
Lio-OidNot AvailableIS
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Estringring2 mgvaginalPharmacia and Upjohn Company1996-04-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle-dotpatch, extended release.0375 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle-dotpatch, extended release.05 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle-dotpatch, extended release.075 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle-dotpatch, extended release.1 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle-dotpatch, extended release.025 mg/dtransdermalNovartis Pharmaceuticals Corporation1999-01-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vagifemtablet, film coated10 ugvaginalNovo Nordisk2010-01-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Divigelgel.25 mg/gtopicalUpsher Smith Laboratories, Inc.2011-02-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Divigelgel.5 mg/gtopicalUpsher Smith Laboratories, Inc.2011-02-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Divigelgel1 mg/gtopicalUpsher Smith Laboratories, Inc.2011-02-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Femringring.05 mg/dvaginalWarner Chilcott (US), LLC2003-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Femringring.1 mg/dvaginalWarner Chilcott (US), LLC2003-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch, extended release.025 mg/dtransdermalSandoz Inc2014-12-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch, extended release.0375 mg/dtransdermalSandoz Inc2014-12-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch, extended release.05 mg/dtransdermalSandoz Inc2014-12-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch, extended release.075 mg/dtransdermalSandoz Inc2014-12-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch, extended release.1 mg/dtransdermalSandoz Inc2014-12-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estrogelgel, metered.75 mg/1.25gtransdermalASCEND Therapeutics US, LLC2004-02-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estrogelgel, metered.75 mg/1.25gtransdermalASCEND Therapeutics US, LLC2004-02-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Elestringel.6 mg/gtransdermalJazz Pharmaceuticals Commercial Corp.2007-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Elestringel.6 mg/gtransdermalJazz Pharmaceuticals Commercial Corp.2007-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Valerateinjection10 mg/mLintramuscularJHP Pharmaceuticals, LLC2012-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Valerateinjection20 mg/mLintramuscularJHP Pharmaceuticals, LLC2012-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Valerateinjection40 mg/mLintramuscularJHP Pharmaceuticals, LLC2012-06-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Transdermal Systempatch.025 mg/dtransdermalAlvogen, Inc.2011-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Transdermal Systempatch.0375 mg/dtransdermalAlvogen, Inc.2011-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Transdermal Systempatch.05 mg/dtransdermalAlvogen, Inc.2011-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Transdermal Systempatch.06 mg/dtransdermalAlvogen, Inc.2011-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Transdermal Systempatch.075 mg/dtransdermalAlvogen, Inc.2011-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Transdermal Systempatch.1 mg/dtransdermalAlvogen, Inc.2011-12-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Climarapatch.05 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.1994-12-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Climarapatch.1 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.1994-12-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Climarapatch.075 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.1998-03-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Climarapatch.025 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.1999-03-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Menostarpatch14 ug/dtransdermalBayer Health Care Pharmaceuticals Inc.2004-06-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Climarapatch.0375 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.2003-05-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Climarapatch.06 mg/dtransdermalBayer Health Care Pharmaceuticals Inc.2008-01-03Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Alorapatch.05 mg/dtransdermalActavis Pharma, Inc.1996-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Alorapatch.075 mg/dtransdermalActavis Pharma, Inc.1996-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Alorapatch.1 mg/dtransdermalActavis Pharma, Inc.1996-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Alorapatch.025 mg/dtransdermalActavis Pharma, Inc.2002-04-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle Dotpatch, extended release.05 mg/dtransdermalPhysicians Total Care, Inc.2003-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle Dotpatch, extended release.075 mg/dtransdermalPhysicians Total Care, Inc.2003-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle Dotpatch, extended release.1 mg/dtransdermalPhysicians Total Care, Inc.2003-06-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vivelle Dotpatch, extended release.0375 mg/dtransdermalPhysicians Total Care, Inc.2003-09-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estringring2 mgvaginalPhysicians Total Care, Inc.2006-02-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Femringring.1 mg/24[USP'U]vaginalPhysicians Total Care, Inc.2009-05-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Divigelgel1 mg/gtopicalPhysicians Total Care, Inc.2009-08-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Evamistspray, metered1.53 mgtransdermalPhysicians Total Care, Inc.2010-08-23Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Vagifemtablet, film coated10 ugvaginalPhysicians Total Care, Inc.2010-09-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estringring2 mgvaginalU.S. Pharmaceuticals1996-04-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Evamistspray, metered1.53 mgtransdermalTher Rx Corporation2009-07-08Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Divigelgel.25 mg/gtopicalVertical Pharmaceuticals, LLC2014-10-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Divigelgel.5 mg/gtopicalVertical Pharmaceuticals, LLC2014-10-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Divigelgel1 mg/gtopicalVertical Pharmaceuticals, LLC2014-10-27Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Minivellefilm, extended release.1 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Minivellefilm, extended release.025 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Minivellefilm, extended release.0375 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Minivellefilm, extended release.05 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Minivellefilm, extended release.075 mg/dtransdermalNOVEN THERAPEUTICS, LLC2012-12-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Depo-estradiolinjection5 mg/mLintramuscularPharmacia and Upjohn Company1979-08-15Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralKAISER FOUNDATION HOSPITALS2010-10-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralKAISER FOUNDATION HOSPITALS2010-10-20Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralKAISER FOUNDATION HOSPITALS2012-09-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralMylan Pharmaceuticals Inc.1999-06-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralMylan Pharmaceuticals Inc.1999-06-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralMylan Pharmaceuticals Inc.1999-06-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.025 mg/dtransdermalMylan Pharmaceuticals Inc.2005-03-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.05 mg/dtransdermalMylan Pharmaceuticals Inc.2000-02-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.075 mg/dtransdermalMylan Pharmaceuticals Inc.2005-03-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.1 mg/dtransdermalMylan Pharmaceuticals Inc.2000-02-24Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.0375 mg/dtransdermalMylan Pharmaceuticals Inc.2006-08-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.06 mg/dtransdermalMylan Pharmaceuticals Inc.2006-08-10Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.1 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.075 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.05 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.0375 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.025 mg/dtransdermalMylan Pharmaceuticals Inc.2014-12-19Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estracetablet.5 mgoralWarner Chilcott (US), LLC2011-12-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estracetablet1 mgoralWarner Chilcott (US), LLC2011-12-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estracetablet2 mgoralWarner Chilcott (US), LLC2011-12-26Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estracecream.1 mg/gvaginalWarner Chilcott (US), LLC2001-07-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralBarr Laboratories Inc.1997-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralBarr Laboratories Inc.1997-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralBarr Laboratories Inc.1997-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Valerateinjection, solution20 mg/mLintramuscularPerrigo Company2010-03-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiol Valerateinjection, solution40 mg/mLintramuscularPerrigo Company2010-03-31Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralWatson Laboratories, Inc.1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralWatson Laboratories, Inc.1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralWatson Laboratories, Inc.1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralStat Rx USA1997-10-22Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralSTAT Rx USA LLC1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralRebel Distributors Corp1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralRebel Distributors Corp1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralHeritage Pharmaceuticals Inc2010-11-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralHeritage Pharmaceuticals Inc2010-11-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralHeritage Pharmaceuticals Inc2010-11-05Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralAidarex Pharmaceuticals LLC1997-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralAidarex Pharmaceuticals LLC1997-10-28Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralPd Rx Pharmaceuticals, Inc.1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralPd Rx Pharmaceuticals, Inc.1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralLake Erie Medical & Surgical Supply DBA Quality Care Products LLC2012-03-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralAv Pak2014-02-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralAv Pak2014-02-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralAv Pak2014-02-12Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Depo-estradiolinjection5 mg/mLintramuscularPhysicians Total Care, Inc.1998-10-16Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralPhysicians Total Care, Inc.2000-09-18Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralPhysicians Total Care, Inc.2003-05-07Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralPhysicians Total Care, Inc.2003-06-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch.97 mg/48[USP'U]transdermalPhysicians Total Care, Inc.2003-06-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch1.46 mg/48[USP'U]transdermalPhysicians Total Care, Inc.2003-06-09Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradiolpatch1.94 mg/48[USP'U]transdermalPhysicians Total Care, Inc.2008-12-11Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralCardinal Health2009-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralPd Rx Pharmaceuticals, Inc.2009-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralPd Rx Pharmaceuticals, Inc.2009-12-17Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralbryant ranch prepack1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralbryant ranch prepack1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralbryant ranch prepack1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet.5 mgoralbryant ranch prepack1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralReady Meds1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet2 mgoralReady Meds1996-03-14Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralPreferred Pharmaceuticals, Inc.2014-12-04Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Estradioltablet1 mgoralPreferred Pharmaceuticals, Inc.2012-02-13Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Over the Counter ProductsNot Available
International Brands
NameCompany
Estraderm MXNovartis
Estraderm TTSNovartis
EstrasorbMedicis
EstrofemNovo Nordisk
FemtraceWarner Chilcott
InnofemNovo Nordisk
VivelleNovartis
Brand mixtures
Brand NameIngredients
ActivellaEstradiol + norethindrone acetate
AngeliQEstradiol + drospirenone
Climacteron InjectionEstradiol Benzoate + Estradiol Dienanthate + Testosterone Enanthate Benzilic Acid Hydrazone
ClimagestEstradiol and Norethisterone
ClimenEstradiol and Cyproterone
CombiPatchNorethindrone + Estradiol
Cyclo-Progynovaestradiol valerate + norgestrel
Gynodian Depot Estradiol and Prasterone
Linoladiol H NEstradiol and Prednisolone
MimveyNorethindrone + Estradiol
TrivinaEstradiol and Medroxyprogesterone
Wellnara Estradiol and Levonorgestrel
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 valerate
Thumb
  • InChI Key: RSEPBGGWRJCQGY-RBRWEJTLSA-N
  • Monoisotopic Mass: 356.23514489
  • Average Mass: 356.4984
DBSALT000068
Categories
CAS number50-28-2
WeightAverage: 272.382
Monoisotopic: 272.177630012
Chemical FormulaC18H24O2
InChI KeyVOXZDWNPVJITMN-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[C@H](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.
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
Androgen and Estrogen MetabolismMetabolicSMP00068
Aromatase deficiencyDiseaseSMP00565
17-Beta Hydroxysteroid Dehydrogenase III DeficiencyDiseaseSMP00356
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 substrateNon-inhibitor0.939
CYP450 2D6 substrateNon-inhibitor0.9574
CYP450 2C19 substrateNon-inhibitor0.9025
CYP450 3A4 substrateNon-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
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
Creamvaginal.1 mg/g
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
Geltopical.25 mg/g
Geltopical.5 mg/g
Geltopical1 mg/g
Geltransdermal.6 mg/g
Gel, meteredtransdermal.75 mg/1.25g
Injectionintramuscular10 mg/mL
Injectionintramuscular20 mg/mL
Injectionintramuscular40 mg/mL
Injectionintramuscular5 mg/mL
Injection, solutionintramuscular20 mg/mL
Injection, solutionintramuscular40 mg/mL
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]
Patchtransdermal14 ug/d
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
Ringvaginal.05 mg/d
Ringvaginal.1 mg/24[USP'U]
Ringvaginal.1 mg/d
Ringvaginal2 mg
Spray, meteredtransdermal1.53 mg
Tabletoral.5 mg
Tabletoral1 mg
Tabletoral2 mg
Tablet, film coatedvaginal10 ug
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
CountryPatent NumberApprovedExpires (estimated)
Canada13386601996-10-222013-10-22
Canada23068812008-09-022018-11-19
United States52232611993-06-292010-06-29
United States75727792004-03-022024-03-02
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)
SpectraGC-MSMS/MSMS1D NMR2D NMR
References
Synthesis Reference

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

US5248676
General Reference
  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
  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
  3. Raman JD, Schlegel PN: Aromatase inhibitors for male infertility. J Urol. 2002 Feb;167(2 Pt 1):624-9. Pubmed
  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
  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
  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
  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
  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
External Links
ATC CodesG03CA03
AHFS Codes
  • 68:16.04
PDB EntriesNot Available
FDA labelDownload (89.1 KB)
MSDSDownload (73.8 KB)
Interactions
Drug Interactions
Drug
AmobarbitalThe enzyme inducer, amobarbital, decreases the effect of the hormone agent, estradiol.
AprobarbitalThe enzyme inducer, aprobarbital, decreases the effect of the hormone agent, estradiol.
ButabarbitalThe enzyme inducer, butabarbital, decreases the effect of the hormone agent, estradiol.
ButalbitalThe enzyme inducer, butalbital, decreases the effect of the hormone agent, estradiol.
ButethalThe enzyme inducer, butethal, decreases the effect of the hormone agent, estradiol.
EthotoinThe enzyme inducer, ethotoin, decreases the effect of the hormone agent, estradiol.
FosphenytoinThe enzyme inducer, fosphenytoin, decreases the effect of the hormone agent, estradiol.
GriseofulvinThe enzyme inducer, griseofulvin, decreases the effect of the hormone agent, estradiol.
HeptabarbitalThe enzyme inducer, heptabarbital, decreases the effect of the hormone agent, estradiol.
HexobarbitalThe enzyme inducer, hexobarbital, decreases the effect of the hormone agent, estradiol.
MephenytoinThe enzyme inducer, mephenytoin, decreases the effect of the hormone agent, estradiol.
MethohexitalThe enzyme inducer, methohexital, decreases the effect of the hormone agent, estradiol.
MethylphenobarbitalThe enzyme inducer, methylphenobarbital, decreases the effect of the hormone agent, estradiol.
PentobarbitalThe enzyme inducer, pentobarbital, decreases the effect of the hormone agent, estradiol.
PhenobarbitalThe enzyme inducer, phenobarbital, decreases the effect of the hormone agent, estradiol.
PhenytoinThe enzyme inducer, phenytoin, decreases the effect of the hormone agent, estradiol.
PrednisoloneThe estrogenic agent, estradiol, may increase the effect of the corticosteroid, prednisolone.
PrednisoneThe estrogenic agent, estradiol, may increase the effect of corticosteroid, prednisone.
PrimidoneThe enzyme inducer, primidone, decreases the effect of the hormone agent, estradiol.
RaloxifeneAssociation not recommended
SecobarbitalThe enzyme inducer, secobarbital, decreases the effect of the hormone agent, estradiol.
TalbutalThe enzyme inducer, talbutal, decreases the effect of the hormone agent, estradiol.
TipranavirEstradiol may increase the adverse dermatological effects (i.e. skin rash) of Tipranavir. Tipranavir may decrease the serum concentration Estradiol. Use an alternate form of contraception or monitor for estrogen deficiency if Estradiol is used for hormone replacement therapy.
Ursodeoxycholic acidEstrogens decreases the effect of ursodiol
Food Interactions
  • Take with food to decrease nausea.

Targets

1. Estrogen receptor

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Estrogen receptor P03372 Details

References:

  1. Brama M, Gnessi L, Basciani S, Cerulli N, Politi L, Spera G, Mariani S, Cherubini S, d’Abusco AS, 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
  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
  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
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

2. Estrogen receptor beta

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: agonist

Components

Name UniProt ID Details
Estrogen receptor beta Q92731 Details

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
  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

3. Nuclear receptor subfamily 1 group I member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Nuclear receptor subfamily 1 group I member 2 O75469 Details

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

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. 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. Epub 2009 Nov 24. Pubmed
  3. 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

2. Cytochrome P450 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A2 P05177 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.
  2. 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. Epub 2009 Nov 24. Pubmed
  3. 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

3. Cytochrome P450 3A5

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A5 P20815 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

4. Cytochrome P450 3A7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A7 P24462 Details

References:

  1. Flockhart DA. Drug Interactions: Cytochrome P450 Drug Interaction Table. Indiana University School of Medicine (2007). Accessed May 28, 2010.

5. UDP-glucuronosyltransferase 1-1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
UDP-glucuronosyltransferase 1-1 P22309 Details

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. Epub 2010 Jul 8. Pubmed
  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
  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
  4. 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
  5. 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
  6. 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
  7. 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
  8. 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
  9. 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
  10. 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
  11. 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
  12. 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
  13. 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
  14. 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
  15. 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
  16. 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

6. Cytochrome P450 1A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1A1 P04798 Details

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. Epub 2009 Nov 24. Pubmed

7. Cytochrome P450 1B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 1B1 Q16678 Details

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. Epub 2009 Nov 24. Pubmed

8. Cytochrome P450 2C19

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C19 P33261 Details

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. Epub 2009 Nov 24. Pubmed

9. Cytochrome P450 2C8

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C8 P10632 Details

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. Epub 2009 Nov 24. Pubmed
  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
  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

10. Cytochrome P450 2C9

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 2C9 P11712 Details

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. Epub 2009 Nov 24. Pubmed

Carriers

1. Sex hormone-binding globulin

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Sex hormone-binding globulin P04278 Details

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
  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
  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
  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
  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
  6. O’Connell MB: Pharmacokinetic and pharmacologic variation between different estrogen products. J Clin Pharmacol. 1995 Sep;35(9 Suppl):18S-24S. Pubmed
  7. Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. Pubmed

2. Serum albumin

Kind: protein

Organism: Human

Pharmacological action: no

Components

Name UniProt ID Details
Serum albumin P02768 Details

References:

  1. O’Connell MB: Pharmacokinetic and pharmacologic variation between different estrogen products. J Clin Pharmacol. 1995 Sep;35(9 Suppl):18S-24S. Pubmed

3. Fatty acid-binding protein, intestinal

Kind: protein

Organism: Human

Pharmacological action: no

Components

Name UniProt ID Details
Fatty acid-binding protein, intestinal P12104 Details

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. Epub 2009 Apr 27. Pubmed

Transporters

1. Solute carrier family 22 member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 2 O15244 Details

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
  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

2. Solute carrier family 22 member 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 1 O15245 Details

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
  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

3. Solute carrier family 22 member 3

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 3 O75751 Details

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
  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

4. Solute carrier organic anion transporter family member 2B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 2B1 O94956 Details

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

5. Solute carrier organic anion transporter family member 1A2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1A2 P46721 Details

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
  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
  3. Kullak-Ublick, G.A. et al. Organic anion-transporting polypeptide B (OATP- B) and its functional comparison with three other OATPs of human liver. Gastroenterology 120, 525-533 (2001).Pubmed

6. Multidrug resistance-associated protein 7

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Multidrug resistance-associated protein 7 Q5T3U5 Details

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

7. Solute carrier family 22 member 11

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier family 22 member 11 Q9NSA0 Details

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

8. ATP-binding cassette sub-family G member 2

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
ATP-binding cassette sub-family G member 2 Q9UNQ0 Details

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
  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

9. Solute carrier organic anion transporter family member 1B1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: inhibitor

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1B1 Q9Y6L6 Details

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
  2. Kullak-Ublick, G.A. et al. Organic anion-transporting polypeptide B (OATP- B) and its functional comparison with three other OATPs of human liver. Gastroenterology 120, 525-533 (2001).Pubmed

10. Multidrug resistance protein 1

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Multidrug resistance protein 1 P08183 Details

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
  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

11. Solute carrier family 22 member 8

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier family 22 member 8 Q8TCC7 Details

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

12. Solute carrier organic anion transporter family member 1B3

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1B3 Q9NPD5 Details

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

13. Solute carrier organic anion transporter family member 1C1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 1C1 Q9NYB5 Details

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

14. Solute carrier organic anion transporter family member 4A1

Kind: protein

Organism: Human

Pharmacological action: unknown

Components

Name UniProt ID Details
Solute carrier organic anion transporter family member 4A1 Q96BD0 Details

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

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Drug created on June 13, 2005 07:24 / Updated on September 16, 2013 17:12