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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
Salts
Name/CAS Structure Properties
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
Brand names
NameCompany
AloraWatson
ClimaraBayer
Depo-EstradiolNot Available
DivigelOrion
ElestrinJazz Pharmaceuticals
EstraceBristol-Myers Squibb
Estraderm MXNovartis
Estraderm TTSNovartis
EstrasorbMedicis
EstringPfizer
EstrofemNovo Nordisk
EstrogelSchering-Plough
EvaMistKV Pharmaceutical
FemringWarner Chilcott
FemtraceWarner Chilcott
InnofemNovo Nordisk
MenostarBayer
MinivelleNot Available
VagifemNot Available
VivelleNovartis
Vivelle-DotNovartis
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
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[8.7.0.0^{2,7}.0^{11,15}]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
Mass Specshow(9.34 KB)
Taxonomy
KingdomOrganic Compounds
SuperclassLipids
ClassSteroids and Steroid Derivatives
SubclassHydroxysteroids
Direct parentHydroxysteroids
Alternative parentsPhenanthrenes and Derivatives; Tetralins; Phenols and Derivatives; Cyclic Alcohols and Derivatives; Secondary Alcohols; Enols; Polyamines
Substituentsphenanthrene; tetralin; phenol derivative; benzene; cyclic alcohol; secondary alcohol; polyamine; enol; alcohol
Classification descriptionThis compound belongs to the hydroxysteroids. These are compounds containing an steroid backbone, with at least one hydrogen substituted by an hydroxyl group.
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
17-Beta Hydroxysteroid Dehydrogenase III DeficiencyDiseaseSMP00356
Androgen and Estrogen MetabolismMetabolicSMP00068
Aromatase deficiencyDiseaseSMP00565
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
ADMET
Predicted ADMET features
Property Value Probability
Human Intestinal Absorption + 1.0
Blood Brain Barrier + 0.8917
Caco-2 permeable + 0.8867
P-glycoprotein substrate Substrate 0.7058
P-glycoprotein inhibitor I Non-inhibitor 0.9147
P-glycoprotein inhibitor II Non-inhibitor 0.9403
Renal organic cation transporter Non-inhibitor 0.8008
CYP450 2C9 substrate Non-substrate 0.727
CYP450 2D6 substrate Non-substrate 0.801
CYP450 3A4 substrate Substrate 0.7132
CYP450 1A2 substrate Inhibitor 0.9106
CYP450 2C9 substrate Non-inhibitor 0.939
CYP450 2D6 substrate Non-inhibitor 0.9574
CYP450 2C19 substrate Non-inhibitor 0.9025
CYP450 3A4 substrate Non-inhibitor 0.8309
CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.7887
Ames test Non AMES toxic 0.9198
Carcinogenicity Non-carcinogens 0.8829
Biodegradation Not ready biodegradable 0.9746
Rat acute toxicity 2.2272 LD50, mol/kg Not applicable
hERG inhibition (predictor I) Weak inhibitor 0.8647
hERG inhibition (predictor II) Inhibitor 0.6624
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
DiscTransdermal
GelTransdermal
LiquidIntramuscular
PatchTransdermal
RingIntravaginal
TabletIntravaginal
TabletOral
Prices
Unit descriptionCostUnit
Femring 0.1 mg/24hr Ring218.6USDring
Estring 2 mg Ring Box210.39USDbox
Femring 0.10 mg vaginal ring210.19USDring
Femring 0.05 mg/24hr Ring205.15USDring
Estring 2 mg vaginal ring202.3USDring
Femring 0.05 mg vaginal ring197.26USDring
Elestrin 0.52 mg/0.87 gm(0.06%) Gel 144 gm Bottle162.06USDbottle
Ethinyl estradiol powder140.0USDg
Vagifem 18 25 mcg tablet Box139.78USDbox
Estrace 0.1 mg/gm Cream 42.5 gm Tube133.27USDtube
Estradiol cypionate powder88.74USDg
Delestrogen 10 mg/ml Oil 5ml Vial88.04USDvial
Evamist 1.53 mg/spray Solution 8.1ml Bottle87.18USDbottle
Divigel 1 mg/gm Gel Box Of 30 gm85.53USDbox
Estrogel 0.75 mg/1.25 gm(0.06%) Gel 50 gm Bottle84.24USDbottle
Divigel 30 0.25 mg/0.25 gm Gel 30 Patches/box81.24USDbox
Climara 4 0.025 mg/24hr Patches Box75.58USDbox
Climara 4 0.05 mg/24hr Patches Box75.58USDbox
Climara 4 0.1 mg/24hr Patches Box75.58USDbox
Menostar 4 14 mcg/24hr Patches Box73.18USDbox
Divigel 0.5 mg/0.5 gm Gel Box72.99USDbox
Estraderm 8 0.1 mg/24hr Patches Box72.47USDbox
Vivelle-Dot 8 0.1 mg/24hr Patches Box72.46USDbox
Vivelle-Dot 8 0.025 mg/24hr Patches Box70.69USDbox
Climara 4 0.075 mg/24hr Patches Box69.04USDbox
Climara Pro 4 0.045-0.015 mg/day Patches Box69.04USDbox
Vivelle-Dot 8 0.0375 mg/24hr Patches Box68.84USDbox
Vivelle-Dot 8 0.075 mg/24hr Patches Box66.89USDbox
CombiPatch 8 0.05-0.25 mg/day Patches Box66.45USDbox
Estraderm 8 0.05 mg/24hr Patches Box66.35USDbox
Vivelle-Dot 8 0.05 mg/24hr Patches Box65.99USDbox
Estring 2 mg Slow-Release Ring65.39USDring
Alora 8 0.1 mg/24hr Patches Box62.99USDbox
Alora 8 0.05 mg/24hr Patches Box60.99USDbox
Alora 8 0.075 mg/24hr Patches Box58.27USDbox
Vagifem 8 25 mcg tablet Box58.23USDbox
Vagifem 8 10 mcg tablet Box54.99USDbox
Vivelle 8 0.05 mg/24hr Patches Box49.99USDbox
Estradiol benzoate powder42.0USDg
Estradiol 4 0.025 mg/24hr Patches Box40.92USDbox
Estradiol 4 0.05 mg/24hr Patches Box40.92USDbox
Estradiol 4 0.075 mg/24hr Patches Box40.92USDbox
Estradiol 4 0.1 mg/24hr Patches Box40.92USDbox
Estradiol 4 0.06 mg/24hr Patches Box39.99USDbox
Delestrogen 40 mg/ml Oil39.52USDml
Estradiol 4 0.0375 mg/24hr Patches Box39.35USDbox
Delestrogen 40 mg/ml vial38.0USDml
Estradiol valerate 40 mg/ml vial35.62USDml
Estradiol valerate powder32.13USDg
Delestrogen 20 mg/ml Oil23.82USDml
Delestrogen 20 mg/ml vial22.91USDml
Estradiol valerate 20 mg/ml vial21.25USDml
Estradiol 0.1 mg/day patch20.55USDpatch
Estradiol powder17.86USDg
Climara 0.0375 mg/24hr Patches17.26USDpatch
Climara 0.06 mg/24hr Patches17.26USDpatch
Estradiol 0.05 mg/day patch16.91USDpatch
Delestrogen 10 mg/ml vial16.25USDml
Climara 0.025 mg/day patch15.77USDpatch
Climara 0.0375 mg/day patch15.77USDpatch
Climara 0.05 mg/day patch15.77USDpatch
Climara 0.06/mg day patch15.77USDpatch
Climara 0.075 mg/day patch15.77USDpatch
Climara 0.1 mg/day patch15.77USDpatch
Climara pro patch15.77USDpatch
Estradiol valerate 10 mg/ml vial15.24USDml
Evamist 1.53 mg/spray10.43USDml
Estradiol tds 0.025 mg/day9.84USDeach
Estradiol tds 0.0375 mg/day9.84USDeach
Estradiol tds 0.06 mg/day9.84USDeach
Estradiol tds 0.075 mg/day9.84USDeach
Depo-Estradiol 5 mg/ml Oil9.66USDml
Estraderm 0.1 mg patch8.66USDpatch
CombiPatch 0.05-0.14 mg/day Patches8.65USDpatch
Vivelle-dot 0.075 mg patch8.49USDpatch
Estraderm 0.05 mg patch8.07USDpatch
Combipatch 0.05-0.14 mg ptch7.92USDpatch
Combipatch 0.05-0.25 mg ptch7.91USDpatch
Depo-estradiol 5 mg/ml vial7.89USDml
Vivelle-dot 0.1 mg patch7.89USDpatch
Vivelle-dot 0.05 mg patch7.61USDpatch
Vivelle-dot 0.0375 mg patch7.54USDpatch
Vivelle-dot 0.025 mg patch7.53USDpatch
Alora 0.1 mg patch7.16USDpatch
Alora 0.075 mg patch7.0USDpatch
Alora 0.05 mg patch6.86USDpatch
Vagifem 10 mcg vaginal tab6.78USDeach
Vagifem 25 mcg vaginal tab6.78USDeach
Climara 100 (7.8 Mg/Pth) 100 mcg/day Patch6.67USDpatch
Climara 75 (5.7 Mg/Pth) 75 mcg/day Patch6.31USDpatch
Alora 0.025 mg patch6.26USDpatch
Vivelle 0.1 mg patch5.94USDpatch
Climara 50 (3.9 Mg/Pth) 50 mcg/day Patch5.91USDpatch
Vivelle 0.05 mg patch5.74USDpatch
Climara 25 (2 Mg/Pth) 25 mcg/day Patch5.54USDpatch
Estraderm-100 (8.0 Mg/Pth) 100 mcg/day Patch4.52USDpatch
Estraderm-25 (2 Mg/Pth) 25 mcg/day Patch3.74USDpatch
Estradot 100 (1.56 Mg/Pth) 100 mcg/day Patch3.49USDpatch
Estradot 75 (1.17 Mg/Pth) 75 mcg/day Patch3.3USDpatch
Vagifem 25 mcg Tablet3.21USDtablet
Estradot 50 (0.78 Mg/Pth) 50 mcg/day Patch3.07USDpatch
Oesclim 50 (10 Mg/Pth) 50 mcg/day Patch3.06USDpatch
Estrace 0.01% cream3.05USDg
Estrace 2 mg tablet2.98USDtablet
Estradot 37.5 (0.585 Mg/Pth) 37.5 mcg/day Patch2.88USDpatch
Estradot 25 (0.39 Mg/Pth) 25 mcg/day Patch2.86USDpatch
Estrasorb 4.35 mg/1.74 gm Emulsion 1.74 gm Packet2.83USDpacket
Oesclim 25 (5 Mg/Pth) 25 mcg/day Patch2.83USDpatch
Divigel 0.25 mg gel packet2.74USDeach
Divigel 0.5 mg gel packet2.74USDeach
Divigel 1 mg gel packet2.74USDg
Sandoz Estradiol Derm 100 (8 Mg/Pth) 100 mcg/day Patch2.64USDpatch
Menest 2.5 mg tablet2.6USDtablet
Femtrace 1.8 mg tablet2.59USDtablet
Sandoz Estradiol Derm 75 (6 Mg/Pth) 75 mcg/day Patch2.5USDpatch
Sandoz Estradiol Derm 50 (4 Mg/Pth) 50 mcg/day Patch2.34USDpatch
Estrace 0.5 mg tablet2.29USDtablet
Femtrace 0.45 mg tablet2.02USDtablet
Femtrace 0.9 mg tablet2.02USDtablet
Estrace 1 mg tablet1.93USDtablet
Estrogel 0.06% gel1.63USDg
Menest 1.25 mg tablet1.56USDtablet
Menest 0.625 mg tablet1.41USDtablet
Estrasorb packet1.21USDg
Elestrin 0.06% gel0.94USDg
Menest 0.3 mg tablet0.89USDtablet
Gynodiol 1.5 mg tablet0.5USDtablet
Estradiol 2 mg tablet0.49USDtablet
Estrace 2 mg Tablet0.44USDtablet
Estradiol 1 mg tablet0.42USDtablet
Estradiol 0.5 mg tablet0.36USDtablet
Estrogel 0.06 % Gel0.31USDg
Estrace 1 mg Tablet0.25USDtablet
Estrace 0.5 mg Tablet0.13USDtablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States75727792004-03-022024-03-02
United States52232611993-06-292010-06-29
Canada23068812008-09-022018-11-19
Canada13386601996-10-222013-10-22
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 Solubility0.0213ALOGPS
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
Spectra
SpectraGC-MSMS/MS1D 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
ResourceLink
KEGG DrugD00105
KEGG CompoundC00951
PubChem Compound5757
PubChem Substance46508115
ChemSpider5554
BindingDB17292
ChEBI16469
ChEMBLCHEMBL135
Therapeutic Targets DatabaseDAP000854
PharmGKBPA449503
IUPHAR1013
Guide to Pharmacology1013
HETECO
Drug Product Database2246969
RxListhttp://www.rxlist.com/cgi/generic3/estrogel.htm
Drugs.comhttp://www.drugs.com/estradiol.html
WikipediaEstradiol
ATC CodesG03CA01G03CA03L02AA02L02AA03
AHFS Codes
  • 68:16.04
PDB EntriesNot Available
FDA labelshow(89.1 KB)
MSDSshow(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