Identification

Name
Estradiol
Accession Number
DB00783  (APRD00311)
Type
Small Molecule
Groups
Approved, Investigational, Vet approved
Description

Estradiol (also known as E2 or 17β-estradiol) is a naturally occurring hormone that circulates endogenously within the human body. It is the most potent form of mammalian estrogenic steroids and acts as the major female sex hormone. As such, estradiol plays an essential role in the regulation of the menstrual cycle, in the development of puberty and secondary female sex characteristics, as well as in ageing and several hormonally-mediated disease states. Estrogen mediates its effects across the body through potent agonism of the Estrogen Receptor (ER), which is located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. Estradiol binds to both subtypes of the Estrogen Receptor: Estrogen Receptor Alpha (ERα) and Estrogen Receptor Beta (ERβ). Estradiol also acts as a potent agonist of G Protein-coupled Estrogen Receptor (GPER), which has recently been recognized as a major mediator of estradiol's rapid cellular effects [9].

Estradiol is commercially available in several hormone therapy products for managing conditions associated with reduced estrogen production such as menopausal and peri-menopausal symptoms as well as hypoestrogenism. It is also used in transgender hormone therapy, as a component of oral contraceptive pills for preventing pregnancy (most commonly as Ethinylestradiol, a synthetic form of estradiol), and is sometimes used for the palliative treatment of some hormone-sensitive cancers like breast and prostate cancer. Estradiol is available in a number of formulations including oral, transdermal, and injectable.

The primary source of estrogen in normally cycling adult women is the ovarian follicle, which secretes 70 to 500 mcg of estradiol daily, depending on the phase of the menstrual cycle. However, after menopause, most endogenous estrogen is produced by conversion of androstenedione, secreted by the adrenal cortex, to estrone by peripheral tissues. Thus, estrone and the sulphate conjugated form, estrone sulphate, are the most abundant circulating estrogens in postmenopausal women [Label]. Although circulating estrogens exist in a dynamic equilibrium of metabolic interconversions, estradiol is the principal intracellular human estrogen and is substantially more potent than its metabolites, estrone and estriol at the receptor level. Because of the difference in potency between estradiol and estrone, menopause (and a change in primary hormone from estradiol to estrone) is associated with a number of symptoms associated with this reduction in potency and in estrogenic effects. These include hot flashes, vaginal dryness, mood changes, irregular menses, chills, and sleeping problems.

When used for oral or IM administration, estradiol is commonly synthesized as a pro-drug ester (such as Estradiol acetate, Estradiol benzoate, Estradiol cypionate, Estradiol dienanthate, and Estradiol valerate). It is commonly produced with an ester side-chain as endogenous estradiol has very low oral bioavailability on its own (2-10%). First-pass metabolism by the gut and the liver quickly degrades the estradiol molecule before it gets a chance to enter the systemic circulation and exert its estrogenic effects [10]. Esterification of estradiol aims to improve absorption after oral administration (such as with Estradiol valerate) or to sustain release from intramuscular depot injections (such as with Estradiol Cypionate) through improved lipophilicity [14]. Following absorption, the esters are cleaved, resulting in the release of endogenous estradiol, or 17β-estradiol.

Recommendations for treatment of menopausal symptoms changed drastically following the release of results and early termination of the Women's Health Initiative (WHI) studies in 2002 as a number of concerns were raised regarding the use of estrogen [11]. Specifically, the combined estrogen–progestin arm was discontinued after approximately five years of follow up due to a statistically significant increase in invasive breast cancer and in cardiovascular events [12]. Following extensive critique of the WHI results in the years following its release, Hormone Replacement Therapy (HRT) is now recommended to be used only for a short period (for 3-5 years post-menopause) in low doses, and in women without a history of breast cancer or at increased risk of cardiovascular or thromboembolic disease [13]. Notably, use of estrogen for menopausal symptoms should always be accompanied by a progestin component due to estrogen's effects on the endometrium; in women with an intact uterus, unopposed estrogen has been shown to promote the growth of the endometrium which can lead to endometrial hyperplasia and possibly cancer in the long-term.

Ethinylestradiol (EE) is a synthetic form of estradiol commonly used as the estrogenic component of most combination Oral Contraceptive Pills (OCPs). Ethinyl Estradiol differs from Estradiol in that it has improved biovailability and greater resistance to metabolism, making it more suitable for oral administration.

Structure
Thumb
Synonyms
  • (17β)-estra-1,3,5(10)-triene-3,17-diol
  • 17beta oestradiol
  • 17β-estra-1,3,5(10)-triene-3,17-diol
  • 17β-estradiol
  • 17β-oestradiol
  • beta-Estradiol
  • cis-Estradiol
  • Estradiol
  • Estradiol-17beta
  • Estradiolum
External IDs
E3A / NSC 17590 / NSC-20293 / NSC-9895 / SQ 16150 / WC-3011 / WC3011
Product Ingredients
IngredientUNIICASInChI Key
Estradiol hemihydrateCXY7B3Q98Z35380-71-3ZVVGLAMWAQMPDR-WVEWYJOQSA-N
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
AloraPatch0.05 mg/1dTransdermalAllergan1996-12-20Not applicableUs
AloraPatch0.1 mg/1dTransdermalActavis Pharma Company1996-12-20Not applicableUs
AloraPatch0.05 mg/1dTransdermalActavis Pharma Company1996-12-20Not applicableUs
AloraPatch0.1 mg/1dTransdermalAllergan1996-12-20Not applicableUs
AloraPatch0.025 mg/1dTransdermalAllergan2002-04-05Not applicableUs
AloraPatch0.025 mg/1dTransdermalActavis Pharma Company2002-04-05Not applicableUs
AloraPatch0.075 mg/1dTransdermalAllergan1996-12-20Not applicableUs
AloraPatch0.075 mg/1dTransdermalActavis Pharma Company1996-12-20Not applicableUs
ClimaraPatch0.075 mg/1dTransdermalBayer1998-03-23Not applicableUs
ClimaraPatch0.05 mg/1dTransdermalBayer1994-12-22Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
EstraceTablet1 mg/1OralAllergan2011-12-26Not applicableUs
EstraceTablet1 mg/1OralWarner Chilcott2009-06-012012-10-15Us
EstraceTablet0.5 mg/1OralPhysicians Total Care, Inc.2002-04-182006-11-30Us
EstraceTablet0.5 mg/1OralAllergan2011-12-26Not applicableUs
EstraceTablet0.5 mg/1OralWarner Chilcott2009-06-012012-10-15Us
EstraceTablet2 mg/1OralPhysicians Total Care, Inc.1996-06-272011-05-31Us
EstraceCream0.1 mg/1gVaginalAllergan2001-07-01Not applicableUs
EstraceCream0.1 mg/1gVaginalPhysicians Total Care, Inc.2003-06-142013-06-30Us
EstraceTablet2 mg/1OralAllergan2011-12-26Not applicableUs
EstraceCream0.1 mg/1gVaginalA-S Medication Solutions2001-07-01Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
ActivellaEstradiol (1 mg/1) + Norethisterone acetate (0.5 mg/1)Tablet, film coatedOralGemini Pharmaceuticals, Inc.2016-05-12Not applicableUs
ActivellaEstradiol (0.5 mg/1) + Norethisterone acetate (0.1 mg/1)Tablet, film coatedOralNovo Nordisk2007-04-092017-04-30Us
ActivellaEstradiol (1 mg/1) + Norethisterone acetate (0.5 mg/1)Tablet, film coatedOralNovo Nordisk2003-07-222018-10-31Us
ActivellaEstradiol (0.5 mg/1) + Norethisterone acetate (0.1 mg/1)Tablet, film coatedOralGemini Pharmaceuticals, Inc.2016-05-12Not applicableUs
ActivelleEstradiol (1.0 mg) + Norethisterone acetate (0.5 mg)TabletOralNovo Nordisk2008-05-16Not applicableCanada
Activelle LdEstradiol (0.5 mg) + Norethisterone acetate (0.1 mg)TabletOralNovo Nordisk2008-05-16Not applicableCanada
AmabelzEstradiol (1 mg/1) + Norethisterone (0.5 mg/1)TabletOralLupin Pharmaceuticals2016-10-21Not applicableUs
AmabelzEstradiol (0.5 mg/1) + Norethisterone (0.1 mg/1)TabletOralLupin Pharmaceuticals2016-10-21Not applicableUs
AngeliqEstradiol (0.5 mg/1) + Drospirenone (0.25 mg/1)Tablet, film coatedOralBayer2012-02-29Not applicableUs
AngeliqEstradiol (1 mg/1) + Drospirenone (0.5 mg/1)Tablet, film coatedOralPhysicians Total Care, Inc.2010-09-29Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
EstradermEstradiol (4 mg/1)Patch, extended releaseTransdermalNovartis2007-03-30Not applicableUs
EstradermEstradiol (8 mg/1)Patch, extended releaseTransdermalNovartis2007-03-30Not applicableUs
EstradiolEstradiol (20 mg/1)PelletOralQualgen Llc2015-09-012018-02-13Us
EstradiolEstradiol (18 mg/1)PelletOralQualgen Llc2015-09-012018-02-13Us
EstradiolEstradiol (15 mg/1)PelletOralQualgen Llc2015-09-012018-02-13Us
EstradiolEstradiol (25 mg/1)PelletOralQualgen Llc2015-09-012018-02-13Us
EstradiolEstradiol (12.5 mg/1)PelletOralQualgen Llc2015-09-012018-02-13Us
EstradiolEstradiol (22 mg/1)PelletOralQualgen Llc2015-09-012018-02-13Us
EstradiolEstradiol (6 mg/1)PelletOralQualgen Llc2015-09-012018-02-13Us
EstradiolEstradiol (10 mg/1)PelletOralQualgen Llc2015-09-012018-02-13Us
International/Other Brands
Estraderm MX (Novartis) / Estraderm TTS (Novartis) / Estrasorb (Medicis) / Estrofem (Novo Nordisk) / Femtrace (Warner Chilcott) / Innofem (Novo Nordisk) / Vivelle (Novartis)
Categories
UNII
4TI98Z838E
CAS number
50-28-2
Weight
Average: 272.382
Monoisotopic: 272.177630012
Chemical Formula
C18H24O2
InChI Key
VOXZDWNPVJITMN-ZBRFXRBCSA-N
InChI
InChI=1S/C18H24O2/c1-18-9-8-14-13-5-3-12(19)10-11(13)2-4-15(14)16(18)6-7-17(18)20/h3,5,10,14-17,19-20H,2,4,6-9H2,1H3/t14-,15-,16+,17+,18+/m1/s1
IUPAC Name
(1S,10R,11S,14S,15S)-15-methyltetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-2(7),3,5-triene-5,14-diol
SMILES
[H][C@@]12CC[C@H](O)[C@@]1(C)CC[C@]1([H])C3=C(CC[C@@]21[H])C=C(O)C=C3

Pharmacology

Indication

Estradiol is indicated for the treatment of moderate to severe vasomotor symptoms and vulvar and vaginal atrophy due to menopause, for the treatment of hypoestrogenism due to hypogonadism, castration, or primary ovarian failure, and for the prevention of post-menopausal osteoarthritis. It is also used for the treatment of breast cancer (for palliation only) in appropriately selected women and men with metastatic disease, and for the treatment of advanced androgen-dependent carcinoma of the prostate (for palliation only).

Associated Conditions
Associated Therapies
Pharmacodynamics

Estradiol, the principal intracellular human estrogen, is substantially more active than its metabolites, estrone and estriol, at the cellular level.

Mechanism of action

Estrogen mediates its effects across the body through potent agonism of the Estrogen Receptor (ER), which is located in various tissues including in the breasts, uterus, ovaries, skin, prostate, bone, fat, and brain. Estradiol binds to both subtypes of the Estrogen Receptor: Estrogen Receptor Alpha (ERα) and Estrogen Receptor Beta (ERβ). Estradiol also acts as a potent agonist of G Protein-coupled Estrogen Receptor (GPER), which has recently been recognized as a major mediator of estradiol's rapid cellular effects [9].

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.

TargetActionsOrganism
AEstrogen receptor alpha
agonist
Human
AEstrogen receptor beta
agonist
Human
UNuclear receptor subfamily 1 group I member 2Not AvailableHuman
UNeuronal acetylcholine receptor subunit alpha-4Not AvailableHuman
UNuclear receptor coactivator 2Not AvailableHuman
UG-protein coupled estrogen receptor 1Not AvailableHuman
UATP synthase subunit aNot AvailableHuman
UBeclin-1Not AvailableHuman
UEstradiol 17-beta-dehydrogenase 2Not AvailableHuman
UEstrogen-related receptor gamma
ligand
Human
Absorption

43%

Volume of distribution
Not Available
Protein binding

>95% - estrogens circulate in the blood largely bound to sex hormone binding globulin (SHBG) and albumin.

Metabolism

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

Route of elimination

Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates.

Half life

36 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
PathwayCategory
Estrone MetabolismMetabolic
Estrone MetabolismMetabolic
Androgen and Estrogen MetabolismMetabolic
17-beta Hydroxysteroid Dehydrogenase III DeficiencyDisease
Aromatase DeficiencyDisease
Androgen and Estrogen MetabolismMetabolic
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteraction
(R)-warfarinEstradiol may decrease the anticoagulant activities of (R)-warfarin.
(S)-WarfarinEstradiol may decrease the anticoagulant activities of (S)-Warfarin.
2,4-thiazolidinedioneThe therapeutic efficacy of 2,4-thiazolidinedione can be decreased when used in combination with Estradiol.
3-isobutyl-1-methyl-7H-xanthineThe serum concentration of 3-isobutyl-1-methyl-7H-xanthine can be increased when it is combined with Estradiol.
4-hydroxycoumarinEstradiol may decrease the anticoagulant activities of 4-hydroxycoumarin.
6-O-benzylguanineThe serum concentration of 6-O-benzylguanine can be increased when it is combined with Estradiol.
7-DeazaguanineThe serum concentration of 7-Deazaguanine can be increased when it is combined with Estradiol.
7,9-DimethylguanineThe serum concentration of 7,9-Dimethylguanine can be increased when it is combined with Estradiol.
8-azaguanineThe serum concentration of 8-azaguanine can be increased when it is combined with Estradiol.
8-chlorotheophyllineThe serum concentration of 8-chlorotheophylline can be increased when it is combined with Estradiol.
Food Interactions
  • Take with food to decrease nausea.

References

Synthesis Reference

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

US5248676
General References
  1. Pentikainen V, Erkkila K, Suomalainen L, Parvinen M, Dunkel L: Estradiol acts as a germ cell survival factor in the human testis in vitro. J Clin Endocrinol Metab. 2000 May;85(5):2057-67. [PubMed:10843196]
  2. Sharpe RM, Skakkebaek NE: Are oestrogens involved in falling sperm counts and disorders of the male reproductive tract? Lancet. 1993 May 29;341(8857):1392-5. [PubMed:8098802]
  3. Raman JD, Schlegel PN: Aromatase inhibitors for male infertility. J Urol. 2002 Feb;167(2 Pt 1):624-9. [PubMed:11792932]
  4. Carani C, Qin K, Simoni M, Faustini-Fustini M, Serpente S, Boyd J, Korach KS, Simpson ER: Effect of testosterone and estradiol in a man with aromatase deficiency. N Engl J Med. 1997 Jul 10;337(2):91-5. [PubMed:9211678]
  5. Behl C, Widmann M, Trapp T, Holsboer F: 17-beta estradiol protects neurons from oxidative stress-induced cell death in vitro. Biochem Biophys Res Commun. 1995 Nov 13;216(2):473-82. [PubMed:7488136]
  6. Schmidt JW, Wollner D, Curcio J, Riedlinger J, Kim LS: Hormone replacement therapy in menopausal women: Past problems and future possibilities. Gynecol Endocrinol. 2006 Oct;22(10):564-77. [PubMed:17135036]
  7. Foresta C, Zuccarello D, Biagioli A, De Toni L, Prana E, Nicoletti V, Ambrosini G, Ferlin A: Oestrogen stimulates endothelial progenitor cells via oestrogen receptor-alpha. Clin Endocrinol (Oxf). 2007 Oct;67(4):520-5. Epub 2007 Jun 15. [PubMed:17573901]
  8. Garcia-Segura LM, Sanz A, Mendez P: Cross-talk between IGF-I and estradiol in the brain: focus on neuroprotection. Neuroendocrinology. 2006;84(4):275-9. Epub 2006 Nov 23. [PubMed:17124377]
  9. Prossnitz ER, Barton M: Estrogen biology: new insights into GPER function and clinical opportunities. Mol Cell Endocrinol. 2014 May 25;389(1-2):71-83. doi: 10.1016/j.mce.2014.02.002. Epub 2014 Feb 12. [PubMed:24530924]
  10. O'Connell MB: Pharmacokinetic and pharmacologic variation between different estrogen products. J Clin Pharmacol. 1995 Sep;35(9 Suppl):18S-24S. [PubMed:8530713]
  11. Rossouw JE, Anderson GL, Prentice RL, LaCroix AZ, Kooperberg C, Stefanick ML, Jackson RD, Beresford SA, Howard BV, Johnson KC, Kotchen JM, Ockene J: Risks and benefits of estrogen plus progestin in healthy postmenopausal women: principal results From the Women's Health Initiative randomized controlled trial. JAMA. 2002 Jul 17;288(3):321-33. [PubMed:12117397]
  12. Speroff L: Clinical appraisal of the Women's Health Initiative. J Obstet Gynaecol Res. 2005 Apr;31(2):80-93. doi: 10.1111/j.1447-0756.2005.00251.x. [PubMed:15771632]
  13. Marjoribanks J, Farquhar C, Roberts H, Lethaby A, Lee J: Long-term hormone therapy for perimenopausal and postmenopausal women. Cochrane Database Syst Rev. 2017 Jan 17;1:CD004143. doi: 10.1002/14651858.CD004143.pub5. [PubMed:28093732]
  14. W. KuhnzH. BlodeH. Zimmermann (1993). Pharmacokinetics of Exogenous Natural and Synthetic Estrogens and Antiestrogens. In: Estrogens and Antiestrogens II.. Springer, Berlin, Heidelberg. [ISBN:978-3-642-60107-1]
External Links
Human Metabolome Database
HMDB0000151
KEGG Drug
D00105
KEGG Compound
C00951
PubChem Compound
5757
PubChem Substance
46508115
ChemSpider
5554
BindingDB
17292
ChEBI
16469
ChEMBL
CHEMBL135
Therapeutic Targets Database
DAP000854
PharmGKB
PA449503
IUPHAR
1013
Guide to Pharmacology
GtP Drug Page
HET
EST
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Estradiol_(medication)
ATC Codes
G03FA12 — Medroxyprogesterone and estrogenG03FA17 — Drospirenone and estrogenG03FB12 — Nomegestrol and estrogenG03FA11 — Levonorgestrel and estrogenG03FA16 — Trimegestone and estrogenG03FA14 — Dydrogesterone and estrogenG03EA02 — Testosterone and estrogenG03FA08 — Megestrol and estrogenG03EA03 — Prasterone and estrogenG03AA14 — Nomegestrol and estradiolG03AB08 — Dienogest and estradiolG03FB01 — Norgestrel and estrogenG03FB09 — Levonorgestrel and estrogenG03FA05 — Methylnortestosterone and estrogenG03FB05 — Norethisterone and estrogenG03FB04 — Megestrol and estrogenG03CA53 — Estradiol, combinationsG03FA07 — Lynestrenol and estrogenG03HB01 — Cyproterone and estrogenG03FB11 — Trimegestone and estrogenG03FB07 — Medrogestone and estrogenG03FB02 — Lynestrenol and estrogenG03FA15 — Dienogest and estrogenG03CA03 — EstradiolG03FB10 — Desogestrel and estrogenG03FA06 — Etynodiol and estrogenG03EA01 — Methyltestosterone and estrogenG03FA09 — Noretynodrel and estrogenG03FA13 — Norgestimate and estrogenG03FB03 — Chlormadinone and estrogenG03FA10 — Norgestrel and estrogenG03FA04 — Progesterone and estrogenG03FB08 — Dydrogesterone and estrogenG03FA02 — Hydroxyprogesterone and estrogenG02BB01 — Vaginal ring with progestogen and estrogenG03FA03 — Ethisterone and estrogenG03FB06 — Medroxyprogesterone and estrogenG03FA01 — Norethisterone and estrogen
AHFS Codes
  • 68:16.04 — Estrogens
PDB Entries
1a27 / 1a52 / 1aqu / 1e6w / 1ere / 1fds / 1fdt / 1fdu / 1fdw / 1g50
show 30 more
FDA label
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MSDS
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Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0Active Not RecruitingBasic ScienceAging / Menopause1
0RecruitingBasic SciencePolycystic Ovaries Syndrome1
0WithdrawnBasic ScienceMuscle Wasting1
1Active Not RecruitingBasic ScienceNormal Healthy Volunteers1
1CompletedNot AvailableContraception / Oral Contraceptives (OC) / Ovulation Inhibition / Pharmacology, Clinical1
1CompletedNot AvailableHIV Prevention1
1CompletedNot AvailableHealthy Volunteers3
1CompletedBasic ScienceBone Loss, Age-Related1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceMigrainous Headache1
1CompletedDiagnosticPostmenopausal Syndrome1
1CompletedDiagnosticOne to five years postmenopausal1
1CompletedTreatmentMenopause2
1CompletedTreatmentMenopause / Postmenopausal Vaginal Atrophy2
1RecruitingSupportive CareMenopause1
1TerminatedTreatmentHuman Immunodeficiency Virus (HIV) Infections1
1WithdrawnBasic ScienceDiabetes, Diabetes Mellitus Type 11
1WithdrawnTreatmentAnorexia Nervosa (AN)1
1, 2CompletedOtherAging / One to five years postmenopausal1
1, 2CompletedOtherCognitive Changes / Memory Losses / Postmenopausal Syndrome1
1, 2CompletedTreatmentHealthy Volunteers1
1, 2RecruitingPreventionPerimenopausal Disorder / Stress, Emotional1
2Active Not RecruitingTreatmentEstrogen Levels Among Breast Cancer Patients1
2CompletedBasic ScienceOrthostatic Intolerance1
2CompletedPreventionContraception1
2CompletedPreventionEndometrial Safety / Vasomotor Symptoms1
2CompletedSupportive CareInfertilities1
2CompletedSupportive CareSexual Dysfunction, Physiological1
2CompletedTreatmentAging1
2CompletedTreatmentAlzheimer's Disease (AD)2
2CompletedTreatmentAnorexia Nervosa (AN) / Bone destruction1
2CompletedTreatmentAtherosclerosis / Chlamydial Infections / Infections, Cytomegalovirus / One to five years postmenopausal / Pneumonia, Bacterial1
2CompletedTreatmentAtherosclerosis / Healthy Volunteers / Vascular Diseases1
2CompletedTreatmentAtrophy1
2CompletedTreatmentCancers / Hormonal Cycling / Prostate1
2CompletedTreatmentCancers / Prostate Neoplasms1
2CompletedTreatmentCicatrix / Wound-healing1
2CompletedTreatmentContraception1
2CompletedTreatmentHeavy Uterine Bleeding / Uterine Leiomyomas2
2CompletedTreatmentHereditary Haemorrhagic Telangiectasia (HHT) / Nasal Bleeding1
2CompletedTreatmentHigh Blood Cholesterol Level / One to five years postmenopausal1
2CompletedTreatmentHigh Blood Pressure (Hypertension) / One to five years postmenopausal / Pre-Hypertension1
2CompletedTreatmentMenopausal Hot Flushes / Menopause1
2CompletedTreatmentMenopause / Painful Intercourse / Vulvovaginal Atrophy2
2CompletedTreatmentNeoplasms, Breast1
2CompletedTreatmentOvarian Diseases1
2CompletedTreatmentRelapsing Remitting Multiple Sclerosis (RRMS)1
2CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder2
2CompletedTreatmentSchizoaffective Disorders / Schizophrenic Disorders / Schizophreniform Disorder(Not in Manic Phase)1
2CompletedTreatmentShock, Hemorrhagic1
2CompletedTreatmentTraumatic Brain Injury (TBI)1
2Not Yet RecruitingTreatmentIVF1
2RecruitingDiagnosticCancer, Breast1
2RecruitingTreatmentCancer, Breast / Estrogen Receptor Positive Breast Cancer1
2RecruitingTreatmentCardiovascular Disease (CVD) / Estrogen Deficiency / Hypothalamic Amenorrhea1
2RecruitingTreatmentCerebral Aneurysms / Menopause / Perimenopause / Treatments1
2RecruitingTreatmentEstrogen Receptor Positive Breast Cancer1
2TerminatedTreatmentCancer of the Breast / Cancer, Breast / Neoplasms, Breast1
2TerminatedTreatmentCancer of the Prostate1
2TerminatedTreatmentDepression / Postpartum Depression1
2TerminatedTreatmentFemale Breast Cancer1
2TerminatedTreatmentBone destruction / Hypercalciuria / Hypercalciuria, Familial Idiopathic / Osteopenia1
2TerminatedTreatmentMenopausal Depression1
2TerminatedTreatmentMenopause1
2TerminatedTreatmentProstate Cancer2
2Unknown StatusDiagnosticPremenstrual Syndrome1
2Unknown StatusTreatmentEndometrial Cancers / Endometrial Hyperplasia1
2Unknown StatusTreatmentMenopause1
2Unknown StatusTreatmentPremenstrual Syndrome1
2WithdrawnPreventionAtrophy of Vagina / Vaginal Inflammation / Vaginal Ulceration1
2, 3Active Not RecruitingOtherHealthy Volunteers1
2, 3CompletedPreventionAtherosclerosis1
2, 3CompletedTreatmentAlzheimer's Disease (AD)1
2, 3CompletedTreatmentAnorexia Nervosa (AN)1
2, 3CompletedTreatmentDepression / Menopause / Perimenopause1
2, 3CompletedTreatmentFailed Induction of Labor1
2, 3CompletedTreatmentMenopause1
3Active Not RecruitingTreatmentHeavy Menstrual Bleeding / Uterine Leiomyomas2
3Active Not RecruitingTreatmentVulvar and Vaginal Atrophy1
3CompletedNot AvailableAtrophic Vaginitis1
3CompletedNot AvailableStrokes1
3CompletedPreventionAlzheimer's Disease (AD) / Memory Disorders1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Infarction / Myocardial Ischemia1
3CompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Ischemia / One to five years postmenopausal1
3CompletedPreventionOsteopenia1
3CompletedTreatmentAlzheimer's Disease (AD)1
3CompletedTreatmentAtrophic Vaginitis2
3CompletedTreatmentAtrophic Vaginitis Due to Menopause1
3CompletedTreatmentAtrophy1
3CompletedTreatmentBMI >30 kg/m21
3CompletedTreatmentContraception1
3CompletedTreatmentHigh Blood Pressure (Hypertension) / One to five years postmenopausal1
3CompletedTreatmentHormone Replacement Therapy1
3CompletedTreatmentHypogonadism1
3CompletedTreatmentInsomniac Postmenopausal Women1
3CompletedTreatmentMenopausal Hot Flushes2
3CompletedTreatmentMenopausal Hot Flushes / Vasomotor Symptoms1
3CompletedTreatmentMenopause1
3CompletedTreatmentMenopause / Painful Intercourse / Vulvovaginal Atrophy1
3CompletedTreatmentMenopause / Postmenopausal Vaginal Atrophy4
3CompletedTreatmentMetrorrhagia3
3CompletedTreatmentPostmenopausal Syndrome1
3CompletedTreatmentPrimary Dysmenorrhoea1
3CompletedTreatmentSexual Dysfunctions1
3CompletedTreatmentMinor burns / Traumas / Varicose Ulcers1
3CompletedTreatmentTurner's Syndrome1
3CompletedTreatmentVasomotor Symptoms2
3CompletedTreatmentVulvar and Vaginal Atrophy1
3CompletedTreatmentVulvovaginal Atrophy4
3CompletedTreatmentOne to five years postmenopausal2
3Not Yet RecruitingTreatmentFertility Disorders1
3RecruitingTreatmentAnemias / Bone destruction / Cardiovascular Complications / Menopausal Hot Flushes / Prostate Cancer1
3RecruitingTreatmentAnorexia Nervosa (AN)1
3RecruitingTreatmentEndometriosis2
3RecruitingTreatmentEndometriosis related pain2
3RecruitingTreatmentHeavy Menstrual Bleeding / Uterine Leiomyomas1
3RecruitingTreatmentPrimary Ovarian Insufficiency2
3TerminatedTreatmentAtrophic Vaginitis1
3TerminatedTreatmentAtrophy of vulva / Vulvovaginal Atrophy1
3TerminatedTreatmentMenopause / Urinary Tract Infections (UTIs)1
3TerminatedTreatmentBone destruction / Osteopenia1
3Unknown StatusTreatmentDisseminated Sclerosis1
3Unknown StatusTreatmentPostmenopausal Syndrome1
3WithdrawnTreatmentAmenorrhea / Bone Loss1
3WithdrawnTreatmentContraception1
4Active Not RecruitingBasic ScienceContraception / Fertility1
4CompletedBasic ScienceHormone Replacement1
4CompletedBasic ScienceTranssexualism1
4CompletedPreventionCardiovascular Disease (CVD)1
4CompletedPreventionContraception / Pregnancy1
4CompletedPreventionBone destruction1
4CompletedTreatmentAtrophy of Vagina / Dyspareunia (Female) / Menopause / Vaginal Creams / Vaginal Discharge / Vaginal Symptoms1
4CompletedTreatmentDepression / Menopause1
4CompletedTreatmentDepression / Perimenopausal Depression1
4CompletedTreatmentDepression / Sleep Initiation and Maintenance Disorders1
4CompletedTreatmentHypogonadism / Premature Ovarian Failure (POF) / Turner's Syndrome1
4CompletedTreatmentInfertilities3
4CompletedTreatmentMenopausal Hot Flushes2
4CompletedTreatmentMenopause1
4CompletedTreatmentPolycystic Ovaries Syndrome1
4CompletedTreatmentPostmenopausal Disorder / Urinary Bladder, Overactive / Urination Disorders1
4CompletedTreatmentPostmenopausal Syndrome2
4CompletedTreatmentPremature Ovarian Failure (POF)1
4CompletedTreatmentTurner's Syndrome1
4CompletedTreatmentBone destruction / One to five years postmenopausal1
4CompletedTreatmentOne to five years postmenopausal2
4Not Yet RecruitingBasic ScienceSuicidal Ideation1
4Not Yet RecruitingTreatmentEndometrium1
4Not Yet RecruitingTreatmentVulvovaginal Atrophy2
4RecruitingBasic ScienceGender Dysphoria1
4RecruitingBasic SciencePerimenopausal Depression1
4RecruitingOtherHealthy Volunteers / Stress Disorders, Post-Traumatic1
4RecruitingTreatmentAnovulatory cycle / Infertilities1
4RecruitingTreatmentAsymptomatic Microscopic Hematuria1
4RecruitingTreatmentFrozen Embryo Transfer / Pregnancy Loss1
4RecruitingTreatmentIncontinence / Nocturia / Urinary Bladder, Overactive1
4RecruitingTreatmentInfertilities2
4RecruitingTreatmentInfertilities / Polycystic Ovarian Syndrome1
4RecruitingTreatmentPainful Intercourse1
4TerminatedPreventionMenopause1
4TerminatedScreeningContraception / Hypercoagulability1
4TerminatedTreatmentPostpartum Depression1
4TerminatedTreatmentSexual Dysfunction, Physiological1
4Unknown StatusPreventionArteriosclerosis / Menopause1
4Unknown StatusTreatmentMajor Depressive Disorder (MDD) / Menopause1
4Unknown StatusTreatmentMenstrual Bleeding / Menstrual Migraines / Menstrual Spotting1
4WithdrawnTreatmentEstrogens / General Surgery / Menopause / Pelvic Floor Disorders1
4WithdrawnTreatmentInfertilities1
Not AvailableActive Not RecruitingNot AvailableConstitutional Tall Stature1
Not AvailableActive Not RecruitingNot AvailableContraception / Human Immunodeficiency Virus (HIV) / Immune Cells (Mucosal and Systemic) / Microbiota1
Not AvailableActive Not RecruitingNot AvailableInsulin Resistance1
Not AvailableActive Not RecruitingBasic ScienceAging / Arterial Stiffening / Menopause1
Not AvailableActive Not RecruitingBasic ScienceAging / Insulin Resistance1
Not AvailableActive Not RecruitingBasic ScienceHyperandrogenemia / Polycystic Ovaries Syndrome1
Not AvailableActive Not RecruitingBasic ScienceHyperandrogenism / Polycystic Ovaries Syndrome1
Not AvailableActive Not RecruitingBasic ScienceMenstruation Disturbances1
Not AvailableActive Not RecruitingOtherEndothelial Dysfunction1
Not AvailableActive Not RecruitingTreatmentMenopause1
Not AvailableAvailableNot AvailableHealthy Naturally Cycling Women1
Not AvailableCompletedNot AvailableAbnormal Mammogram / Mammographic Density1
Not AvailableCompletedNot AvailableMenopause / Postmenopausal Vaginal Atrophy1
Not AvailableCompletedNot AvailableMyocardial Infarction1
Not AvailableCompletedNot AvailablePostmenopausal Osteoporosis (PMO) / Postmenopausal Period1
Not AvailableCompletedBasic ScienceBMI >30 kg/m2 / Infertilities1
Not AvailableCompletedBasic ScienceBMI >30 kg/m2 / Menopausal Syndromes1
Not AvailableCompletedBasic ScienceCardiovascular Disease (CVD) / Cognitive Impairments / Endothelial Dysfunction / Executive Dysfunction1
Not AvailableCompletedBasic ScienceCoronary Heart Disease (CHD)1
Not AvailableCompletedBasic ScienceHyperandrogenemia / Polycystic Ovary Syndrome (PCOS)1
Not AvailableCompletedBasic SciencePostpartum Depression1
Not AvailableCompletedDiagnosticEndometrial Thickness1
Not AvailableCompletedHealth Services ResearchWomen's Health1
Not AvailableCompletedOtherBMI >30 kg/m2 / Obstructive Sleep Apnea (OSA) / Polycystic Ovaries Syndrome / Polycystic Ovary Syndrome (PCOS)1
Not AvailableCompletedPreventionCardiovascular Disease (CVD) / Coronary Heart Disease (CHD) / Heart Diseases / Myocardial Infarction / Myocardial Ischemia1
Not AvailableCompletedPreventionContraception / Haemorrhage1
Not AvailableCompletedPreventionMetrorrhagia1
Not AvailableCompletedScreeningOther Diseases or Conditions1
Not AvailableCompletedTreatmentCardiovascular Disease (CVD) / Postmenopausal Vasomotor Symptoms1
Not AvailableCompletedTreatmentFlow-mediated Dilation Evaluation of the Brachial Artery1
Not AvailableCompletedTreatmentInfertilities1
Not AvailableCompletedTreatmentInfertilities / OHSS1
Not AvailableCompletedTreatmentMenopausal Syndromes1
Not AvailableCompletedTreatmentMenopausal and Other Perimenopausal Disorders1
Not AvailableCompletedTreatmentMenopausal and Postmenopausal Disorders1
Not AvailableCompletedTreatmentMenopause / One to five years postmenopausal1
Not AvailableCompletedTreatmentOvarian Failure, Premature1
Not AvailableCompletedTreatmentSystemic Lupus Erythematosus (SLE)1
Not AvailableCompletedTreatmentTurner's Syndrome1
Not AvailableCompletedTreatmentBone destruction / One to five years postmenopausal1
Not AvailableCompletedTreatmentOne to five years postmenopausal3
Not AvailableNot Yet RecruitingBasic ScienceMenopause1
Not AvailableRecruitingNot AvailableEmbryo Transfer / Infertilities1
Not AvailableRecruitingNot AvailableInfertilities1
Not AvailableRecruitingNot AvailableProvoked Localized Vulvodynia1
Not AvailableRecruitingBasic ScienceMenopause1
Not AvailableRecruitingOtherPelvic Floor Disorders1
Not AvailableRecruitingPreventionIntrauterine Adhesions2
Not AvailableRecruitingTreatmentGender Dysphoria1
Not AvailableRecruitingTreatmentInfertilities1
Not AvailableTerminatedBasic ScienceAging / Aging [G07.700.320.124] / Blood Pressures / Exercise [G11.427.590.530.698.277] / Menopause / Physiological Processes [G07.700]1
Not AvailableTerminatedBasic ScienceHyperandrogenism / Polycystic Ovaries Syndrome1
Not AvailableTerminatedTreatmentCognition Disorders / Moods Disorders1
Not AvailableUnknown StatusTreatmentInfertilities3
Not AvailableUnknown StatusTreatmentMenopausal Hot Flushes / Night Sweats1
Not AvailableUnknown StatusTreatmentMenstrual Cycle and Uterine Bleeding Disorders1
Not AvailableUnknown StatusTreatmentPrepubertal Labial Adhesions1
Not AvailableUnknown StatusTreatmentUrodynamic Stress Incontinence1
Not AvailableWithdrawnPreventionPlanned RRSO1
Not AvailableWithdrawnTreatmentIVF Poor Responders1

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
  • Apotheca Inc.
  • Ascend Therapeutics
  • AzurPharma Inc.
  • Bayer Healthcare
  • Carlisle Laboratories Inc.
  • Clint Pharmaceutical Inc.
  • Consolidated Midland Corp.
  • Darby Dental Supply Co. Inc.
  • Direct Dispensing Inc.
  • Dispensing Solutions
  • E.R. Squibb and Sons LLC
  • Gallipot
  • Graceway Pharmaceuticals
  • Group Health Cooperative
  • JHP Pharmaceuticals LLC
  • King Pharmaceuticals Inc.
  • Lunsco Inc.
  • Martica Enterprises Inc.
  • Martin Surgical Supply
  • Medisca Inc.
  • Merit Pharmaceuticals
  • Monarch Pharmacy
  • Murfreesboro Pharmaceutical Nursing Supply
  • Mylan
  • National Pharmaceuticals
  • Novartis AG
  • Novavax Inc.
  • Novo Nordisk Inc.
  • Paddock Labs
  • PD-Rx Pharmaceuticals Inc.
  • Pharmacia Inc.
  • Physicians Total Care Inc.
  • Prepackage Specialists
  • Primedics Laboratories
  • Professional Co.
  • San Jose Surgical Supply Inc.
  • Sandhills Packaging Inc.
  • Sandoz
  • Spectrum Pharmaceuticals
  • Ther-Rx Corp.
  • Upsher Smith Laboratories
  • Watson Pharmaceuticals
  • WC Pharmaceuticals
Dosage forms
FormRouteStrength
TabletOral
Tablet, film coatedOral
PatchTransdermal0.05 mg/1
PatchTransdermal100 mcg
PatchTransdermal50 mcg
Patch, extended releaseTransdermal
GelTopical0.25 mg/0.25g
GelTopical0.25 mg/1g
GelTopical0.5 mg/1g
GelTopical0.5 mg/0.5g
GelTopical1 mg/1g
GelTopical1.0 mg/1g
GelTransdermal0.1 %
GelTransdermal0.6 mg/1g
Gel, meteredTopical0.52 mg/0.87g
Gel, meteredTopical0.52 mg/1g
CreamVaginal0.1 mg/1g
TabletOral0.5 mg
TabletOral1 mg
TabletOral2 mg
PatchTransdermal
Patch, extended releaseTransdermal4 mg/1
Patch, extended releaseTransdermal8 mg/1
Patch, extended releaseTransdermal8 mg
Patch, extended releaseTransdermal2 mg
Patch, extended releaseTransdermal4 mg
PatchTransdermal0.025 mg/1d
PatchTransdermal0.0375 mg/1d
PatchTransdermal0.05 mg/1d
PatchTransdermal0.075 mg/1d
PatchTransdermal0.1 mg/1d
PatchTransdermal0.97 mg/48[USP'U]
PatchTransdermal1.46 mg/48[USP'U]
PatchTransdermal1.94 mg/48[USP'U]
PelletOral10 mg/1
PelletOral12.5 mg/1
PelletOral15 mg/1
PelletOral18 mg/1
PelletOral20 mg/1
PelletOral22 mg/1
PelletOral25 mg/1
PelletOral6 mg/1
TabletOral0.5 mg/1
TabletOral1 mg/1
TabletOral2 mg/1
PatchTransdermal0.06 mg/1d
PatchTransdermal37.5 mcg
PatchTransdermal75 mcg
EmulsionTopical.025 mg/1d
EmulsionTopical2.5 mg/1g
RingVaginal2 mg
RingVaginal2 mg/1
GelTransdermal0.06 %
GelTransdermal0.75 mg/1.25g
Gel, meteredTopical0.75 mg/1.25g
Gel, meteredTransdermal0.75 mg/1.25g
Capsule; gel, meteredOral; Transdermal
SprayTransdermal1.53 mg/1
Spray, meteredTransdermal1.53 mg/1
InsertVaginal4 ug/1
Tablet, film coatedOral0.5 mg/1
Tablet, film coatedOral1 mg/1
Tablet, film coatedOral2 mg/1
PatchTransdermal14 ug/1d
Film, extended releaseTransdermal0.025 mg/1d
Film, extended releaseTransdermal0.0375 mg/1d
Film, extended releaseTransdermal0.05 mg/1d
Film, extended releaseTransdermal0.075 mg/1d
Film, extended releaseTransdermal0.10 mg/1d
PatchTransdermal10 mg
PatchTransdermal25 mcg
PatchTransdermal5 mg
Kit
InsertVaginal10 ug/1
TabletVaginal25 mcg
Tablet, film coatedVaginal10 ug/1
Tablet, film coatedVaginal25 ug/1
TabletVaginal10 mcg
Patch, extended releaseTransdermal2.17 mg/1
Patch, extended releaseTransdermal3.28 mg/1
Patch, extended releaseTransdermal4.33 mg/1
Patch, extended releaseTransdermal6.57 mg/1
Patch, extended releaseTransdermal8.66 mg/1
PatchTransdermal8.66 mg
PatchTransdermal3.28 mg
PatchTransdermal4.33 mg
PatchTransdermal6.56 mg
Patch, extended releaseTransdermal0.025 mg/1d
Patch, extended releaseTransdermal0.0375 mg/1d
Patch, extended releaseTransdermal0.05 mg/1d
Patch, extended releaseTransdermal0.075 mg/1d
Patch, extended releaseTransdermal0.1 mg/1d
TabletVaginal10 ug/1
Prices
Unit descriptionCostUnit
Femring 0.1 mg/24hr Ring218.6USD ring
Estring 2 mg Ring Box210.39USD box
Femring 0.10 mg vaginal ring210.19USD ring
Femring 0.05 mg/24hr Ring205.15USD ring
Estring 2 mg vaginal ring202.3USD ring
Femring 0.05 mg vaginal ring197.26USD ring
Elestrin 0.52 mg/0.87 gm(0.06%) Gel 144 gm Bottle162.06USD bottle
Ethinyl estradiol powder140.0USD g
Vagifem 18 25 mcg tablet Box139.78USD box
Estrace 0.1 mg/gm Cream 42.5 gm Tube133.27USD tube
Estradiol cypionate powder88.74USD g
Delestrogen 10 mg/ml Oil 5ml Vial88.04USD vial
Evamist 1.53 mg/spray Solution 8.1ml Bottle87.18USD bottle
Divigel 1 mg/gm Gel Box Of 30 gm85.53USD box
Estrogel 0.75 mg/1.25 gm(0.06%) Gel 50 gm Bottle84.24USD bottle
Divigel 30 0.25 mg/0.25 gm Gel 30 Patches/box81.24USD box
Climara 4 0.025 mg/24hr Patches Box75.58USD box
Climara 4 0.05 mg/24hr Patches Box75.58USD box
Climara 4 0.1 mg/24hr Patches Box75.58USD box
Menostar 4 14 mcg/24hr Patches Box73.18USD box
Divigel 0.5 mg/0.5 gm Gel Box72.99USD box
Estraderm 8 0.1 mg/24hr Patches Box72.47USD box
Vivelle-Dot 8 0.1 mg/24hr Patches Box72.46USD box
Vivelle-Dot 8 0.025 mg/24hr Patches Box70.69USD box
Climara 4 0.075 mg/24hr Patches Box69.04USD box
Climara Pro 4 0.045-0.015 mg/day Patches Box69.04USD box
Vivelle-Dot 8 0.0375 mg/24hr Patches Box68.84USD box
Vivelle-Dot 8 0.075 mg/24hr Patches Box66.89USD box
CombiPatch 8 0.05-0.25 mg/day Patches Box66.45USD box
Estraderm 8 0.05 mg/24hr Patches Box66.35USD box
Vivelle-Dot 8 0.05 mg/24hr Patches Box65.99USD box
Estring 2 mg Slow-Release Ring65.39USD ring
Alora 8 0.1 mg/24hr Patches Box62.99USD box
Alora 8 0.05 mg/24hr Patches Box60.99USD box
Alora 8 0.075 mg/24hr Patches Box58.27USD box
Vagifem 8 25 mcg tablet Box58.23USD box
Vagifem 8 10 mcg tablet Box54.99USD box
Vivelle 8 0.05 mg/24hr Patches Box49.99USD box
Estradiol benzoate powder42.0USD g
Estradiol 4 0.025 mg/24hr Patches Box40.92USD box
Estradiol 4 0.05 mg/24hr Patches Box40.92USD box
Estradiol 4 0.075 mg/24hr Patches Box40.92USD box
Estradiol 4 0.1 mg/24hr Patches Box40.92USD box
Estradiol 4 0.06 mg/24hr Patches Box39.99USD box
Delestrogen 40 mg/ml Oil39.52USD ml
Estradiol 4 0.0375 mg/24hr Patches Box39.35USD box
Delestrogen 40 mg/ml vial38.0USD ml
Estradiol valerate 40 mg/ml vial35.62USD ml
Estradiol valerate powder32.13USD g
Delestrogen 20 mg/ml Oil23.82USD ml
Delestrogen 20 mg/ml vial22.91USD ml
Estradiol valerate 20 mg/ml vial21.25USD ml
Estradiol 0.1 mg/day patch20.55USD patch
Estradiol powder17.86USD g
Climara 0.0375 mg/24hr Patches17.26USD patch
Climara 0.06 mg/24hr Patches17.26USD patch
Estradiol 0.05 mg/day patch16.91USD patch
Delestrogen 10 mg/ml vial16.25USD ml
Climara 0.025 mg/day patch15.77USD patch
Climara 0.0375 mg/day patch15.77USD patch
Climara 0.05 mg/day patch15.77USD patch
Climara 0.06/mg day patch15.77USD patch
Climara 0.075 mg/day patch15.77USD patch
Climara 0.1 mg/day patch15.77USD patch
Climara pro patch15.77USD patch
Estradiol valerate 10 mg/ml vial15.24USD ml
Evamist 1.53 mg/spray10.43USD ml
Estradiol tds 0.025 mg/day9.84USD each
Estradiol tds 0.0375 mg/day9.84USD each
Estradiol tds 0.06 mg/day9.84USD each
Estradiol tds 0.075 mg/day9.84USD each
Depo-Estradiol 5 mg/ml Oil9.66USD ml
Estraderm 0.1 mg patch8.66USD patch
CombiPatch 0.05-0.14 mg/day Patches8.65USD patch
Vivelle-dot 0.075 mg patch8.49USD patch
Estraderm 0.05 mg patch8.07USD patch
Combipatch 0.05-0.14 mg ptch7.92USD patch
Combipatch 0.05-0.25 mg ptch7.91USD patch
Depo-estradiol 5 mg/ml vial7.89USD ml
Vivelle-dot 0.1 mg patch7.89USD patch
Vivelle-dot 0.05 mg patch7.61USD patch
Vivelle-dot 0.0375 mg patch7.54USD patch
Vivelle-dot 0.025 mg patch7.53USD patch
Alora 0.1 mg patch7.16USD patch
Alora 0.075 mg patch7.0USD patch
Alora 0.05 mg patch6.86USD patch
Vagifem 10 mcg vaginal tab6.78USD each
Vagifem 25 mcg vaginal tab6.78USD each
Climara 100 (7.8 Mg/Pth) 100 mcg/day Patch6.67USD patch
Climara 75 (5.7 Mg/Pth) 75 mcg/day Patch6.31USD patch
Alora 0.025 mg patch6.26USD patch
Vivelle 0.1 mg patch5.94USD patch
Climara 50 (3.9 Mg/Pth) 50 mcg/day Patch5.91USD patch
Vivelle 0.05 mg patch5.74USD patch
Climara 25 (2 Mg/Pth) 25 mcg/day Patch5.54USD patch
Estraderm-100 (8.0 Mg/Pth) 100 mcg/day Patch4.52USD patch
Estraderm-25 (2 Mg/Pth) 25 mcg/day Patch3.74USD patch
Estradot 100 (1.56 Mg/Pth) 100 mcg/day Patch3.49USD patch
Estradot 75 (1.17 Mg/Pth) 75 mcg/day Patch3.3USD patch
Vagifem 25 mcg Tablet3.21USD tablet
Estradot 50 (0.78 Mg/Pth) 50 mcg/day Patch3.07USD patch
Oesclim 50 (10 Mg/Pth) 50 mcg/day Patch3.06USD patch
Estrace 0.01% cream3.05USD g
Estrace 2 mg tablet2.98USD tablet
Estradot 37.5 (0.585 Mg/Pth) 37.5 mcg/day Patch2.88USD patch
Estradot 25 (0.39 Mg/Pth) 25 mcg/day Patch2.86USD patch
Estrasorb 4.35 mg/1.74 gm Emulsion 1.74 gm Packet2.83USD packet
Oesclim 25 (5 Mg/Pth) 25 mcg/day Patch2.83USD patch
Divigel 0.25 mg gel packet2.74USD each
Divigel 0.5 mg gel packet2.74USD each
Divigel 1 mg gel packet2.74USD g
Sandoz Estradiol Derm 100 (8 Mg/Pth) 100 mcg/day Patch2.64USD patch
Menest 2.5 mg tablet2.6USD tablet
Femtrace 1.8 mg tablet2.59USD tablet
Sandoz Estradiol Derm 75 (6 Mg/Pth) 75 mcg/day Patch2.5USD patch
Sandoz Estradiol Derm 50 (4 Mg/Pth) 50 mcg/day Patch2.34USD patch
Estrace 0.5 mg tablet2.29USD tablet
Femtrace 0.45 mg tablet2.02USD tablet
Femtrace 0.9 mg tablet2.02USD tablet
Estrace 1 mg tablet1.93USD tablet
Estrogel 0.06% gel1.63USD g
Menest 1.25 mg tablet1.56USD tablet
Menest 0.625 mg tablet1.41USD tablet
Estrasorb packet1.21USD g
Elestrin 0.06% gel0.94USD g
Menest 0.3 mg tablet0.89USD tablet
Gynodiol 1.5 mg tablet0.5USD tablet
Estradiol 2 mg tablet0.49USD tablet
Estrace 2 mg Tablet0.44USD tablet
Estradiol 1 mg tablet0.42USD tablet
Estradiol 0.5 mg tablet0.36USD tablet
Estrogel 0.06 % Gel0.31USD g
Estrace 1 mg Tablet0.25USD tablet
Estrace 0.5 mg Tablet0.13USD tablet
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5223261No1993-06-292010-06-29Us
CA2306881No2008-09-022018-11-19Canada
CA1338660No1996-10-222013-10-22Canada
US7018992No2002-09-172022-09-17Us
US5860946No1997-07-012017-07-01Us
US6299900No1997-02-192017-02-19Us
US6818226No1997-02-192017-02-19Us
US6923983No1997-02-192017-02-19Us
US6978945No2002-07-312022-07-31Us
US6747019No2000-03-202020-03-20Us
US7320970No2000-03-302020-03-30Us
US6933395No1997-08-112017-08-11Us
US8906890No2011-10-222031-10-22Us
US5855906No1995-12-192015-12-19Us
US7572779No2005-10-022025-10-02Us
US6962908No2001-12-212021-12-21Us
US7799771No2001-12-212021-12-21Us
US5891868No1997-11-212017-11-21Us
US6692763No1997-11-212017-11-21Us
US7470433No2001-08-032021-08-03Us
US7198801No2002-06-252022-06-25Us
US6133251No1996-10-252016-10-25Us
US8071577No2006-05-132026-05-13Us
US8153616No2008-01-302028-01-30Us
US6884793No1996-10-252016-10-25Us
US8231906No2010-07-042030-07-04Us
US6841716No2000-04-272020-04-27Us
US9730900No2008-07-102028-07-10Us
US9724310No2008-07-102028-07-10Us
US9833419No2008-07-102028-07-10Us
US9180091No2013-12-202033-12-20Us
US9289382No2012-11-212032-11-21Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)151-152Ott, 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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+1.0
Blood Brain Barrier+0.8917
Caco-2 permeable+0.8867
P-glycoprotein substrateSubstrate0.7058
P-glycoprotein inhibitor INon-inhibitor0.9147
P-glycoprotein inhibitor IINon-inhibitor0.9403
Renal organic cation transporterNon-inhibitor0.8008
CYP450 2C9 substrateNon-substrate0.727
CYP450 2D6 substrateNon-substrate0.801
CYP450 3A4 substrateSubstrate0.7132
CYP450 1A2 substrateInhibitor0.9106
CYP450 2C9 inhibitorNon-inhibitor0.939
CYP450 2D6 inhibitorNon-inhibitor0.9574
CYP450 2C19 inhibitorNon-inhibitor0.9025
CYP450 3A4 inhibitorNon-inhibitor0.8309
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.7887
Ames testNon AMES toxic0.9198
CarcinogenicityNon-carcinogens0.8829
BiodegradationNot ready biodegradable0.9746
Rat acute toxicity2.2272 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.8647
hERG inhibition (predictor II)Inhibitor0.6624
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Download (9.34 KB)
Spectra
SpectrumSpectrum TypeSplash Key
GC-MS Spectrum - GC-MS (2 TMS)GC-MSsplash10-017r-1791100000-7b16254894cdcb8ee86d
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
GC-MS Spectrum - EI-BGC-MSsplash10-00di-1980000000-b2dec84718861de189ec
GC-MS Spectrum - EI-BGC-MSsplash10-00di-3940000000-f3692a81f624f15d3e0b
GC-MS Spectrum - EI-BGC-MSsplash10-00di-0960000000-be4e96105398cb805cd9
GC-MS Spectrum - EI-BGC-MSsplash10-00di-0790000000-5c858378c15135811824
GC-MS Spectrum - GC-MSGC-MSsplash10-017r-1791100000-7b16254894cdcb8ee86d
Mass Spectrum (Electron Ionization)MSsplash10-075a-2920000000-10218bfa5b56f829853e
MS/MS Spectrum - Quattro_QQQ 10V, PositiveLC-MS/MSsplash10-05fr-0590000000-1dd83cbcb3d21edfbdbd
MS/MS Spectrum - Quattro_QQQ 25V, PositiveLC-MS/MSsplash10-0a4i-2900000000-f3279d6cdab9cf3800fd
MS/MS Spectrum - Quattro_QQQ 40V, PositiveLC-MS/MSsplash10-0a4i-8900000000-0efe28378f612aab8c3d
MS/MS Spectrum - EI-B (JEOL JMS-01-SG-2) , PositiveLC-MS/MSsplash10-00di-1980000000-b2dec84718861de189ec
MS/MS Spectrum - EI-B (HITACHI RMU-6E) , PositiveLC-MS/MSsplash10-00di-3940000000-f3692a81f624f15d3e0b
MS/MS Spectrum - EI-B (HITACHI M-52) , PositiveLC-MS/MSsplash10-00di-0960000000-be4e96105398cb805cd9
MS/MS Spectrum - EI-B (HITACHI M-80) , PositiveLC-MS/MSsplash10-00di-0790000000-5c83456da6e28375ad51
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - Linear Ion Trap , negativeLC-MS/MSsplash10-00di-0490000000-c3c4658cfae36bedff30
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-1900000000-51d28e077b0aefa6aa1c
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0a4i-2900000000-a22a9233ffbb9eb05a1b
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-0960000000-d2ee002f4c0363c04e83
LC-MS/MS Spectrum - LC-ESI-ITFT , positiveLC-MS/MSsplash10-0002-0960000000-2ad7c6e17386448419df
1H NMR Spectrum1D NMRNot Applicable
[1H,13C] 2D NMR Spectrum2D NMRNot Applicable

Taxonomy

Description
This compound belongs to the class of organic compounds known as estrogens and derivatives. These are steroids with a structure containing a 3-hydroxylated estrane.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Estrane steroids
Direct Parent
Estrogens and derivatives
Alternative Parents
3-hydroxysteroids / 17-hydroxysteroids / Phenanthrenes and derivatives / Tetralins / 1-hydroxy-2-unsubstituted benzenoids / Secondary alcohols / Cyclic alcohols and derivatives / Hydrocarbon derivatives
Substituents
Estrogen-skeleton / 17-hydroxysteroid / Hydroxysteroid / 3-hydroxysteroid / Phenanthrene / Tetralin / 1-hydroxy-2-unsubstituted benzenoid / Benzenoid / Cyclic alcohol / Secondary alcohol
Molecular Framework
Aromatic homopolycyclic compounds
External Descriptors
17beta-hydroxy steroid, estradiol (CHEBI:16469) / C18 steroids (estrogens) and derivatives, Estrane and derivatives, Estrogens (C00951) / C18 steroids (estrogens) and derivatives (LMST02010001)

Targets

Details
1. Estrogen receptor alpha
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissu...
Gene Name
ESR1
Uniprot ID
P03372
Uniprot Name
Estrogen receptor
Molecular Weight
66215.45 Da
References
  1. Brama M, Gnessi L, Basciani S, Cerulli N, Politi L, Spera G, Mariani S, Cherubini S, Scotto d'Abusco A, Scandurra R, Migliaccio S: Cadmium induces mitogenic signaling in breast cancer cell by an ERalpha-dependent mechanism. Mol Cell Endocrinol. 2007 Jan 29;264(1-2):102-8. Epub 2006 Nov 27. [PubMed:17125913]
  2. Lehnes K, Winder AD, Alfonso C, Kasid N, Simoneaux M, Summe H, Morgan E, Iann MC, Duncan J, Eagan M, Tavaluc R, Evans CH Jr, Russell R, Wang A, Hu F, Stoica A: The effect of estradiol on in vivo tumorigenesis is modulated by the human epidermal growth factor receptor 2/phosphatidylinositol 3-kinase/Akt1 pathway. Endocrinology. 2007 Mar;148(3):1171-80. Epub 2006 Nov 30. [PubMed:17138652]
  3. Sasson S: Equilibrium binding analysis of estrogen agonists and antagonists: relation to the activation of the estrogen receptor. Pathol Biol (Paris). 1991 Jan;39(1):59-69. [PubMed:2011412]
  4. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Details
2. Estrogen receptor beta
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Agonist
General Function
Zinc ion binding
Specific Function
Nuclear hormone receptor. Binds estrogens with an affinity similar to that of ESR1, and activates expression of reporter genes containing estrogen response elements (ERE) in an estrogen-dependent m...
Gene Name
ESR2
Uniprot ID
Q92731
Uniprot Name
Estrogen receptor beta
Molecular Weight
59215.765 Da
References
  1. Vijayanathan V, Greenfield NJ, Thomas TJ, Ivanova MM, Tyulmenkov VV, Klinge CM, Gallo MA, Thomas T: Effects of estradiol and 4-hydroxytamoxifen on the conformation, thermal stability, and DNA recognition of estrogen receptor beta. Biochem Cell Biol. 2007 Feb;85(1):1-10. [PubMed:17464340]
  2. Sasson S: Equilibrium binding analysis of estrogen agonists and antagonists: relation to the activation of the estrogen receptor. Pathol Biol (Paris). 1991 Jan;39(1):59-69. [PubMed:2011412]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Zinc ion binding
Specific Function
Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism an...
Gene Name
NR1I2
Uniprot ID
O75469
Uniprot Name
Nuclear receptor subfamily 1 group I member 2
Molecular Weight
49761.245 Da
References
  1. Xue Y, Moore LB, Orans J, Peng L, Bencharit S, Kliewer SA, Redinbo MR: Crystal structure of the pregnane X receptor-estradiol complex provides insights into endobiotic recognition. Mol Endocrinol. 2007 May;21(5):1028-38. Epub 2007 Feb 27. [PubMed:17327420]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Ligand-gated ion channel activity
Specific Function
After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeabl...
Gene Name
CHRNA4
Uniprot ID
P43681
Uniprot Name
Neuronal acetylcholine receptor subunit alpha-4
Molecular Weight
69956.47 Da
References
  1. Paradiso K, Zhang J, Steinbach JH: The C terminus of the human nicotinic alpha4beta2 receptor forms a binding site required for potentiation by an estrogenic steroid. J Neurosci. 2001 Sep 1;21(17):6561-8. [PubMed:11517245]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Transcription coactivator activity
Specific Function
Transcriptional coactivator for steroid receptors and nuclear receptors. Coactivator of the steroid binding domain (AF-2) but not of the modulating N-terminal domain (AF-1). Required with NCOA1 to ...
Gene Name
NCOA2
Uniprot ID
Q15596
Uniprot Name
Nuclear receptor coactivator 2
Molecular Weight
159155.645 Da
References
  1. Geistlinger TR, McReynolds AC, Guy RK: Ligand-selective inhibition of the interaction of steroid receptor coactivators and estrogen receptor isoforms. Chem Biol. 2004 Feb;11(2):273-81. [PubMed:15123288]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Steroid hormone binding
Specific Function
G-protein coupled estrogen receptor that binds to 17-beta-estradiol (E2) with high affinity, leading to rapid and transient activation of numerous intracellular signaling pathways. Stimulates cAMP ...
Gene Name
GPER1
Uniprot ID
Q99527
Uniprot Name
G-protein coupled estrogen receptor 1
Molecular Weight
42247.12 Da
References
  1. Thomas P, Dong J: Binding and activation of the seven-transmembrane estrogen receptor GPR30 by environmental estrogens: a potential novel mechanism of endocrine disruption. J Steroid Biochem Mol Biol. 2006 Dec;102(1-5):175-9. Epub 2006 Nov 7. [PubMed:17088055]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Mitochondrial membrane ATP synthase (F(1)F(0) ATP synthase or Complex V) produces ATP from ADP in the presence of a proton gradient across the membrane which is generated by electron transport complexes of the respiratory chain. F-type ATPases consist of two structural domains, F(1) - containing the extramembraneous catalytic core and F(0) - containing the membrane proton channel, linked together by a central stalk and a peripheral stalk. During catalysis, ATP synthesis in the catalytic domain of F(1) is coupled via a rotary mechanism of the central stalk subunits to proton translocation. Key component of the proton channel; it may play a direct role in the translocation of protons across the membrane.
Specific Function
Hydrogen ion transmembrane transporter activity
Gene Name
MT-ATP6
Uniprot ID
P00846
Uniprot Name
ATP synthase subunit a
Molecular Weight
24816.865 Da
References
  1. Van Dorst B, Mehta J, Rouah-Martin E, De Coen W, Blust R, Robbens J: The identification of cellular targets of 17beta estradiol using a lytic (T7) cDNA phage display approach. Toxicol In Vitro. 2011 Feb;25(1):388-93. doi: 10.1016/j.tiv.2010.10.012. Epub 2010 Oct 27. [PubMed:21034808]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Plays a central role in autophagy (PubMed:23184933). Acts as core subunit of the PI3K complex that mediates formation of phosphatidylinositol 3-phosphate; different complex forms are believed to play a role in multiple membrane trafficking pathways: PI3KC3-C1 is involved in initiation of autophagosomes and PI3KC3-C2 in maturation of autophagosomes and endocytosis. Involved in regulation of degradative endocytic trafficking and required for the abcission step in cytokinesis, probably in the context of PI3KC3-C2 (PubMed:20643123, PubMed:20208530). Essential for the formation of PI3KC3-C2 but not PI3KC3-C1 PI3K complex forms. Involved in endocytosis (PubMed:25275521). Protects against infection by a neurovirulent strain of Sindbis virus (PubMed:9765397). May play a role in antiviral host defense.
Specific Function
Phosphatidylinositol 3-kinase binding
Gene Name
BECN1
Uniprot ID
Q14457
Uniprot Name
Beclin-1
Molecular Weight
51895.945 Da
References
  1. Van Dorst B, Mehta J, Rouah-Martin E, De Coen W, Blust R, Robbens J: The identification of cellular targets of 17beta estradiol using a lytic (T7) cDNA phage display approach. Toxicol In Vitro. 2011 Feb;25(1):388-93. doi: 10.1016/j.tiv.2010.10.012. Epub 2010 Oct 27. [PubMed:21034808]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Testosterone dehydrogenase (nad+) activity
Specific Function
Capable of catalyzing the interconversion of testosterone and androstenedione, as well as estradiol and estrone. Also has 20-alpha-HSD activity. Uses NADH while EDH17B3 uses NADPH.
Gene Name
HSD17B2
Uniprot ID
P37059
Uniprot Name
Estradiol 17-beta-dehydrogenase 2
Molecular Weight
42784.75 Da
References
  1. Wetzel M, Marchais-Oberwinkler S, Perspicace E, Moller G, Adamski J, Hartmann RW: Introduction of an electron withdrawing group on the hydroxyphenylnaphthol scaffold improves the potency of 17beta-hydroxysteroid dehydrogenase type 2 (17beta-HSD2) inhibitors. J Med Chem. 2011 Nov 10;54(21):7547-57. doi: 10.1021/jm2008453. Epub 2011 Oct 19. [PubMed:21972996]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Ligand
General Function
Zinc ion binding
Specific Function
Orphan receptor that acts as transcription activator in the absence of bound ligand. Binds specifically to an estrogen response element and activates reporter genes controlled by estrogen response ...
Gene Name
ESRRG
Uniprot ID
P62508
Uniprot Name
Estrogen-related receptor gamma
Molecular Weight
51305.485 Da
References
  1. Babu S, Vellore NA, Kasibotla AV, Dwayne HJ, Stubblefield MA, Uppu RM: Molecular docking of bisphenol A and its nitrated and chlorinated metabolites onto human estrogen-related receptor-gamma. Biochem Biophys Res Commun. 2012 Sep 21;426(2):215-20. doi: 10.1016/j.bbrc.2012.08.065. Epub 2012 Aug 23. [PubMed:22935422]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Lee AJ, Cai MX, Thomas PE, Conney AH, Zhu BT: Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98. [PubMed:12865317]
  3. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
General Function
Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A2
Uniprot ID
P05177
Uniprot Name
Cytochrome P450 1A2
Molecular Weight
58293.76 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Lee AJ, Cai MX, Thomas PE, Conney AH, Zhu BT: Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology. 2003 Aug;144(8):3382-98. [PubMed:12865317]
  3. Hong CC, Tang BK, Hammond GL, Tritchler D, Yaffe M, Boyd NF: Cytochrome P450 1A2 (CYP1A2) activity and risk factors for breast cancer: a cross-sectional study. Breast Cancer Res. 2004;6(4):R352-65. doi: 10.1186/bcr798. Epub 2004 May 7. [PubMed:15217502]
  4. Ren J, Chen GG, Liu Y, Su X, Hu B, Leung BC, Wang Y, Ho RL, Yang S, Lu G, Lee CG, Lai PB: Cytochrome P450 1A2 Metabolizes 17beta-Estradiol to Suppress Hepatocellular Carcinoma. PLoS One. 2016 Apr 19;11(4):e0153863. doi: 10.1371/journal.pone.0153863. eCollection 2016. [PubMed:27093553]
  5. Pollock BG, Wylie M, Stack JA, Sorisio DA, Thompson DS, Kirshner MA, Folan MM, Condifer KA: Inhibition of caffeine metabolism by estrogen replacement therapy in postmenopausal women. J Clin Pharmacol. 1999 Sep;39(9):936-40. [PubMed:10471985]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Drug Interactions: Cytochrome P450 Drug Interaction Table [Link]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid binding
Specific Function
UDPGT is of major importance in the conjugation and subsequent elimination of potentially toxic xenobiotics and endogenous compounds. This isoform glucuronidates bilirubin IX-alpha to form both the...
Gene Name
UGT1A1
Uniprot ID
P22309
Uniprot Name
UDP-glucuronosyltransferase 1-1
Molecular Weight
59590.91 Da
References
  1. Hanioka N, Tanabe N, Jinno H, Tanaka-Kagawa T, Nagaoka K, Naito S, Koeda A, Narimatsu S: Functional characterization of human and cynomolgus monkey UDP-glucuronosyltransferase 1A1 enzymes. Life Sci. 2010 Aug 14;87(7-8):261-8. doi: 10.1016/j.lfs.2010.07.001. Epub 2010 Jul 8. [PubMed:20620155]
  2. Guillemette C, Belanger A, Lepine J: Metabolic inactivation of estrogens in breast tissue by UDP-glucuronosyltransferase enzymes: an overview. Breast Cancer Res. 2004;6(6):246-54. Epub 2004 Sep 27. [PubMed:15535854]
  3. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Vitamin d 24-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1A1
Uniprot ID
P04798
Uniprot Name
Cytochrome P450 1A1
Molecular Weight
58164.815 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]
  2. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256]

Carriers

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

Transporters

Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Quaternary ammonium group transmembrane transporter activity
Specific Function
Mediates tubular uptake of organic compounds from circulation. Mediates the influx of agmatine, dopamine, noradrenaline (norepinephrine), serotonin, choline, famotidine, ranitidine, histamin, creat...
Gene Name
SLC22A2
Uniprot ID
O15244
Uniprot Name
Solute carrier family 22 member 2
Molecular Weight
62579.99 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Secondary active organic cation transmembrane transporter activity
Specific Function
Translocates a broad array of organic cations with various structures and molecular weights including the model compounds 1-methyl-4-phenylpyridinium (MPP), tetraethylammonium (TEA), N-1-methylnico...
Gene Name
SLC22A1
Uniprot ID
O15245
Uniprot Name
Solute carrier family 22 member 1
Molecular Weight
61153.345 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Toxin transporter activity
Specific Function
Mediates potential-dependent transport of a variety of organic cations. May play a significant role in the disposition of cationic neurotoxins and neurotransmitters in the brain.
Gene Name
SLC22A3
Uniprot ID
O75751
Uniprot Name
Solute carrier family 22 member 3
Molecular Weight
61279.485 Da
References
  1. Hayer-Zillgen M, Bruss M, Bonisch H: Expression and pharmacological profile of the human organic cation transporters hOCT1, hOCT2 and hOCT3. Br J Pharmacol. 2002 Jul;136(6):829-36. [PubMed:12110607]
  2. Wu X, Kekuda R, Huang W, Fei YJ, Leibach FH, Chen J, Conway SJ, Ganapathy V: Identity of the organic cation transporter OCT3 as the extraneuronal monoamine transporter (uptake2) and evidence for the expression of the transporter in the brain. J Biol Chem. 1998 Dec 4;273(49):32776-86. [PubMed:9830022]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as taurocholate, the prostaglandins PGD2, PGE1, PGE2, leukotriene C4, thromboxane B2 and iloprost.
Gene Name
SLCO2B1
Uniprot ID
O94956
Uniprot Name
Solute carrier organic anion transporter family member 2B1
Molecular Weight
76709.98 Da
References
  1. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A: Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res. 2001 Sep;18(9):1262-9. [PubMed:11683238]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Kanai N, Lu R, Bao Y, Wolkoff AW, Vore M, Schuster VL: Estradiol 17 beta-D-glucuronide is a high-affinity substrate for oatp organic anion transporter. Am J Physiol. 1996 Feb;270(2 Pt 2):F326-31. [PubMed:8779894]
  2. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [PubMed:8786566]
  3. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Atpase activity, coupled to transmembrane movement of substances
Specific Function
ATP-dependent transporter probably involved in cellular detoxification through lipophilic anion extrusion.
Gene Name
ABCC10
Uniprot ID
Q5T3U5
Uniprot Name
Multidrug resistance-associated protein 7
Molecular Weight
161627.375 Da
References
  1. Chen ZS, Hopper-Borge E, Belinsky MG, Shchaveleva I, Kotova E, Kruh GD: Characterization of the transport properties of human multidrug resistance protein 7 (MRP7, ABCC10). Mol Pharmacol. 2003 Feb;63(2):351-8. [PubMed:12527806]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates saturable uptake of estrone sulfate, dehydroepiandrosterone sulfate and related compounds.
Gene Name
SLC22A11
Uniprot ID
Q9NSA0
Uniprot Name
Solute carrier family 22 member 11
Molecular Weight
59970.945 Da
References
  1. Cha SH, Sekine T, Kusuhara H, Yu E, Kim JY, Kim DK, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of multispecific organic anion transporter 4 expressed in the placenta. J Biol Chem. 2000 Feb 11;275(6):4507-12. [PubMed:10660625]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
Inducer
General Function
Xenobiotic-transporting atpase activity
Specific Function
High-capacity urate exporter functioning in both renal and extrarenal urate excretion. Plays a role in porphyrin homeostasis as it is able to mediates the export of protoporhyrin IX (PPIX) both fro...
Gene Name
ABCG2
Uniprot ID
Q9UNQ0
Uniprot Name
ATP-binding cassette sub-family G member 2
Molecular Weight
72313.47 Da
References
  1. Imai Y, Asada S, Tsukahara S, Ishikawa E, Tsuruo T, Sugimoto Y: Breast cancer resistance protein exports sulfated estrogens but not free estrogens. Mol Pharmacol. 2003 Sep;64(3):610-8. [PubMed:12920197]
  2. Imai Y, Tsukahara S, Ishikawa E, Tsuruo T, Sugimoto Y: Estrone and 17beta-estradiol reverse breast cancer resistance protein-mediated multidrug resistance. Jpn J Cancer Res. 2002 Mar;93(3):231-5. [PubMed:11927002]
  3. Mao Q, Unadkat JD: Role of the breast cancer resistance protein (BCRP/ABCG2) in drug transport--an update. AAPS J. 2015 Jan;17(1):65-82. doi: 10.1208/s12248-014-9668-6. Epub 2014 Sep 19. [PubMed:25236865]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. Tamai I, Nozawa T, Koshida M, Nezu J, Sai Y, Tsuji A: Functional characterization of human organic anion transporting polypeptide B (OATP-B) in comparison with liver-specific OATP-C. Pharm Res. 2001 Sep;18(9):1262-9. [PubMed:11683238]
  2. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Rao US, Fine RL, Scarborough GA: Antiestrogens and steroid hormones: substrates of the human P-glycoprotein. Biochem Pharmacol. 1994 Jul 19;48(2):287-92. [PubMed:7914405]
  2. Kim WY, Benet LZ: P-glycoprotein (P-gp/MDR1)-mediated efflux of sex-steroid hormones and modulation of P-gp expression in vitro. Pharm Res. 2004 Jul;21(7):1284-93. [PubMed:15290871]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. Cha SH, Sekine T, Fukushima JI, Kanai Y, Kobayashi Y, Goya T, Endou H: Identification and characterization of human organic anion transporter 3 expressing predominantly in the kidney. Mol Pharmacol. 2001 May;59(5):1277-86. [PubMed:11306713]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as 17-beta-glucuronosyl estradiol, taurocholate, triiodothyronine (T3), leukotriene C4, dehydroepiandrosterone sulfate (DHEAS), methotre...
Gene Name
SLCO1B3
Uniprot ID
Q9NPD5
Uniprot Name
Solute carrier organic anion transporter family member 1B3
Molecular Weight
77402.175 Da
References
  1. Kullak-Ublick GA, Ismair MG, Stieger B, Landmann L, Huber R, Pizzagalli F, Fattinger K, Meier PJ, Hagenbuch B: Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001 Feb;120(2):525-33. [PubMed:11159893]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Thyroid hormone transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent high affinity transport of organic anions such as the thyroid hormones thyroxine (T4) and rT3. Other potential substrates, such as triiodothyronine (T3), 17-beta-gluc...
Gene Name
SLCO1C1
Uniprot ID
Q9NYB5
Uniprot Name
Solute carrier organic anion transporter family member 1C1
Molecular Weight
78695.625 Da
References
  1. Pizzagalli F, Hagenbuch B, Stieger B, Klenk U, Folkers G, Meier PJ: Identification of a novel human organic anion transporting polypeptide as a high affinity thyroxine transporter. Mol Endocrinol. 2002 Oct;16(10):2283-96. [PubMed:12351693]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
General Function
Thyroid hormone transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent transport of organic anions such as the thyroid hormones T3 (triiodo-L-thyronine), T4 (thyroxine) and rT3, and of estrone-3-sulfate and taurocholate.
Gene Name
SLCO4A1
Uniprot ID
Q96BD0
Uniprot Name
Solute carrier organic anion transporter family member 4A1
Molecular Weight
77192.505 Da
References
  1. Tamai I, Nezu J, Uchino H, Sai Y, Oku A, Shimane M, Tsuji A: Molecular identification and characterization of novel members of the human organic anion transporter (OATP) family. Biochem Biophys Res Commun. 2000 Jun 24;273(1):251-60. [PubMed:10873595]

Drug created on June 13, 2005 07:24 / Updated on September 21, 2018 20:42