Identification
- Summary
Estrone sulfate is an estrogen used as monotherapy or in several combination hormone replacement products for managing menopause symptoms and hormone disorders.
- Generic Name
- Estrone sulfate
- DrugBank Accession Number
- DB04574
- Background
Estrone sulfate (as estropipate) is a form of estrogen. It has several uses such as: alleviate symptoms of menopause as hormone replacement therapy, treatment some types of infertility, treatment of some conditions leading to underdevelopment of female sexual characteristics, treatment of vaginal atrophy, treatment of some types of breast cancer (particularly in men and postmenopausal women), treatment of prostate cancer and prevention of osteoporosis.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Estrone sulfate (DB04574)
- Weight
- Average: 350.429
Monoisotopic: 350.118794504 - Chemical Formula
- C18H22O5S
- Synonyms
- Estra-1,3,5 (10)-triene-17-one-3-yl-sulfate
- Estrone 3-sulfate
- Estrone bisulfate
- Estrone hemisulfate
- Estrone hydrogen sulfate
- Estrone sulphate
- Estrone-3-sulphate
- Estrone, hydrogen sulfate
- External IDs
- US 2917522
- US-2917522
Pharmacology
- Indication
Estropipate is used for the treatment of moderate to severe vasomotor symptoms associated with the monopause, and moderate to severe symptoms of vulval and vaginal atrophy associated with the menopause. It is also used to treat hypoestrogenism due to hypogonadism, castration or primary ovarian failure, and prevent postmenopausal osteoporosis.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Prevention of Postmenopausal osteoporosis •••••••••••• Treatment of Hypoestrogenism •••••••••••• Treatment of Hypoestrogenism •••••••••••• Treatment of Hypoestrogenism •••••••••••• Treatment of Hypoestrogenism •••••••••••• - Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Estropipate is an estrogenic substance. It acts as naturally produced estrogen does. Estrogens act through binding to nuclear receptors in estrogen-responsive tissues. Circulating estrogens modulate the pituitary secretion of the gonadotropins, luteinizing hormone (LH) and follicle stimulating hormone (FSH), through a negative feedback mechanism. Estrogens act to reduce the elevated levels of these hormones seen in postmenopausal women.
- Mechanism of action
Estradiol 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.
Target Actions Organism AEstrogen receptor alpha agonistHumans UEstrogen receptor beta agonistHumans - Absorption
Estropipate is well absorbed through the skin and gastrointestinal tract. When applied for a local action, absorption is usually sufficient to cause systemic effects.
- Volume of distribution
Not Available
- Protein binding
Not Available
- Metabolism
Exogenous estrogens are metabolized in the same manner as endogenous estrogens. Circulating estrogens exist in a dynamic equilibrium of metabolic interconversions. These transformations take place mainly in the liver. Estradiol is converted reversibly to estrone, and both can be converted to estriol, which is the major urinary metabolite. Estrogens also undergo enterohepatic recirculation via sulfate and glucuronide conjugation in the liver, biliary secretion of conjugates into the intestine, and hydrolysis in the gut followed by reabsorption. In postmenopausal women, a significant proportion of the circulating estrogens exist as sulfate conjugates, especially estrone sulfate, which serves as a circulating reservoir for the formation of more active estrogens.
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- Route of elimination
Estradiol, estrone and estriol are excreted in the urine along with glucuronide and sulfate conjugates
- Half-life
Not Available
- Clearance
Not Available
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Not Available
- Pathways
Pathway Category Sulfite Oxidase Deficiency Disease Estrone Metabolism Metabolic Sulfate/Sulfite Metabolism Metabolic 17-beta Hydroxysteroid Dehydrogenase III Deficiency Disease Androgen and Estrogen Metabolism Metabolic Aromatase Deficiency Disease - Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbacavir Abacavir may decrease the excretion rate of Estrone sulfate which could result in a higher serum level. Abametapir The serum concentration of Estrone sulfate can be increased when it is combined with Abametapir. Abatacept The metabolism of Estrone sulfate can be increased when combined with Abatacept. Abciximab Estrone sulfate may decrease the anticoagulant activities of Abciximab. Abemaciclib The excretion of Abemaciclib can be decreased when combined with Estrone sulfate. - Food Interactions
- Take with food. Food decreases nausea.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Estrone sodium sulfate 6K6FDA543A 438-67-5 VUCAHVBMSFIGAI-ZFINNJDLSA-M Estropipate SVI38UY019 7280-37-7 HZEQBCVBILBTEP-ZFINNJDLSA-N Potassium estrone sulfate C354LET0O4 1240-04-6 CUQHOFAEIPGLBH-ZFINNJDLSA-M - Active Moieties
Name Kind UNII CAS InChI Key Estrone prodrug 2DI9HA706A 53-16-7 DNXHEGUUPJUMQT-CBZIJGRNSA-N - Product Images
- International/Other Brands
- ORTHO-EST
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Ogen .625 Tablet 0.75 mg Oral Pfizer Canada Ulc 1994-12-31 2012-08-24 Canada 
Ogen 1.25 Tablet 1.5 mg Oral Pfizer Canada Ulc 1994-12-31 2012-08-24 Canada Ogen 2.5 Tablet 3.0 mg Oral Pfizer Canada Ulc 1994-12-31 2012-08-24 Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Estropipate Tablet 1.5 mg/1 Oral Avera McKennan Hospital 2015-07-07 2017-05-24 US 
Estropipate Tablet 3 mg/1 Oral Actavis Pharma, Inc. 1993-09-23 Not applicable US Estropipate Tablet 1.5 mg/1 Oral Barr Laboratories 1998-01-23 2011-10-31 US Estropipate Tablet 1.5 mg/1 Oral Watson Pharma, Inc. 1993-09-23 2002-06-19 US Estropipate Tablet 0.75 mg/1 Oral Mylan Pharmaceuticals 1999-11-10 2013-06-30 US - Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Eemt D.S. Estrone sodium sulfate (0.625 mg/1) + Methyltestosterone (1.25 mg/1) Tablet, coated Oral Breckenridge Pharmaceutical, Inc. 2003-11-01 2012-01-31 US Eemt H.S. Estrone sodium sulfate (0.625 mg/1) + Methyltestosterone (1.25 mg/1) Tablet, coated Oral Breckenridge Pharmaceutical, Inc. 2003-11-01 2012-01-31 US Esterified Estrogens and Methyltestosterone Estrone sodium sulfate (1.25 mg/1) + Methyltestosterone (2.5 mg/1) Tablet, film coated Oral Tal Pharma Llc 2010-09-17 Not applicable US Esterified Estrogens and Methyltestosterone Estrone sodium sulfate (0.625 mg/1) + Methyltestosterone (1.25 mg/1) Tablet, film coated Oral Tal Pharma Llc 2010-09-17 Not applicable US 
Categories
- Drug Categories
- 17-Ketosteroids
- Adrenal Cortex Hormones
- Contraceptive Agents, Hormonal
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (strength unknown)
- Cytochrome P-450 CYP1A2 Substrates
- Cytochrome P-450 CYP2C9 Inhibitors
- Cytochrome P-450 CYP2C9 Inhibitors (strength unknown)
- Cytochrome P-450 CYP2C9 Substrates
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 Enzyme Inhibitors
- Cytochrome P-450 Substrates
- Drugs that are Mainly Renally Excreted
- Estradiol Congeners
- Estranes
- Estrenes
- Estrogens
- Estrogens, Conjugated (USP)
- Fused-Ring Compounds
- Gonadal Hormones
- Gonadal Steroid Hormones
- Hormonal Contraceptives for Systemic Use
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hyperglycemia-Associated Agents
- Ketosteroids
- MATE 1 Substrates
- MATE 2 Substrates
- MATE substrates
- NTCP Inhibitors
- Reproductive Control Agents
- Steroids
- Thyroxine-binding globulin inducers
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as sulfated steroids. These are sterol lipids containing a sulfate group attached to the steroid skeleton.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Sulfated steroids
- Direct Parent
- Sulfated steroids
- Alternative Parents
- Estrane steroids / 17-oxosteroids / Phenanthrenes and derivatives / Tetralins / Arylsulfates / Sulfuric acid monoesters / Ketones / Organic oxides / Hydrocarbon derivatives
- Substituents
- 17-oxosteroid / Aromatic homopolycyclic compound / Arylsulfate / Benzenoid / Carbonyl group / Estrane-skeleton / Hydrocarbon derivative / Ketone / Organic oxide / Organic oxygen compound
- Molecular Framework
- Aromatic homopolycyclic compounds
- External Descriptors
- steroid sulfate, 17-oxo steroid (CHEBI:17474) / sulfates, C18 steroids (estrogens) and derivatives, Estrogens (C02538) / C18 steroids (estrogens) and derivatives (LMST02010043)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- QTL48N278K
- CAS number
- 481-97-0
- InChI Key
- JKKFKPJIXZFSSB-CBZIJGRNSA-N
- InChI
- InChI=1S/C18H22O5S/c1-18-9-8-14-13-5-3-12(23-24(20,21)22)10-11(13)2-4-15(14)16(18)6-7-17(18)19/h3,5,10,14-16H,2,4,6-9H2,1H3,(H,20,21,22)/t14-,15-,16+,18+/m1/s1
- IUPAC Name
- [(3aS,3bR,9bS,11aS)-11a-methyl-1-oxo-1H,2H,3H,3aH,3bH,4H,5H,9bH,10H,11H,11aH-cyclopenta[a]phenanthren-7-yl]oxidanesulfonic acid
- SMILES
- [H][C@@]12CCC(=O)[C@@]1(C)CC[C@]1([H])C3=C(CC[C@@]21[H])C=C(OS(O)(=O)=O)C=C3
References
- General References
- Not Available
- External Links
- Human Metabolome Database
- HMDB0001425
- KEGG Compound
- C02538
- PubChem Compound
- 3001028
- PubChem Substance
- 46508976
- ChemSpider
- 2272513
- BindingDB
- 50366524
- ChEBI
- 17474
- ChEMBL
- CHEMBL494753
- ZINC
- ZINC000003876186
- PharmGKB
- PA165958342
- RxList
- RxList Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Estropipate
Clinical Trials
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Tablet, coated Oral Tablet, film coated Oral Tablet Oral 0.75 mg/1 Tablet Oral 1.5 mg/1 Tablet Oral 3 mg/1 Tablet Oral 6 mg/1 Tablet, film coated Oral 20.83 mg Cream Vaginal 1.5 mg/1g Tablet Oral 0.75 mg Tablet Oral 1.5 mg Tablet Oral 3.0 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0059 mg/mL ALOGPS logP 0.29 ALOGPS logP 3.83 Chemaxon logS -4.8 ALOGPS pKa (Strongest Acidic) -1.7 Chemaxon pKa (Strongest Basic) -7.5 Chemaxon Physiological Charge -1 Chemaxon Hydrogen Acceptor Count 4 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 80.67 Å2 Chemaxon Rotatable Bond Count 2 Chemaxon Refractivity 89.07 m3·mol-1 Chemaxon Polarizability 36.61 Å3 Chemaxon Number of Rings 4 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter Yes Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.9974 Blood Brain Barrier + 0.935 Caco-2 permeable - 0.8343 P-glycoprotein substrate Non-substrate 0.5376 P-glycoprotein inhibitor I Non-inhibitor 0.5591 P-glycoprotein inhibitor II Non-inhibitor 0.9751 Renal organic cation transporter Non-inhibitor 0.8407 CYP450 2C9 substrate Non-substrate 0.7526 CYP450 2D6 substrate Non-substrate 0.8214 CYP450 3A4 substrate Substrate 0.6275 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9071 CYP450 2D6 inhibitor Non-inhibitor 0.923 CYP450 2C19 inhibitor Non-inhibitor 0.9026 CYP450 3A4 inhibitor Non-inhibitor 0.9421 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8808 Ames test Non AMES toxic 0.5621 Carcinogenicity Carcinogens 0.5507 Biodegradation Not ready biodegradable 0.9558 Rat acute toxicity 2.2402 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.5746 hERG inhibition (predictor II) Inhibitor 0.8077
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 194.2515647 predictedDarkChem Lite v0.1.0 [M-H]- 194.4666647 predictedDarkChem Lite v0.1.0 [M-H]- 193.8859647 predictedDarkChem Lite v0.1.0 [M-H]- 188.28293 predictedDeepCCS 1.0 (2019) [M-H]- 194.2515647 predictedDarkChem Lite v0.1.0 [M-H]- 194.4666647 predictedDarkChem Lite v0.1.0 [M-H]- 193.8859647 predictedDarkChem Lite v0.1.0 [M-H]- 188.28293 predictedDeepCCS 1.0 (2019) [M+H]+ 194.8820647 predictedDarkChem Lite v0.1.0 [M+H]+ 195.0746647 predictedDarkChem Lite v0.1.0 [M+H]+ 195.4949647 predictedDarkChem Lite v0.1.0 [M+H]+ 190.68744 predictedDeepCCS 1.0 (2019) [M+H]+ 194.8820647 predictedDarkChem Lite v0.1.0 [M+H]+ 195.0746647 predictedDarkChem Lite v0.1.0 [M+H]+ 195.4949647 predictedDarkChem Lite v0.1.0 [M+H]+ 190.68744 predictedDeepCCS 1.0 (2019) [M+Na]+ 194.5896647 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.3450647 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.5279647 predictedDarkChem Lite v0.1.0 [M+Na]+ 199.19106 predictedDeepCCS 1.0 (2019) [M+Na]+ 194.5896647 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.3450647 predictedDarkChem Lite v0.1.0 [M+Na]+ 194.5279647 predictedDarkChem Lite v0.1.0 [M+Na]+ 199.19106 predictedDeepCCS 1.0 (2019)
Targets
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Use our structured and evidence-based datasets to unlock newinsights and accelerate drug research.
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- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- 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. [Article]
- 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. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- Curator comments
- Enzyme action based on in vitro data.
- 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
- Egnell AC, Eriksson C, Albertson N, Houston B, Boyer S: Generation and evaluation of a CYP2C9 heteroactivation pharmacophore. J Pharmacol Exp Ther. 2003 Dec;307(3):878-87. Epub 2003 Oct 13. [Article]
- Modugno F, Knoll C, Kanbour-Shakir A, Romkes M: A potential role for the estrogen-metabolizing cytochrome P450 enzymes in human breast carcinogenesis. Breast Cancer Res Treat. 2003 Dec;82(3):191-7. doi: 10.1023/B:BREA.0000004376.21491.44. [Article]
- Daly AK, Rettie AE, Fowler DM, Miners JO: Pharmacogenomics of CYP2C9: Functional and Clinical Considerations. J Pers Med. 2017 Dec 28;8(1). pii: jpm8010001. doi: 10.3390/jpm8010001. [Article]
- Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [Article]
- CYP2C19 and CYP2C9: New aspects of pharmacogenetics and transcriptional regulation [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
- Gene Name
- CYP1A2
- Uniprot ID
- P05177
- Uniprot Name
- Cytochrome P450 1A2
- Molecular Weight
- 58293.76 Da
References
- 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. [Article]
- Cribb AE, Knight MJ, Dryer D, Guernsey J, Hender K, Tesch M, Saleh TM: Role of polymorphic human cytochrome P450 enzymes in estrone oxidation. Cancer Epidemiol Biomarkers Prev. 2006 Mar;15(3):551-8. doi: 10.1158/1055-9965.EPI-05-0801. [Article]
- Ueno T, Tamura S, Frels WI, Shou M, Gonzalez FJ, Kimura S: A transgenic mouse expressing human CYP1A2 in the pancreas. Biochem Pharmacol. 2000 Sep 15;60(6):857-63. [Article]
- Yamazaki H, Shaw PM, Guengerich FP, Shimada T: Roles of cytochromes P450 1A2 and 3A4 in the oxidation of estradiol and estrone in human liver microsomes. Chem Res Toxicol. 1998 Jun;11(6):659-65. doi: 10.1021/tx970217f. [Article]
- CYP1A2 document, cancer.gov [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- 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. [Article]
- Williams ET, Leyk M, Wrighton SA, Davies PJ, Loose DS, Shipley GL, Strobel HW: Estrogen regulation of the cytochrome P450 3A subfamily in humans. J Pharmacol Exp Ther. 2004 Nov;311(2):728-35. Epub 2004 Jul 28. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- O'Connell MB: Pharmacokinetic and pharmacologic variation between different estrogen products. J Clin Pharmacol. 1995 Sep;35(9S):18S-24S. doi: 10.1002/j.1552-4604.1995.tb04143.x. [Article]
- Pardridge WM: Serum bioavailability of sex steroid hormones. Clin Endocrinol Metab. 1986 May;15(2):259-78. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- 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
- O'Connell MB: Pharmacokinetic and pharmacologic variation between different estrogen products. J Clin Pharmacol. 1995 Sep;35(9S):18S-24S. doi: 10.1002/j.1552-4604.1995.tb04143.x. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Monovalent cation:proton antiporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfat...
- Gene Name
- SLC47A1
- Uniprot ID
- Q96FL8
- Uniprot Name
- Multidrug and toxin extrusion protein 1
- Molecular Weight
- 61921.585 Da
References
- Tanihara Y, Masuda S, Sato T, Katsura T, Ogawa O, Inui K: Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H(+)-organic cation antiporters. Biochem Pharmacol. 2007 Jul 15;74(2):359-71. doi: 10.1016/j.bcp.2007.04.010. Epub 2007 Apr 13. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- Curator comments
- Datas supported only by an in vitro study.
- General Function
- Drug transmembrane transporter activity
- Specific Function
- Solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acy...
- Gene Name
- SLC47A2
- Uniprot ID
- Q86VL8
- Uniprot Name
- Multidrug and toxin extrusion protein 2
- Molecular Weight
- 65083.915 Da
References
- Tanihara Y, Masuda S, Sato T, Katsura T, Ogawa O, Inui K: Substrate specificity of MATE1 and MATE2-K, human multidrug and toxin extrusions/H(+)-organic cation antiporters. Biochem Pharmacol. 2007 Jul 15;74(2):359-71. doi: 10.1016/j.bcp.2007.04.010. Epub 2007 Apr 13. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Virus receptor activity
- Specific Function
- The hepatic sodium/bile acid uptake system exhibits broad substrate specificity and transports various non-bile acid organic compounds as well. It is strictly dependent on the extracellular presenc...
- Gene Name
- SLC10A1
- Uniprot ID
- Q14973
- Uniprot Name
- Sodium/bile acid cotransporter
- Molecular Weight
- 38118.64 Da
References
Drug created at September 07, 2007 21:12 / Updated at February 19, 2024 14:23