Identification
- Summary
Conjugated estrogens is a mixture of estrogens used in estrogen replacement therapy for menopause and hypoestrogenism, used in the treatment of various malignancies, and used in the treatment of postmenopausal osteoporosis.
- Brand Names
- Congest, Duavee, Duavive, Premarin, Premphase 28 Day, Prempro 0.625/2.5 28 Day
- Generic Name
- Conjugated estrogens
- DrugBank Accession Number
- DB00286
- Background
The conjugated estrogens are noncrystalline mixtures of purified female sex hormones obtained either by its isolation from the urine of pregnant mares or by synthetic generation from vegetal material. Both of these products are later conjugated to natrium sulfate by ester bonds in order to make them more water soluble.10,7
The conjugated estrogen product contains a mix of estrogen from which about 50% is represented by estrone sulfate followed by 25% of equilin sulfate, 15% of 17-alpha-dehydroequilenin sulfate, 3% of equilenin sulfate, 5% of 17-alpha and 17-beta-dihydroequilenin sulfate, 2% of 17-alpha-estradiolsulfate and 3% of 17-beta-estradiolsulfate. It also presents a large number of unidentified molecules with weak estrogenic activity as well as non-human molecules when it is obtained from pregnant mares urine.7
The conjugated estrogen mixture was approved for marketing in US in 1942 based on the efficacy against certain conditions. However, until 1986 official clinical trials were performed and this product was determined to be effective for the treatment of osteoporosis.9 The currently approved product of conjugated estrogens was developed by Wyeth Ayerst and FDA approved in 2003.11
- Type
- Small Molecule
- Groups
- Approved
- Synonyms
- Conjugated equine estrogens
- Conjugated estrogens
- Estrogens, Conjugated
- Estrogens,conjugated
Pharmacology
- Indication
The conjugated estrogens are indicated for several different conditions including:
- Treatment of moderate to severe vasomotor symptoms due to menopause.
- Treatment of moderate to severe symptoms of vulvar and vaginal atrophy due to menopause.
- Treatment of hypoestrogenism due to hypogonadism, castration or primary ovarian failure.
- Palliative treatment of breast cancer in appropriately selected patients with metastatic disease.
- Palliative treatment of androgen-dependent carcinoma of the prostate.
- Preventive therapy of postmenopausal osteoporosis.2
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Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Treatment of Abnormal uterine bleeding •••••••••••• ••••••••• Treatment of Atrophic vaginitis •••••••••••• •••••• ••••••• •••••••• ••••••• Treatment of Kraurosis vulvae •••••••••••• ••••• Symptomatic treatment of Menopause •••••••••••• ••••••••••• •••••••••••••• ••••••• •••••••• ••••••• Symptomatic treatment of Metastatic breast cancer •••••••••••• •••••• - Associated Therapies
- 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
The binding of estrogens to the estrogen receptor produces the activation of nuclear receptors in order to bind to estrogen response elements in certain target genes. This mechanistic cascade results in histone acetylation, alteration of chromatin conformation and the initiation of transcription of certain specific drugs.10
In preclinical studies, the conjugated estrogens are known to have a similar estrogenic potency than estrone and the equilin components of the conjugated estrogens have similar potency in the liver when compared to bioidentical estradiol.4 It has also been tested and confirmed that conjugated estrogens present a selective estrogen receptor modulator profile which allows it to have a large beneficial effect on the bone and cardiovascular system.5
Clinically, the administration of conjugated estrogens is known to promote vasomotor stability, maintain genitourinary function, and normal growth and development of female sex hormones. It has also been shown to prevent accelerated bone loss by inhibiting bone resorption and restoring the balance of bone resorption. In the hormonal area, it is shown to inhibit luteinizing hormone and decrease the serum concentration of testosterone.8
- Mechanism of action
The conjugated estrogens, equally to the normal physiological estrogen, work by agonistically binding to the estrogen receptors alpha and beta. The estrogen receptors vary in quantity and proportion according to the tissues and hence, the activity of this conjugated estrogens is very variable.2
The activity made by the conjugated estrogens is driven by the increase in the synthesis of DNA, RNA and various proteins in responsive tissues which in order will reduce the release of gonadotropin-releasing hormone, follicle-stimulating hormone and leuteinizing hormone.8
The specific mechanism of action cannot be described only in terms of total estrogenic action as the pharmacokinetic profile, the tissue specificity and the tissue metabolism is different for each component of the product.7
Target Actions Organism AEstrogen receptor beta agonistHumans AEstrogen receptor alpha agonistHumans - Absorption
The conjugated estrogens are well absorbed in the gastrointestinal tract and the maximum plasma concentration of the conjugated estrogens is reached after 7 hours depending on the estrone component.1 The maximal plasma concentration of conjugated estrogens after multiple doses of 0.45 mg is reported to be of 2.6 ng/ml with an AUC in the steady state of 35 ng.h/ml.2 Unconjugated estrogens are known to be cleared from the circulation at a faster rate than their ester forms.3
- Volume of distribution
The physiological distribution of estrogens in the body is very similar to what is seen in endogenous estrogens and hence, it is widely distributed.2 The conjugated estrogens are mainly found in the sex hormone target organs.12
- Protein binding
Conjugated estrogens are bound to plasma proteins and this bound state can represent around 50-80% of the administered dose.8 It circulates in the blood mainly bound to sex-hormone binding globulin and albumin.2
- Metabolism
The conjugated estrogens are metabolized by a number of different pathways. One of the metabolic pathways of the conjugated estrogens is driven by the action of the cytochrome isoenzyme CYP3A4.1 On the other hand, the conjugated estrogens can also be processed by a dynamic equilibrium of metabolic interconversion and sulfate conjugation. Some of the principal metabolic reactions of the conjugated estrogens are driven by the conversion of 17beta-estradiol to estrone and the further change to estriol. A portion of the administered conjugated estrogens will remain in the blood as sulfate conjugates which serve as a circulating reservoir for the generation of new estrogens.2
In the endometrium, equilin is metabolized to 2-hydroxy and 4-hydroxy equilin as well as 2-hydroxy and 4-hydroxy estradiol. This hydroxylation process is very large in various of the components of the conjugated estrogens and hence, the major metabolites in urine are known to be 17-ketosteroid-16-alpha-hydroxy estrone, 16-alpha-hydroxy-17-beta-dihydro equilin and 16-alpha-hydroxy-17-beta-dihydroequilenin.3
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- Route of elimination
The conjugated estrogens are eliminated mainly in the urine.1 In this renal elimination, it is possible to find 17 beta-estradiol, estrone, estriol, as well as the glucuronide and sulfate conjugates of the estrogens.2
- Half-life
The median half-life of the conjugated estrogens is reported to be of 17 hours.1
- Clearance
The reported normal clearance rate for estrogens is of approximately 615 L/m2.6
- Adverse Effects
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The reported oral LD50 in the rat is of more than 5000 mg/kg.13 Serious overdosage symptoms have not been reported. There have been only reports of nausea, vomiting, and withdrawal in bleeding in females.Label
Long-term continuous administration of estrogens is correlated to increased risk on the incidence of carcinomas of the breast, uterus, cervix, vagina, testis, and liver.Label
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- 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 Conjugated estrogens may decrease the excretion rate of Abacavir which could result in a higher serum level. Abametapir The serum concentration of Conjugated estrogens can be increased when it is combined with Abametapir. Abatacept The metabolism of Conjugated estrogens can be increased when combined with Abatacept. Abciximab Conjugated estrogens may decrease the anticoagulant activities of Abciximab. Abemaciclib Abemaciclib may decrease the excretion rate of Conjugated estrogens which could result in a higher serum level. - Food Interactions
- Take with or without food. Consult individual product monograph for specific instructions.
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 Images
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image C.E.S. Tablet 0.625 mg Oral Bausch Health, Canada Inc. 1963-12-31 Not applicable Canada 
C.E.S. Tablets Tablet 0.3 mg Oral Valeant Canada Lp Valeant Canada S.E.C. 1997-03-14 2014-07-30 Canada C.E.S. Tablets Tablet 0.9 mg Oral Valeant Canada Lp Valeant Canada S.E.C. 1997-03-14 2014-07-30 Canada C.E.S. Tablets Tablet 1.25 mg Oral Valeant Canada Lp Valeant Canada S.E.C. 1963-12-31 2014-07-30 Canada Congest Tablet 2.5 mg Oral Laboratoire Riva Inc 1990-12-31 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Apo-conest Tab 0.3mg Tablet 0.3 mg Oral Apotex Corporation 1994-12-31 2009-10-09 Canada Apo-conest Tab 0.625mg Tablet 0.625 mg Oral Apotex Corporation 1994-12-31 2009-10-09 Canada Apo-conest Tab 0.9mg Tablet 0.9 mg Oral Apotex Corporation 1994-12-31 2009-10-09 Canada Apo-conest Tab 1.25mg Tablet 1.25 mg Oral Apotex Corporation 1994-12-31 2009-10-09 Canada Apo-conest Tab 2.5mg Tablet 2.5 mg Oral Apotex Corporation 1994-12-31 2009-10-09 Canada - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Duavee Conjugated estrogens (0.45 mg/1) + Bazedoxifene acetate (20 mg/1) Tablet, film coated Oral U.S. Pharmaceuticals 2013-11-15 Not applicable US 
Duavee Conjugated estrogens (0.45 mg/1) + Bazedoxifene acetate (20 mg/1) Tablet, film coated Oral U.S. Pharmaceuticals 2013-11-15 Not applicable US Duavee Conjugated estrogens (0.45 mg/1) + Bazedoxifene acetate (20 mg/1) Tablet, film coated Oral Wyeth Pharmaceuticals Llc, a Subsidiary of Pfizer Inc. 2013-10-03 Not applicable US Duavive Conjugated estrogens (0.45 mg) + Bazedoxifene (20 mg) Tablet, multilayer, extended release Oral Pfizer Europe Ma Eeig 2016-09-08 Not applicable EU 
DUAVIVE Conjugated estrogens (0.45 MG) + Bazedoxifene (20 MG) Tablet, delayed release Oral Pfizer Europe Ma Eeig 2015-03-31 Not applicable Italy 
- Unapproved/Other Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Esterified Estrogens and Methyltestosterone Conjugated estrogens (0.625 mg/1) + Methyltestosterone (1.25 mg/1) Tablet, film coated Oral Seton Pharmaceuticals 2005-10-10 2017-02-23 US Esterified Estrogens and Methyltestosterone Conjugated estrogens (1.25 mg/1) + Methyltestosterone (2.5 mg/1) Tablet, film coated Oral Seton Pharmaceuticals 2010-05-05 2017-01-26 US
Categories
- ATC Codes
- G03CA57 — Conjugated estrogens
- G03CA — Natural and semisynthetic estrogens, plain
- G03C — ESTROGENS
- G03 — SEX HORMONES AND MODULATORS OF THE GENITAL SYSTEM
- G — GENITO URINARY SYSTEM AND SEX HORMONES
- Drug Categories
- Agents causing angioedema
- BCRP/ABCG2 Substrates
- COMT Substrates
- Cytochrome P-450 CYP1A2 Inhibitors
- Cytochrome P-450 CYP1A2 Inhibitors (weak)
- Cytochrome P-450 CYP1A2 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
- Estrogens
- Estrogens, Conjugated (USP)
- Genito Urinary System and Sex Hormones
- Gonadal Hormones
- Gonadal Steroid Hormones
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Natural and Semisynthetic Estrogens, Plain
- OAT3/SLC22A8 Inhibitors
- OAT3/SLC22A8 Substrates
- OATP1B1/SLCO1B1 Inhibitors
- OATP1B1/SLCO1B1 Substrates
- OATP1B3 substrates
- OATP2B1/SLCO2B1 substrates
- P-glycoprotein substrates
- Sex Hormones and Modulators of the Genital System
- Thyroxine-binding globulin inducers
- Classification
- Not classified
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- IU5QR144QX
- CAS number
- 12126-59-9
References
- Synthesis Reference
- US20020156303
- General References
- Authors unspecified: Conjugated oestrogens/bazedoxifene. Aust Prescr. 2017 Jun;40(3):114-115. doi: 10.18773/austprescr.2017.039. Epub 2017 May 10. [Article]
- Cada DJ, Baker DE: Conjugated estrogens and bazedoxifene. Hosp Pharm. 2014 Mar;49(3):273-83. doi: 10.1310/hpj4903-273. [Article]
- Bhavnani BR: Pharmacokinetics and pharmacodynamics of conjugated equine estrogens: chemistry and metabolism. Proc Soc Exp Biol Med. 1998 Jan;217(1):6-16. [Article]
- Kuhl H: Pharmacology of estrogens and progestogens: influence of different routes of administration. Climacteric. 2005 Aug;8 Suppl 1:3-63. doi: 10.1080/13697130500148875. [Article]
- Cline JM: Assessing the mammary gland of nonhuman primates: effects of endogenous hormones and exogenous hormonal agents and growth factors. Birth Defects Res B Dev Reprod Toxicol. 2007 Apr;80(2):126-46. doi: 10.1002/bdrb.20112. [Article]
- Hembree WC, Bardin CW, Lipsett MB: A study of estrogen metabolic clearance rates and transfer factors. J Clin Invest. 1969 Oct;48(10):1809-19. doi: 10.1172/JCI106147. [Article]
- Lauritzen C. and Studd J. (2005). Current management of the menopause. Taylor and Francis. [ISBN:0-203-62272-3]
- Arthur H. Jeske (2017). Mosby's Dental Drug Reference - E-Book. Elsevier Health Sciences. [ISBN:9780323511216]
- Kelsey J. and Marcus R. (2000). Menopause. Academic Press.
- NIH [Link]
- FDA approvals [Link]
- Pfizer [Link]
- Pfizer Safety Data Sheet [File]
- External Links
- KEGG Drug
- D04070
- PubChem Substance
- 46505680
- ChemSpider
- 9532
- 4099
- ChEBI
- 8389
- ChEMBL
- CHEMBL2106240
- Therapeutic Targets Database
- DNC001150
- PharmGKB
- PA164754789
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Conjugated_estrogens
- FDA label
- Download (434 KB)
- MSDS
- Download (393 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Basic Science Atrophic Vaginitis / Menopause / Urinary Tract Infections, Recurrent 1 4 Completed Basic Science Depression / Perimenopausal Disorder 1 4 Completed Basic Science Female Urogenital Diseases / Genitourinary Disease / Postmenopausal Atrophic Vaginitis / Postmenopausal Syndrome / Vulvo Vaginal Atrophy 1 4 Completed Basic Science Menopause / Pelvic Organ Prolapse (POP) 1 4 Completed Prevention Glucose Homeostasis / Obesity / Postmenopausal Syndrome 1
Pharmacoeconomics
- Manufacturers
- Wyeth pharmaceuticals inc
- Duramed research inc
- Teva womens health inc
- Roche palo alto llc
- Packagers
- Amerisource Health Services Corp.
- Apotheca Inc.
- A-S Medication Solutions LLC
- Cardinal Health
- Caremark LLC
- Comprehensive Consultant Services Inc.
- Dept Health Central Pharmacy
- Direct Dispensing Inc.
- Direct Pharmaceuticals Inc.
- Dispensing Solutions
- Diversified Healthcare Services Inc.
- Duramed
- Group Health Cooperative
- H.E. Butt Grocery Co.
- H.J. Harkins Co. Inc.
- Heartland Repack Services LLC
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Liberty Pharmaceuticals
- Mallinckrodt Inc.
- Martin Surgical Supply
- Mckesson Corp.
- Medvantx Inc.
- Murfreesboro Pharmaceutical Nursing Supply
- Neuman Distributors Inc.
- Noxzema Inc.
- Nucare Pharmaceuticals Inc.
- Patheon Inc.
- PCA LLC
- PD-Rx Pharmaceuticals Inc.
- Pharmaceutical Utilization Management Program VA Inc.
- Pharmacy Service Center
- Pharmedix
- Physicians Total Care Inc.
- Preferred Pharmaceuticals Inc.
- Prepackage Specialists
- Primedics Laboratories
- Remedy Repack
- Resource Optimization and Innovation LLC
- Rite Aid Corp.
- Sandhills Packaging Inc.
- Southwood Pharmaceuticals
- Talbert Medical Management Corp.
- Tya Pharmaceuticals
- Vangard Labs Inc.
- Wyeth Pharmaceuticals
- Dosage Forms
Form Route Strength Tablet Oral 0.3 mg Tablet Oral 0.625 mg Tablet Oral 1.25 mg Tablet Oral 2.5 mg Tablet, film coated Oral Tablet Oral Tablet, multilayer, extended release Oral Tablet, delayed release Oral Tablet, film coated Oral 0.625 mg Tablet, coated Oral 0.3 mg Cream Cream Topical; Vaginal 0.625 mg/1g Injection, powder, lyophilized, for solution Intramuscular; Intravenous 25 mg/5mL Tablet Oral Tablet, extended release Oral 0.3 mg Tablet, extended release Oral 0.625 mg Tablet, extended release Oral 1.25 mg Tablet, film coated Oral 0.3 mg/1 Tablet, film coated Oral 0.45 mg/1 Tablet, film coated Oral 0.625 mg/1 Tablet, film coated Oral 0.9 mg/1 Tablet, film coated Oral 1.25 mg/1 Tablet, film coated Oral 2.5 mg/1 Tablet, sugar coated Oral 0.3 mg/1 Tablet, sugar coated Oral 0.45 mg/1 Tablet, sugar coated Oral 0.625 mg/1 Tablet, sugar coated Oral 0.9 mg/1 Tablet, coated Oral 0.625 mg Cream Vaginal 4.0096 g Cream Topical; Vaginal .625 mg / g Powder, for solution Intramuscular; Intravenous 25 mg / 5 mL Powder, for solution Intramuscular; Intravenous 25 mg / vial Tablet, sugar coated Oral 0.3 mg Tablet Oral 0.9 mg Cream Vaginal 0.625 mg/1g Cream Vaginal 0.625 mg/g Cream Vaginal 0.625 mg / g Cream Vaginal Cream Vaginal 62.5 mg Cream Vaginal 0.0625 g Tablet Oral 20.833 mg Kit Oral Kit; tablet; tablet, sugar coated Oral Kit; tablet Oral Tablet, sugar coated Oral Tablet, coated Oral Cream Vaginal 62.500 mg Granule Oral 2.5 mg/1 Tablet, sugar coated Oral 0.625 mg - Prices
Unit description Cost Unit Premarin 0.625 mg/gm Cream 42.5 gm Tube 134.05USD tube Premarin 25 mg vial 107.54USD vial Premphase 28 0.625-5 mg tablet Disp Pack 69.99USD disp Premarin vaginal cream-appl 3.07USD g Prempro 0.3 mg-1.5 mg tablet 2.34USD tablet Prempro 0.45-1.5 mg tablet 2.34USD tablet Prempro 0.625-2.5 mg tablet 2.34USD tablet Prempro 0.625-5 mg tablet 2.34USD tablet Premarin 0.45 mg tablet 1.97USD tablet Premarin 0.9 mg tablet 1.97USD tablet Premarin 2.5 mg tablet 1.83USD tablet Premarin 2.5 mg Tabs 1.82USD tablet Premarin 0.3 mg tablet 1.42USD tablet Premarin 0.625 mg tablet 1.42USD tablet Premarin 1.25 mg tablet 1.42USD tablet Premarin 0.625 mg/g Cream 0.69USD g C.E.S. 0.625 mg Tablet 0.11USD tablet DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5908638 No 1999-06-01 2015-07-26 US US5547948 No 1996-08-20 2015-01-17 US US5998402 No 1999-12-07 2017-04-04 US US6479535 No 2002-11-12 2019-05-06 US US7138392 No 2006-11-21 2017-04-04 US US7683051 No 2010-03-23 2027-03-10 US US8815934 No 2014-08-26 2019-05-06 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) Can range from 173-282 °C depending of the component Report on carcinogens. 12th edition. NIH. water solubility Soluble 'MSDS' logP 3.7 Hsieh R. et al. 2007. Steroids. pKa 10 Hurwitz AR. and Liu ST. J Pharm Sci. 1977. (based on the average of different estrogens) - Predicted Properties
- Not Available
- Predicted ADMET Features
Property Value Probability Human Intestinal Absorption + 0.997 Blood Brain Barrier + 0.9486 Caco-2 permeable - 0.8738 P-glycoprotein substrate Non-substrate 0.5295 P-glycoprotein inhibitor I Non-inhibitor 0.5198 P-glycoprotein inhibitor II Non-inhibitor 0.9431 Renal organic cation transporter Non-inhibitor 0.8313 CYP450 2C9 substrate Non-substrate 0.7886 CYP450 2D6 substrate Non-substrate 0.8125 CYP450 3A4 substrate Substrate 0.6454 CYP450 1A2 substrate Non-inhibitor 0.8152 CYP450 2C9 inhibitor Non-inhibitor 0.8454 CYP450 2D6 inhibitor Non-inhibitor 0.9026 CYP450 2C19 inhibitor Non-inhibitor 0.8017 CYP450 3A4 inhibitor Non-inhibitor 0.9204 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8461 Ames test Non AMES toxic 0.5177 Carcinogenicity Non-carcinogens 0.5338 Biodegradation Not ready biodegradable 0.6303 Rat acute toxicity 2.3418 LD50, mol/kg Not applicable hERG inhibition (predictor I) Strong inhibitor 0.6053 hERG inhibition (predictor II) Inhibitor 0.7941
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Not Available
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- 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
- Cada DJ, Baker DE: Conjugated estrogens and bazedoxifene. Hosp Pharm. 2014 Mar;49(3):273-83. doi: 10.1310/hpj4903-273. [Article]
- Ropero AB, Eghbali M, Minosyan TY, Tang G, Toro L, Stefani E: Heart estrogen receptor alpha: distinct membrane and nuclear distribution patterns and regulation by estrogen. J Mol Cell Cardiol. 2006 Sep;41(3):496-510. Epub 2006 Jul 28. [Article]
- Stroud FC, Appt SE, Wilson ME, Franke AA, Adams MR, Kaplan JR: Concentrations of isoflavones in macaques consuming standard laboratory monkey diet. J Am Assoc Lab Anim Sci. 2006 Jul;45(4):20-3. [Article]
- Hou NN, Zhu YM, Huang HF: [The expression of estrogen receptor alpha and beta in the intervention of different estrogens in rat bone metabolism]. Fen Zi Xi Bao Sheng Wu Xue Bao. 2006 Aug;39(4):289-96. [Article]
- 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
- Ropero AB, Eghbali M, Minosyan TY, Tang G, Toro L, Stefani E: Heart estrogen receptor alpha: distinct membrane and nuclear distribution patterns and regulation by estrogen. J Mol Cell Cardiol. 2006 Sep;41(3):496-510. Epub 2006 Jul 28. [Article]
- Stroud FC, Appt SE, Wilson ME, Franke AA, Adams MR, Kaplan JR: Concentrations of isoflavones in macaques consuming standard laboratory monkey diet. J Am Assoc Lab Anim Sci. 2006 Jul;45(4):20-3. [Article]
- Hou NN, Zhu YM, Huang HF: [The expression of estrogen receptor alpha and beta in the intervention of different estrogens in rat bone metabolism]. Fen Zi Xi Bao Sheng Wu Xue Bao. 2006 Aug;39(4):289-96. [Article]
- Gouva L, Tsatsoulis A: The role of estrogens in cardiovascular disease in the aftermath of clinical trials. Hormones (Athens). 2004 Jul-Sep;3(3):171-83. [Article]
- Smith MR: Selective estrogen receptor modulators to prevent treatment-related osteoporosis. Rev Urol. 2005;7 Suppl 3:S30-5. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- 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]
- Authors unspecified: Conjugated oestrogens/bazedoxifene. Aust Prescr. 2017 Jun;40(3):114-115. doi: 10.18773/austprescr.2017.039. Epub 2017 May 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Lin Y, Lu P, Tang C, Mei Q, Sandig G, Rodrigues AD, Rushmore TH, Shou M: Substrate inhibition kinetics for cytochrome P450-catalyzed reactions. Drug Metab Dispos. 2001 Apr;29(4 Pt 1):368-74. [Article]
- O'Connell MB, Frye RF, Matzke GR, St Peter JV, Willhite LA, Welch MR, Kowal P, LaValleur J: Effect of conjugated equine estrogens on oxidative metabolism in middle-aged and elderly postmenopausal women. J Clin Pharmacol. 2006 Nov;46(11):1299-307. doi: 10.1177/0091270006292249. [Article]
- CTEP CYP1A2 DOCUMENT [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- O-methyltransferase activity
- Specific Function
- Catalyzes the O-methylation, and thereby the inactivation, of catecholamine neurotransmitters and catechol hormones. Also shortens the biological half-lives of certain neuroactive drugs, like L-DOP...
- Gene Name
- COMT
- Uniprot ID
- P21964
- Uniprot Name
- Catechol O-methyltransferase
- Molecular Weight
- 30036.77 Da
References
- Zhu BT, Wu KY, Wang P, Cai MX, Conney AH: O-methylation of catechol estrogens by human placental catechol-o-methyltransferase: interindividual differences in sensitivity to heat inactivation and to inhibition by dietary polyphenols. Drug Metab Dispos. 2010 Oct;38(10):1892-9. doi: 10.1124/dmd.110.033548. Epub 2010 Jul 6. [Article]
- Jobe SO, Ramadoss J, Koch JM, Jiang Y, Zheng J, Magness RR: Estradiol-17beta and its cytochrome P450- and catechol-O-methyltransferase-derived metabolites stimulate proliferation in uterine artery endothelial cells: role of estrogen receptor-alpha versus estrogen receptor-beta. Hypertension. 2010 Apr;55(4):1005-11. doi: 10.1161/HYPERTENSIONAHA.109.146399. Epub 2010 Mar 8. [Article]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- General Function
- Serine-type endopeptidase inhibitor activity
- Specific Function
- Major thyroid hormone transport protein in serum.
- Gene Name
- SERPINA7
- Uniprot ID
- P05543
- Uniprot Name
- Thyroxine-binding globulin
- Molecular Weight
- 46324.12 Da
References
- CYTOMEL (liothyronine) FDA label [File]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- 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
- Cada DJ, Baker DE: Conjugated estrogens and bazedoxifene. Hosp Pharm. 2014 Mar;49(3):273-83. doi: 10.1310/hpj4903-273. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Binder
- 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
- Cada DJ, Baker DE: Conjugated estrogens and bazedoxifene. Hosp Pharm. 2014 Mar;49(3):273-83. doi: 10.1310/hpj4903-273. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- May act as an inducible transporter in the biliary and intestinal excretion of organic anions. Acts as an alternative route for the export of bile acids and glucuronides from cholestatic hepatocyte...
- Gene Name
- ABCC3
- Uniprot ID
- O15438
- Uniprot Name
- Canalicular multispecific organic anion transporter 2
- Molecular Weight
- 169341.14 Da
References
- Hirohashi T, Suzuki H, Sugiyama Y: Characterization of the transport properties of cloned rat multidrug resistance-associated protein 3 (MRP3). J Biol Chem. 1999 May 21;274(21):15181-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Atpase activity, coupled to transmembrane movement of substances
- Specific Function
- May be an organic anion pump relevant to cellular detoxification.
- Gene Name
- ABCC4
- Uniprot ID
- O15439
- Uniprot Name
- Multidrug resistance-associated protein 4
- Molecular Weight
- 149525.33 Da
References
- Zelcer N, Reid G, Wielinga P, Kuil A, van der Heijden I, Schuetz JD, Borst P: Steroid and bile acid conjugates are substrates of human multidrug-resistance protein (MRP) 4 (ATP-binding cassette C4). Biochem J. 2003 Apr 15;371(Pt 2):361-7. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Transporter activity
- Specific Function
- Mediates export of organic anions and drugs from the cytoplasm. Mediates ATP-dependent transport of glutathione and glutathione conjugates, leukotriene C4, estradiol-17-beta-o-glucuronide, methotre...
- Gene Name
- ABCC1
- Uniprot ID
- P33527
- Uniprot Name
- Multidrug resistance-associated protein 1
- Molecular Weight
- 171589.5 Da
References
- Qian YM, Song WC, Cui H, Cole SP, Deeley RG: Glutathione stimulates sulfated estrogen transport by multidrug resistance protein 1. J Biol Chem. 2001 Mar 2;276(9):6404-11. Epub 2000 Dec 1. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Gao B, Hagenbuch B, Kullak-Ublick GA, Benke D, Aguzzi A, Meier PJ: Organic anion-transporting polypeptides mediate transport of opioid peptides across blood-brain barrier. J Pharmacol Exp Ther. 2000 Jul;294(1):73-9. [Article]
- Kullak-Ublick GA, Fisch T, Oswald M, Hagenbuch B, Meier PJ, Beuers U, Paumgartner G: Dehydroepiandrosterone sulfate (DHEAS): identification of a carrier protein in human liver and brain. FEBS Lett. 1998 Mar 13;424(3):173-6. [Article]
- 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. [Article]
- 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. [Article]
- Kontaxi M, Echkardt U, Hagenbuch B, Stieger B, Meier PJ, Petzinger E: Uptake of the mycotoxin ochratoxin A in liver cells occurs via the cloned organic anion transporting polypeptide. J Pharmacol Exp Ther. 1996 Dec;279(3):1507-13. [Article]
- Pang KS, Wang PJ, Chung AY, Wolkoff AW: The modified dipeptide, enalapril, an angiotensin-converting enzyme inhibitor, is transported by the rat liver organic anion transport protein. Hepatology. 1998 Nov;28(5):1341-6. [Article]
- Bossuyt X, Muller M, Meier PJ: Multispecific amphipathic substrate transport by an organic anion transporter of human liver. J Hepatol. 1996 Nov;25(5):733-8. [Article]
- Hagenbuch B, Adler ID, Schmid TE: Molecular cloning and functional characterization of the mouse organic-anion-transporting polypeptide 1 (Oatp1) and mapping of the gene to chromosome X. Biochem J. 2000 Jan 1;345 Pt 1:115-20. [Article]
- Lee TK, Koh AS, Cui Z, Pierce RH, Ballatori N: N-glycosylation controls functional activity of Oatp1, an organic anion transporter. Am J Physiol Gastrointest Liver Physiol. 2003 Aug;285(2):G371-81. Epub 2003 Apr 17. [Article]
- Kouzuki H, Suzuki H, Ito K, Ohashi R, Sugiyama Y: Contribution of organic anion transporting polypeptide to uptake of its possible substrates into rat hepatocytes. J Pharmacol Exp Ther. 1999 Feb;288(2):627-34. [Article]
- Eckhardt U, Schroeder A, Stieger B, Hochli M, Landmann L, Tynes R, Meier PJ, Hagenbuch B: Polyspecific substrate uptake by the hepatic organic anion transporter Oatp1 in stably transfected CHO cells. Am J Physiol. 1999 Apr;276(4 Pt 1):G1037-42. [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
- Schroeder A, Eckhardt U, Stieger B, Tynes R, Schteingart CD, Hofmann AF, Meier PJ, Hagenbuch B: Substrate specificity of the rat liver Na(+)-bile salt cotransporter in Xenopus laevis oocytes and in CHO cells. Am J Physiol. 1998 Feb;274(2 Pt 1):G370-5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inhibitor
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Not Available
- Gene Name
- SLC22A10
- Uniprot ID
- Q63ZE4
- Uniprot Name
- Solute carrier family 22 member 10
- Molecular Weight
- 60256.57 Da
References
- Youngblood GL, Sweet DH: Identification and functional assessment of the novel murine organic anion transporter Oat5 (Slc22a19) expressed in kidney. Am J Physiol Renal Physiol. 2004 Aug;287(2):F236-44. Epub 2004 Apr 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Ohtsuki S, Kikkawa T, Mori S, Hori S, Takanaga H, Otagiri M, Terasaki T: Mouse reduced in osteosclerosis transporter functions as an organic anion transporter 3 and is localized at abluminal membrane of blood-brain barrier. J Pharmacol Exp Ther. 2004 Jun;309(3):1273-81. Epub 2004 Feb 4. [Article]
- Mori S, Takanaga H, Ohtsuki S, Deguchi T, Kang YS, Hosoya K, Terasaki T: Rat organic anion transporter 3 (rOAT3) is responsible for brain-to-blood efflux of homovanillic acid at the abluminal membrane of brain capillary endothelial cells. J Cereb Blood Flow Metab. 2003 Apr;23(4):432-40. [Article]
- Nagata Y, Kusuhara H, Endou H, Sugiyama Y: Expression and functional characterization of rat organic anion transporter 3 (rOat3) in the choroid plexus. Mol Pharmacol. 2002 May;61(5):982-8. [Article]
- 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. [Article]
- Sweet DH, Miller DS, Pritchard JB, Fujiwara Y, Beier DR, Nigam SK: Impaired organic anion transport in kidney and choroid plexus of organic anion transporter 3 (Oat3 (Slc22a8)) knockout mice. J Biol Chem. 2002 Jul 26;277(30):26934-43. Epub 2002 May 13. [Article]
- Kobayashi Y, Ohshiro N, Tsuchiya A, Kohyama N, Ohbayashi M, Yamamoto T: Renal transport of organic compounds mediated by mouse organic anion transporter 3 (mOat3): further substrate specificity of mOat3. Drug Metab Dispos. 2004 May;32(5):479-83. [Article]
- Kusuhara H, Sekine T, Utsunomiya-Tate N, Tsuda M, Kojima R, Cha SH, Sugiyama Y, Kanai Y, Endou H: Molecular cloning and characterization of a new multispecific organic anion transporter from rat brain. J Biol Chem. 1999 May 7;274(19):13675-80. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- Tohyama K, Kusuhara H, Sugiyama Y: Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier. Endocrinology. 2004 Sep;145(9):4384-91. Epub 2004 May 27. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInhibitor
- 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
- 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. [Article]
- Nozawa T, Tamai I, Sai Y, Nezu J, Tsuji A: Contribution of organic anion transporting polypeptide OATP-C to hepatic elimination of the opioid pentapeptide analogue [D-Ala2, D-Leu5]-enkephalin. J Pharm Pharmacol. 2003 Jul;55(7):1013-20. [Article]
- Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. [Article]
- Hirano M, Maeda K, Shitara Y, Sugiyama Y: Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46. Epub 2004 May 24. [Article]
- Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, Tsuji A, Tamai I: Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos. 2004 Mar;32(3):291-4. [Article]
- Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [Article]
- van Montfoort JE, Schmid TE, Adler ID, Meier PJ, Hagenbuch B: Functional characterization of the mouse organic-anion-transporting polypeptide 2. Biochim Biophys Acta. 2002 Aug 19;1564(1):183-8. [Article]
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- 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. [Article]
- 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. [Article]
- Kobayashi D, Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Involvement of human organic anion transporting polypeptide OATP-B (SLC21A9) in pH-dependent transport across intestinal apical membrane. J Pharmacol Exp Ther. 2003 Aug;306(2):703-8. Epub 2003 Apr 30. [Article]
- Nozawa T, Imai K, Nezu J, Tsuji A, Tamai I: Functional characterization of pH-sensitive organic anion transporting polypeptide OATP-B in human. J Pharmacol Exp Ther. 2004 Feb;308(2):438-45. Epub 2003 Nov 10. [Article]
- Satoh H, Yamashita F, Tsujimoto M, Murakami H, Koyabu N, Ohtani H, Sawada Y: Citrus juices inhibit the function of human organic anion-transporting polypeptide OATP-B. Drug Metab Dispos. 2005 Apr;33(4):518-23. Epub 2005 Jan 7. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Involved in the renal elimination of endogenous and exogenous organic anions. Functions as organic anion exchanger when the uptake of one molecule of organic anion is coupled with an efflux of one ...
- Gene Name
- SLC22A6
- Uniprot ID
- Q4U2R8
- Uniprot Name
- Solute carrier family 22 member 6
- Molecular Weight
- 61815.78 Da
References
- Sweet DH, Miller DS, Pritchard JB, Fujiwara Y, Beier DR, Nigam SK: Impaired organic anion transport in kidney and choroid plexus of organic anion transporter 3 (Oat3 (Slc22a8)) knockout mice. J Biol Chem. 2002 Jul 26;277(30):26934-43. Epub 2002 May 13. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Essential component of the Ost-alpha/Ost-beta complex, a heterodimer that acts as the intestinal basolateral transporter responsible for bile acid export from enterocytes into portal blood. Efficie...
- Gene Name
- SLC51A
- Uniprot ID
- Q86UW1
- Uniprot Name
- Organic solute transporter subunit alpha
- Molecular Weight
- 37734.575 Da
References
- Seward DJ, Koh AS, Boyer JL, Ballatori N: Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82. Epub 2003 Apr 28. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Transporter activity
- Specific Function
- Essential component of the Ost-alpha/Ost-beta complex, a heterodimer that acts as the intestinal basolateral transporter responsible for bile acid export from enterocytes into portal blood. Efficie...
- Gene Name
- SLC51B
- Uniprot ID
- Q86UW2
- Uniprot Name
- Organic solute transporter subunit beta
- Molecular Weight
- 14346.195 Da
References
- Seward DJ, Koh AS, Boyer JL, Ballatori N: Functional complementation between a novel mammalian polygenic transport complex and an evolutionarily ancient organic solute transporter, OSTalpha-OSTbeta. J Biol Chem. 2003 Jul 25;278(30):27473-82. Epub 2003 Apr 28. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Organic anion transmembrane transporter activity
- Specific Function
- Mediates hepatobiliary excretion of numerous organic anions. May function as a cellular cisplatin transporter.
- Gene Name
- ABCC2
- Uniprot ID
- Q92887
- Uniprot Name
- Canalicular multispecific organic anion transporter 1
- Molecular Weight
- 174205.64 Da
References
- Spears KJ, Ross J, Stenhouse A, Ward CJ, Goh LB, Wolf CR, Morgan P, Ayrton A, Friedberg TH: Directional trans-epithelial transport of organic anions in porcine LLC-PK1 cells that co-express human OATP1B1 (OATP-C) and MRP2. Biochem Pharmacol. 2005 Feb 1;69(3):415-23. Epub 2004 Dec 22. [Article]
- Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Purine nucleotide transmembrane transporter activity
- Specific Function
- Participates in physiological processes involving bile acids, conjugated steroids and cyclic nucleotides. Enhances the cellular extrusion of cAMP and cGMP. Stimulates the ATP-dependent uptake of a ...
- Gene Name
- ABCC11
- Uniprot ID
- Q96J66
- Uniprot Name
- ATP-binding cassette sub-family C member 11
- Molecular Weight
- 154299.625 Da
References
- Chen ZS, Guo Y, Belinsky MG, Kotova E, Kruh GD: Transport of bile acids, sulfated steroids, estradiol 17-beta-D-glucuronide, and leukotriene C4 by human multidrug resistance protein 8 (ABCC11). Mol Pharmacol. 2005 Feb;67(2):545-57. Epub 2004 Nov 10. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Cui Y, Konig J, Leier I, Buchholz U, Keppler D: Hepatic uptake of bilirubin and its conjugates by the human organic anion transporter SLC21A6. J Biol Chem. 2001 Mar 30;276(13):9626-30. Epub 2000 Dec 27. [Article]
- 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. [Article]
- Hirano M, Maeda K, Shitara Y, Sugiyama Y: Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004 Oct;311(1):139-46. Epub 2004 May 24. [Article]
- Nozawa T, Sugiura S, Nakajima M, Goto A, Yokoi T, Nezu J, Tsuji A, Tamai I: Involvement of organic anion transporting polypeptides in the transport of troglitazone sulfate: implications for understanding troglitazone hepatotoxicity. Drug Metab Dispos. 2004 Mar;32(3):291-4. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Sodium-independent organic anion transmembrane transporter activity
- Specific Function
- Mediates the Na(+)-independent transport of organic anions such as estrone-3-sulfate (PubMed:10873595). Mediates transport of prostaglandins (PG) E1 and E2, thyroxine (T4), deltorphin II, BQ-123 an...
- Gene Name
- SLCO3A1
- Uniprot ID
- Q9UIG8
- Uniprot Name
- Solute carrier organic anion transporter family member 3A1
- Molecular Weight
- 76552.135 Da
References
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- 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
- Matsushima S, Maeda K, Kondo C, Hirano M, Sasaki M, Suzuki H, Sugiyama Y: Identification of the hepatic efflux transporters of organic anions using double-transfected Madin-Darby canine kidney II cells expressing human organic anion-transporting polypeptide 1B1 (OATP1B1)/multidrug resistance-associated protein 2, OATP1B1/multidrug resistance 1, and OATP1B1/breast cancer resistance protein. J Pharmacol Exp Ther. 2005 Sep;314(3):1059-67. Epub 2005 May 18. [Article]
- Suzuki M, Suzuki H, Sugimoto Y, Sugiyama Y: ABCG2 transports sulfated conjugates of steroids and xenobiotics. J Biol Chem. 2003 Jun 20;278(25):22644-9. Epub 2003 Apr 7. [Article]
- 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. [Article]
Drug created at June 13, 2005 13:24 / Updated at February 20, 2024 23:55