Explore a selection of our essential drug information below, or:
Identification
- Summary
Budesonide is a corticosteroid used to treat Crohn's disease, asthma, COPD, hay fever and allergies, and ulcerative colitis.
- Brand Names
- Airsupra, Breyna, Breztri, Cortiment, Entocort, Eohilia, Pulmicort, Pulmicort Turbuhaler, Rhinocort, Symbicort, Tarpeyo, Uceris
- Generic Name
- Budesonide
- DrugBank Accession Number
- DB01222
- Background
Budesonide is a glucocorticoid that is a mix of the 22R and 22S epimer used to treat inflammatory conditions of the lungs and intestines such as asthma, COPD, Crohn's disease, and ulcerative colitis.5,6
Budesonide was granted FDA approval on 14 February 1994.8 It is also available in a combination product with formoterol.14
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Budesonide (DB01222)
- Weight
- Average: 430.5339
Monoisotopic: 430.23553882 - Chemical Formula
- C25H34O6
- Synonyms
- (11β,16α)-16,17-(Butylidenebis(oxy))-11,21-dihydroxypregna-1,4-diene-3,20-dione
- Budesónida
- Budesonide
- External IDs
- MAP-0010
- MAP0010
- S-1320
Pharmacology
- Indication
Budesonide extended-release capsules are indicated for the treatment and maintenance of mild to moderate Crohn’s disease.9,10 Various inhaled budesonide products are indicated for prophylactic therapy in asthma 11,12,14 and to reduce exacerbations of COPD.14 A budesonide nasal spray is available over the counter for symptoms of hay fever and upper respiratory allergies.13 Extended-release capsules are indicated to induce remission of mild to moderate ulcerative colitis15 and a rectal foam is used for mild to moderate distal ulcerative colitis.16 In addition, a delayed-release capsule formulation of budesonide is indicated to reduce proteinuria in adults with IgA nephropathy at risk of rapid disease progression.18,21 Budesonide is indicated to treat eosinophilic esophagitis (EoE): For this indication, it is only approved for use in adults in Europe 19 while it is approved for short-term use (12 weeks) in patients 11 years of age and older in the US.22
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 Management of Allergic rhinitis •••••••••••• ••••• Management of Allergies ••• ••• ••••• Used in combination to manage Asthma Combination Product in combination with: Formoterol (DB00983) •••••••••••• ••••••• Management of Asthma •••••••••••• ••••••••• •••••••••• Used in combination to manage Asthma Combination Product in combination with: Formoterol (DB00983) •••••••••••• •••••••• - 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
Budesonide is a glucocorticoid used to treat respiratory and digestive conditions by reducing inflammation.9,10,11,12,14,15,16 It has a wide therapeutic index, as dosing varies highly from patient to patient.9,10,11,12,14,15,16 Patients should be counselled regarding the risk of hypercorticism and adrenal axis suppression.9,10,11,12,14,15,16
- Mechanism of action
The short term effects of corticosteroids are decreased vasodilation and permeability of capillaries, as well as decreased leukocyte migration to sites of inflammation.1 Corticosteroids binding to the glucocorticoid receptor mediates changes in gene expression that lead to multiple downstream effects over hours to days.1
Glucocorticoids inhibit neutrophil apoptosis and demargination; they inhibit phospholipase A2, which decreases the formation of arachidonic acid derivatives; they inhibit NF-Kappa B and other inflammatory transcription factors; they promote anti-inflammatory genes like interleukin-10.1
Lower doses of corticosteroids provide an anti-inflammatory effect, while higher doses are immunosuppressive.1 High doses of glucocorticoids for an extended period bind to the mineralocorticoid receptor, raising sodium levels and decreasing potassium levels.1
Target Actions Organism AGlucocorticoid receptor agonistHumans UAnnexin A1 substrateHumans - Absorption
Extended release oral capsules are 9-21% bioavailable.9,10 A 9mg dose reaches a Cmax of 1.50±0.79ng/mL with a Tmax of 2-8h and an AUC of 7.33ng*hr/mL.9,10 A high fat meal increases the Tmax by 2.3h but otherwise does not affect the pharmacokinetics of budesonide.9,10
180-360µg metered inhaled doses of budesonide are 34% deposited in the lungs, 39% bioavailable, and reach a Cmax of 0.6-1.6nmol/L with a Tmax of 10 minutes.11
A 1mg nebulized dose is 6% bioavailable, reaching a Cmax of 2.6nmol/L with a Tmax of 20 minutes.12
A 9mg oral extended release tablet reaches a Cmax of 1.35±0.96ng/mL with a Tmax of 13.3±5.9h and an AUC of 16.43±10.52ng*hr/mL.15
Budesonide rectal foam 2mg twice daily has an AUC of 4.31ng*hr/mL.16
- Volume of distribution
The volume of distribution of budesonide is 2.2-3.9L/kg.9,10,11,12,15,16
- Protein binding
Corticosteroids are generally bound to corticosteroid binding globulin2 and serum albumin3 in plasma. Budesonide is 85-90% protein bound in plasma.9,10,11,12,15,16
- Metabolism
Budesonide is 80-90% metabolized at first pass.4 Budesonide is metabolized by CYP3A to its 2 major metabolites, 6beta-hydroxybudesonide and 16alpha-hydroxyprednisolone.4,7 The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.4 CYP3A4 is the strongest metabolizer of budesonide, followed by CYP3A5, and CYP3A7.7
Hover over products below to view reaction partners
- Route of elimination
Approximately 60% of a budesonide dose is recovered in the urine as the major metabolites 6beta-hydroxybudesonide, 16alpha-hydroxyprednisolone, and their conjugates.9,10,11,12,14,15,16 No unchanged budesonide is recovered in urine.9,10,11,12,14,15,16
- Half-life
Budesonide has a plasma elimination half life of 2-3.6h.9,10,11,15 The terminal elimination half life in asthmatic children 4-6 years old is 2.3h.12
- Clearance
Budesonide has a plasma clearance of 0.9-1.8L/min.9,10,15,16 The 22R form has a clearance of 1.4L/min while the 22S form has a clearance of 1.0L/min.11 The clearance in asthmatic children 4-6 years old is 0.5L/min.12,14
- Adverse Effects
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Acute overdose of corticosteroids is rare, however prolonged high dosing of corticosteroids can lead to hypercorticism and adrenal axis suppression.9,10,11,12,14,15,16 In the case of overdose, reduce the dosage of corticosteroids temporarily.9,10,11,12,14,15,16
A 200mg oral dose is lethal to female mice while a 400mg oral dose is lethal to male mice.9,10,15
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
Interacting Gene/Enzyme Allele name Genotype(s) Defining Change(s) Type(s) Description Details T-box transcription factor TBX21 --- (C;G) CG allele (heterozygotes) Effect Directly Studied The presence of this polymorphism in TBX21 may be associated with improved responsiveness to budenoside for the treatment of asthma. Details
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 Budesonide which could result in a higher serum level. Abametapir The serum concentration of Budesonide can be increased when it is combined with Abametapir. Abatacept The risk or severity of adverse effects can be increased when Budesonide is combined with Abatacept. Abemaciclib The metabolism of Abemaciclib can be increased when combined with Budesonide. Acalabrutinib The metabolism of Acalabrutinib can be increased when combined with Budesonide. - Food Interactions
- Take with or without food. Food delays drug absorption, but not to a clinically significant extent.
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
- International/Other Brands
- Bidien / Budeson / Budicort / Noex (Eurofarma) / Pulmicort (AstraZeneca) / Rhinosol / Spirocort
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Budesonide Capsule 3 mg/1 Oral Padagis US LLC 2018-06-29 Not applicable US 
Budesonide Spray, metered 32 ug/1 Nasal Astra Zeneca Lp 2014-05-13 2018-02-28 US Budesonide Capsule, extended release 3 mg Oral Tillotts Pharma Gmbh 2020-01-17 Not applicable Canada 
Budesonide Aerosol, foam 28 mg/1 Rectal Oceanside Pharmaceuticals 2022-07-15 Not applicable US Cortiment Tablet, extended release 9 mg Oral Ferring Pharmaceuticals 2016-07-25 Not applicable Canada - Generic Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Budesonide Capsule, delayed release 3 mg/1 Oral Mylan Pharmaceuticals Inc. 2011-05-16 2022-08-31 US Budesonide Suspension 0.25 mg/2mL Respiratory (inhalation) Teva Pharmaceuticals USA, Inc. 2008-11-19 Not applicable US Budesonide Aerosol, foam 2 mg/1 Rectal Padagis Israel Pharmaceuticals Ltd 2023-04-17 Not applicable US Budesonide Capsule, delayed release 3 mg/1 Oral bryant ranch prepack 2017-09-15 Not applicable US Budesonide Suspension 1 mg/2mL Respiratory (inhalation) Apotex Corp. 2009-03-30 2009-03-31 US - Over the Counter Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Budesonide Spray, metered 32 ug/1 Nasal Walmart 2016-08-22 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Walgreens 2016-04-11 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal RUGBY LABORATORIES 2016-07-13 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Rite Aid 2016-07-13 Not applicable US Budesonide Spray, metered 32 ug/1 Nasal Apotex Corp. 2018-04-26 Not applicable US - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image AIRBIR 3/100 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 KPS Budesonide (100 mcg) + Arformoterol (3 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey 
AIRBIR 3/100 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 KPS Budesonide (100 mcg) + Arformoterol (3 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey AIRBIR 3/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL ,120 KAPSÜL Budesonide (200 mcg) + Arformoterol (3 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey AIRBIR 3/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL ,60 KAPSÜL Budesonide (200 mcg) + Arformoterol (3 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey AIRBIR 6/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 ADET Budesonide (200 mcg) + Arformoterol (6 mcg) Powder Respiratory (inhalation) NEUTEC İNHALER İLAÇ SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey
Categories
- ATC Codes
- R03AK15 — Salbutamol and budesonide
- R03AK — Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- R03AL — Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- D07AC — Corticosteroids, potent (group III)
- D07A — CORTICOSTEROIDS, PLAIN
- D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
- D — DERMATOLOGICALS
- R01AD — Corticosteroids
- R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
- R01 — NASAL PREPARATIONS
- R — RESPIRATORY SYSTEM
- R03AK — Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- A07EA — Corticosteroids acting locally
- A07E — INTESTINAL ANTIINFLAMMATORY AGENTS
- A07 — ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
- A — ALIMENTARY TRACT AND METABOLISM
- R03BA — Glucocorticoids
- R03B — OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- Drug Categories
- Adrenal Cortex Hormones
- Adrenals
- Agents to Treat Airway Disease
- Alimentary Tract and Metabolism
- Anti-Asthmatic Agents
- Anti-Inflammatory Agents
- Antidiarrheals, Intestinal Antiinflammatory/antiinfective Agents
- Autonomic Agents
- Bronchodilator Agents
- BSEP/ABCB11 Substrates
- Corticosteroid Hormone Receptor Agonists
- Corticosteroids
- Corticosteroids Acting Locally
- Corticosteroids for Systemic Use
- Corticosteroids, Dermatological Preparations
- Corticosteroids, Potent (Group III)
- Cytochrome P-450 CYP2A6 Inducers
- Cytochrome P-450 CYP2B6 Inducers
- Cytochrome P-450 CYP2B6 Inducers (strength unknown)
- Cytochrome P-450 CYP2C19 Inducers
- Cytochrome P-450 CYP2C19 Inducers (strength unknown)
- Cytochrome P-450 CYP2C8 Inducers
- Cytochrome P-450 CYP2C8 Inducers (strength unknown)
- Cytochrome P-450 CYP2C9 Inducers
- Cytochrome P-450 CYP2C9 Inducers (strength unknown)
- Cytochrome P-450 CYP3A Inducers
- Cytochrome P-450 CYP3A Substrates
- Cytochrome P-450 CYP3A4 Inducers
- Cytochrome P-450 CYP3A4 Inducers (strength unknown)
- Cytochrome P-450 CYP3A4 Substrates
- Cytochrome P-450 CYP3A5 Inducers
- Cytochrome P-450 CYP3A5 Inducers (moderate)
- Cytochrome P-450 Enzyme Inducers
- Cytochrome P-450 Substrates
- Dermatologicals
- Drugs for Obstructive Airway Diseases
- Drugs that are Mainly Renally Excreted
- Fused-Ring Compounds
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Immunosuppressive Agents
- Intestinal Antiinflammatory Agents
- Nasal Preparations
- OAT3/SLC22A8 Substrates
- P-glycoprotein substrates
- Peripheral Nervous System Agents
- Pregnanes
- Pregnenediones
- Pregnenes
- Respiratory System Agents
- Steroids
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as 21-hydroxysteroids. These are steroids carrying a hydroxyl group at the 21-position of the steroid backbone.
- Kingdom
- Organic compounds
- Super Class
- Lipids and lipid-like molecules
- Class
- Steroids and steroid derivatives
- Sub Class
- Hydroxysteroids
- Direct Parent
- 21-hydroxysteroids
- Alternative Parents
- Gluco/mineralocorticoids, progestogins and derivatives / 20-oxosteroids / 3-oxo delta-1,4-steroids / 11-beta-hydroxysteroids / Delta-1,4-steroids / Alpha-hydroxy ketones / 1,3-dioxolanes / Secondary alcohols / Cyclic ketones / Cyclic alcohols and derivatives show 5 more
- Substituents
- 11-beta-hydroxysteroid / 11-hydroxysteroid / 20-oxosteroid / 21-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / Acetal / Alcohol / Aliphatic heteropolycyclic compound / Alpha-hydroxy ketone show 17 more
- Molecular Framework
- Aliphatic heteropolycyclic compounds
- External Descriptors
- 11beta-hydroxy steroid, glucocorticoid, cyclic acetal, 20-oxo steroid, 3-oxo-Delta(1),Delta(4)-steroid, 21-hydroxy steroid (CHEBI:3207)
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- Q3OKS62Q6X
- CAS number
- 51333-22-3
- InChI Key
- VOVIALXJUBGFJZ-KWVAZRHASA-N
- InChI
- InChI=1S/C25H34O6/c1-4-5-21-30-20-11-17-16-7-6-14-10-15(27)8-9-23(14,2)22(16)18(28)12-24(17,3)25(20,31-21)19(29)13-26/h8-10,16-18,20-22,26,28H,4-7,11-13H2,1-3H3/t16-,17-,18-,20+,21?,22+,23-,24-,25+/m0/s1
- IUPAC Name
- (1S,2S,4R,8S,9S,11S,12S,13R)-11-hydroxy-8-(2-hydroxyacetyl)-9,13-dimethyl-6-propyl-5,7-dioxapentacyclo[10.8.0.0^{2,9}.0^{4,8}.0^{13,18}]icosa-14,17-dien-16-one
- SMILES
- [H][C@@]12C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@H](O)[C@@]1([H])[C@@]2([H])CCC2=CC(=O)C=C[C@]12C
References
- Synthesis Reference
Peter Gruber, Hans Joachim Lach, Norbert Otterbeck, "Budesonide pellets with a controlled released pattern and process for producing the same." U.S. Patent US5932249, issued May, 1991.
US5932249- General References
- Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
- Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]
- Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]
- O'Donnell S, O'Morain CA: Therapeutic benefits of budesonide in gastroenterology. Ther Adv Chronic Dis. 2010 Jul;1(4):177-86. doi: 10.1177/2040622310379293. [Article]
- Ellul-Micallef R, Hansson E, Johansson SA: Budesonide: a new corticosteroid in bronchial asthma. Eur J Respir Dis. 1980 Jun;61(3):167-73. [Article]
- Roth G, Wikby A, Nilsson L, Thalen A: High-performance liquid chromatographic determination of epimers, impurities, and content of the glucocorticoid budesonide and preparation of primary standard. J Pharm Sci. 1980 Jul;69(7):766-70. doi: 10.1002/jps.2600690705. [Article]
- Moore CD, Roberts JK, Orton CR, Murai T, Fidler TP, Reilly CA, Ward RM, Yost GS: Metabolic pathways of inhaled glucocorticoids by the CYP3A enzymes. Drug Metab Dispos. 2013 Feb;41(2):379-89. doi: 10.1124/dmd.112.046318. Epub 2012 Nov 9. [Article]
- FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Aerosol (Discontinued) [Link]
- FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
- FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
- FDA Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
- FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
- FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Spray [Link]
- FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
- FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
- FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]
- BioSpace News: Viatris Inc. Announces Receipt of the First FDA Approval for Generic Version of Symbicort® Inhalation Aerosol, Breyna™ (Budesonide and Formoterol Fumarate Dihydrate Inhalation Aerosol), in Partnership with Kindeva [Link]
- EMA Approved Drug Products: Kinpeygo (budesonide) Oral Capsules [Link]
- EMA Approved Drug Products: Jorveza (budesonide) Oral Tablets [Link]
- FDA Approved Drug Products: AIRSUPRA (albuterol and budesonide) inhalation aerosol, for oral inhalation use [Link]
- FDA Approved Drug Products: TARPEYO (budesonide) delayed release capsules, for oral use (December 2023) [Link]
- FDA Approved Drug Products: EOHILIA (budesonide) oral suspension [Link]
- External Links
- Human Metabolome Database
- HMDB0015353
- KEGG Drug
- D00246
- PubChem Compound
- 5281004
- PubChem Substance
- 46504869
- ChemSpider
- 4444479
- BindingDB
- 50354850
- 19831
- ChEBI
- 3207
- ChEMBL
- CHEMBL1370
- Therapeutic Targets Database
- DAP000320
- PharmGKB
- PA448681
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- PDRhealth
- PDRhealth Drug Page
- Wikipedia
- Budesonide
- FDA label
- Download (52.3 KB)
- MSDS
- Download (73.7 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Chronic Obstructive Pulmonary Disease (COPD) 2 somestatus stop reason just information to hide Not Available Completed Not Available Asthma 6 somestatus stop reason just information to hide Not Available Completed Not Available Asthma / Chronic Obstructive Pulmonary Disease (COPD) 1 somestatus stop reason just information to hide Not Available Completed Not Available Chronic Obstructive (MeSH) / Lung Disorder / Retrospective Studies 1 somestatus stop reason just information to hide Not Available Completed Not Available Crohn's Disease (CD) / Inflammatory Bowel Diseases (IBD) 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- 3M Health Care
- A-S Medication Solutions LLC
- Astra Pharma Inc.
- AstraZeneca Inc.
- Dispensing Solutions
- Galderma Laboratories
- Ivax Pharmaceuticals
- Kaiser Foundation Hospital
- Lake Erie Medical and Surgical Supply
- Physicians Total Care Inc.
- Prometheus Laboratories Inc.
- Redpharm Drug
- Spectrum Pharmaceuticals
- Teva Pharmaceutical Industries Ltd.
- Dosage Forms
Form Route Strength Aerosol; suspension Respiratory (inhalation) 200 mcg Aerosol; suspension Respiratory (inhalation) 400 mcg Spray Nasal 100 MICROGRAMMI Spray Nasal 50 MICROGRAMMI Spray Nasal 50 UG Aerosol Buccal 50 mcg Aerosol Buccal 5000000 mcg Solution Nasal; Respiratory (inhalation) 0.1 g Aerosol Oral; Respiratory (inhalation) 0.3256 % Ointment Topical 25 mg Capsule, delayed release Oral 3 MG Aerosol Respiratory (inhalation) 200 cg Suspension Nasal 0.640 mg Spray, suspension Nasal 50 mcg/1dose Spray Nasal 1.28 mg Spray, metered Nasal Lotion Topical 0.025 g Cream Topical 0025 % Ointment Cutaneous 0025 % Solution Topical 0025 % Spray, suspension Respiratory (inhalation) 0.25 MG/ML Spray, suspension Respiratory (inhalation) 0.5 MG/ML Powder Respiratory (inhalation) Aerosol, metered Respiratory (inhalation) Solution Nasal; Respiratory (inhalation) 80 mg Suspension Buccal; Respiratory (inhalation) 400 cg Suspension Respiratory (inhalation) 0.05 mg Spray Nasal 0.05 mg/0.051g Aerosol, metered Respiratory (inhalation) Aerosol Respiratory (inhalation) 0.2 % w/v Aerosol Respiratory (inhalation) 0.132 g Aerosol Respiratory (inhalation) 0.263 g Suspension Respiratory (inhalation) 0.025 % w/v Spray, metered Nasal 32 mcg Spray, metered Nasal 64 mcg Spray Nasal 0.128 %w/v Capsule, coated Oral 3 mg Capsule 3 mg Suppository 4 mg Capsule Oral 3 mg Aerosol, foam Rectal 2 mg/1dose Aerosol, foam Rectal 2 mg Aerosol Rectal 2 mg Aerosol Rectal 200000 mg Suspension Respiratory (inhalation) 0.25 mg/1ml Suspension Respiratory (inhalation) 0.5 mg/1ml Gas Respiratory (inhalation) 0.2 MG Spray Nasal 32 UG Spray Nasal 64 UG Spray Nasal 0.05 mg/0.051mL Solution; suspension Respiratory (inhalation) 0.25 MG/ML Solution; suspension Respiratory (inhalation) 0.5 MG/ML Aerosol Respiratory (inhalation) 0.25 g Aerosol, powder Respiratory (inhalation) 0.2 MG Aerosol, powder Respiratory (inhalation) 0.4 MG Aerosol, powder Respiratory (inhalation) 0.1 MG Suspension Respiratory (inhalation) 0.5 mg Suspension Respiratory (inhalation) 0.022 g Suspension Respiratory (inhalation) 1 mg Suspension Respiratory (inhalation) 200 cg Aerosol Respiratory (inhalation) 200 mcg Suspension Respiratory (inhalation) 0.4 g Suspension Respiratory (inhalation) 0.01 g Suspension Oral 0.1 mg Aerosol, foam Rectal 2 mg/1 Capsule, coated pellets Oral 3 mg/1 Capsule, delayed release Oral 3 mg/1 Inhalant Respiratory (inhalation) 0.25 mg/2mL Inhalant Respiratory (inhalation) 0.5 mg/2mL Powder Not applicable 1 g/1g Suspension Respiratory (inhalation) 1 mg/2mL Tablet, extended release Oral 9 mg/1 Tablet, film coated, extended release Oral 9 mg/1 Capsule, delayed release pellets Oral 3 mg/1 Aerosol Respiratory (inhalation) 0.25 MG/ML Aerosol Respiratory (inhalation) 0.5 MG/ML Inhalant Oral 0.25 mg/2mL Inhalant Oral 0.5 mg/2mL Inhalant Oral 1 mg/2mL Spray, suspension Nasal 64 mcg/dose Suspension Respiratory (inhalation) 25 MG/ML Suspension Respiratory (inhalation) 5 MG/ML Suspension Respiratory (inhalation) 0.25 MG/ML Suspension Respiratory (inhalation) 0.5 MG/ML Aerosol, powder Respiratory (inhalation) 200 mcg Suspension Respiratory (inhalation) 100 mcg/1dose Suspension Respiratory (inhalation) 200 mcg/1dose Aerosol Respiratory (inhalation) 100 mcg Suspension Buccal; Respiratory (inhalation) 40 mg Suspension Buccal; Respiratory (inhalation) 4000000 mg Suspension Respiratory (inhalation) 200 mcg Aerosol, metered Respiratory (inhalation) 200 MICROGRAMMI Solution Respiratory (inhalation) 200 mcg Gas Respiratory (inhalation) 0.2 mg/1 Aerosol, metered Respiratory (inhalation) 200 Mikrogramm Gas Respiratory (inhalation) 200 UG Aerosol, metered Respiratory (inhalation) 0.2 mg/actuation Aerosol, foam Rectal 2 mg/spray Granule, delayed release Oral 9 mg Spray, suspension Nasal 32 mcg Spray, suspension Nasal 64 mcg Suspension Buccal 23.000 mg Suspension 0.25 MG/ML Capsule Spray Nasal 64 mcg Solution Respiratory (inhalation) Suspension Nasal; Respiratory (inhalation) 100 cg Suspension Oral 200 cg Aerosol Respiratory (inhalation) 0.3125 g Aerosol Respiratory (inhalation) 0.4 mg Tablet, extended release Oral 9 mg Tablet Oral 9.000 mg Tablet, extended release Oral 900000 mg Tablet, film coated, extended release Oral 9 mg Capsule Respiratory (inhalation) 0.2 mg/1 Capsule Respiratory (inhalation) 0.4 mg/1 Suspension Respiratory (inhalation) 0.500 mg Capsule Respiratory (inhalation) Capsule, coated Oral 0.4 mg Capsule, coated Oral 0.1 mg Powder, metered Respiratory (inhalation) 160 mcg/inhalation Powder, metered Respiratory (inhalation) 320 mcg/inhalation Spray, suspension Nasal Capsule, extended release Oral 3 mg Tablet Rectal 0.02 mg/ml Enema; tablet Rectal 2.3 mg Capsule Oral 3 mg/1 Enema; kit; tablet Rectal 2.3 mg Tablet, soluble Oral 2.3 mg Suspension Oral 2 mg/10mL Spray Nasal 2.0 mg/ml Capsule Respiratory (inhalation) Suspension Respiratory (inhalation) 0.250 mg Suspension Nasal 1.280 mg Powder Respiratory (inhalation) 400 mcg/1dose Powder, metered Respiratory (inhalation) 200 mcg/dose Powder Respiratory (inhalation) 100 mcg/1dose Powder Respiratory (inhalation) Powder, metered Respiratory (inhalation) 100 mcg Powder, metered Respiratory (inhalation) 200 mcg Aerosol Respiratory (inhalation) 4 mg Solution Respiratory (inhalation) 4 mg Solution Respiratory (inhalation) 1 mg Aerosol, metered Respiratory (inhalation) 50 mcg Suspension Nasal; Respiratory (inhalation) 100 mcg Suspension Respiratory (inhalation) 0.2 mg Granule Tablet, orally disintegrating Oral 0.5 mg Tablet, orally disintegrating Oral 1 mg Capsule Oral 4 mg Capsule, extended release Oral 4 mg Suspension Respiratory (inhalation) 1.000 mg Cream Topical 0.25 g Aerosol, metered Respiratory (inhalation) 200 MCG Powder, metered Respiratory (inhalation) 400 MCG Capsule Buccal 200.000 mcg Capsule Respiratory (inhalation) 200 Mikrogramm Capsule Respiratory (inhalation) 200 UG Capsule Respiratory (inhalation) 400 Mikrogramm Capsule Respiratory (inhalation) 400 UG Capsule, liquid filled Oral 200 cg Capsule, coated Respiratory (inhalation) 400 mcg Spray, metered Nasal 100 mcg / act Spray, metered Nasal 64 mcg / act Suspension Intrasinal; Respiratory (inhalation) 1 mg Suspension Intrasinal; Respiratory (inhalation) 2 mg Suspension Nasal 1.28 mg Powder Respiratory (inhalation) 200 Mikrogramm Powder Respiratory (inhalation) 400 Mikrogramm Powder, metered Respiratory (inhalation) 200 mcg/1dose Capsule Oral 6 mg/1 Capsule Oral 9 mg/1 Suspension 0.50 MG/ML Cream Topical Ointment Powder Respiratory (inhalation) 100 MCG Powder Respiratory (inhalation) 200 MCG Powder Respiratory (inhalation) 400 MCG Spray, suspension Respiratory (inhalation) 0125 MG/ML Aerosol, powder Respiratory (inhalation) Aerosol, powder Respiratory (inhalation) 180 ug/1 Aerosol, powder Respiratory (inhalation) 90 ug/1 Spray Nasal 64 μg Suspension Respiratory (inhalation) 0.125 mg / mL Suspension Respiratory (inhalation) 0.25 mg / mL Suspension Respiratory (inhalation) 0.5 mg / mL Aerosol Respiratory (inhalation) 0.25 MG Aerosol Respiratory (inhalation) 0.5 MG Aerosol; solution Respiratory (inhalation) 0.25 MG/ML Aerosol; solution Respiratory (inhalation) 0.5 MG/ML Suspension Respiratory (inhalation) 0.25 mg/2mL Suspension Respiratory (inhalation) 0.5 mg/2mL Aerosol Respiratory (inhalation) 0.5 mg/2ml Aerosol Respiratory (inhalation) 1 mg/2ml Solution Respiratory (inhalation) 500 mcg/2ml Solution Respiratory (inhalation) 1 mg/2ml Aerosol, powder Respiratory (inhalation) 200 UG Aerosol, powder Respiratory (inhalation) 400 UG Powder Respiratory (inhalation) 0.1 mg Powder Buccal 100 mcg Powder Respiratory (inhalation) 200 mcg/1dose Powder, metered Respiratory (inhalation) 100 mcg / act Powder, metered Respiratory (inhalation) 200 ug/1 Powder, metered Respiratory (inhalation) 200 mcg / act Powder, metered Respiratory (inhalation) 400 mcg / act Aerosol, metered Respiratory (inhalation) 100 MCG Powder Respiratory (inhalation) 100 cg Powder Respiratory (inhalation) 200 cg Powder Respiratory (inhalation) 400 cg Capsule Oral 200 mcg Powder Nasal Spray Nasal Spray, metered Nasal 32 ug/1 Suspension Respiratory (inhalation) 1.28 mg Spray, suspension Nasal 1.28 mg/mL Aerosol, metered Nasal 100 mcg / act Powder Nasal; Respiratory (inhalation) 100 mcg / act Powder, metered Nasal 100 mcg Solution Respiratory (inhalation) 40 mg Aerosol Buccal 4.285 mg Solution Respiratory (inhalation) 48 % w/w Capsule, coated Respiratory (inhalation) 0.1 mg Aerosol, metered Respiratory (inhalation) 200 mcg/1dose Suspension Respiratory (inhalation) 0.25 mg Powder, metered Respiratory (inhalation) Spray, suspension Respiratory (inhalation) Aerosol Respiratory (inhalation) Aerosol, metered; suspension Respiratory (inhalation) Suspension Respiratory (inhalation) Aerosol, metered Respiratory (inhalation) 160 mcg Aerosol, metered Respiratory (inhalation) 40 mcg Aerosol, metered Respiratory (inhalation) 80 mcg Suspension Buccal; Respiratory (inhalation) Powder Buccal Powder, metered Respiratory (inhalation) 160 mcg Powder, metered Respiratory (inhalation) 80 mcg Powder, metered Respiratory (inhalation) Kit Cutaneous Capsule, delayed release Oral 4 mg/1 Solution Respiratory (inhalation) 0.4 g Aerosol Respiratory (inhalation) 0.01 g Suspension Respiratory (inhalation) 0.1 g Suspension Nasal; Respiratory (inhalation) 0.2 % w/v Suspension Nasal; Respiratory (inhalation) 0.2 g Suspension Respiratory (inhalation) 0.50 MG/ML Suspension Buccal Aerosol, foam Rectal 28 mg/1 Kit Rectal 2 mg / act Aerosol Buccal Aerosol Buccal 100 mcg Aerosol Respiratory (inhalation) 100 mcg/1dose Aerosol Respiratory (inhalation) 50 mcg/1dose Spray Nasal 100 mcg/1dose Capsule Respiratory (inhalation) 100 mcg Capsule Respiratory (inhalation) 400 mcg Spray Nasal 1.28 mg/mL Capsule Respiratory (inhalation) 200 mcg Spray Nasal 32 mcg/1dose Spray, suspension Nasal 64 mcg/1dose Aerosol Respiratory (inhalation) 200 mcg/1dose - Prices
Unit description Cost Unit Budesonide micronized powder 346.5USD g DesOwen Lot w/Cetaphil Cream 0.05% Kit Box 255.84USD box Desowen 0.05% ointment kit 217.2USD kit Desowen 0.05% cream kit 212.4USD kit DesOwen 0.05% Lotion 118ml Bottle 183.17USD bottle Pulmicort Flexhaler 180 mcg/act Aerosol Inhaler 163.34USD inhaler Pulmicort 180 mcg flexhaler 157.06USD inhaler DesOwen 0.05% Lotion 59ml Bottle 123.38USD bottle Pulmicort Flexhaler 90 mcg/act Aerosol Inhaler 121.98USD inhaler Pulmicort 90 mcg flexhaler 117.29USD inhaler Rhinocort Aqua 32 mcg/act 8.6 gm Bottle 111.96USD bottle Rhinocort aqua nasal spray 13.93USD g Entocort EC 3 mg 24 Hour Capsule 13.86USD capsule Entocort ec 3 mg capsule 12.22USD capsule Budesonide 0.5 mg/2ml Suspension 2ml Plastic Container 9.73USD plastic Pulmicort 0.5 mg/2ml Suspension 2ml Plastic Container 9.24USD plastic Budesonide 0.25 mg/2ml Suspension 2ml Plastic Container 9.07USD plastic Entocort (115 Ml) 2.3 mg/enm Enema 8.93USD enema Pulmicort 1 mg/2 ml respule 8.89USD ml Pulmicort 0.25 mg/2ml Suspension 2ml Plastic Container 7.85USD plastic Pulmicort 0.5 mg/2 ml respule 4.45USD ml Pulmicort 0.25 mg/2 ml respul 3.78USD ml Desowen 0.05% cream 2.43USD g Pulmicort Nebuamp 0.5 mg/ml Suspension 0.93USD ml Pulmicort Turbuhaler 400 mcg/dose Metered Inhalation Powder 0.62USD dose Pulmicort Nebuamp 0.25 mg/ml Suspension 0.46USD ml Pulmicort Turbuhaler 200 mcg/dose Metered Inhalation Powder 0.34USD dose Pulmicort Nebuamp 0.125 mg/ml Suspension 0.23USD ml Pulmicort Turbuhaler 100 mcg/dose Metered Inhalation Powder 0.17USD dose Rhinocort Turbuhaler 100 mcg/dose Metered Dose Aerosol 0.13USD dose Mylan-Budesonide Aq 100 mcg/dose Metered Dose Spray 0.1USD dose DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US6423340 No 2002-07-23 2010-11-15 US CA2071518 No 2002-11-12 2010-11-15 Canada US6598603 Yes 2003-07-29 2019-06-23 US US6899099 Yes 2005-05-31 2019-06-23 US US7524834 Yes 2009-04-28 2019-05-11 US US7759328 Yes 2010-07-20 2023-07-29 US US7897646 Yes 2011-03-01 2019-03-09 US US8143239 Yes 2012-03-27 2023-07-29 US US8461211 Yes 2013-06-11 2019-03-09 US US8575137 Yes 2013-11-05 2023-07-29 US US6123924 No 2000-09-26 2017-09-26 US US7967011 Yes 2011-06-28 2022-02-11 US US8616196 Yes 2013-12-31 2029-10-07 US US8387615 Yes 2013-03-05 2025-05-10 US US7587988 Yes 2009-09-15 2026-10-10 US US7367333 Yes 2008-05-06 2019-05-11 US US8528545 Yes 2013-09-10 2029-04-16 US US8875699 Yes 2014-11-04 2025-05-10 US US6027714 No 2000-02-22 2018-01-09 US US7143764 No 2006-12-05 2018-03-13 US US6142145 No 2000-11-07 2018-05-08 US US6287540 No 2001-09-11 2018-01-09 US US9320716 No 2016-04-26 2020-06-09 US US9192581 No 2015-11-24 2031-09-07 US US7410651 No 2008-08-12 2020-06-09 US USRE43799 No 2012-11-13 2020-06-09 US US8895064 No 2014-11-25 2031-09-07 US US7431943 No 2008-10-07 2020-06-09 US US9132093 No 2015-09-15 2031-09-07 US US8784888 No 2014-07-22 2020-06-09 US US8293273 No 2012-10-23 2020-06-09 US US5914122 No 1999-06-22 2015-12-19 US US9532954 No 2017-01-03 2020-06-09 US US9463161 No 2016-10-11 2030-05-28 US US9415009 No 2016-08-16 2030-05-28 US US8808713 No 2014-08-19 2030-05-28 US US8324266 No 2012-12-04 2030-05-28 US US8703806 No 2014-04-22 2030-05-28 US US8815258 No 2014-08-26 2031-03-17 US US10064878 No 2018-09-04 2020-06-09 US US10105374 No 2018-10-23 2020-06-09 US US10166247 Yes 2019-01-01 2023-07-29 US US10143698 No 2018-12-04 2020-06-09 US US9707182 No 2017-07-18 2036-09-09 US US10172802 No 2019-01-08 2036-09-09 US US10307375 No 2019-06-04 2031-09-07 US US10660858 No 2020-05-26 2031-09-07 US US10716753 No 2020-07-21 2030-05-28 US US8491932 No 2013-07-23 2029-05-07 US US11311558 Yes 2003-07-29 2023-07-29 US US11331442 No 2018-05-10 2038-05-10 US US11833292 No 2018-10-05 2038-10-05 US US11896719 No 2023-01-23 2043-01-23 US US9119863 No 2006-11-09 2026-11-09 US US8975243 No 2006-11-09 2026-11-09 US US8497258 No 2006-11-09 2026-11-09 US US8324192 No 2009-08-03 2029-08-03 US US11564934 No 2019-01-10 2039-01-10 US US11357859 No 2008-11-12 2028-11-12 US US11197822 No 2006-11-09 2026-11-09 US US11413296 No 2006-11-09 2026-11-09 US US10293052 No 2008-11-22 2028-11-22 US US11260064 No 2019-01-10 2039-01-10 US US8679545 No 2006-11-09 2026-11-09 US US9050368 No 2009-08-01 2029-08-01 US
Properties
- State
- Solid
- Experimental Properties
Property Value Source melting point (°C) 226°C PhysProp boiling point (°C) 599.7 ChemSpider logP 1.914 ChemSpider - Predicted Properties
Property Value Source Water Solubility 0.0457 mg/mL ALOGPS logP 2.42 ALOGPS logP 2.73 Chemaxon logS -4 ALOGPS pKa (Strongest Acidic) 13.75 Chemaxon pKa (Strongest Basic) -2.9 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 6 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 93.06 Å2 Chemaxon Rotatable Bond Count 4 Chemaxon Refractivity 116.11 m3·mol-1 Chemaxon Polarizability 46.88 Å3 Chemaxon Number of Rings 5 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 + 0.9872 Blood Brain Barrier + 0.9533 Caco-2 permeable - 0.6097 P-glycoprotein substrate Substrate 0.804 P-glycoprotein inhibitor I Non-inhibitor 0.5881 P-glycoprotein inhibitor II Non-inhibitor 0.5911 Renal organic cation transporter Non-inhibitor 0.7867 CYP450 2C9 substrate Non-substrate 0.8488 CYP450 2D6 substrate Non-substrate 0.9116 CYP450 3A4 substrate Substrate 0.7337 CYP450 1A2 substrate Non-inhibitor 0.9046 CYP450 2C9 inhibitor Non-inhibitor 0.9075 CYP450 2D6 inhibitor Non-inhibitor 0.9441 CYP450 2C19 inhibitor Non-inhibitor 0.939 CYP450 3A4 inhibitor Inhibitor 0.796 CYP450 inhibitory promiscuity Low CYP Inhibitory Promiscuity 0.8886 Ames test Non AMES toxic 0.9117 Carcinogenicity Non-carcinogens 0.9466 Biodegradation Not ready biodegradable 0.9759 Rat acute toxicity 2.1601 LD50, mol/kg Not applicable hERG inhibition (predictor I) Weak inhibitor 0.9483 hERG inhibition (predictor II) Non-inhibitor 0.5627
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Adduct CCS Value (Å2) Source type Source [M-H]- 215.9174337 predictedDarkChem Lite v0.1.0 [M-H]- 216.9685337 predictedDarkChem Lite v0.1.0 [M-H]- 210.0115337 predictedDarkChem Lite v0.1.0 [M-H]- 204.13078 predictedDeepCCS 1.0 (2019) [M+H]+ 215.4578337 predictedDarkChem Lite v0.1.0 [M+H]+ 216.0536337 predictedDarkChem Lite v0.1.0 [M+H]+ 210.2206337 predictedDarkChem Lite v0.1.0 [M+H]+ 206.01816 predictedDeepCCS 1.0 (2019) [M+Na]+ 215.6822337 predictedDarkChem Lite v0.1.0 [M+Na]+ 215.6190337 predictedDarkChem Lite v0.1.0 [M+Na]+ 212.47716 predictedDeepCCS 1.0 (2019)
Targets
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- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor for glucocorticoids (GC) (PubMed:27120390, PubMed:37478846). Has a dual mode of action: as a transcription factor that binds to glucocorticoid response elements (GRE), both for nuclear and mitochondrial DNA, and as a modulator of other transcription factors (PubMed:28139699). Affects inflammatory responses, cellular proliferation and differentiation in target tissues. Involved in chromatin remodeling (PubMed:9590696). Plays a role in rapid mRNA degradation by binding to the 5' UTR of target mRNAs and interacting with PNRC2 in a ligand-dependent manner which recruits the RNA helicase UPF1 and the mRNA-decapping enzyme DCP1A, leading to RNA decay (PubMed:25775514). Could act as a coactivator for STAT5-dependent transcription upon growth hormone (GH) stimulation and could reveal an essential role of hepatic GR in the control of body growth (By similarity)
- Specific Function
- Core promoter sequence-specific dna binding
- Gene Name
- NR3C1
- Uniprot ID
- P04150
- Uniprot Name
- Glucocorticoid receptor
- Molecular Weight
- 85658.57 Da
References
- Zhang X, Moilanen E, Kankaanranta H: Enhancement of human eosinophil apoptosis by fluticasone propionate, budesonide, and beclomethasone. Eur J Pharmacol. 2000 Oct 20;406(3):325-32. [Article]
- Henriksson G, Norlander T, Forsgren J, Stierna P: Effects of topical budesonide treatment on glucocorticoid receptor mRNA down-regulation and cytokine patterns in nasal polyps. Am J Rhinol. 2001 Jan-Feb;15(1):1-8. [Article]
- Zhang X, Moilanen E, Kankaanranta H: Beclomethasone, budesonide and fluticasone propionate inhibit human neutrophil apoptosis. Eur J Pharmacol. 2001 Nov 23;431(3):365-71. [Article]
- Kompella UB, Bandi N, Ayalasomayajula SP: Subconjunctival nano- and microparticles sustain retinal delivery of budesonide, a corticosteroid capable of inhibiting VEGF expression. Invest Ophthalmol Vis Sci. 2003 Mar;44(3):1192-201. [Article]
- Kunz S, Sandoval R, Carlsson P, Carlstedt-Duke J, Bloom JW, Miesfeld RL: Identification of a novel glucocorticoid receptor mutation in budesonide-resistant human bronchial epithelial cells. Mol Endocrinol. 2003 Dec;17(12):2566-82. Epub 2003 Aug 14. [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
- Substrate
- General Function
- Plays important roles in the innate immune response as effector of glucocorticoid-mediated responses and regulator of the inflammatory process. Has anti-inflammatory activity (PubMed:8425544). Plays a role in glucocorticoid-mediated down-regulation of the early phase of the inflammatory response (By similarity). Contributes to the adaptive immune response by enhancing signaling cascades that are triggered by T-cell activation, regulates differentiation and proliferation of activated T-cells (PubMed:17008549). Promotes the differentiation of T-cells into Th1 cells and negatively regulates differentiation into Th2 cells (PubMed:17008549). Has no effect on unstimulated T cells (PubMed:17008549). Negatively regulates hormone exocytosis via activation of the formyl peptide receptors and reorganization of the actin cytoskeleton (PubMed:19625660). Has high affinity for Ca(2+) and can bind up to eight Ca(2+) ions (By similarity). Displays Ca(2+)-dependent binding to phospholipid membranes (PubMed:2532504, PubMed:8557678). Plays a role in the formation of phagocytic cups and phagosomes. Plays a role in phagocytosis by mediating the Ca(2+)-dependent interaction between phagosomes and the actin cytoskeleton (By similarity)
- Specific Function
- Cadherin binding involved in cell-cell adhesion
- Gene Name
- ANXA1
- Uniprot ID
- P04083
- Uniprot Name
- Annexin A1
- Molecular Weight
- 38713.855 Da
References
- Serres M, Viac J, Comera C, Schmitt D: Expression of annexin I in freshly isolated human epidermal cells and in cultured keratinocytes. Arch Dermatol Res. 1994;286(5):268-72. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)
- Specific Function
- Aromatase activity
- Gene Name
- CYP3A5
- Uniprot ID
- P20815
- Uniprot Name
- Cytochrome P450 3A5
- Molecular Weight
- 57108.065 Da
References
- 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]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- SubstrateInducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
Components:
| Name | UniProt ID |
|---|---|
| Cytochrome P450 3A4 | P08684 |
| Cytochrome P450 3A43 | Q9HB55 |
| Cytochrome P450 3A5 | P20815 |
| Cytochrome P450 3A7 | P24462 |
References
- Roberts JK, Moore CD, Romero EG, Ward RM, Yost GS, Reilly CA: Regulation of CYP3A genes by glucocorticoids in human lung cells. F1000Res. 2013 Aug 13;2:173. doi: 10.12688/f1000research.2-173.v2. eCollection 2013. [Article]
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity
- Specific Function
- Arachidonic acid epoxygenase activity
- Gene Name
- CYP2A6
- Uniprot ID
- P11509
- Uniprot Name
- Cytochrome P450 2A6
- Molecular Weight
- 56517.005 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:15258110, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:10681376, PubMed:11555828, PubMed:12865317, PubMed:15258110, PubMed:20972997). Exhibits catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2- and 4-hydroxy E1 and E2. Displays a predominant hydroxylase activity toward E2 at the C-4 position (PubMed:11555828, PubMed:12865317). Metabolizes testosterone and progesterone to B or D ring hydroxylated metabolites (PubMed:10426814). May act as a major enzyme for all-trans retinoic acid biosynthesis in extrahepatic tissues. Catalyzes two successive oxidative transformation of all-trans retinol to all-trans retinal and then to the active form all-trans retinoic acid (PubMed:10681376, PubMed:15258110). Catalyzes the epoxidation of double bonds of certain PUFA. Converts arachidonic acid toward epoxyeicosatrienoic acid (EpETrE) regioisomers, 8,9-, 11,12-, and 14,15- EpETrE, that function as lipid mediators in the vascular system (PubMed:20972997). Additionally, displays dehydratase activity toward oxygenated eicosanoids hydroperoxyeicosatetraenoates (HpETEs). This activity is independent of cytochrome P450 reductase, NADPH, and O2 (PubMed:21068195). Also involved in the oxidative metabolism of xenobiotics, particularly converting polycyclic aromatic hydrocarbons and heterocyclic aryl amines procarcinogens to DNA-damaging products (PubMed:10426814). Plays an important role in retinal vascular development. Under hyperoxic O2 conditions, promotes retinal angiogenesis and capillary morphogenesis, likely by metabolizing the oxygenated products generated during the oxidative stress. Also, contributes to oxidative homeostasis and ultrastructural organization and function of trabecular meshwork tissue through modulation of POSTN expression (By similarity)
- Specific Function
- Aromatase activity
- Gene Name
- CYP1B1
- Uniprot ID
- Q16678
- Uniprot Name
- Cytochrome P450 1B1
- Molecular Weight
- 60845.33 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of endocannabinoids and steroids (PubMed:12865317, PubMed:21289075). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the epoxidation of double bonds of arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:21289075). Hydroxylates steroid hormones, including testosterone at C-16 and estrogens at C-2 (PubMed:12865317, PubMed:21289075). Plays a role in the oxidative metabolism of xenobiotics, including plant lipids and drugs (PubMed:11695850, PubMed:22909231). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850)
- Specific Function
- Anandamide 11,12 epoxidase activity
- Gene Name
- CYP2B6
- Uniprot ID
- P20813
- Uniprot Name
- Cytochrome P450 2B6
- Molecular Weight
- 56277.81 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:11093772, PubMed:14559847, PubMed:15766564, PubMed:19965576, PubMed:7574697). Primarily catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) with a preference for the last double bond (PubMed:15766564, PubMed:19965576, PubMed:7574697). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes all trans-retinoic acid toward its 4-hydroxylated form (PubMed:11093772). Displays 16-alpha hydroxylase activity toward estrogen steroid hormones, 17beta-estradiol (E2) and estrone (E1) (PubMed:14559847). Plays a role in the oxidative metabolism of xenobiotics. It is the principal enzyme responsible for the metabolism of the anti-cancer drug paclitaxel (taxol) (PubMed:26427316)
- Specific Function
- Arachidonic acid epoxygenase activity
- Gene Name
- CYP2C8
- Uniprot ID
- P10632
- Uniprot Name
- Cytochrome P450 2C8
- Molecular Weight
- 55824.275 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids and steroids (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:12865317, PubMed:15766564, PubMed:19965576, PubMed:21576599, PubMed:7574697, PubMed:9435160, PubMed:9866708). Catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) (PubMed:15766564, PubMed:19965576, PubMed:7574697, PubMed:9866708). Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes cholesterol toward 25-hydroxycholesterol, a physiological regulator of cellular cholesterol homeostasis (PubMed:21576599). Exhibits low catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes bisallylic hydroxylation and hydroxylation with double-bond migration of polyunsaturated fatty acids (PUFA) (PubMed:9435160, PubMed:9866708). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). Contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenytoin, tolbutamide and losartan (PubMed:25994031)
- Specific Function
- (r)-limonene 6-monooxygenase activity
- Gene Name
- CYP2C9
- Uniprot ID
- P11712
- Uniprot Name
- Cytochrome P450 2C9
- Molecular Weight
- 55627.365 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Inducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of polyunsaturated fatty acids (PUFA) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase) (PubMed:18577768, PubMed:19965576, PubMed:20972997). Catalyzes the hydroxylation of carbon-hydrogen bonds. Hydroxylates PUFA specifically at the omega-1 position (PubMed:18577768). Catalyzes the epoxidation of double bonds of PUFA (PubMed:19965576, PubMed:20972997). Also metabolizes plant monoterpenes such as limonene. Oxygenates (R)- and (S)-limonene to produce carveol and perillyl alcohol (PubMed:11950794). 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 imipramine. Hydroxylates fenbendazole at the 4' position (PubMed:23959307)
- Specific Function
- (r)-limonene 6-monooxygenase activity
- Gene Name
- CYP2C19
- Uniprot ID
- P33261
- Uniprot Name
- Cytochrome P450 2C19
- Molecular Weight
- 55944.565 Da
References
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- SubstrateInducer
- General Function
- A cytochrome P450 monooxygenase involved in the metabolism of sterols, steroid hormones, retinoids and fatty acids (PubMed:10681376, PubMed:11093772, PubMed:11555828, PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:19965576, PubMed:20702771, PubMed:21490593, PubMed:21576599). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:12865317, PubMed:14559847, PubMed:15373842, PubMed:15764715, PubMed:21490593, PubMed:21576599, PubMed:2732228). Exhibits high catalytic activity for the formation of hydroxyestrogens from estrone (E1) and 17beta-estradiol (E2), namely 2-hydroxy E1 and E2, as well as D-ring hydroxylated E1 and E2 at the C-16 position (PubMed:11555828, PubMed:12865317, PubMed:14559847). Plays a role in the metabolism of androgens, particularly in oxidative deactivation of testosterone (PubMed:15373842, PubMed:15764715, PubMed:22773874, PubMed:2732228). Metabolizes testosterone to less biologically active 2beta- and 6beta-hydroxytestosterones (PubMed:15373842, PubMed:15764715, PubMed:2732228). Contributes to the formation of hydroxycholesterols (oxysterols), particularly A-ring hydroxylated cholesterol at the C-4beta position, and side chain hydroxylated cholesterol at the C-25 position, likely contributing to cholesterol degradation and bile acid biosynthesis (PubMed:21576599). Catalyzes bisallylic hydroxylation of polyunsaturated fatty acids (PUFA) (PubMed:9435160). Catalyzes the epoxidation of double bonds of PUFA with a preference for the last double bond (PubMed:19965576). Metabolizes endocannabinoid arachidonoylethanolamide (anandamide) to 8,9-, 11,12-, and 14,15-epoxyeicosatrienoic acid ethanolamides (EpETrE-EAs), potentially modulating endocannabinoid system signaling (PubMed:20702771). Plays a role in the metabolism of retinoids. Displays high catalytic activity for oxidation of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376). Further metabolizes atRA toward 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Responsible for oxidative metabolism of xenobiotics. Acts as a 2-exo-monooxygenase for plant lipid 1,8-cineole (eucalyptol) (PubMed:11159812). Metabolizes the majority of the administered drugs. Catalyzes sulfoxidation of the anthelmintics albendazole and fenbendazole (PubMed:10759686). Hydroxylates antimalarial drug quinine (PubMed:8968357). Acts as a 1,4-cineole 2-exo-monooxygenase (PubMed:11695850). Also involved in vitamin D catabolism and calcium homeostasis. Catalyzes the inactivation of the active hormone calcitriol (1-alpha,25-dihydroxyvitamin D(3)) (PubMed:29461981)
- Specific Function
- 1,8-cineole 2-exo-monooxygenase activity
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
References
- Jonsson G, Astrom A, Andersson P: Budesonide is metabolized by cytochrome P450 3A (CYP3A) enzymes in human liver. Drug Metab Dispos. 1995 Jan;23(1):137-42. [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]
- Chen N, Cui D, Wang Q, Wen Z, Finkelman RD, Welty D: In vitro drug-drug interactions of budesonide: inhibition and induction of transporters and cytochrome P450 enzymes. Xenobiotica. 2018 Jun;48(6):637-646. doi: 10.1080/00498254.2017.1344911. Epub 2017 Jul 21. [Article]
- Zimmermann C, van Waterschoot RA, Harmsen S, Maier A, Gutmann H, Schinkel AH: PXR-mediated induction of human CYP3A4 and mouse Cyp3a11 by the glucocorticoid budesonide. Eur J Pharm Sci. 2009 Mar 2;36(4-5):565-71. doi: 10.1016/j.ejps.2008.12.007. Epub 2008 Dec 24. [Article]
- Usui T, Saitoh Y, Komada F: Induction of CYP3As in HepG2 cells by several drugs. Association between induction of CYP3A4 and expression of glucocorticoid receptor. Biol Pharm Bull. 2003 Apr;26(4):510-7. doi: 10.1248/bpb.26.510. [Article]
- Pichard L, Fabre I, Daujat M, Domergue J, Joyeux H, Maurel P: Effect of corticosteroids on the expression of cytochromes P450 and on cyclosporin A oxidase activity in primary cultures of human hepatocytes. Mol Pharmacol. 1992 Jun;41(6):1047-55. [Article]
- Matoulkova P, Pavek P, Maly J, Vlcek J: Cytochrome P450 enzyme regulation by glucocorticoids and consequences in terms of drug interaction. Expert Opin Drug Metab Toxicol. 2014 Mar;10(3):425-35. doi: 10.1517/17425255.2014.878703. Epub 2014 Jan 23. [Article]
- FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
- FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
- FDA Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
- FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
- FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Spray [Link]
- FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
- FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
- FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]
Carriers
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species
- Specific Function
- Serine-type endopeptidase inhibitor activity
- Gene Name
- SERPINA6
- Uniprot ID
- P08185
- Uniprot Name
- Corticosteroid-binding globulin
- Molecular Weight
- 45140.49 Da
References
- Gardill BR, Vogl MR, Lin HY, Hammond GL, Muller YA: Corticosteroid-binding globulin: structure-function implications from species differences. PLoS One. 2012;7(12):e52759. doi: 10.1371/journal.pone.0052759. Epub 2012 Dec 26. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Binder
- General Function
- Binds water, Ca(2+), Na(+), K(+), fatty acids, hormones, bilirubin and drugs (Probable). Its main function is the regulation of the colloidal osmotic pressure of blood (Probable). Major zinc transporter in plasma, typically binds about 80% of all plasma zinc (PubMed:19021548). Major calcium and magnesium transporter in plasma, binds approximately 45% of circulating calcium and magnesium in plasma (By similarity). Potentially has more than two calcium-binding sites and might additionally bind calcium in a non-specific manner (By similarity). The shared binding site between zinc and calcium at residue Asp-273 suggests a crosstalk between zinc and calcium transport in the blood (By similarity). The rank order of affinity is zinc > calcium > magnesium (By similarity). Binds to the bacterial siderophore enterobactin and inhibits enterobactin-mediated iron uptake of E.coli from ferric transferrin, and may thereby limit the utilization of iron and growth of enteric bacteria such as E.coli (PubMed:6234017). Does not prevent iron uptake by the bacterial siderophore aerobactin (PubMed:6234017)
- Specific Function
- Antioxidant activity
- Gene Name
- ALB
- Uniprot ID
- P02768
- Uniprot Name
- Albumin
- Molecular Weight
- 69365.94 Da
References
- Czock D, Keller F, Rasche FM, Haussler U: Pharmacokinetics and pharmacodynamics of systemically administered glucocorticoids. Clin Pharmacokinet. 2005;44(1):61-98. doi: 10.2165/00003088-200544010-00003. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Catalyzes the transport of the major hydrophobic bile salts, such as taurine and glycine-conjugated cholic acid across the canalicular membrane of hepatocytes in an ATP-dependent manner, therefore participates in hepatic bile acid homeostasis and consequently to lipid homeostasis through regulation of biliary lipid secretion in a bile salts dependent manner (PubMed:15791618, PubMed:16332456, PubMed:18985798, PubMed:19228692, PubMed:20010382, PubMed:20398791, PubMed:22262466, PubMed:24711118, PubMed:29507376, PubMed:32203132). Transports taurine-conjugated bile salts more rapidly than glycine-conjugated bile salts (PubMed:16332456). Also transports non-bile acid compounds, such as pravastatin and fexofenadine in an ATP-dependent manner and may be involved in their biliary excretion (PubMed:15901796, PubMed:18245269)
- Specific Function
- Abc-type bile acid transporter activity
- Gene Name
- ABCB11
- Uniprot ID
- O95342
- Uniprot Name
- Bile salt export pump
- Molecular Weight
- 146405.83 Da
References
- Pedersen JM, Matsson P, Bergstrom CA, Hoogstraate J, Noren A, LeCluyse EL, Artursson P: Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11). Toxicol Sci. 2013 Dec;136(2):328-43. doi: 10.1093/toxsci/kft197. Epub 2013 Sep 6. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- Translocates drugs and phospholipids across the membrane (PubMed:2897240, PubMed:35970996, PubMed:8898203, PubMed:9038218). Catalyzes the flop of phospholipids from the cytoplasmic to the exoplasmic leaflet of the apical membrane. Participates mainly to the flop of phosphatidylcholine, phosphatidylethanolamine, beta-D-glucosylceramides and sphingomyelins (PubMed:8898203). Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells (PubMed:2897240, PubMed:35970996, PubMed:9038218)
- Specific Function
- Abc-type xenobiotic transporter activity
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- ATP-dependent translocase ABCB1
- Molecular Weight
- 141477.255 Da
References
- Chen N, Cui D, Wang Q, Wen Z, Finkelman RD, Welty D: In vitro drug-drug interactions of budesonide: inhibition and induction of transporters and cytochrome P450 enzymes. Xenobiotica. 2018 Jun;48(6):637-646. doi: 10.1080/00498254.2017.1344911. Epub 2017 Jul 21. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Na(+)-independent transporter that mediates the cellular uptake of a broad range of organic anions such as the endogenous bile salts cholate and deoxycholate, either in their unconjugated or conjugated forms (taurocholate and glycocholate), at the plasmam membrane (PubMed:19129463, PubMed:7557095). Responsible for intestinal absorption of bile acids (By similarity). Transports dehydroepiandrosterone 3-sulfate (DHEAS), a major circulating steroid secreted by the adrenal cortex, as well as estrone 3-sulfate and 17beta-estradiol 17-O-(beta-D-glucuronate) (PubMed:11159893, PubMed:12568656, PubMed:19129463, PubMed:23918469, PubMed:25560245, PubMed:9539145). Mediates apical uptake of all-trans-retinol (atROL) across human retinal pigment epithelium, which is essential to maintaining the integrity of the visual cycle and thus vision (PubMed:25560245). Involved in the uptake of clinically used drugs (PubMed:17301733, PubMed:20686826, PubMed:27777271). Capable of thyroid hormone transport (both T3 or 3,3',5'-triiodo-L-thyronine, and T4 or L-tyroxine) (PubMed:19129463, PubMed:20358049). Also transports prostaglandin E2 (PubMed:19129463). Plays roles in blood-brain and -cerebrospinal fluid barrier transport of organic anions and signal mediators, and in hormone uptake by neural cells (By similarity). May also play a role in the reuptake of neuropeptides such as substance P/TAC1 and vasoactive intestinal peptide/VIP released from retinal neurons (PubMed:25132355). May play an important role in plasma and tissue distribution of the structurally diverse chemotherapeutic drugs methotrexate and paclitaxel (PubMed:23243220). Shows a pH-sensitive substrate specificity which may be ascribed to the protonation state of the binding site and leads to a stimulation of substrate transport in an acidic microenvironment (PubMed:19129463). Hydrogencarbonate/HCO3(-) acts as the probable counteranion that exchanges for organic anions (PubMed:19129463). May contribute to regulate the transport of organic compounds in testis across the blood-testis-barrier (Probable)
- Specific Function
- Bile acid transmembrane transporter activity
- Gene Name
- SLCO1A2
- Uniprot ID
- P46721
- Uniprot Name
- Solute carrier organic anion transporter family member 1A2
- Molecular Weight
- 74144.105 Da
References
- 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]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Functions as an organic anion/dicarboxylate exchanger that couples organic anion uptake indirectly to the sodium gradient (PubMed:14586168, PubMed:15644426, PubMed:15846473, PubMed:16455804, PubMed:31553721). Transports organic anions such as estrone 3-sulfate (E1S) and urate in exchange for dicarboxylates such as glutarate or ketoglutarate (2-oxoglutarate) (PubMed:14586168, PubMed:15846473, PubMed:15864504, PubMed:22108572, PubMed:23832370). Plays an important role in the excretion of endogenous and exogenous organic anions, especially from the kidney and the brain (PubMed:11306713, PubMed:14586168, PubMed:15846473). E1S transport is pH- and chloride-dependent and may also involve E1S/cGMP exchange (PubMed:26377792). Responsible for the transport of prostaglandin E2 (PGE2) and prostaglandin F2(alpha) (PGF2(alpha)) in the basolateral side of the renal tubule (PubMed:11907186). Involved in the transport of neuroactive tryptophan metabolites kynurenate and xanthurenate (PubMed:22108572, PubMed:23832370). Functions as a biopterin transporters involved in the uptake and the secretion of coenzymes tetrahydrobiopterin (BH4), dihydrobiopterin (BH2) and sepiapterin to urine, thereby determining baseline levels of blood biopterins (PubMed:28534121). May be involved in the basolateral transport of steviol, a metabolite of the popular sugar substitute stevioside (PubMed:15644426). May participate in the detoxification/ renal excretion of drugs and xenobiotics, such as the histamine H(2)-receptor antagonists fexofenadine and cimetidine, the antibiotic benzylpenicillin (PCG), the anionic herbicide 2,4-dichloro-phenoxyacetate (2,4-D), the diagnostic agent p-aminohippurate (PAH), the antiviral acyclovir (ACV), and the mycotoxin ochratoxin (OTA), by transporting these exogenous organic anions across the cell membrane in exchange for dicarboxylates such as 2-oxoglutarate (PubMed:11669456, PubMed:15846473, PubMed:16455804). Contributes to the renal uptake of potent uremic toxins (indoxyl sulfate (IS), indole acetate (IA), hippurate/N-benzoylglycine (HA) and 3-carboxy-4-methyl-5-propyl-2-furanpropionate (CMPF)), pravastatin, PCG, E1S and dehydroepiandrosterone sulfate (DHEAS), and is partly involved in the renal uptake of temocaprilat (an angiotensin-converting enzyme (ACE) inhibitor) (PubMed:14675047). May contribute to the release of cortisol in the adrenals (PubMed:15864504). Involved in one of the detoxification systems on the choroid plexus (CP), removes substrates such as E1S or taurocholate (TC), PCG, 2,4-D and PAH, from the cerebrospinal fluid (CSF) to the blood for eventual excretion in urine and bile (By similarity). Also contributes to the uptake of several other organic compounds such as the prostanoids prostaglandin E(2) and prostaglandin F(2-alpha), L-carnitine, and the therapeutic drugs allopurinol, 6-mercaptopurine (6-MP) and 5-fluorouracil (5-FU) (By similarity). Mediates the transport of PAH, PCG, and the statins pravastatin and pitavastatin, from the cerebrum into the blood circulation across the blood-brain barrier (BBB). In summary, plays a role in the efflux of drugs and xenobiotics, helping reduce their undesired toxicological effects on the body (By similarity)
- Specific Function
- Organic anion transmembrane transporter activity
- Gene Name
- SLC22A8
- Uniprot ID
- Q8TCC7
- Uniprot Name
- Organic anion transporter 3
- Molecular Weight
- 59855.585 Da
References
- VanWert AL, Gionfriddo MR, Sweet DH: Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010 Jan;31(1):1-71. doi: 10.1002/bdd.693. [Article]
Drug created at June 13, 2005 13:24 / Updated at September 15, 2024 21:55