Identification

Name
Budesonide
Accession Number
DB01222  (APRD00442)
Type
Small Molecule
Groups
Approved
Description

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 1994.7

Structure
Thumb
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
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BudesonideCapsule3 mg/1OralPaddock Laboratories, LLC2018-06-29Not applicableUs
BudesonideCapsule, extended release3 mgOralTillotts Pharma Gmbh2020-01-17Not applicableCanada
BudesonideSpray, metered32 ug/1NasalAstra Zeneca Lp2014-05-132018-02-28Us
Budesonide/formoterol TevaRespiratory (inhalation)Teva Pharma B.V.2014-11-192017-01-31Eu
Budesonide/formoterol TevaRespiratory (inhalation)Teva Pharma B.V.2014-11-192017-01-31Eu
CortimentTablet, extended releaseOralFerring Pharmaceuticals2016-07-25Not applicableCanada
EntocortCapsule, extended releaseOralTillotts Pharma Gmbh1997-01-30Not applicableCanada
Entocort ECCapsule3 mg/1OralPhysicians Total Care, Inc.2006-05-22Not applicableUs65483 0702 10 nlmimage10 f6387b33
Entocort ECCapsule3 mg/1OralPrometheus Laboratories2001-10-29Not applicableUs
Entocort ECCapsule3 mg/1OralPaddock Laboratories, LLC2001-10-29Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BudesonideCapsule, coated pellets3 mg/1OralNorthstar Rx Llc.2018-06-25Not applicableUs
BudesonideTablet, film coated, extended release9 mg/1OralGolden State Medical Supply Inc.2018-07-03Not applicableUs
BudesonideSuspension1 mg/2mLRespiratory (inhalation)Sandoz Inc2015-07-24Not applicableUs
BudesonideCapsule3 mg/1OralCarilion Materials Management2013-08-23Not applicableUs
BudesonideSuspension0.5 mg/2mLRespiratory (inhalation)Sandoz Inc2015-07-24Not applicableUs
BudesonideSuspension0.5 mg/2mLRespiratory (inhalation)Cardinal Health2019-01-11Not applicableUs
BudesonideCapsule3 mg/1OralGolden State Medical Supply, Inc.2011-05-16Not applicableUs
BudesonideCapsule3 mg/1OralAmerican Health Packaging2018-12-182020-05-31Us
BudesonideCapsule, coated pellets3 mg/1OralZydus Pharmaceuticals (USA) Inc.2017-06-08Not applicableUs
BudesonideSuspension0.5 mg/2mLRespiratory (inhalation)Preferred Pharmaceuticals Inc.2016-11-032020-04-07Us
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BudesonideSpray, metered32 ug/1NasalWalgreens2016-04-11Not applicableUs
BudesonideSpray, metered32 ug/1NasalSafeway2016-09-15Not applicableUs
BudesonideSpray, metered32 ug/1NasalTopco Associates LLC2016-08-31Not applicableUs
BudesonideSpray, metered32 ug/1NasalRUGBY LABORATORIES2016-07-13Not applicableUs
BudesonideSpray, metered32 ug/1NasalApotex Corp.2016-04-19Not applicableUs
BudesonideSpray, metered32 ug/1NasalRite Aid2019-10-10Not applicableUs
BudesonideSpray, metered32 ug/1NasalCVS Health2016-04-09Not applicableUs
BudesonideSpray, metered32 ug/1NasalWalmart2016-08-22Not applicableUs
BudesonideSpray, metered32 ug/1NasalRite Aid2016-07-13Not applicableUs
BudesonideSpray, metered32 ug/1NasalApotex Corp.2018-04-26Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

    Learn more
  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

    Learn more
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Budesonide and Formoterol Fumarate DihydrateBudesonide (80 ug/1) + Formoterol fumarate (4.5 ug/1)AerosolRespiratory (inhalation)AstraZeneca Pharmaceuticals LP2020-01-03Not applicableUs
Budesonide and Formoterol Fumarate DihydrateBudesonide (160 ug/1) + Formoterol fumarate (4.5 ug/1)AerosolRespiratory (inhalation)AstraZeneca Pharmaceuticals LP2020-01-03Not applicableUs
Entocort EnemaBudesonide (2.3 mg) + Sodium chloride (115 ml)Enema; Kit; TabletRectalTillotts Pharma Gmbh1994-12-31Not applicableCanada
SymbicortBudesonide (80 ug/1) + Formoterol fumarate (4.5 ug/1)AerosolRespiratory (inhalation)AstraZeneca Pharmaceuticals LP2007-05-29Not applicableUs
SymbicortBudesonide (160 ug/1) + Formoterol fumarate (4.5 ug/1)AerosolRespiratory (inhalation)AstraZeneca Pharmaceuticals LP2007-05-29Not applicableUs
SymbicortBudesonide (160 ug/1) + Formoterol fumarate (4.5 ug/1)AerosolRespiratory (inhalation)Remedy Repack2016-04-042016-04-05Us
SymbicortBudesonide (160 ug/1) + Formoterol fumarate (4.5 ug/1)AerosolRespiratory (inhalation)A-S Medication Solutions2007-05-29Not applicableUs
Symbicort 100 TurbuhalerBudesonide (100 mcg) + Formoterol fumarate (6 mcg)PowderRespiratory (inhalation)Astra Zeneca2002-02-08Not applicableCanada
Symbicort 200 TurbuhalerBudesonide (200 mcg) + Formoterol fumarate (6 mcg)PowderRespiratory (inhalation)Astra Zeneca2002-02-08Not applicableCanada
Symbicort Forte TurbuhalerBudesonide (400 mcg) + Formoterol fumarate (12 mcg)PowderRespiratory (inhalation)Astra ZenecaNot applicableNot applicableCanada
International/Other Brands
Bidien / Budeson / Budicort / Noex (Eurofarma) / Pulmicort (AstraZeneca) / Rhinosol / Spirocort
Categories
UNII
Q3OKS62Q6X
CAS number
51333-22-3
Weight
Average: 430.5339
Monoisotopic: 430.23553882
Chemical Formula
C25H34O6
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[10.8.0.0²,⁹.0⁴,⁸.0¹³,¹⁸]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

Pharmacology

Indication

Budesonide extended release capsules are indicated for the treatment and maintenance of mild to moderate Crohn’s disease.8,9 Various inhaled budesonide products are indicated for prophylactic therapy in asthma10,11,13 and reducing exacerbations of COPD.13 A budesonide nasal spray is available over the counter for symptoms of hay fever and upper respiratory allergies.12 Extended release capsules are indicated to induce remission of mild to moderate ulcerative colitis14 and a rectal foam is used for mild to moderate distal ulcerative colitis.15

Associated Conditions
Pharmacodynamics

Budesonide is a glucocorticoid used to treat respiratory and digestive conditions by reducing inflammation.8,9,10,11,13,14,15 It has a wide therapeutic index, as dosing varies highly from patient to patient.8,9,10,11,13,14,15 Patients should be counselled regarding the risk of hypercorticism and adrenal axis suppression.8,9,10,11,13,14,15

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

TargetActionsOrganism
AGlucocorticoid receptor
antagonist
Humans
UAnnexin A1
substrate
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

Learn more
Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

Learn more
Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

Learn more
Absorption

Extended release oral capsules are 9-21% bioavailable.8,9 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.8,9 A high fat meal increases the Tmax by 2.3h but otherwise does not affect the pharmacokinetics of budesonide.8,9

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.10

A 1mg nebulized dose is 6% bioavailable, reaching a Cmax of 2.6nmol/L with a Tmax of 20 minutes.11

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.14

Budesonide rectal foam 2mg twice daily has an AUC of 4.31ng*hr/mL.15

Volume of distribution

The volume of distribution of budesonide is 2.2-3.9L/kg.8,9,10,11,14,15

Protein binding

Corticosteroids are generally bound to corticosteroid binding globulin2 and serum albumin3 in plasma. Budesonide is 85-90% protein bound in plasma.8,9,10,11,14,15

Metabolism

Budesonide is 80-90% metabolized at first pass.4 Budesonide is metabolized by CYP3A4 to its 2 major metabolites, 6beta-hydroxybudesonide and 16alpha-hydroxyprednisolone.4 The glucocorticoid activity of these metabolites is negligible (<1/100) in relation to that of the parent compound.4

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.8,9,10,11,13,14,15 No unchanged budesonide is recovered in urine.8,9,10,11,13,14,15

Half life

Budesonide has a plasma elimination half life of 2-3.6h.8,9,10,14 The terminal elimination half life in asthmatic children 4-6 years old is 2.3h.11

Clearance

Budesonide has a plasma clearance of 0.9-1.8L/min.8,9,14,15 The 22R form has a clearance of 1.4L/min while the 22S form has a clearance of 1.0L/min.10 The clearance in asthmatic children 4-6 years old is 0.5L/min.11,13

Toxicity

Acute overdose of corticosteroids is rare, however prolonged high dosing of corticosteroids can lead to hypercorticism and adrenal axis suppression.8,9,10,11,13,14,15 In the case of overdose, reduce the dosage of corticosteroids temporarily.8,9,10,11,13,14,15

A 200mg oral dose is lethal to female mice while a 400mg oral dose is lethal to male mice.8,9,14

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Interacting Gene/EnzymeAllele nameGenotype(s)Defining Change(s)Type(s)DescriptionDetails
T-box transcription factor TBX21---(C;G)CG allele (heterozygotes)Effect Directly StudiedThe 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.
DrugInteraction
(R)-warfarinThe metabolism of (R)-warfarin can be increased when combined with Budesonide.
(S)-WarfarinThe metabolism of (S)-Warfarin can be increased when combined with Budesonide.
1-TestosteroneThe risk or severity of edema formation can be increased when 1-Testosterone is combined with Budesonide.
1,10-PhenanthrolineThe therapeutic efficacy of 1,10-Phenanthroline can be decreased when used in combination with Budesonide.
16-BromoepiandrosteroneThe risk or severity of edema formation can be increased when 16-Bromoepiandrosterone is combined with Budesonide.
19-norandrostenedioneThe risk or severity of edema formation can be increased when 19-norandrostenedione is combined with Budesonide.
1alpha-Hydroxyvitamin D5The therapeutic efficacy of 1alpha-Hydroxyvitamin D5 can be decreased when used in combination with Budesonide.
1alpha,24S-Dihydroxyvitamin D2The therapeutic efficacy of 1alpha,24S-Dihydroxyvitamin D2 can be decreased when used in combination with Budesonide.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when Budesonide is combined with 2-Methoxyethanol.
2,4-thiazolidinedioneThe risk or severity of hyperglycemia can be increased when Budesonide is combined with 2,4-thiazolidinedione.
Additional Data Available
  • Extended Description
    Extended Description

    Extended description of the mechanism of action and particular properties of each drug interaction.

    Learn more
  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

    Learn more
  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

    Learn more
  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

    Learn more
Food Interactions
  • Take with or without food. Food delays drug absorption, but not to a clinically significant extent.

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
  1. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [PubMed:30285357]
  2. 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. [PubMed:23300763]
  3. 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. [PubMed:15634032]
  4. 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. [PubMed:23251737]
  5. Ellul-Micallef R, Hansson E, Johansson SA: Budesonide: a new corticosteroid in bronchial asthma. Eur J Respir Dis. 1980 Jun;61(3):167-73. [PubMed:7002575]
  6. 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. [PubMed:7391935]
  7. FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Aerosol (Discontinued) [Link]
  8. FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
  9. FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
  10. FDA Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
  11. FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
  12. FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Spray [Link]
  13. FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
  14. FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
  15. FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]
External Links
Human Metabolome Database
HMDB0015353
KEGG Drug
D00246
PubChem Compound
5281004
PubChem Substance
46504869
ChemSpider
4444479
BindingDB
50354850
RxNav
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
ATC Codes
D07AC09 — BudesonideR01AD05 — BudesonideR03AK07 — Formoterol and budesonideA07EA06 — BudesonideR03BA02 — BudesonideR03AK12 — Salmeterol and budesonide
AHFS Codes
  • 68:04.00 — Adrenals
  • 52:08.00 — Anti-inflammatory Agents
  • 56:36.00 — Anti-inflammatory Agents
  • 52:08.08 — Corticosteroids
FDA label
Download (52.3 KB)
MSDS
Download (73.7 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedBasic ScienceChronic Obstructive Pulmonary Disease Method Evaluation / COPD Method Evaluation1
0CompletedTreatmentAllergic Rhinitis (AR)1
0CompletedTreatmentChronic Rhinosinusitis (Diagnosis)1
0Not Yet RecruitingTreatmentAllergic Fungal Sinusitis / Chronic Rhinosinusitis With Nasal Polyps1
1CompletedNot AvailableHealthy Volunteers2
1CompletedBasic ScienceAsthma1
1CompletedBasic ScienceHealthy Volunteers1
1CompletedBasic ScienceStudy is Being Conducted in Healthy Volunteers1
1CompletedHealth Services ResearchHealthy Volunteers1
1CompletedOtherHealthy Volunteers1
1CompletedPreventionAcute Chest Syndrome / Asthma / Sickle Cell Disease (SCD)1
1CompletedPreventionOther and unspecified effects of high altitude1
1CompletedTreatmentAllergies1
1CompletedTreatmentAsthma13
1CompletedTreatmentAsthma / Chronic Obstructive Pulmonary Disease (COPD)2
1CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)4
1CompletedTreatmentGraft Versus Host Disease (GVHD) / Transplantation, Stem Cell1
1CompletedTreatmentHealthy Volunteers2
1CompletedTreatmentLiver Cirrhosis, Biliary / Sclerosing Cholangitis1
1CompletedTreatmentLung Cancers / Precancerous Conditions1
1CompletedTreatmentMild Asthma / Reactive Airways Disease (RAD) / Wheezing1
1CompletedTreatmentRelative Bioavailability1
1CompletedTreatmentSnoring1
1Not Yet RecruitingTreatmentBronchiolitis; Respiratory Syncytial Virus1
1RecruitingTreatmentAsthma Acute1
1, 2CompletedPreventionBronchopulmonary Dysplasia (BPD)1
1, 2CompletedTreatmentAsthma1
1, 2Not Yet RecruitingPreventionChronic Lung Disease of Prematurity / Respiratory Distress Syndrome In Premature Infants1
1, 2Not Yet RecruitingTreatmentCough Variant Asthma1
1, 2RecruitingDiagnosticIntubation Complications1
2Active Not RecruitingTreatmentAsthma1
2Active Not RecruitingTreatmentChronic Frontal Rhinosinusitis / Vertex to Floor Position1
2CompletedNot AvailableAsthma1
2CompletedDiagnosticLung Diseases, Obstructive1
2CompletedPreventionAcute Respiratory Distress Syndrome (ARDS)1
2CompletedPreventionLung Cancers2
2CompletedTreatmentAcute Cellular Graft Rejection / New Onset Diabetes After Transplant1
2CompletedTreatmentAllergic Rhinitis (AR)1
2CompletedTreatmentAllogeneic Stem Cell Transplantation / Bronchiolitis Obliterans (BO)1
2CompletedTreatmentAsthma10
2CompletedTreatmentAsthma in Children1
2CompletedTreatmentAsthma, Exercise-Induced / Exercised Induced Asthma1
2CompletedTreatmentAsthma / Bronchial Asthma / Chronic Asthma1
2CompletedTreatmentBronchial Asthma1
2CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)4
2CompletedTreatmentCopd Bronchitis1
2CompletedTreatmentCrohn's Disease (CD)2
2CompletedTreatmentEosinophilic Esophagitis (EoE)1
2CompletedTreatmentEosinophilic Esophagitis (EoE) / Oesophagitis, Eosinophilic1
2CompletedTreatmentEsophageal Strictures1
2CompletedTreatmentIgA Nephropathy1
2CompletedTreatmentMelanoma, Malignant1
2CompletedTreatmentObstructive Airway Disease1
2CompletedTreatmentOesophagitis, Eosinophilic3
2CompletedTreatmentPrimary IgA Nephropathy1
2CompletedTreatmentProctitis1
2CompletedTreatmentSeasonal Allergic Rhinitis (SAR)3
2CompletedTreatmentStable Asthma1
2CompletedTreatmentUlcerative Colitis1
2Not Yet RecruitingTreatmentAcute Respiratory Distress Syndrome (ARDS)1
2Not Yet RecruitingTreatmentAnosmia / Novel Coronavirus Infectious Disease (COVID-19)1
2Not Yet RecruitingTreatmentInfections, Coronavirus / Novel Coronavirus Infectious Disease (COVID-19)1
2Not Yet RecruitingTreatmentSevere Acute Malnutrition1
2RecruitingPreventionRadiation Pneumonitis1
2RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD)1
2RecruitingTreatmentChronic Rhinosinusitis1
2RecruitingTreatmentEarly Stage HER2+ Breast Cancer1
2TerminatedPreventionBronchiolitis Obliterans (BO) / Cryptogenic Organizing Pneumonia / Lung Diseases, Interstitial / Respiratory Tract Infections (RTI)1
2TerminatedPreventionProphylaxis of Radiation proctitis1
2TerminatedTreatmentDiarrhea1
2TerminatedTreatmentInflammatory Bowel Diseases (IBD) / Ulcerative Colitis1
2TerminatedTreatmentOesophagitis, Eosinophilic1
2Unknown StatusPreventionChronic Lung Disease of Prematurity1
2Unknown StatusTreatmentChronic Obstructive Pulmonary Disease (COPD)1
2Unknown StatusTreatmentTransient Tachypnea of the Newborn1
2WithdrawnTreatmentChronic Lung Disease of Prematurity1
2WithdrawnTreatmentGraft Versus Host Disease, Acute / Intestinal Graft Versus Host Disease1
2WithdrawnTreatmentOlfaction Disorders / Paranasal Sinus Diseases / Sinusitis1
2, 3CompletedPreventionLung Cancers1
2, 3CompletedTreatmentAllergies1
2, 3CompletedTreatmentAspergillosis, Allergic Bronchopulmonary1
2, 3CompletedTreatmentEE / Gastro-esophageal Reflux Disease (GERD) / Oesophagitis, Eosinophilic1
2, 3CompletedTreatmentHepatitis, Autoimmune1
2, 3CompletedTreatmentPolyps, Nasal1
2, 3CompletedTreatmentSinusitis1
2, 3CompletedTreatmentStatus Asthmaticus1
2, 3Not Yet RecruitingTreatmentChronic Rhinosinusitis / Chronic Sinus Congestion / Chronic Sinus Infection / Chronic Sinusitis - Ethmoidal, Posterior1
2, 3Not Yet RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19)1
2, 3RecruitingTreatmentAcute Pharyngitis1
2, 3TerminatedTreatmentDiarrhea / Lymphocytic Colitis1
2, 3Unknown StatusTreatmentAsthma1
3Active Not RecruitingTreatmentBacterial Sinusitis1
3Active Not RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD)1
3Active Not RecruitingTreatmentEosinophilic Esophagitis (EoE)1
3Active Not RecruitingTreatmentIncomplete Microscopic Colitis1
3Active Not RecruitingTreatmentOesophagitis, Eosinophilic1
3CompletedNot AvailableAsthma1
3CompletedPreventionChronic Lung Disease of Prematurity1
3CompletedPreventionGraft Versus Host Disease (GVHD) / Leukemias1
3CompletedPreventionOther and unspecified effects of high altitude1
3CompletedTreatmentAllergic Rhinitis (AR)1
3CompletedTreatmentAllergic Rhinitis (AR) / Conjunctivitis, Seasonal Allergic / Hayfever1
3CompletedTreatmentAsthma63
3CompletedTreatmentAsthma / Bioequivalence1
3CompletedTreatmentAsthma / Chronic Lung Diseases1
3CompletedTreatmentBronchial Asthma2
3CompletedTreatmentCOPD Patients1
3CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)12
3CompletedTreatmentChronic Obstructive Pulmonary Disorder2
3CompletedTreatmentChronic Rhinosinusitis With Polyposis1
3CompletedTreatmentChronic / Chronic Rhinosinusitis / Polyposis / Sinusitis1
3CompletedTreatmentCollagenous Colitis2
3CompletedTreatmentCrohn's Disease (CD)4
3CompletedTreatmentEosinophilic Esophagitis (EoE)1
3CompletedTreatmentEosinophilic Esophagitis (EoE) / Eosinophilic Esophagitis (EoE) Dysphagia1
3CompletedTreatmentGraft Versus Host Disease (GVHD)1
3CompletedTreatmentInduction and Maintaining Remission of Collagenous Colitis1
3CompletedTreatmentLymphocytic Colitis1
3CompletedTreatmentMicroscopic Colitis1
3CompletedTreatmentMild to Moderate Asthma1
3CompletedTreatmentOSAS (Obstructive Sleep Apneas Syndrome)1
3CompletedTreatmentOesophagitis, Eosinophilic1
3CompletedTreatmentOral Chronic Graft vs Host Disease1
3CompletedTreatmentProctitis / Proctosigmoiditis2
3CompletedTreatmentSeasonal Allergic Rhinitis (SAR)1
3CompletedTreatmentUlcerative Colitis7
3Enrolling by InvitationTreatmentAsthma, Allergic1
3Enrolling by InvitationTreatmentChronic Obstructive Pulmonary Disease (COPD) / Chronic Respiratory Failure1
3Not Yet RecruitingTreatmentAsthma2
3Not Yet RecruitingTreatmentAsthma in Children / Chronic Asthma1
3Not Yet RecruitingTreatmentChronic Rhinosinusitis (Diagnosis)1
3RecruitingTreatmentAcute Respiratory Failure / Hypoxemia / Novel Coronavirus Infectious Disease (COVID-19) / Pneumonia1
3RecruitingTreatmentAnosmia / Budesonide / Novel Coronavirus Infectious Disease (COVID-19) / Olfaction Disorders1
3RecruitingTreatmentAsthma3
3RecruitingTreatmentBacterial Sinusitis / Chronic Polyposis1
3RecruitingTreatmentBronchial Asthma1
3RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD)2
3RecruitingTreatmentChronic Rhinosinusitis (Diagnosis), Nasal Polyposis1
3RecruitingTreatmentChronic Rhinosinusitis With Nasal Polyps1
3RecruitingTreatmentCovid-19 Infection / Hospitalization in Respiratory Disease Department / Novel Coronavirus Infectious Disease (COVID-19)1
3RecruitingTreatmentExercise Induced Bronchospasm / Exercise-Induced Bronchospasm1
3RecruitingTreatmentPrimary IgA Nephropathy1
3SuspendedTreatmentAsthma1
3SuspendedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
3TerminatedTreatmentAsthma1
3TerminatedTreatmentBronchial Asthma1
3TerminatedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
3TerminatedTreatmentPrimary Biliary Cholangitis1
3TerminatedTreatmentProctitis / Proctosigmoiditis1
3Unknown StatusTreatmentBronchial Asthma1
3Unknown StatusTreatmentCollagenous Colitis1
3Unknown StatusTreatmentEmphysema / Poor Sleeping Quality1
3WithdrawnPreventionAltitude Sickness1
3WithdrawnTreatmentRhinitis, Allergic, Perennial2
4Active Not RecruitingBasic ScienceChronic Obstructive Pulmonary Disease (COPD)1
4Active Not RecruitingTreatmentAirway Inflammation / Asthma1
4CompletedNot AvailableAsthma2
4CompletedBasic ScienceChronic Obstructive Pulmonary Disease (COPD)1
4CompletedBasic ScienceMild Asthma1
4CompletedPreventionAsthma1
4CompletedSupportive CareAsthma1
4CompletedSupportive CareLung Cancers1
4CompletedTreatmentAllergic Rhinitis (AR)1
4CompletedTreatmentAllergic Rhinosinusitis / Bacterial Sinusitis / Chronic Eosinophilic Rhinosinusitis1
4CompletedTreatmentAsthma19
4CompletedTreatmentAsthma / Asthma Acute2
4CompletedTreatmentAsthma / Asthma Acute / Reactive Airway Exacerbation1
4CompletedTreatmentAsthma / Pediatric ALL1
4CompletedTreatmentBronchial Asthma1
4CompletedTreatmentBronchiectasis1
4CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)20
4CompletedTreatmentCrohn's Disease (CD)1
4CompletedTreatmentEosinophilic Bronchitis1
4CompletedTreatmentHealthy Volunteers1
4CompletedTreatmentOSAS (Obstructive Sleep Apneas Syndrome)1
4CompletedTreatmentOesophagitis, Eosinophilic2
4CompletedTreatmentPerennial Allergic Rhinitis (PAR)2
4Enrolling by InvitationTreatmentBronchiectasis / Chronic Obstructive Pulmonary Disease (COPD)1
4Not Yet RecruitingBasic ScienceEnvironmental Exposures / Epigenetic Effects of Intranasal Steroids1
4Not Yet RecruitingPreventionChronic Lung Disease of Prematurity / Respiratory Distress Syndrome1
4Not Yet RecruitingPreventionChronic Obstructive Pulmonary Disease (COPD) / Lung Cancers / Post Operative Complication, Pulmonary1
4Not Yet RecruitingTreatmentAsthma1
4Not Yet RecruitingTreatmentAsthma / Severe Eosinophilic Asthma1
4Not Yet RecruitingTreatmentNovel Coronavirus Infectious Disease (COVID-19) / Olfactory Disorders1
4Not Yet RecruitingTreatmentUlcerative Colitis1
4RecruitingNot AvailableAsthma1
4RecruitingBasic ScienceAsthma1
4RecruitingPreventionChronic Lung Disease of Prematurity / Infants, Premature / Respiratory Distress Syndrome1
4RecruitingPreventionExposure to Pollution / Glucocorticoid Resistance1
4RecruitingTreatmentAsthma1
4RecruitingTreatmentAsthma-chronic obstructive pulmonary disease overlap syndrome / Chronic Obstructive Pulmonary Disease (COPD) / Quality of Life / Small Airways Disease1
4RecruitingTreatmentAutoimmune Enteropathy / Collagenous Sprue / CVID Enteropathy / Enteropathy / Gluten Enteropathy1
4RecruitingTreatmentBronchial Asthma1
4RecruitingTreatmentChronic Obstructive Airways Disease Exacerbated / Chronic Obstructive Pulmonary Disease (COPD)1
4RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD) / Exercise / Lung Function Decreased / Quality of Life1
4RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD) / Pulmonary Disease,Chronic Obstructive1
4RecruitingTreatmentCough Variant Asthma1
4RecruitingTreatmentInfections, Coronavirus / Novel Coronavirus Infectious Disease (COVID-19)1
4RecruitingTreatmentRhinitis1
4TerminatedPreventionBronchoalveolar Lavage Fluid / Chronic Lung Diseases / Cytokines / Infants, Premature / Respiratory Distress Syndrome1
4TerminatedTreatmentAsthma2
4TerminatedTreatmentAsthma, Exercise-Induced / Exercised Induced Asthma1
4TerminatedTreatmentChronic Obstructive Pulmonary Disease (COPD)2
4TerminatedTreatmentSevere IgE-mediated Asthma1
4Unknown StatusPreventionChronic Lung Disease of Prematurity / Respiratory Distress Syndrome1
4Unknown StatusTreatmentAsthma3
4Unknown StatusTreatmentOSAS (Obstructive Sleep Apneas Syndrome)1
4WithdrawnNot AvailableOsteoporosis1
4WithdrawnBasic ScienceAsthma1
4WithdrawnTreatmentAcute Cellular Graft Rejection / Liver Transplant Rejection1
4WithdrawnTreatmentAsthma2
Not AvailableActive Not RecruitingBasic ScienceAsthma1
Not AvailableActive Not RecruitingTreatmentAsthma1
Not AvailableCompletedNot AvailableAsthma3
Not AvailableCompletedNot AvailableAsthma / Chronic Obstructive Pulmonary Disease (COPD)1
Not AvailableCompletedNot AvailableAsthma / Focus of Study is to Improve Asthma Control Based on Phenotype, NO and Sputum Cell Count1
Not AvailableCompletedNot AvailableCrohn's Disease (CD) / Inflammatory Bowel Diseases (IBD)1
Not AvailableCompletedNot AvailableHealthy Volunteers1
Not AvailableCompletedNot AvailablePatients Satisfaction1
Not AvailableCompletedNot AvailablePerception of Physicians & Patients of AMD1
Not AvailableCompletedNot AvailableUlcerative Colitis1
Not AvailableCompletedBasic ScienceAsthma3
Not AvailableCompletedDiagnosticAsthma2
Not AvailableCompletedHealth Services ResearchAsthma1
Not AvailableCompletedTreatmentAllergic Rhinitis (AR) / Hypersensitivity / Inflammatory Reaction / Respiratory Tract Diseases1
Not AvailableCompletedTreatmentAsthma2
Not AvailableCompletedTreatmentAsthma / Chronic Lung Diseases2
Not AvailableCompletedTreatmentBronchiectasis1
Not AvailableCompletedTreatmentChronic Rhinosinusitis / Nasal Polyposis1
Not AvailableCompletedTreatmentModerate to Severe Persistent Bronchial Asthma1
Not AvailableCompletedTreatmentOesophagitis, Eosinophilic1
Not AvailableCompletedTreatmentPolyps, Nasal / Sinusitis1
Not AvailableCompletedTreatmentRespiratory Distress Syndrome1
Not AvailableNot Yet RecruitingPreventionAnastomotic stenosis / Imperforate oesophagus1
Not AvailableNot Yet RecruitingTreatmentAsthma-chronic obstructive pulmonary disease overlap syndrome1
Not AvailableNot Yet RecruitingTreatmentCrohn's Disease (CD)1
Not AvailableNot Yet RecruitingTreatmentHealthy Volunteers1
Not AvailableRecruitingNot AvailableAdrenal Insufficiency / Arrhythmia / Asthma in Children / Chronic Lung Disease of Prematurity / Coronavirus Infection (COVID-19) / Edema / Fibrinolysis; Hemorrhage / Heart Failure / Hemophilia Prior to Tooth Extraction / High Blood Pressure (Hypertension) / Hypermenorrhea / Hyperphosphataemia / Hypertension, Resistant to Conventional Therapy / Hypokalemia / Insomnia / Pain / Pneumonia / Primary Hyperaldosteronism / Pulmonary Arterial Hypertension (PAH) / Skin-structure infections / Urinary Tract Infections in Children1
Not AvailableRecruitingNot AvailableAsthma2
Not AvailableRecruitingOtherChronic Rhinosinusitis1
Not AvailableRecruitingPreventionAir Pollution / Chronic Obstructive Airways Disease Exacerbated1
Not AvailableRecruitingTreatmentDetermination of the Efficacy of Different Medications for Idiopathic Rhinitis / Impact of Different Medications on Biomarkers of Idiopathic Rhinitis / Safety and Tolerance of Different Medications for Idiopathic Rhinitis1
Not AvailableTerminatedTreatmentAsthma1
Not AvailableTerminatedTreatmentChronic Rhinosinusitis1
Not AvailableTerminatedTreatmentColitis1
Not AvailableUnknown StatusNot AvailableAllergic Rhinitis (AR) / Asthma1
Not AvailableUnknown StatusPreventionExacerbation of asthma1
Not AvailableUnknown StatusPreventionRespiratory Sounds2
Not AvailableUnknown StatusTreatmentAsthma2
Not AvailableUnknown StatusTreatmentStridor1
Not AvailableWithdrawnTreatmentHepatitis, Autoimmune / Primary Biliary Cholangitis1

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
FormRouteStrength
Capsule, coated pelletsOral3 mg/1
Capsule, extended releaseOral3 mg
Capsule, gelatin coatedOral3 mg/1
InhalantRespiratory (inhalation)0.25 mg/2mL
InhalantRespiratory (inhalation)0.5 mg/2mL
PowderNot applicable1 g/1g
SuspensionRespiratory (inhalation)1 mg/2mL
Tablet, extended releaseOral9 mg/1
Tablet, film coated, extended releaseOral9 mg/1
Capsule, delayed release pelletsOral3 mg/1
InhalantOral0.25 mg/2mL
InhalantOral0.5 mg/2mL
InhalantOral1 mg/2mL
Tablet, extended releaseOral
Capsule, extended releaseOral
CapsuleOral3 mg/1
Enema; kit; tabletRectal
Tablet, orally disintegratingOral
Spray, meteredNasal
CapsuleOral6 mg/1
CapsuleOral9 mg/1
Aerosol, powderRespiratory (inhalation)180 ug/1
Aerosol, powderRespiratory (inhalation)90 ug/1
SuspensionRespiratory (inhalation)
SuspensionRespiratory (inhalation)0.25 mg/2mL
SuspensionRespiratory (inhalation)0.5 mg/2mL
Powder, meteredRespiratory (inhalation)100 mcg
Powder, meteredRespiratory (inhalation)200 mcg
Powder, meteredRespiratory (inhalation)200 ug/1
Powder, meteredRespiratory (inhalation)400 mcg
Spray, meteredNasal32 ug/1
Spray, meteredNasal64 mcg
Aerosol, meteredNasal
PowderNasal; Respiratory (inhalation)
AerosolRespiratory (inhalation)
PowderRespiratory (inhalation)
Aerosol, foamRectal28 mg/1
KitRectal2 mg
Prices
Unit descriptionCostUnit
Budesonide micronized powder346.5USD g
DesOwen Lot w/Cetaphil Cream 0.05% Kit Box255.84USD box
Desowen 0.05% ointment kit217.2USD kit
Desowen 0.05% cream kit212.4USD kit
DesOwen 0.05% Lotion 118ml Bottle183.17USD bottle
Pulmicort Flexhaler 180 mcg/act Aerosol Inhaler163.34USD inhaler
Pulmicort 180 mcg flexhaler157.06USD inhaler
DesOwen 0.05% Lotion 59ml Bottle123.38USD bottle
Pulmicort Flexhaler 90 mcg/act Aerosol Inhaler121.98USD inhaler
Pulmicort 90 mcg flexhaler117.29USD inhaler
Rhinocort Aqua 32 mcg/act 8.6 gm Bottle111.96USD bottle
Rhinocort aqua nasal spray13.93USD g
Entocort EC 3 mg 24 Hour Capsule13.86USD capsule
Entocort ec 3 mg capsule12.22USD capsule
Budesonide 0.5 mg/2ml Suspension 2ml Plastic Container9.73USD plastic
Pulmicort 0.5 mg/2ml Suspension 2ml Plastic Container9.24USD plastic
Budesonide 0.25 mg/2ml Suspension 2ml Plastic Container9.07USD plastic
Entocort (115 Ml) 2.3 mg/enm Enema8.93USD enema
Pulmicort 1 mg/2 ml respule8.89USD ml
Pulmicort 0.25 mg/2ml Suspension 2ml Plastic Container7.85USD plastic
Pulmicort 0.5 mg/2 ml respule4.45USD ml
Pulmicort 0.25 mg/2 ml respul3.78USD ml
Desowen 0.05% cream2.43USD g
Pulmicort Nebuamp 0.5 mg/ml Suspension0.93USD ml
Pulmicort Turbuhaler 400 mcg/dose Metered Inhalation Powder0.62USD dose
Pulmicort Nebuamp 0.25 mg/ml Suspension0.46USD ml
Pulmicort Turbuhaler 200 mcg/dose Metered Inhalation Powder0.34USD dose
Pulmicort Nebuamp 0.125 mg/ml Suspension0.23USD ml
Pulmicort Turbuhaler 100 mcg/dose Metered Inhalation Powder0.17USD dose
Rhinocort Turbuhaler 100 mcg/dose Metered Dose Aerosol0.13USD dose
Mylan-Budesonide Aq 100 mcg/dose Metered Dose Spray0.1USD dose
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6423340No2002-07-232010-11-15Us
CA2071518No2002-11-122010-11-15Canada
US6598603Yes2003-07-292019-06-23Us
US6899099Yes2005-05-312019-06-23Us
US7524834Yes2009-04-282019-05-11Us
US7759328Yes2010-07-202023-07-29Us
US7897646Yes2011-03-012019-03-09Us
US8143239Yes2012-03-272023-07-29Us
US8461211Yes2013-06-112019-03-09Us
US8575137Yes2013-11-052023-07-29Us
US6123924No2000-09-262017-09-26Us
US7967011Yes2011-06-282022-02-11Us
US8616196Yes2013-12-312029-10-07Us
US8387615Yes2013-03-052025-05-10Us
US7587988Yes2009-09-152026-10-10Us
US7367333Yes2008-05-062019-05-11Us
US8528545Yes2013-09-102029-04-16Us
US8875699Yes2014-11-042025-05-10Us
US6027714No2000-02-222018-01-09Us
US7143764No2006-12-052018-03-13Us
US6142145No2000-11-072018-05-08Us
US6287540No2001-09-112018-01-09Us
US9320716No2016-04-262020-06-09Us
US9192581No2015-11-242031-09-07Us
US7410651No2008-08-122020-06-09Us
USRE43799No2012-11-132020-06-09Us
US8895064No2014-11-252031-09-07Us
US7431943No2008-10-072020-06-09Us
US9132093No2015-09-152031-09-07Us
US8784888No2014-07-222020-06-09Us
US8293273No2012-10-232020-06-09Us
US5914122No1999-06-222015-12-19Us
US9532954No2017-01-032020-06-09Us
US10064878No2018-09-042020-06-09Us
US10105374No2018-10-232020-06-09Us
US10166247Yes2019-01-012023-07-29Us
US10143698No2018-12-042020-06-09Us
US9707182No2017-07-182036-09-09Us
US10172802No2019-01-082036-09-09Us
US10307375No2019-06-042031-09-07Us
Additional Data Available
  • Filed On
    Filed On

    The date on which a patent was filed with the relevant government.

    Learn more

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)226°CPhysProp
boiling point (°C)599.7ChemSpider
logP1.914ChemSpider
Predicted Properties
PropertyValueSource
Water Solubility0.0457 mg/mLALOGPS
logP2.42ALOGPS
logP2.73ChemAxon
logS-4ALOGPS
pKa (Strongest Acidic)13.74ChemAxon
pKa (Strongest Basic)-2.9ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area93.06 Å2ChemAxon
Rotatable Bond Count4ChemAxon
Refractivity116.11 m3·mol-1ChemAxon
Polarizability47.11 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleNoChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9872
Blood Brain Barrier+0.9533
Caco-2 permeable-0.6097
P-glycoprotein substrateSubstrate0.804
P-glycoprotein inhibitor INon-inhibitor0.5881
P-glycoprotein inhibitor IINon-inhibitor0.5911
Renal organic cation transporterNon-inhibitor0.7867
CYP450 2C9 substrateNon-substrate0.8488
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7337
CYP450 1A2 substrateNon-inhibitor0.9046
CYP450 2C9 inhibitorNon-inhibitor0.9075
CYP450 2D6 inhibitorNon-inhibitor0.9441
CYP450 2C19 inhibitorNon-inhibitor0.939
CYP450 3A4 inhibitorInhibitor0.796
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8886
Ames testNon AMES toxic0.9117
CarcinogenicityNon-carcinogens0.9466
BiodegradationNot ready biodegradable0.9759
Rat acute toxicity2.1601 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9483
hERG inhibition (predictor II)Non-inhibitor0.5627
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
LC-MS/MS Spectrum - LC-ESI-qTof , PositiveLC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03k9-1794300000-d4cdef973973a6b24ba4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-00dj-3950000000-8e98d604876730f53851

Taxonomy

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
Progestogin-skeleton / 21-hydroxysteroid / Pregnane-skeleton / 20-oxosteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 11-hydroxysteroid / 11-beta-hydroxysteroid / Oxosteroid / Delta-1,4-steroid
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)

Targets

Details
1. Glucocorticoid receptor
Kind
Protein
Organism
Humans
Pharmacological action
Yes
Actions
Antagonist
General Function
Zinc ion binding
Specific Function
Receptor for glucocorticoids (GC). 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 modula...
Gene Name
NR3C1
Uniprot ID
P04150
Uniprot Name
Glucocorticoid receptor
Molecular Weight
85658.57 Da
References
  1. 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. [PubMed:11040338]
  2. 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. [PubMed:11258648]
  3. 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. [PubMed:11730731]
  4. 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. [PubMed:12601049]
  5. 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. [PubMed:12920235]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Structural molecule activity
Specific 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). Play...
Gene Name
ANXA1
Uniprot ID
P04083
Uniprot Name
Annexin A1
Molecular Weight
38713.855 Da
References
  1. 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. [PubMed:8060156]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
Molecular Weight
57342.67 Da
References
  1. 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. [PubMed:7720517]
  2. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
  3. 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. [PubMed:28730856]
  4. 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. [PubMed:19138736]
  5. 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. [PubMed:12673034]
  6. 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. [PubMed:1614409]
  7. 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. [PubMed:24451000]
  8. FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
  9. FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
  10. FDA Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
  11. FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
  12. FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Spray [Link]
  13. FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
  14. FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
  15. FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP3A5
Uniprot ID
P20815
Uniprot Name
Cytochrome P450 3A5
Molecular Weight
57108.065 Da
References
  1. Rendic S: Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev. 2002 Feb-May;34(1-2):83-448. [PubMed:11996015]
Kind
Protein group
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inducer
General Function
Vitamin d3 25-hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...

Components:
References
  1. 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. [PubMed:24555085]
  2. 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. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific 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. Const...
Gene Name
CYP2A6
Uniprot ID
P11509
Uniprot Name
Cytochrome P450 2A6
Molecular Weight
56501.005 Da
References
  1. 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. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Oxygen binding
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP1B1
Uniprot ID
Q16678
Uniprot Name
Cytochrome P450 1B1
Molecular Weight
60845.33 Da
References
  1. 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. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2B6
Uniprot ID
P20813
Uniprot Name
Cytochrome P450 2B6
Molecular Weight
56277.81 Da
References
  1. 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. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C8
Uniprot ID
P10632
Uniprot Name
Cytochrome P450 2C8
Molecular Weight
55824.275 Da
References
  1. 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. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally un...
Gene Name
CYP2C9
Uniprot ID
P11712
Uniprot Name
Cytochrome P450 2C9
Molecular Weight
55627.365 Da
References
  1. 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. [PubMed:24451000]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Inducer
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and im...
Gene Name
CYP2C19
Uniprot ID
P33261
Uniprot Name
Cytochrome P450 2C19
Molecular Weight
55930.545 Da
References
  1. 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. [PubMed:24451000]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Binder
General Function
Steroid binding
Specific Function
Major transport protein for glucocorticoids and progestins in the blood of almost all vertebrate species.
Gene Name
SERPINA6
Uniprot ID
P08185
Uniprot Name
Corticosteroid-binding globulin
Molecular Weight
45140.49 Da
References
  1. 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. [PubMed:23300763]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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
  1. 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. [PubMed:15634032]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Transporter activity
Specific Function
Involved in the ATP-dependent secretion of bile salts into the canaliculus of hepatocytes.
Gene Name
ABCB11
Uniprot ID
O95342
Uniprot Name
Bile salt export pump
Molecular Weight
146405.83 Da
References
  1. 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. [PubMed:24014644]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. 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. [PubMed:28730856]
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 sulfobromophthalein (BSP) and conjugated (taurocholate) and unconjugated (cholate) bile acids (By similarity). Selectively inhibit...
Gene Name
SLCO1A2
Uniprot ID
P46721
Uniprot Name
Solute carrier organic anion transporter family member 1A2
Molecular Weight
74144.105 Da
References
  1. Bossuyt X, Muller M, Hagenbuch B, Meier PJ: Polyspecific drug and steroid clearance by an organic anion transporter of mammalian liver. J Pharmacol Exp Ther. 1996 Mar;276(3):891-6. [PubMed:8786566]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Plays an important role in the excretion/detoxification of endogenous and exogenous organic anions, especially from the brain and kidney. Involved in the transport basolateral of steviol, fexofenad...
Gene Name
SLC22A8
Uniprot ID
Q8TCC7
Uniprot Name
Solute carrier family 22 member 8
Molecular Weight
59855.585 Da
References
  1. 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. [PubMed:19953504]

Drug created on June 13, 2005 07:24 / Updated on July 06, 2020 07:41

Logo pink
Are you a
new drug developer?
Contact us to learn more about our customized products and solutions.
Logo pink
Stay in the know!
As part of our commitment to providing the most up-to-date drug information, we will be releasing #DrugBankUpdates with our newly added curated drug pages.
#DrugBankUpdates