Budesonide

Identification

Summary

Budesonide is a corticosteroid used to treat Crohn's disease, asthma, COPD, hay fever and allergies, and ulcerative colitis.

Brand Names

Breyna, Breztri, Cortiment, Entocort, Ortikos, 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

3D

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MOLSDF3D-SDFPDBSMILESInChI

Similar Structures

Structure for Budesonide (DB01222)

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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.¹⁷

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Associated Conditions

• Allergic Reaction
• Allergic Rhinitis (AR)
• Asthma
• Chronic Obstructive Pulmonary Disease (COPD)
• Collagenous Colitis
• Crohn's Disease (CD)
• Eosinophilic Esophagitis (EoE)
• Nasal Congestion
• Polyps, Nasal
• Proteinuria
• Pruritus
• Rhino Sinusitis
• Ulcerative Colitis
• Vasomotor Rhinitis
• Corticosteroid-responsive dermatoses
• Mild Crohn’s Disease
• Moderate Crohn’s Disease

Associated Therapies

• Maintenance therapy

Contraindications & Blackbox Warnings

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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	agonist	Humans
UAnnexin A1	substrate	Humans

Absorption

Extended release oral capsules are 9-21% bioavailable.^9,10 A 9mg dose reaches a C_max of 1.50±0.79ng/mL with a T_max of 2-8h and an AUC of 7.33ng*hr/mL.^9,10 A high fat meal increases the T_max 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 C_max of 0.6-1.6nmol/L with a T_max of 10 minutes.¹¹

A 1mg nebulized dose is 6% bioavailable, reaching a C_max of 2.6nmol/L with a T_max of 20 minutes.¹²

A 9mg oral extended release tablet reaches a C_max of 1.35±0.96ng/mL with a T_max 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

• Budesonide
  • 6-beta-hydroxybudesonide
  • 22-hydroxy Intermediate Metabolite of Budesonide
    • 16alpha-butyrloxyprednisolone
      • 16-alpha-hydroxyprednisolone
  • delta6-budesonide
  • 23-hydroxybudesonide

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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Toxicity

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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abacavir	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.
Acarbose	The risk or severity of hyperglycemia can be increased when Budesonide is combined with Acarbose.
Aceclofenac	The risk or severity of gastrointestinal irritation can be increased when Budesonide is combined with Aceclofenac.
Acemetacin	The risk or severity of gastrointestinal irritation can be increased when Budesonide is combined with Acemetacin.
Acenocoumarol	Budesonide may increase the anticoagulant activities of Acenocoumarol.
Acetaminophen	Acetaminophen may decrease the excretion rate of Budesonide which could result in a higher serum level.

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Food Interactions

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

Products

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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	Aerosol, foam	28 mg/1	Rectal	Oceanside Pharmaceuticals	2014-12-01	Not applicable
Budesonide	Capsule	3 mg/1	Oral	Padagis US LLC	2018-06-29	Not applicable
Budesonide	Spray, metered	32 ug/1	Nasal	Astra Zeneca Lp	2014-05-13	2018-02-28
Budesonide	Capsule, extended release	3 mg	Oral	Tillotts Pharma Gmbh	2020-01-17	Not applicable
Cortiment	Tablet, extended release	9 mg	Oral	Ferring Pharmaceuticals	2016-07-25	Not applicable
Entocort	Capsule, extended release	3 mg	Oral	Tillotts Pharma Gmbh	1997-01-30	Not applicable
Entocort EC	Capsule	3 mg/1	Oral	Prometheus Laboratories	2001-10-29	Not applicable
Entocort EC	Capsule	3 mg/1	Oral	Physicians Total Care, Inc.	2006-05-22	Not applicable
Entocort EC	Capsule	3 mg/1	Oral	Padagis US LLC	2001-10-29	Not applicable
Entocort EC	Capsule	3 mg/1	Oral	AstraZeneca Pharmaceuticals LP	2001-10-02	2019-01-31

Generic Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Budesonide	Suspension	1 mg/2mL	Respiratory (inhalation)	Sandoz Inc	2015-07-24	Not applicable
Budesonide	Capsule	3 mg/1	Oral	Par Pharmaceutical Inc.	2011-08-18	2018-04-30
Budesonide	Suspension	0.5 mg/2mL	Respiratory (inhalation)	Sun Pharmaceutical Industries, Inc.	2021-05-01	Not applicable
Budesonide	Suspension	0.5 mg/2mL	Respiratory (inhalation)	Dispensing Solutions, Inc.	2008-11-19	Not applicable
Budesonide	Inhalant	0.25 mg/2mL	Respiratory (inhalation)	Nephron Pharmaceuticals Corporation	2013-10-01	Not applicable
Budesonide	Capsule, delayed release	3 mg/1	Oral	Mylan Pharmaceuticals Inc.	2011-05-16	2022-08-31
Budesonide	Capsule	3 mg/1	Oral	Mylan Institutional Inc.	2011-09-02	2022-04-30
Budesonide	Tablet, film coated, extended release	9 mg/1	Oral	Mylan Pharmaceuticals Inc.	2020-10-20	2030-01-31
Budesonide	Suspension	0.5 mg/2mL	Respiratory (inhalation)	Apotex Corp.	2009-03-30	2021-06-20
Budesonide	Capsule, delayed release	3 mg/1	Oral	Golden State Medical Supply, Inc.	2011-05-16	2022-08-31

Over the Counter Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Budesonide	Spray, metered	32 ug/1	Nasal	Topco Associates LLC	2016-08-31	2020-07-31
Budesonide	Spray, metered	32 ug/1	Nasal	CVS PHARMACY	2016-04-09	Not applicable
Budesonide	Spray, metered	32 ug/1	Nasal	Walmart	2016-08-22	Not applicable
Budesonide	Spray, metered	32 ug/1	Nasal	Walgreens	2016-04-11	Not applicable
Budesonide	Spray, metered	32 ug/1	Nasal	RUGBY LABORATORIES	2016-07-13	Not applicable
Budesonide	Spray, metered	32 ug/1	Nasal	Rite Aid	2016-07-13	Not applicable
Budesonide	Spray, metered	32 ug/1	Nasal	Apotex Corp.	2018-04-26	Not applicable
Budesonide	Spray, metered	32 ug/1	Nasal	Safeway	2016-09-15	2023-10-24
Budesonide	Spray, metered	32 ug/1	Nasal	Apotex Corp.	2016-04-19	Not applicable
Budesonide	Spray, metered	32 ug/1	Nasal	Rite Aid	2019-10-10	Not applicable

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 İLAÇ SAN. TİC. A.Ş.	2020-08-14	Not applicable
AIRBIR 3/100 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 KPS	Budesonide (100 mcg) + Arformoterol (3 mcg)	Powder	Respiratory (inhalation)	NEUTEC İLAÇ SAN. TİC. A.Ş.	2020-08-14	Not applicable
AIRBIR 3/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL ,120 KAPSÜL	Budesonide (200 mcg) + Arformoterol (3 mcg)	Powder	Respiratory (inhalation)	NEUTEC İLAÇ SAN. TİC. A.Ş.	2020-08-14	Not applicable
AIRBIR 3/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL ,60 KAPSÜL	Budesonide (200 mcg) + Arformoterol (3 mcg)	Powder	Respiratory (inhalation)	NEUTEC İLAÇ SAN. TİC. A.Ş.	2020-08-14	Not applicable
AIRBIR 6/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 ADET	Budesonide (200 mcg) + Arformoterol (6 mcg)	Powder	Respiratory (inhalation)	NEUTEC İLAÇ SAN. TİC. A.Ş.	2020-08-14	Not applicable
AIRBIR 6/200 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 ADET	Budesonide (200 mcg) + Arformoterol (6 mcg)	Powder	Respiratory (inhalation)	NEUTEC İLAÇ SAN. TİC. A.Ş.	2020-08-14	Not applicable
AIRBIR 6/400 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 120 KPS	Budesonide (400 mcg) + Arformoterol (6 mcg)	Powder	Respiratory (inhalation)	NEUTEC İLAÇ SAN. TİC. A.Ş.	2020-08-14	Not applicable
AIRBIR 6/400 MCG INHALASYON IÇIN TOZ IÇEREN KAPSÜL, 60 KPS	Budesonide (400 mcg) + Arformoterol (6 mcg)	Powder	Respiratory (inhalation)	NEUTEC İLAÇ SAN. TİC. A.Ş.	2020-08-14	Not applicable
AIRBUFO FORSPIRO 160/4.5UG	Budesonide (160 µg) + Formoterol fumarate (4.5 µg)	Powder	Respiratory (inhalation)		2016-07-01	Not applicable
AIRBUFO FORSPIRO 160/4.5UG	Budesonide (160 µg) + Formoterol fumarate (4.5 µg)	Powder	Respiratory (inhalation)		2016-07-01	Not applicable

Categories

ATC Codes

R03AL11 — Formoterol, glycopyrronium bromide and budesonide

• R03AL — Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
• R03A — ADRENERGICS, INHALANTS
• R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
• R — RESPIRATORY SYSTEM

D07AC09 — Budesonide

• D07AC — Corticosteroids, potent (group III)
• D07A — CORTICOSTEROIDS, PLAIN
• D07 — CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS
• D — DERMATOLOGICALS

R01AD05 — Budesonide

• R01AD — Corticosteroids
• R01A — DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE
• R01 — NASAL PREPARATIONS
• R — RESPIRATORY SYSTEM

R03AK07 — Formoterol 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

A07EA06 — Budesonide

• A07EA — Corticosteroids acting locally
• A07E — INTESTINAL ANTIINFLAMMATORY AGENTS
• A07 — ANTIDIARRHEALS, INTESTINAL ANTIINFLAMMATORY/ANTIINFECTIVE AGENTS
• A — ALIMENTARY TRACT AND METABOLISM

R03BA02 — Budesonide

• R03BA — Glucocorticoids
• R03B — OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS
• R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
• R — RESPIRATORY SYSTEM

R03AK12 — Salmeterol 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

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 / Oxacyclic compounds / Acetals / Primary alcohols / Organic oxides / Hydrocarbon 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 / Carbonyl group / Cyclic alcohol / Cyclic ketone / Delta-1,4-steroid / Hydrocarbon derivative / Ketone / Meta-dioxolane / Organic oxide / Organic oxygen compound / Organoheterocyclic compound / Organooxygen compound / Oxacycle / Oxosteroid / Pregnane-skeleton / Primary alcohol / Progestogin-skeleton / Secondary alcohol

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

1. Yasir M, Sonthalia S: Corticosteroid Adverse Effects . [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
7. 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]
8. FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Aerosol (Discontinued) [Link]
9. FDA Approved Drug Products: Entocort Budesonide Oral Extended Release Capsules [Link]
10. FDA Approved Drug Products: Ortikos Budesonide Oral Extended Release Capsules [Link]
11. FDA Approved Drug Products: Pulmicort Budesonide Inhalation Powder [Link]
12. FDA Approved Drug Products: Pulmicort Budesonide Inhalation Suspension [Link]
13. FDA Approved Drug Products: Rhinocort Budesonide Nasal Metered Spray [Link]
14. FDA Approved Drug Products: Symbicort (budesonide/formoterol fumarate) inhalation aerosol [Link]
15. FDA Approved Drug Products: Uceris Budesonide Oral Extended Release Tablets [Link]
16. FDA Approved Drug Products: Uceris Budesonide Rectal Aerosol Foam [Link]
17. FDA Approved Drug Products: Tarpeyo (budesonide) delayed-release capsules for oral use [Link]
18. 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]

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

FDA label

Download (52.3 KB)

MSDS

Download (73.7 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Asthma / Severe Eosinophilic Asthma	1
4	Completed	Not Available	Asthma	1
4	Completed	Basic Science	Chronic Obstructive Pulmonary Disease (COPD)	2
4	Completed	Basic Science	Mild Intermittent Asthma	1
4	Completed	Other	Asthma	1
4	Completed	Prevention	Asthma	1
4	Completed	Supportive Care	Asthma	1
4	Completed	Supportive Care	Lung Cancers	1
4	Completed	Treatment	ALL, Pediatric / Asthma	1
4	Completed	Treatment	Allergic Rhinitis (AR)	1

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
Powder, metered	Respiratory (inhalation)
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
Solution	Nasal; Respiratory (inhalation)	0.1 g
Aerosol	Oral; Respiratory (inhalation)	0.3256 %
Ointment	Topical	25 mg
Aerosol	Respiratory (inhalation)	200 cg
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
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)	100 mcg
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
Capsule
Capsule, coated	Oral	3 mg
Capsule		3 mg
Capsule	Oral
Capsule	Oral	3 mg
Aerosol, foam	Rectal	2 mg/1dose
Aerosol, foam	Rectal	2 mg
Aerosol	Rectal	2 mg
Gas	Respiratory (inhalation)	0.2 MG
Spray	Nasal	32 UG
Spray	Nasal	64 UG
Spray	Nasal	0.05 mg/0.051mL
Solution	Respiratory (inhalation)
Aerosol	Respiratory (inhalation)	0.25 g
Aerosol, powder	Respiratory (inhalation)	0.1 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
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)
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
Aerosol, powder	Respiratory (inhalation)	200 mcg
Powder, metered	Respiratory (inhalation)	400 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	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	Nasal	64 mcg
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
Tablet, extended release	Oral	9 mg
Tablet, film coated, extended release	Oral	9 mg
Capsule	Respiratory (inhalation)	0.2 mg/1
Capsule	Respiratory (inhalation)	0.4 mg/1
Aerosol, metered	Respiratory (inhalation)	200 MICROGRAMMI
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
Tablet	Rectal
Enema; tablet	Rectal	2.3 mg
Capsule, extended release	Oral	3 mg
Capsule	Oral	3 mg/1
Enema; kit; tablet	Rectal
Tablet, soluble	Oral	2.3 mg
Spray	Nasal	2.0 mg/ml
Solution	Respiratory (inhalation)
Capsule	Respiratory (inhalation)
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
Suspension	Respiratory (inhalation)	0.5 mg
Aerosol	Respiratory (inhalation)	4 mg
Solution	Respiratory (inhalation)	4 mg
Suspension	Nasal; Respiratory (inhalation)
Suspension	Respiratory (inhalation)	0.2 mg
Granule
Tablet, orally disintegrating	Oral	0.5 mg
Tablet, orally disintegrating	Oral	1 mg
Cream	Topical	0.25 g
Aerosol, metered	Respiratory (inhalation)	200 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
Powder	Respiratory (inhalation)	200 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
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
Cream	Topical
Ointment
Powder	Respiratory (inhalation)	100 MCG
Powder	Respiratory (inhalation)	400 MCG
Spray, suspension	Respiratory (inhalation)	0125 MG/ML
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
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
Suspension	Respiratory (inhalation)
Suspension	Respiratory (inhalation)	0.5 mg/ml
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
Aerosol, powder	Respiratory (inhalation)	0.2 mg
Aerosol, powder	Respiratory (inhalation)	0.4 mg
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
Powder	Respiratory (inhalation)	100 cg
Powder	Respiratory (inhalation)	200 cg
Aerosol, metered	Respiratory (inhalation)
Powder	Respiratory (inhalation)	400 cg
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
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, powder	Respiratory (inhalation)
Powder	Respiratory (inhalation)
Suspension	Respiratory (inhalation)
Aerosol, metered; 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, metered	Respiratory (inhalation)	160 mcg
Powder, metered	Respiratory (inhalation)	80 mcg
Powder, metered	Respiratory (inhalation)	320 mcg
Patch	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
Aerosol, foam	Rectal	28 mg/1
Kit	Rectal	2 mg / act
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
CA2071518	No	2002-11-12	2010-11-15
US6598603	Yes	2003-07-29	2019-06-23
US6899099	Yes	2005-05-31	2019-06-23
US7524834	Yes	2009-04-28	2019-05-11
US7759328	Yes	2010-07-20	2023-07-29
US7897646	Yes	2011-03-01	2019-03-09
US8143239	Yes	2012-03-27	2023-07-29
US8461211	Yes	2013-06-11	2019-03-09
US8575137	Yes	2013-11-05	2023-07-29
US6123924	No	2000-09-26	2017-09-26
US7967011	Yes	2011-06-28	2022-02-11
US8616196	Yes	2013-12-31	2029-10-07
US8387615	Yes	2013-03-05	2025-05-10
US7587988	Yes	2009-09-15	2026-10-10
US7367333	Yes	2008-05-06	2019-05-11
US8528545	Yes	2013-09-10	2029-04-16
US8875699	Yes	2014-11-04	2025-05-10
US6027714	No	2000-02-22	2018-01-09
US7143764	No	2006-12-05	2018-03-13
US6142145	No	2000-11-07	2018-05-08
US6287540	No	2001-09-11	2018-01-09
US9320716	No	2016-04-26	2020-06-09
US9192581	No	2015-11-24	2031-09-07
US7410651	No	2008-08-12	2020-06-09
USRE43799	No	2012-11-13	2020-06-09
US8895064	No	2014-11-25	2031-09-07
US7431943	No	2008-10-07	2020-06-09
US9132093	No	2015-09-15	2031-09-07
US8784888	No	2014-07-22	2020-06-09
US8293273	No	2012-10-23	2020-06-09
US5914122	No	1999-06-22	2015-12-19
US9532954	No	2017-01-03	2020-06-09
US9463161	No	2016-10-11	2030-05-28
US9415009	No	2016-08-16	2030-05-28
US8808713	No	2014-08-19	2030-05-28
US8324266	No	2012-12-04	2030-05-28
US8703806	No	2014-04-22	2030-05-28
US8815258	No	2014-08-26	2031-03-17
US10064878	No	2018-09-04	2020-06-09
US10105374	No	2018-10-23	2020-06-09
US10166247	Yes	2019-01-01	2023-07-29
US10143698	No	2018-12-04	2020-06-09
US9707182	No	2017-07-18	2036-09-09
US10172802	No	2019-01-08	2036-09-09
US10307375	No	2019-06-04	2031-09-07
US10660858	No	2020-05-26	2031-09-07
US10716753	No	2020-07-21	2030-05-28
US8491932	No	2013-07-23	2029-05-07

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

ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397)

Spectra

Mass Spec (NIST)

Not Available

Spectra

Spectrum	Spectrum Type	Splash Key
Predicted GC-MS Spectrum - GC-MS	Predicted GC-MS	Not Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)	Predicted LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	Not Available
LC-MS/MS Spectrum - LC-ESI-qTof , Positive	LC-MS/MS	Not Available
MS/MS Spectrum - , positive	LC-MS/MS	splash10-03k9-1794300000-d4cdef973973a6b24ba4
MS/MS Spectrum - , positive	LC-MS/MS	splash10-00dj-3950000000-8e98d604876730f53851

Targets

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insights and accelerate drug research.

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Binding Properties

×

Property	Measurement	pH	Temperature (°C)	References
EC 50 (nM)	12.4	N/A	N/A	A28638

Details

Binding Properties1. Glucocorticoid receptor

Kind

Protein

Organism

Humans

Pharmacological action

Yes

Actions

Agonist

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. [Article]
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. [Article]
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. [Article]
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. [Article]
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. [Article]
6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [Article]

Details2. Annexin A1

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. [Article]

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Drug created at June 13, 2005 13:24 / Updated at July 02, 2022 14:09