Identification

Name
Fluticasone furoate
Accession Number
DB08906
Description

Fluticasone furoate is a synthetic glucocorticoid available as an inhaler and nasal spray for various inflammatory indicationsLabel8. Fluticasone furoate was first approved in 20077.

Type
Small Molecule
Groups
Approved
Structure
Thumb
Weight
Average: 538.576
Monoisotopic: 538.163693965
Chemical Formula
C27H29F3O6S
Synonyms
  • Fluticasone furoate
  • Fluticasonum furoas
  • Furoate de fluticasone
  • Furoato de fluticasona
External IDs
  • GSK 685698
  • GW-685698X
  • GW685698X

Pharmacology

Indication

Fluticasone furoate is indicated as an inhaler for the treatment and management of asthma by prophylaxisLabel8. The fluticasone furoate nasal spray is indicated for treating season and perennial allergic rhinitisLabel4.

Associated Conditions
Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
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Pharmacodynamics

Systemically, in vitro experiments show fluticasone furoate activates glucocorticoid receptors, inhibits nuclear factor kappa b, and inhibits lung eosinophilia in ratsLabel8,4.

Mechanism of action

Fluticasone furoate works through an unknown mechanism to affect the action of various cell types and mediators of inflammationLabel8. In vitro experiments show fluticasone furoate activating glucocorticoid receptors, inhibiting nuclear factor kappa b, and inhibiting lung eosinophilia in ratsLabel8,4.

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Humans
UProgesterone receptor
agonist
Humans
UMineralocorticoid receptor
antagonist
Humans
Absorption

Intranasal exposure of fluticasone furoate results in patients swallowing a larger portion of the doseLabel1. However, absorption is poor and metabolism is high, therefore there is negligible systemic exposure with a nasal bioavailability of 0.50% and oral bioavialability of 1.26%Label5. Inhaled bioavailability is 13.9%8. A study of 24 healthy Caucasian males showed an inhaled bioavailability of 6.3-18.4%5.

Volume of distribution

608L at steady state for intravenous administration of fluticasone furoateLabel. Other reports suggest the mean volume of distribution at steady state is 661L8. A study of 24 healthy Caucasian males showed a volume of distribution at steady state of 704L following intravenous administration5.

Protein binding

Fluticasone furoate is >99%Label protein bound in serum and may be as high as 99.6%8.

Metabolism

Fluticasone furoate is cleared from hepatic metabolism by cytochrome P450 3A4Label8,2. Fluticasone furoate is hydrolysed at the FIVE-S-fluoromethyl carbothioate group, forming an inactive metaboliteLabel1.

Hover over products below to view reaction partners

Route of elimination

Fluticasone furoate is eliminated ≥90% in the feces and 1-2% in the urineLabel8.

Half-life

15.1 hours for intranasal fluticasone furoateLabel and 24 hours for the inhaled formulation8. A study of 24 healthy Caucasian males showed a half life of 13.6 hours following intravenous administration and 17.3-23.9 hours followed inhalation5.

Clearance

57.8L/h for fluticasone furoateLabel. A study of 24 healthy Caucasian males showed a clearance of 71.8L/h following intravenous administration5.

Adverse Effects
Learn about our commercial Adverse Effects data.
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Toxicity

Fluticasone furoate administered nasally may be associated with adrenal suppression or an increase in QTc interval though the association has not been well demonstrated in studiesLabel6. Fluticasone furoate requires no dosage adjustment in renal impairment but must be used in caution in hepatic impairment due to the elimination mechanismsLabel8. Fluticasone furoate is not associated with carcinogenicity, mutagenicity, or impairment of fertilityLabel. There are no well controlled studies in pregnancy or lactation though animal studies have shown teratogenicity and hypoadrenalism in the offspring of treated mothers and other corticosteroids are known to be excreted in breast milkLabel. Generally, there are no reported adverse effects with fluticasone in pregnancy3. Pediatric patients should be given the lowest possible dose and monitored for reduction in growth velocityLabel6. There is insufficient evidence to determine whether geriatric patients respond differently to other patientsLabel. Systemic exposure may be 27-49% higher in Japanese, Korean, and Chinese patients compared to Caucasian patients8. Caution should be exercised in these patients and the benefit and risk should be assessed before deciding on a treatmentLabel.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
DrugInteraction
AbametapirThe serum concentration of Fluticasone furoate can be increased when it is combined with Abametapir.
AbataceptThe metabolism of Fluticasone furoate can be increased when combined with Abatacept.
AbirateroneThe metabolism of Abiraterone can be increased when combined with Fluticasone furoate.
AcalabrutinibThe metabolism of Fluticasone furoate can be increased when combined with Acalabrutinib.
AcarboseThe risk or severity of hyperglycemia can be increased when Fluticasone furoate is combined with Acarbose.
AceclofenacThe risk or severity of gastrointestinal irritation can be increased when Fluticasone furoate is combined with Aceclofenac.
AcemetacinThe risk or severity of gastrointestinal irritation can be increased when Fluticasone furoate is combined with Acemetacin.
AcenocoumarolFluticasone furoate may increase the anticoagulant activities of Acenocoumarol.
AcetohexamideThe risk or severity of hyperglycemia can be increased when Fluticasone furoate is combined with Acetohexamide.
AcetyldigitoxinThe risk or severity of adverse effects can be increased when Fluticasone furoate is combined with Acetyldigitoxin.
Additional Data Available
  • Extended Description
    Extended Description

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

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  • Severity
    Severity

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

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  • Evidence Level
    Evidence Level

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

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  • Action
    Action

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

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Food Interactions
No interactions found.

Products

Brand Name Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
AlisadeSpray, suspension27.5 micrograms/sprayIntrasinalGlaxo Group Limited2008-10-062011-10-18EU flag
AlisadeSpray, suspension27.5 micrograms/sprayIntrasinalGlaxo Group Limited2008-10-062011-10-18EU flag
AlisadeSpray, suspension27.5 micrograms/sprayIntrasinalGlaxo Group Limited2008-10-062011-10-18EU flag
Arnuity ElliptaPowder100 mcgRespiratory (inhalation)Glaxosmithkline Inc2016-01-26Not applicableCanada flag
Arnuity ElliptaPowder100 ug/1Respiratory (inhalation)GlaxoSmithKline LLC2014-08-20Not applicableUS flag
Arnuity ElliptaPowder50 ug/1Respiratory (inhalation)GlaxoSmithKline LLC2018-05-17Not applicableUS flag
Arnuity ElliptaPowder200 mcgRespiratory (inhalation)Glaxosmithkline Inc2015-12-14Not applicableCanada flag
Arnuity ElliptaPowder200 ug/1Respiratory (inhalation)GlaxoSmithKline LLC2014-08-20Not applicableUS flag
AvamysSpray, suspension27.5 micrograms/sprayIntrasinalGlaxo Group Limited2008-01-11Not applicableEU flag
AvamysSpray, meteredNasalGlaxosmithkline Inc2007-10-22Not applicableCanada flag
Additional Data Available
  • Application Number
    Application Number

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

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  • Product Code
    Product Code

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

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Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing EndRegionImage
Flonase Sensimist Allergy ReliefSpray, metered27.5 ug/1NasalGlaxoSmithKline Consumer Healthcare Holdings (US) LLC2017-02-01Not applicableUS flag
Flonase Sensimist Allergy ReliefSpray, metered27.5 ug/1NasalGlaxoSmithKline Consumer Healthcare Holdings (US) LLC2017-07-01Not applicableUS flag
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 EndRegionImage
Breo ElliptaFluticasone furoate (100 ug/1) + Vilanterol trifenatate (25 ug/1)PowderRespiratory (inhalation)REMEDYREPACK INC.2019-04-17Not applicableUS flag
Breo ElliptaFluticasone furoate (100 mcg) + Vilanterol (25 mcg)PowderRespiratory (inhalation)Glaxosmithkline Inc2013-11-29Not applicableCanada flag
Breo ElliptaFluticasone furoate (100 ug/1) + Vilanterol trifenatate (25 ug/1)PowderRespiratory (inhalation)Glaxo Operations UK Ltd2013-08-262018-01-08US flag
Breo ElliptaFluticasone furoate (100 ug/1) + Vilanterol trifenatate (25 ug/1)PowderRespiratory (inhalation)GlaxoSmithKline LLC2013-08-26Not applicableUS flag
Breo ElliptaFluticasone furoate (100 ug/1) + Vilanterol trifenatate (25 ug/1)PowderRespiratory (inhalation)Remedy Repack2016-04-042016-04-05US flag
Breo ElliptaFluticasone furoate (200 mcg) + Vilanterol (25 mcg)PowderRespiratory (inhalation)Glaxosmithkline Inc2015-10-02Not applicableCanada flag
Breo ElliptaFluticasone furoate (200 ug/1) + Vilanterol trifenatate (25 ug/1)PowderRespiratory (inhalation)Glaxo Operations UK Ltd2015-04-302018-01-08US flag
Breo ElliptaFluticasone furoate (200 ug/1) + Vilanterol trifenatate (25 ug/1)PowderRespiratory (inhalation)GlaxoSmithKline LLC2015-04-30Not applicableUS flag
Breo ElliptaFluticasone furoate (200 ug/1) + Vilanterol trifenatate (25 ug/1)PowderRespiratory (inhalation)A-S Medication Solutions2015-04-30Not applicableUS flag
Trelegy ElliptaFluticasone furoate (100 mcg) + Umeclidinium (62.5 mcg) + Vilanterol (25 mcg)PowderRespiratory (inhalation)Glaxosmithkline Inc2018-05-30Not applicableCanada flag

Categories

ATC Codes
R03AL08 — Vilanterol, umeclidinium bromide and fluticasone furoateR01AD12 — Fluticasone furoateR03AK10 — Vilanterol and fluticasone furoateR03BA09 — Fluticasone furoate
Drug Categories
Chemical TaxonomyProvided by Classyfire
Description
This compound belongs to the class of organic compounds known as steroid esters. These are compounds containing a steroid moiety which bears a carboxylic acid ester group.
Kingdom
Organic compounds
Super Class
Lipids and lipid-like molecules
Class
Steroids and steroid derivatives
Sub Class
Steroid esters
Direct Parent
Steroid esters
Alternative Parents
Androgens and derivatives / 11-beta-hydroxysteroids / 3-oxo delta-1,4-steroids / Halogenated steroids / Delta-1,4-steroids / Furoic acid esters / Heteroaromatic compounds / Thioesters / Secondary alcohols / Carbothioic S-esters
show 11 more
Substituents
11-beta-hydroxysteroid / 11-hydroxysteroid / 3-oxo-delta-1,4-steroid / 3-oxosteroid / 6-halo-steroid / 9-halo-steroid / Alcohol / Alkyl fluoride / Alkyl halide / Androgen-skeleton
show 34 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
thioester, 11beta-hydroxy steroid, steroid ester, fluorinated steroid, 3-oxo-Delta(1),Delta(4)-steroid, corticosteroid, 2-furoate ester (CHEBI:74899)

Chemical Identifiers

UNII
JS86977WNV
CAS number
397864-44-7
InChI Key
XTULMSXFIHGYFS-VLSRWLAYSA-N
InChI
InChI=1S/C27H29F3O6S/c1-14-9-16-17-11-19(29)18-10-15(31)6-7-24(18,2)26(17,30)21(32)12-25(16,3)27(14,23(34)37-13-28)36-22(33)20-5-4-8-35-20/h4-8,10,14,16-17,19,21,32H,9,11-13H2,1-3H3/t14-,16+,17+,19+,21+,24+,25+,26+,27+/m1/s1
IUPAC Name
(1R,2S,8S,10S,11S,13R,14R,15S,17S)-1,8-difluoro-14-{[(fluoromethyl)sulfanyl]carbonyl}-17-hydroxy-2,13,15-trimethyl-5-oxotetracyclo[8.7.0.0²,⁷.0¹¹,¹⁵]heptadeca-3,6-dien-14-yl furan-2-carboxylate
SMILES

References

Synthesis Reference

Adrienne KOVACSNE-MEZEI, Roman Gabriel, Alexandr Jegorov, "POLYMORPHS OF FLUTICASONE FUROATE AND PROCESSES FOR PREPARATION THEREOF." U.S. Patent US20100240629, issued September 23, 2010.

US20100240629
General References
  1. Phillipps GH: Structure-activity relationships of topically active steroids: the selection of fluticasone propionate. Respir Med. 1990 Nov;84 Suppl A:19-23. [PubMed:2287791]
  2. Harding SM: The human pharmacology of fluticasone propionate. Respir Med. 1990 Nov;84 Suppl A:25-9. [PubMed:2287792]
  3. Choi JS, Han JY, Kim MY, Velazquez-Armenta EY, Nava-Ocampo AA: Pregnancy outcomes in women using inhaled fluticasone during pregnancy: a case series. Allergol Immunopathol (Madr). 2007 Nov-Dec;35(6):239-42. [PubMed:18047814]
  4. Spadijer Mirkovic C, Peric A, Vukomanovic Durdevic B, Vojvodic D: Effects of Fluticasone Furoate Nasal Spray on Parameters of Eosinophilic Inflammation in Patients With Nasal Polyposis and Perennial Allergic Rhinitis. Ann Otol Rhinol Laryngol. 2017 Aug;126(8):573-580. doi: 10.1177/0003489417713505. Epub 2017 Jun 6. [PubMed:28587510]
  5. Allen A, Bareille PJ, Rousell VM: Fluticasone furoate, a novel inhaled corticosteroid, demonstrates prolonged lung absorption kinetics in man compared with inhaled fluticasone propionate. Clin Pharmacokinet. 2013 Jan;52(1):37-42. doi: 10.1007/s40262-012-0021-x. [PubMed:23184737]
  6. Allen A, Schenkenberger I, Trivedi R, Cole J, Hicks W, Gul N, Jacques L: Inhaled fluticasone furoate/vilanterol does not affect hypothalamic-pituitary-adrenal axis function in adolescent and adult asthma: randomised, double-blind, placebo-controlled study. Clin Respir J. 2013 Oct;7(4):397-406. doi: 10.1111/crj.12026. Epub 2013 Jun 5. [PubMed:23578031]
  7. FDA Fluticasone Furoate Approval 2007 [Link]
  8. Fluticasone Furoate (Arnuity Ellipta) FDA Label [File]
KEGG Drug
D06315
PubChem Compound
9854489
PubChem Substance
175427145
ChemSpider
8030195
BindingDB
50354851
RxNav
705022
ChEBI
74899
ChEMBL
CHEMBL1676
ZINC
ZINC000003992105
PDBe Ligand
GW6
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Fluticasone_furoate
AHFS Codes
  • 52:08.08 — Corticosteroids
PDB Entries
3cld
FDA label
Download (469 KB)
MSDS
Download (309 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
4Active Not RecruitingTreatmentAsthma1
4CompletedNot AvailableRhinitis, Allergic, Perennial1
4CompletedNot AvailableSeasonal Allergic Rhinitis (SAR)1
4CompletedBasic ScienceChildhood Obstructive Sleep Apnea Syndrome (OSAS)1
4CompletedBasic ScienceChronic Obstructive Pulmonary Disease (COPD)1
4CompletedOtherRhinitis, Allergic, Perennial and Seasonal1
4CompletedOtherSeasonal Allergic Rhinitis (SAR)1
4CompletedTreatmentAllergic Conjunctivitis to Tree Pollen or Grass Pollen1
4CompletedTreatmentAllergic Rhinitis (AR)2
4CompletedTreatmentAsthma3

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage Forms
FormRouteStrength
Spray, suspensionIntrasinal27.5 micrograms/spray
PowderRespiratory (inhalation)100 ug/1
PowderRespiratory (inhalation)100 mcg
PowderRespiratory (inhalation)200 mcg
PowderRespiratory (inhalation)200 ug/1
PowderRespiratory (inhalation)50 ug/1
Spray, meteredNasal
Spray, suspensionNasal27.5 mcg/1dose
Spray; suspensionNasal27.5 mcg
SprayNasal27.5 µg
PowderRespiratory (inhalation)
PowderRespiratory (inhalation)92 MCG
SuspensionNasal; Respiratory (inhalation)0.055 g
Aerosol, powderRespiratory (inhalation)100 mcg/1dose
Aerosol, powderRespiratory (inhalation)200 mcg/1dose
PowderRespiratory (inhalation)184 MICROGRAMMI/22MICROGRAMMI
PowderRespiratory (inhalation)92 MICROGRAMMI/22MICROGRAMMI
Aerosol, powderRespiratory (inhalation)100 mcg
PowderRespiratory (inhalation)184 µg
Aerosol, powderRespiratory (inhalation)200 mcg
PowderRespiratory (inhalation)92 µg
PowderRespiratory (inhalation)184 mcg
PowderOral; Respiratory (inhalation)100 cg
PowderRespiratory (inhalation)184 MICROGRAMMI
PowderRespiratory (inhalation)92 MICROGRAMMI
Spray, meteredNasal27.5 ug/1
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)Region
US5873360Yes1999-02-232016-08-23US flag
US6858596No2005-02-222021-08-03US flag
US7101866No2006-09-052021-08-03US flag
US7541350No2009-06-022021-08-03US flag
US8347879No2013-01-082028-07-15US flag
US8752543No2014-06-172026-04-05US flag
US8062264No2011-11-222026-04-05US flag
US8147461No2012-04-032028-10-15US flag
US7439393No2008-10-212022-09-11US flag
US6759398No2004-07-062021-08-03US flag
USRE44874No2014-04-292023-03-23US flag
US6537983No2003-03-252021-08-03US flag
US8511304No2013-08-202027-06-14US flag
US7629335No2009-12-082021-08-03US flag
US8161968No2012-04-242028-02-05US flag
US8746242No2014-06-102030-10-11US flag
US8113199No2012-02-142027-10-23US flag
US7776895No2010-08-172022-09-11US flag
US8534281No2013-09-172029-08-10US flag
US6878698No2005-04-122021-08-03US flag
US8309572No2012-11-132025-04-27US flag
US8183257No2012-05-222025-07-27US flag
US7488827No2009-02-102025-04-27US flag
US7498440No2009-03-032025-04-27US flag
US8201556No2012-06-192029-02-05US flag
US9320862No2016-04-262024-11-06US flag
US9333310No2016-05-102027-10-02US flag
US9750726No2017-09-052030-11-29US flag
US9750762No2017-09-052030-11-29US flag
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)250-252[MSDS]
water solubilityInsoluble [MSDS]
Predicted Properties
PropertyValueSource
Water Solubility0.0434 mg/mLALOGPS
logP3.73ALOGPS
logP4.13ChemAxon
logS-4.1ALOGPS
pKa (Strongest Acidic)13.56ChemAxon
pKa (Strongest Basic)-3.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area93.81 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity130.08 m3·mol-1ChemAxon
Polarizability51.55 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET Features
PropertyValueProbability
Human Intestinal Absorption+0.9917
Blood Brain Barrier+0.9666
Caco-2 permeable-0.5222
P-glycoprotein substrateSubstrate0.7675
P-glycoprotein inhibitor IInhibitor0.784
P-glycoprotein inhibitor IIInhibitor0.604
Renal organic cation transporterNon-inhibitor0.8329
CYP450 2C9 substrateNon-substrate0.8023
CYP450 2D6 substrateNon-substrate0.8893
CYP450 3A4 substrateSubstrate0.7205
CYP450 1A2 substrateNon-inhibitor0.6493
CYP450 2C9 inhibitorNon-inhibitor0.7288
CYP450 2D6 inhibitorNon-inhibitor0.8305
CYP450 2C19 inhibitorNon-inhibitor0.6388
CYP450 3A4 inhibitorInhibitor0.9211
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.69
Ames testNon AMES toxic0.747
CarcinogenicityNon-carcinogens0.9079
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.6232 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9787
hERG inhibition (predictor II)Non-inhibitor0.566
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 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

Targets

Details
1. 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. Fluticasone Furoate (Veramyst) Nasal Spray FDA Label [File]
  2. Fluticasone Furoate (Arnuity Ellipta) FDA Label [File]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Agonist
General Function
Zinc ion binding
Specific Function
The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor ...
Gene Name
PGR
Uniprot ID
P06401
Uniprot Name
Progesterone receptor
Molecular Weight
98979.96 Da
References
  1. Issar M, Sahasranaman S, Buchwald P, Hochhaus G: Differences in the glucocorticoid to progesterone receptor selectivity of inhaled glucocorticoids. Eur Respir J. 2006 Mar;27(3):511-6. [PubMed:16507850]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Antagonist
General Function
Zinc ion binding
Specific Function
Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates targ...
Gene Name
NR3C2
Uniprot ID
P08235
Uniprot Name
Mineralocorticoid receptor
Molecular Weight
107066.575 Da
References
  1. Issar M, Sahasranaman S, Buchwald P, Hochhaus G: Differences in the glucocorticoid to progesterone receptor selectivity of inhaled glucocorticoids. Eur Respir J. 2006 Mar;27(3):511-6. [PubMed:16507850]

Enzymes

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
Curator comments
Induction likely occurs indirectly via transcriptional modulation via the glucocorticoid receptor.
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. Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [PubMed:20482443]
  2. FDA reports [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
Inducer
Curator comments
Induction likely occurs indirectly via transcriptional modulation via the glucocorticoid receptor.
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. Pearce RE, Leeder JS, Kearns GL: Biotransformation of fluticasone: in vitro characterization. Drug Metab Dispos. 2006 Jun;34(6):1035-40. Epub 2006 Mar 24. [PubMed:16565171]
  2. Dvorak Z, Pavek P: Regulation of drug-metabolizing cytochrome P450 enzymes by glucocorticoids. Drug Metab Rev. 2010 Nov;42(4):621-35. doi: 10.3109/03602532.2010.484462. [PubMed:20482443]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
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
CYP3A7
Uniprot ID
P24462
Uniprot Name
Cytochrome P450 3A7
Molecular Weight
57525.03 Da
References
  1. Pearce RE, Leeder JS, Kearns GL: Biotransformation of fluticasone: in vitro characterization. Drug Metab Dispos. 2006 Jun;34(6):1035-40. Epub 2006 Mar 24. [PubMed:16565171]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
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. Backman JT, Filppula AM, Niemi M, Neuvonen PJ: Role of Cytochrome P450 2C8 in Drug Metabolism and Interactions. Pharmacol Rev. 2016 Jan;68(1):168-241. doi: 10.1124/pr.115.011411. [PubMed:26721703]
  2. FDA reports [Link]

Carriers

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
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
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. FDA reports [Link]
Kind
Protein
Organism
Humans
Pharmacological action
Unknown
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. FDA reports [Link]

Transporters

Kind
Protein
Organism
Humans
Pharmacological action
Unknown
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Hughes SC, Shardlow PC, Hollis FJ, Scott RJ, Motivaras DS, Allen A, Rousell VM: Metabolism and disposition of fluticasone furoate, an enhanced-affinity glucocorticoid, in humans. Drug Metab Dispos. 2008 Nov;36(11):2337-44. doi: 10.1124/dmd.108.022137. Epub 2008 Aug 11. [PubMed:18694910]
Kind
Protein
Organism
Humans
Pharmacological action
No
Actions
Inhibitor
General Function
Sodium-independent organic anion transmembrane transporter activity
Specific Function
Mediates the Na(+)-independent uptake of organic anions such as pravastatin, taurocholate, methotrexate, dehydroepiandrosterone sulfate, 17-beta-glucuronosyl estradiol, estrone sulfate, prostagland...
Gene Name
SLCO1B1
Uniprot ID
Q9Y6L6
Uniprot Name
Solute carrier organic anion transporter family member 1B1
Molecular Weight
76447.99 Da
References
  1. FDA reports [Link]

Drug created on June 16, 2013 17:03 / Updated on October 21, 2020 01:55

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