Identification

Name
Fluticasone propionate
Accession Number
DB00588  (APRD00065)
Type
Small Molecule
Groups
Approved
Description

Fluticasone propionate, a medium-potency synthetic corticosteroid, is used topically to relieve inflammatory and pruritic symptoms of dermatoses and psoriasis, intranasally to manage symptoms of allergic and non-allergic rhinitis, and orally for the treatment of asthma. Fluticasone proprionate is marketed under several different brand names such as Flonase®. Fluticasone propionate is also available as a combination product of azelastine hydrochloride and fluticasone propionate called Dymista™. Dymista™ is indicated in patients over 12 years old for symptomatic relief of seasonal allergic rhinitis.

Structure
Thumb
Synonyms
Not Available
External IDs
CCI 18781 / CCI-18781 / PF-00241939
Active Moieties
NameKindUNIICASInChI Key
FluticasoneprodrugCUT2W21N7U90566-53-3MGNNYOODZCAHBA-GQKYHHCASA-N
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Aermony RespiclickPowder, metered113 mcgRespiratory (inhalation)TevaNot applicableNot applicableCanada
Aermony RespiclickPowder, metered55 mcgRespiratory (inhalation)TevaNot applicableNot applicableCanada
Aermony RespiclickPowder, metered232 mcgRespiratory (inhalation)TevaNot applicableNot applicableCanada
ArmonAir RespiClickPowder, metered232 ug/1Respiratory (inhalation)Teva Respiratory, LLC2017-08-07Not applicableUs
ArmonAir RespiClickPowder, metered55 ug/1Respiratory (inhalation)Teva Respiratory, LLC2017-08-07Not applicableUs
ArmonAir RespiClickPowder, metered113 ug/1Respiratory (inhalation)Teva Respiratory, LLC2017-08-07Not applicableUs
CutivateCream0.5 mg/1gTopicalPharma Derm, A Division Of Fougera Pharmaceuticals Inc.1990-12-182013-05-31Us
CutivateLotion0.5 mg/1mLTopicalPharma Derm, A Division Of Fougera Pharmaceuticals Inc.2009-10-05Not applicableUs
CutivateOintment0.05 mg/1gTopicalPhysicians Total Care, Inc.1990-12-142011-05-31Us
CutivateLotion0.5 mg/1mLTopicalPharma Derm, A Division Of Nycomed Us Inc.2009-10-05Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Apo-fluticasoneSpray, metered50 mcgNasalApotex Corporation2007-07-05Not applicableCanada
FluticasoneSpray, metered50 ug/1NasalLake Erie Medical DBA Quality Care Products LLC2018-09-07Not applicableUs
FluticasoneSpray, metered50 ug/1NasalDirectrx2014-01-01Not applicableUs
FluticasoneCream0.5 mg/1gTopicalSandoz2004-05-142011-05-12Us
FluticasoneSpray, metered50 ug/1NasalUnit Dose Services2012-01-09Not applicableUs
FluticasoneSpray, metered50 ug/1NasalMorton Grove Pharmaceuticals, Inc.2012-01-09Not applicableUs
FluticasoneSpray, metered50 ug/1NasalMesource Pharmaceuticals2012-01-09Not applicableUs
FluticasoneSpray, metered50 ug/1NasalUnit Dose Services2012-01-09Not applicableUs
FluticasoneSpray, metered50 ug/1NasalNucare Pharmaceuticals,inc.2012-01-09Not applicableUs
Fluticasone PropionateLotion0.5 mg/1mLTopicalGlenmark Pharmaceuticals Inc.,Usa2011-10-13Not applicableUs
Over the Counter Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
24 Hour Allergy NasalSpray, metered50 ug/1NasalWalgreen2016-05-27Not applicableUs
24 Hour Allergy NasalSpray, metered50 ug/1NasalHyvee2016-08-08Not applicableUs
24 Hour Allergy NasalSpray, metered50 ug/1NasalShopko Stores Operating2016-08-23Not applicableUs
24 Hour Allergy Relief NasalSpray, metered50 ug/1NasalMeijer Distribution2016-11-17Not applicableUs
24 Hour Allergy Relief nasalSpray, metered50 ug/1NasalKroger2016-05-27Not applicableUs
24hr Nasal Allergy ReliefSpray, metered50 mcgNasalApotex CorporationNot applicableNot applicableCanada
Allergy NasalSpray, metered50 ug/1NasalWalgreen2016-07-12Not applicableUs
Allergy ReliefSpray, metered50 ug/1NasalTopco Associates2018-04-18Not applicableUs
Allergy ReliefSpray, metered50 ug/1NasalMeijer Distribution2016-05-27Not applicableUs
Allergy ReliefSpray, metered50 ug/1NasalDiscount Drug Mart2017-07-03Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
Advair 100 DiskusFluticasone propionate (100 mcg) + Salmeterol (50 mcg)PowderRespiratory (inhalation)Glaxosmithkline Inc1999-09-24Not applicableCanada
Advair 125Fluticasone propionate (125 mcg) + Salmeterol (25 mcg)Aerosol, meteredRespiratory (inhalation)Glaxosmithkline Inc2001-12-21Not applicableCanada
Advair 250Fluticasone propionate (250 mcg) + Salmeterol (25 mcg)Aerosol, meteredRespiratory (inhalation)Glaxosmithkline Inc2001-12-21Not applicableCanada
Advair 250 DiskusFluticasone propionate (250 mcg) + Salmeterol (50 mcg)PowderRespiratory (inhalation)Glaxosmithkline Inc1999-09-24Not applicableCanada
Advair 500 DiskusFluticasone propionate (500 mcg) + Salmeterol (50 mcg)PowderRespiratory (inhalation)Glaxosmithkline Inc1999-09-24Not applicableCanada
Advair DiskusFluticasone propionate (250 ug/1) + Salmeterol xinafoate (50 ug/1)PowderOral; Respiratory (inhalation)Dispensing Solutions, Inc.2001-02-05Not applicableUs
Advair DiskusFluticasone propionate (250 ug/1) + Salmeterol xinafoate (50 ug/1)PowderRespiratory (inhalation)Remedy Repack2017-05-15Not applicableUs
Advair DiskusFluticasone propionate (100 ug/1) + Salmeterol xinafoate (50 ug/1)PowderOral; Respiratory (inhalation)Physicians Total Care, Inc.2001-06-21Not applicableUs
Advair DiskusFluticasone propionate (250 ug/1) + Salmeterol xinafoate (50 ug/1)PowderRespiratory (inhalation)Glaxo Wellcome Production2017-12-07Not applicableUs
Advair DiskusFluticasone propionate (250 ug/1) + Salmeterol xinafoate (50 ug/1)PowderOral; Respiratory (inhalation)Rebel Distributors2001-02-05Not applicableUs
Unapproved/Other Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
CenoviaFluticasone propionate (0.025 g/0.025g) + Hydroquinone (2 g/2g) + Tretinoin (0.025 g/0.025g)KitAccumix Pharmaceuticals2014-12-152015-07-17Us
FloventFluticasone propionate (44 ug/1)Aerosol, meteredRespiratory (inhalation)GlaxoSmithKline2006-05-16Not applicableUs
FloventFluticasone propionate (50 ug/1)PowderRespiratory (inhalation)GlaxoSmithKline2006-01-12Not applicableUs
FloventFluticasone propionate (220 ug/1)Aerosol, meteredRespiratory (inhalation)GlaxoSmithKline2006-05-16Not applicableUs
FloventFluticasone propionate (110 ug/1)Aerosol, meteredRespiratory (inhalation)GlaxoSmithKline2006-05-16Not applicableUs
FloventFluticasone propionate (250 ug/1)PowderRespiratory (inhalation)GlaxoSmithKline2006-01-12Not applicableUs
FloventFluticasone propionate (220 ug/1)Aerosol, meteredRespiratory (inhalation)GlaxoSmithKline2006-05-16Not applicableUs
FloventFluticasone propionate (44 ug/1)Aerosol, meteredRespiratory (inhalation)GlaxoSmithKline2006-05-16Not applicableUs
FloventFluticasone propionate (100 ug/1)PowderRespiratory (inhalation)GlaxoSmithKline2006-01-12Not applicableUs
FloventFluticasone propionate (110 ug/1)Aerosol, meteredRespiratory (inhalation)GlaxoSmithKline2006-05-16Not applicableUs
International/Other Brands
Ezicas (Intas) / Flixonase (GlaxoSmithKline) / Flixotide (GlaxoSmithKline) / Flovent (GlaxoSmithKline) / FLOVENTHFA / Flunase (GlaxoSmithKline) / Nasofan (Teva) / Pirinase (GlaxoSmithKline) / Seretide (GlaxoSmithKline)
Categories
UNII
O2GMZ0LF5W
CAS number
80474-14-2
Weight
Average: 500.571
Monoisotopic: 500.184429407
Chemical Formula
C25H31F3O5S
InChI Key
WMWTYOKRWGGJOA-CENSZEJFSA-N
InChI
InChI=1S/C25H31F3O5S/c1-5-20(31)33-25(21(32)34-12-26)13(2)8-15-16-10-18(27)17-9-14(29)6-7-22(17,3)24(16,28)19(30)11-23(15,25)4/h6-7,9,13,15-16,18-19,30H,5,8,10-12H2,1-4H3/t13-,15+,16+,18+,19+,22+,23+,24+,25+/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 propanoate
SMILES
[H][C@@]12C[C@@H](C)[C@](OC(=O)CC)(C(=O)SCF)[C@@]1(C)C[C@H](O)[C@@]1(F)[C@@]2([H])C[C@H](F)C2=CC(=O)C=C[C@]12C

Pharmacology

Indication

Fluticasone propionate, a medium-potency synthetic corticosteroid, is used topically to relieve inflammatory and pruritic symptoms of dermatoses and psoriasis, intranasally to manage symptoms of allergic and non-allergic rhinitis, and orally for the maintenance treatment of asthma as prophylactic therapy and for patients requiring oral corticosteroid therapy for asthma.

Associated Conditions
Pharmacodynamics

Fluticasone is an extremely potent vasoconstrictor and anti-inflammatory agent. Its effectiveness in inhaled forms is due to its direct local effect.

Mechanism of action

Binds to the glucocorticoid receptor. Unbound corticosteroids cross the membranes of cells such as mast cells and eosinophils, binding with high affinity to glucocorticoid receptors (GR). The results include alteration of transcription and protein synthesis, a decreased release of leukocytic acid hydrolases, reduction in fibroblast proliferation, prevention of macrophage accumulation at inflamed sites, reduction of collagen deposition, interference with leukocyte adhesion to the capillary wall, reduction of capillary membrane permeability and subsequent edema, reduction of complement components, inhibition of histamine and kinin release, and interference with the formation of scar tissue. In the management of asthma, the glucocorticoid receptor complexes down-regulates proinflammatory mediators such as interleukin-(IL)-1, 3, and 5, and up-regulates anti-inflammatory mediators such as IkappaB [inhibitory molecule for nuclear factor kappaB1], IL-10, and IL-12. The antiinflammatory actions of corticosteroids are also thought to involve inhibition of cytosolic phospholipase A2 (through activation of lipocortin-1 (annexin)) which controls the biosynthesis of potent mediators of inflammation such as prostaglandins and leukotrienes.

TargetActionsOrganism
AGlucocorticoid receptor
agonist
Human
UProgesterone receptor
agonist
Human
UCytosolic phospholipase A2
inhibitor
Human
UMineralocorticoid receptor
antagonist
Human
Absorption

The extent of percutaneous absorption of topical corticosteroids is determined by many factors, including the vehicle and the integrity of the epidermal barrier. Bioavailability, intranasal = <2%; Oral bioavailability is negligible and the major circulating entity is an inactive metabolite.

Volume of distribution

IV administration = 4.2 L/kg

Protein binding

91%

Metabolism

Fluticasone propionate is metabolized in the liver by cytochrome P450 3A4-mediated hydrolysis of the 5-fluoromethyl carbothioate grouping. This transformation occurs in 1 metabolic step to produce the inactive 17-(beta)-carboxylic acid metabolite, the only known metabolite detected in man.

Route of elimination

Less than 5% of the oral dose was excreted in the urine as metabolites. The rest of the dose is excreted in the feces and parent drug and metabolites.

Half life

Terminal elimination half-life = 7.8 hours

Clearance

The total blood clearance of fluticasone propionate is high (average, 1,093 mL/min), with renal clearance accounting for less than 0.02% of the total.

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

Interactions

Drug Interactions
DrugInteraction
1-TestosteroneThe risk or severity of edema formation can be increased when 1-Testosterone is combined with Fluticasone propionate.
1,10-PhenanthrolineThe therapeutic efficacy of 1,10-Phenanthroline can be decreased when used in combination with Fluticasone propionate.
16-BromoepiandrosteroneThe risk or severity of edema formation can be increased when 16-Bromoepiandrosterone is combined with Fluticasone propionate.
19-norandrostenedioneThe risk or severity of edema formation can be increased when 19-norandrostenedione is combined with Fluticasone propionate.
1alpha-Hydroxyvitamin D5The therapeutic efficacy of 1alpha-Hydroxyvitamin D5 can be decreased when used in combination with Fluticasone propionate.
2-MethoxyethanolThe risk or severity of adverse effects can be increased when 2-Methoxyethanol is combined with Fluticasone propionate.
2,5-Dimethoxy-4-ethylthioamphetamineThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,4-MethylenedioxyamphetamineThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with 3,4-Methylenedioxyamphetamine.
4-Bromo-2,5-dimethoxyamphetamineThe risk or severity of adverse effects can be increased when Fluticasone propionate is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-HydroxytestosteroneThe risk or severity of edema formation can be increased when 4-Hydroxytestosterone is combined with Fluticasone propionate.
Food Interactions
Not Available

References

Synthesis Reference

Joseph Kaspi, Oded Arad, Michael Brand, Moty Shookrun, Simona Malka, Mohammed Alnabari, Shalom Hazan, Vlado Malesevic, "Synthesis and powder preparation of fluticasone propionate." U.S. Patent US20060009435, issued January 12, 2006.

US20060009435
General References
Not Available
External Links
Human Metabolome Database
HMDB0005036
KEGG Drug
D01708
PubChem Compound
444036
PubChem Substance
46506140
ChemSpider
392059
BindingDB
50354849
ChEBI
31441
ChEMBL
CHEMBL1473
Therapeutic Targets Database
DAP001039
PharmGKB
PA449686
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Fluticasone_propionate
AHFS Codes
  • 68:04.00 — Adrenals
  • 84:06.00 — Anti-inflammatory Agents
  • 52:08.00 — Anti-inflammatory Agents
  • 52:08.08 — Corticosteroids
FDA label
Download (159 KB)
MSDS
Download (39 KB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
0CompletedPreventionHypersensitivity / T1DM1
1CompletedNot AvailableAsthma Bronchial1
1CompletedNot AvailablePulmonary Disease, Chronic Obstructive1
1CompletedBasic ScienceChronic Obstructive Pulmonary Disease (COPD) / Smoke-related Lung Diseases1
1CompletedDiagnosticAirway Inflammation1
1CompletedDiagnosticAllergic Rhinitis (AR)1
1CompletedScreeningPulmonary Disease, Chronic Obstructive1
1CompletedTreatmentAllergic Rhinitis (AR)4
1CompletedTreatmentAllergic Rhinitis (AR) / Rhinitis, Allergic, Perennial1
1CompletedTreatmentAsthma Bronchial4
1CompletedTreatmentAsthma Bronchial / Chronic Obstructive Pulmonary Disease (COPD)3
1CompletedTreatmentDiabetes Mellitus (DM) / Healthy Volunteers1
1CompletedTreatmentHealthy Volunteers3
1CompletedTreatmentMild to Moderate Asthma1
1CompletedTreatmentPulmonary Disease, Chronic Obstructive1
1RecruitingTreatmentAsthma, Allergic1
1RecruitingTreatmentVocal Fold Nodules1
2CompletedOtherAsthma Bronchial1
2CompletedPreventionAllergic Rhinitis (AR)1
2CompletedPreventionCarcinoma, Bronchogenic1
2CompletedTreatmentAllergic Rhinitis (AR) / Rhinitis, Allergic, Seasonal2
2CompletedTreatmentAsthma Bronchial16
2CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)3
2CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD) / Pulmonary Disease, Chronic Obstructive1
2CompletedTreatmentEsophagitis1
2CompletedTreatmentObliterative Bronchiolitis1
2CompletedTreatmentOesophagitis, Eosinophilic2
2CompletedTreatmentPulmonary Disease, Chronic Obstructive1
2CompletedTreatmentSeasonal Allergic Rhinitis (SAR)1
2Enrolling by InvitationTreatmentPolyps, Nasal1
2RecruitingDiagnosticChronic Obstructive Pulmonary Disease (COPD)1
2RecruitingPreventionCholera1
2RecruitingTreatmentAllergic Rhinitis (AR)1
2RecruitingTreatmentAsthma Bronchial2
2TerminatedPreventionBronchiectasis / Chronic Bronchitis / Pulmonary Diseases1
2TerminatedTreatmentAsthma Bronchial3
2TerminatedTreatmentBronchiolitis1
2TerminatedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
2TerminatedTreatmentPolyp of Nasal Sinus1
2WithdrawnNot AvailableChronic Obstructive Pulmonary Disease (COPD)1
2WithdrawnTreatmentAsthma Bronchial1
2, 3Not Yet RecruitingTreatmentOesophagitis, Eosinophilic1
2, 3RecruitingTreatmentEosinophilic Esophagitis (EoE) / Eosinophilic Gastrointestinal Disorders (EGIDs)1
3Active Not RecruitingTreatmentAsthma Bronchial1
3Active Not RecruitingTreatmentOesophagitis, Eosinophilic / Swallowing Disorders1
3CompletedNot AvailableAllergic Rhinitis (AR) / Seasonal Allergic Rhinitis (SAR)1
3CompletedNot AvailableSeasonal Allergic Rhinitis (SAR)1
3CompletedPreventionStridor1
3CompletedTreatmentAllergic Rhinitis (AR)1
3CompletedTreatmentAllergic Rhinitis (AR) / Rhinitis, Allergic, Perennial1
3CompletedTreatmentAllergies / Conjunctivitis / Rhinitis / Rhinoconjunctivitis2
3CompletedTreatmentAsthma Bronchial26
3CompletedTreatmentBronchial Asthma1
3CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)5
3CompletedTreatmentChronic Sinusitis With or Without Nasal Polyps1
3CompletedTreatmentChronic Sinusitis With or Without Nasal Polyps / Chronic Sinusitis: [Nos] or [Ethmoidal] or [Chronic Pansinusitis] or [Sphenoidal] / Polyps, Nasal1
3CompletedTreatmentExercised Induced Asthma1
3CompletedTreatmentOesophagitis, Eosinophilic1
3CompletedTreatmentPerennial Allergic Rhinitis (PAR)1
3CompletedTreatmentPulmonary Disease, Chronic Obstructive1
3CompletedTreatmentSeasonal Allergic Rhinitis (SAR)6
3Not Yet RecruitingTreatmentAllergies1
3Not Yet RecruitingTreatmentAsthma Bronchial1
3Not Yet RecruitingTreatmentChronic Rhinosinustis With Polyps1
3RecruitingTreatmentAllergic Rhinitis (AR)1
3RecruitingTreatmentAsthma Bronchial4
3RecruitingTreatmentAsthma, Allergic1
3RecruitingTreatmentObstructive Sleep Apnea Syndrome (OSAS)1
3TerminatedPreventionAtopic Dermatitis (AD)1
3TerminatedTreatmentCroup1
3Unknown StatusNot AvailableSeasonal Allergic Rhinitis (SAR)1
3Unknown StatusTreatmentPulmonary Disease, Chronic Obstructive2
3WithdrawnTreatmentAsthma Bronchial1
3WithdrawnTreatmentBronchial Asthma1
3WithdrawnTreatmentChronic Obstructive Pulmonary Disease (COPD)3
4Active Not RecruitingBasic ScienceHealthy Volunteers1
4Active Not RecruitingTreatmentOesophagitis, Eosinophilic1
4CompletedNot AvailableAsthma Bronchial1
4CompletedNot AvailableOcular Hypertension / Open-angle Glaucoma (OAG)1
4CompletedBasic ScienceAsthma Bronchial1
4CompletedBasic ScienceAsthma Bronchial / Healthy Volunteers1
4CompletedBasic ScienceMild Asthma1
4CompletedDiagnosticAsthma Bronchial1
4CompletedDiagnosticAsthma, Allergic1
4CompletedDiagnosticAsthmatic Smokers / Non-asthmatic Smokers1
4CompletedOtherAsthma Bronchial1
4CompletedPreventionAllergic Rhinitis (AR) / Conjunctivitis, Seasonal Allergic1
4CompletedTreatmentAllergic Rhinitis (AR)3
4CompletedTreatmentAllergic Rhinitis (AR) / Asthma Bronchial1
4CompletedTreatmentAllergic Rhinitis (AR) / Rhinitis, Allergic, Perennial1
4CompletedTreatmentAsthma Bronchial27
4CompletedTreatmentAsthma Bronchial / Mild Asthma1
4CompletedTreatmentAsthmatic Patients1
4CompletedTreatmentAtopic Dermatitis (AD)4
4CompletedTreatmentBronchial Asthma1
4CompletedTreatmentBronchiectasis1
4CompletedTreatmentChronic Bronchitis / Lung Diseases, Obstructive / Pulmonary Disease, Chronic Obstructive1
4CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)6
4CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD) / Depression1
4CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD) / Pulmonary Disease, Chronic Obstructive1
4CompletedTreatmentConjunctivitis, Seasonal Allergic1
4CompletedTreatmentOesophagitis, Eosinophilic1
4CompletedTreatmentPersistent Asthma1
4CompletedTreatmentPsoriasis1
4CompletedTreatmentPulmonary Disease, Chronic Obstructive4
4CompletedTreatmentRhinitis, Allergic, Perennial / Seasonal Allergic Rhinitis (SAR)2
4CompletedTreatmentSeasonal Allergic Rhinitis (SAR)1
4CompletedTreatmentSkin Diseases1
4Enrolling by InvitationTreatmentAsthma Bronchial1
4Not Yet RecruitingTreatmentOtitis Media With Effusion1
4RecruitingBasic ScienceAllergic Rhinitis (AR)1
4RecruitingTreatmentAcute Exacerbation of Chronic Obstructive Pulmonary Disease / Chronic Obstructive Pulmonary Disease (COPD)1
4RecruitingTreatmentAllergic Rhinitis (AR) / Allergies / Asthma, Allergic1
4RecruitingTreatmentAllergic Rhinitis (AR) / House Dust Mite Allergy1
4RecruitingTreatmentAsthma Bronchial1
4RecruitingTreatmentAsthmatic Bronchitis / Obstruction Airway / Wheezing / Wheezy Bronchitis1
4RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4RecruitingTreatmentPulmonary Disease, Chronic Obstructive1
4TerminatedTreatmentAsthma Bronchial3
4TerminatedTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4TerminatedTreatmentPain, Acute / Posttraumatic Stress Disorders / Wound Care1
4TerminatedTreatmentRhinitis, Allergic, Perennial1
4Unknown StatusTreatmentAsthma Bronchial1
4Unknown StatusTreatmentBenign Prostatic Hyperplasia (BPH) / Urinary Bladder, Overactive1
4Unknown StatusTreatmentChronic Obstructive Pulmonary Disease (COPD)1
4Unknown StatusTreatmentCream Compared to NB-UVB Alone in Patients With Non-segmental Vitiligo / Evaluation of the Efficacy of UVB and Fluticason Proprionate 0.05% / Patients With Active Non-segmental Vitiligo1
4Unknown StatusTreatmentPercentage of Annual Acute Exacerbation / Quality of Life1
4WithdrawnTreatmentAllergic Rhinitis (AR)1
4WithdrawnTreatmentAsthma Bronchial1
Not AvailableCompletedNot AvailableAsthma Bronchial8
Not AvailableCompletedNot AvailableAsthma Bronchial / Atopics1
Not AvailableCompletedNot AvailableChronic Obstructive Pulmonary Disease (COPD)1
Not AvailableCompletedNot AvailablePulmonary Disease, Chronic Obstructive2
Not AvailableCompletedNot AvailableRespiratory Disorders2
Not AvailableCompletedNot AvailableRhinitis2
Not AvailableCompletedNot AvailableRhinitis, Allergic, Perennial / Rhinitis, Allergic, Seasonal1
Not AvailableCompletedNot AvailableSmokers / Smoking1
Not AvailableCompletedNot AvailableTobacco Abuse Smoke1
Not AvailableCompletedBasic ScienceAsthma, Allergic1
Not AvailableCompletedBasic ScienceHealthy Volunteers1
Not AvailableCompletedBasic ScienceSeasonal Allergic Rhinitis (SAR)1
Not AvailableCompletedDiagnosticAsthma Bronchial1
Not AvailableCompletedPreventionCystic Fibrosis (CF)1
Not AvailableCompletedTreatmentAllergies1
Not AvailableCompletedTreatmentAsthma Bronchial2
Not AvailableCompletedTreatmentAsthma, Allergic / Mild, Allergic Asthma1
Not AvailableCompletedTreatmentPolyps, Nasal / Sinusitis1
Not AvailableCompletedTreatmentSuspected Eosinophilic Esophagitis1
Not AvailableNot Yet RecruitingDiagnosticChildhood Asthma1
Not AvailableRecruitingNot AvailableAsthma Bronchial2
Not AvailableRecruitingNot AvailableBronchiolitis Obliterans Syndrome (BOS)1
Not AvailableRecruitingSupportive CareBioavailability Study1
Not AvailableRecruitingTreatmentChronic Lung Diseases / Medication Compliance1
Not AvailableRecruitingTreatmentChronic Rhinosinusitis1
Not AvailableRecruitingTreatmentChronic Rhinosinusitis / Chronic Rhinosinusitis Without Polyps / Endoscopic Sinus Surgery / Oral Steroids1
Not AvailableTerminatedTreatmentAsthma Bronchial2
Not AvailableTerminatedTreatmentAsthma Bronchial / Non-Eosinophilic Asthma1
Not AvailableUnknown StatusNot AvailableOesophagitis, Eosinophilic1
Not AvailableUnknown StatusTreatmentAsthma Bronchial1
Not AvailableUnknown StatusTreatmentChronic Obstructive Pulmonary Disease (COPD)1
Not AvailableWithdrawnNot AvailableChronic Obstructive Pulmonary Disease (COPD) / Sleep disorders and disturbances1
Not AvailableWithdrawnTreatmentAsthma Bronchial1
Not AvailableWithdrawnTreatmentVitiligo1

Pharmacoeconomics

Manufacturers
  • Glaxosmithkline
  • Glaxo group ltd dba glaxosmithkline
  • Altana inc
  • G and w laboratories inc
  • Kv pharmaceutical co
  • Perrigo new york inc
  • Tolmar inc
  • Nycomed us inc
  • Taro pharmaceutical industries ltd
  • Apotex inc richmond hill
  • Hi tech pharmacal co inc
  • Roxane laboratories inc
Packagers
  • Apotex Inc.
  • A-S Medication Solutions LLC
  • Dispensing Solutions
  • Diversified Healthcare Services Inc.
  • E. Fougera and Co.
  • G & W Labs
  • GlaxoSmithKline Inc.
  • Hi Tech Pharmacal Co. Inc.
  • Letco Medical Inc.
  • Nycomed Inc.
  • Palmetto Pharmaceuticals Inc.
  • Penn Labs
  • Perrigo Co.
  • Pharmaderm
  • Physicians Total Care Inc.
  • Professional Co.
  • Promex Medical Inc.
  • Rebel Distributors Corp.
  • Redpharm Drug
  • Roxane Labs
  • Sandoz
  • Stat Scripts LLC
  • Taro Pharmaceuticals USA
  • Tolmar Inc.
Dosage forms
FormRouteStrength
PowderRespiratory (inhalation)
Aerosol, meteredRespiratory (inhalation)
PowderOral; Respiratory (inhalation)
Powder, meteredRespiratory (inhalation)113 mcg
Powder, meteredRespiratory (inhalation)232 mcg
Powder, meteredRespiratory (inhalation)55 mcg
Spray, meteredNasal50 mcg
Powder, meteredRespiratory (inhalation)
Powder, meteredRespiratory (inhalation)113 ug/1
Powder, meteredRespiratory (inhalation)232 ug/1
Powder, meteredRespiratory (inhalation)55 ug/1
CreamTopical0.05 %
LotionTopical0.5 mg/1mL
Spray, meteredNasal
Aerosol, metered; suspensionNasal50 mcg
Aerosol, meteredRespiratory (inhalation)110 ug/1
Aerosol, meteredRespiratory (inhalation)220 ug/1
Aerosol, meteredRespiratory (inhalation)44 ug/1
PowderRespiratory (inhalation)100 ug/1
PowderRespiratory (inhalation)250 ug/1
PowderRespiratory (inhalation)50 ug/1
PowderRespiratory (inhalation)100 mcg
PowderRespiratory (inhalation)250 mcg
PowderRespiratory (inhalation)50 mcg
PowderRespiratory (inhalation)500 mcg
Powder, meteredRespiratory (inhalation)100 ug/1
Powder, meteredRespiratory (inhalation)250 ug/1
Powder, meteredRespiratory (inhalation)50 ug/1
Aerosol, meteredOral; Respiratory (inhalation)125 mcg
Aerosol, meteredOral; Respiratory (inhalation)250 mcg
Aerosol, meteredOral; Respiratory (inhalation)50 mcg
Aerosol, meteredOral; Respiratory (inhalation)25 mcg
CreamTopical0.5 mg/1
CreamTopical0.5 mg/1g
OintmentTopical0.05 mg/1g
Spray, meteredNasal50 ug/0.1g
Spray, meteredNasal50 ug/1
Kit50 ug/1
Kit
Spray, meteredNasal93 ug/1
Prices
Unit descriptionCostUnit
Fluticasone propionate powder1500.0USD g
Cutivate 0.05% Lotion 120ml Bottle454.6USD bottle
Advair Diskus 60 500-50 mcg/dose Aerosol Disp Pack328.14USD disp
Advair Diskus 60 250-50 mcg/dose Aerosol Disp Pack249.48USD disp
Flovent HFA 220 mcg/act Aerosol 12 gm Inhaler237.67USD inhaler
Cutivate 0.05% Cream 60 gm Tube217.11USD tube
Advair Diskus 60 100-50 mcg/dose Aerosol Disp Pack200.79USD disp
Advair Diskus 14 500-50 mcg/dose Aerosol Disp Pack156.64USD disp
Flovent HFA 110 mcg/act Aerosol 12 gm Inhaler153.01USD inhaler
Cutivate 0.005% Ointment 60 gm Tube128.28USD tube
Flovent HFA 44 mcg/act Aerosol 10.6 gm Inhaler114.27USD inhaler
Flovent Diskus 60 50 mcg/blist Aerosol Inhaler104.74USD inhaler
Flonase 50 mcg/act Suspension 16 gm Bottle94.59USD bottle
Fluticasone Propionate 50 mcg/act Suspension 16 gm Bottle78.28USD bottle
Cutivate 0.05% Cream 30 gm Tube62.99USD tube
Fluticasone Propionate 0.005% Ointment 60 gm Tube56.27USD tube
Fluticasone Propionate 0.05% Cream 60 gm Tube56.27USD tube
Cutivate 0.005% Ointment 30 gm Tube44.99USD tube
Fluticasone Propionate 0.005% Ointment 30 gm Tube35.67USD tube
Fluticasone Propionate 0.05% Cream 30 gm Tube35.67USD tube
Cutivate 0.005% Ointment 15 gm Tube32.99USD tube
Cutivate 0.05% Cream 15 gm Tube32.99USD tube
Advair hfa 230-21 mcg inhaler25.04USD g
Fluticasone Propionate 0.005% Ointment 15 gm Tube23.14USD tube
Fluticasone Propionate 0.05% Cream 15 gm Tube23.14USD tube
Advair hfa 115-21 mcg inhaler18.13USD g
Flovent hfa 220 mcg inhaler15.54USD g
Advair hfa 45-21 mcg inhaler14.59USD g
Flovent hfa 110 mcg inhaler12.26USD g
Flovent hfa 44 mcg inhaler10.99USD g
Flonase 0.05% nasal spray5.68USD g
Advair 500-50 diskus5.26USD each
Advair 250-50 diskus4.0USD each
Cutivate 0.05% cream3.48USD g
Advair 100-50 diskus3.22USD each
Flovent 250 mcg diskus2.45USD each
Flovent 100 mcg diskus1.83USD each
Flovent 50 mcg diskus1.74USD each
Flovent Diskus 500 mcg/dose Metered Inhalation Powder1.55USD dose
Flovent Diskus 250 mcg/dose Metered Inhalation Powder0.77USD dose
Flovent Hfa 250 mcg/dose Metered Dose Aerosol0.77USD dose
Flovent Hfa 125 mcg/dose Metered Dose Aerosol0.39USD dose
Flovent Hfa 50 mcg/dose Metered Dose Aerosol0.22USD dose
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
USRE40045No1993-09-072010-09-07Us
CA2317999No2004-11-092020-09-11Canada
CA2125667No2000-03-132012-12-04Canada
US5873360Yes1996-08-232016-08-23Us
US6446627No1997-12-182017-12-18Us
US6743413Yes2001-12-012021-12-01Us
US6938796Yes1998-07-162018-07-16Us
US6997349Yes1998-07-162018-07-16Us
US6431168Yes1998-12-082018-12-08Us
US7107986Yes1998-12-062018-12-06Us
US7500444Yes2006-08-262026-08-26Us
US6315173Yes1998-06-232018-06-23Us
US7143908Yes1998-07-162018-07-16Us
US6170717Yes1998-06-232018-06-23Us
US7350676Yes1999-02-242019-02-24Us
US7832351Yes2003-12-192023-12-19Us
US6161724Yes1998-07-162018-07-16Us
US6510969Yes1998-06-232018-06-23Us
US6966467Yes1998-06-232018-06-23Us
US6435372Yes1998-07-162018-07-16Us
US7300669No1999-10-202019-10-20Us
US8163723Yes2004-02-292024-02-29Us
US9259428Yes2003-12-132023-12-13Us
US8168620Yes2006-08-242026-08-24Us
US6871646No2001-06-232021-06-23Us
US8978966No2012-01-132032-01-13Us
US6701917No2001-06-232021-06-23Us
US7540282No2003-05-062023-05-06Us
US6748947No2001-06-232021-06-23Us
US8006690No2001-06-232021-06-23Us
US6718972No2001-06-232021-06-23Us
US9216260No2011-06-282031-06-28Us
US8651103No2008-03-262028-03-26Us
US8327844No2003-10-032023-10-03Us
US7975690No2005-08-182025-08-18Us
US6715485No2000-03-032020-03-03Us
US8550073No2009-10-222029-10-22Us
US8978647No2010-12-062030-12-06Us
US9463288No2005-05-192025-05-19Us
US8714149No2012-02-252032-02-25Us
US9616024No2004-09-012024-09-01Us
US9066957No2014-10-062034-10-06Us
US9415008No2014-10-062034-10-06Us
US9731087No2011-05-182031-05-18Us
US9072857No2001-04-102021-04-10Us
US9468727No2000-07-302020-07-30Us
US8522778No2002-05-112022-05-11Us
US8555878No2000-03-202020-03-20Us
US9901585No2003-06-132023-06-13Us
US9861771No2000-10-112020-10-11Us
US9987229No2004-09-012024-09-01Us
US10022510No2011-05-182031-05-18Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
melting point (°C)272-273 °CNot Available
water solubility0.51 mg/L (insoluble)Not Available
logP3.4Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0114 mg/mLALOGPS
logP3.69ALOGPS
logP3.72ChemAxon
logS-4.6ALOGPS
pKa (Strongest Acidic)13.56ChemAxon
pKa (Strongest Basic)-3.4ChemAxon
Physiological Charge0ChemAxon
Hydrogen Acceptor Count4ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area80.67 Å2ChemAxon
Rotatable Bond Count6ChemAxon
Refractivity121.65 m3·mol-1ChemAxon
Polarizability49.26 Å3ChemAxon
Number of Rings4ChemAxon
Bioavailability1ChemAxon
Rule of FiveNoChemAxon
Ghose FilterNoChemAxon
Veber's RuleNoChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.9964
Blood Brain Barrier+0.9701
Caco-2 permeable+0.5417
P-glycoprotein substrateSubstrate0.7099
P-glycoprotein inhibitor IInhibitor0.7192
P-glycoprotein inhibitor IINon-inhibitor0.8636
Renal organic cation transporterNon-inhibitor0.8689
CYP450 2C9 substrateNon-substrate0.868
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.7407
CYP450 1A2 substrateNon-inhibitor0.9045
CYP450 2C9 inhibitorNon-inhibitor0.9071
CYP450 2D6 inhibitorNon-inhibitor0.9231
CYP450 2C19 inhibitorNon-inhibitor0.9026
CYP450 3A4 inhibitorInhibitor0.8988
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8682
Ames testNon AMES toxic0.798
CarcinogenicityNon-carcinogens0.8901
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.3753 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.99
hERG inhibition (predictor II)Non-inhibitor0.6125
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
MS/MS Spectrum - , positiveLC-MS/MSsplash10-03dl-0497100000-b64248896abdef386eaf

Taxonomy

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 / Thioesters / Secondary alcohols / Carbothioic S-esters / Carboxylic acid esters / Cyclic alcohols and derivatives
show 8 more
Substituents
Steroid ester / Androgen-skeleton / Androstane-skeleton / 3-oxosteroid / Hydroxysteroid / 6-halo-steroid / 9-halo-steroid / Oxosteroid / 3-oxo-delta-1,4-steroid / 11-beta-hydroxysteroid
show 28 more
Molecular Framework
Aliphatic homopolycyclic compounds
External Descriptors
thioester, propanoate ester, 11beta-hydroxy steroid, steroid ester, fluorinated steroid, 3-oxo-Delta(1),Delta(4)-steroid, corticosteroid (CHEBI:31441)

Targets

Details
1. Glucocorticoid receptor
Kind
Protein
Organism
Human
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. Andersson O, Cassel TN, Gronneberg R, Bronnegard M, Stierna P, Nord M: In vivo modulation of glucocorticoid receptor mRNA by inhaled fluticasone propionate in bronchial mucosa and blood lymphocytes in subjects with mild asthma. J Allergy Clin Immunol. 1999 Apr;103(4):595-600. [PubMed:10200007]
  2. Lumry WR: A review of the preclinical and clinical data of newer intranasal steroids used in the treatment of allergic rhinitis. J Allergy Clin Immunol. 1999 Oct;104(4 Pt 1):S150-8. [PubMed:10518812]
  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. Hogger P, Rohdewald P: Binding kinetics of fluticasone propionate to the human glucocorticoid receptor. Steroids. 1994 Oct;59(10):597-602. [PubMed:7878687]
  5. Johnson M: Fluticasone propionate: safety profile. Cutis. 1996 Feb;57(2 Suppl):10-2. [PubMed:8646863]
  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
Human
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]
  2. Austin RJ, Maschera B, Walker A, Fairbairn L, Meldrum E, Farrow SN, Uings IJ: Mometasone furoate is a less specific glucocorticoid than fluticasone propionate. Eur Respir J. 2002 Dec;20(6):1386-92. [PubMed:12503693]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Inhibitor
General Function
Phospholipase a2 activity
Specific Function
Selectively hydrolyzes arachidonyl phospholipids in the sn-2 position releasing arachidonic acid. Together with its lysophospholipid activity, it is implicated in the initiation of the inflammatory...
Gene Name
PLA2G4A
Uniprot ID
P47712
Uniprot Name
Cytosolic phospholipase A2
Molecular Weight
85238.2 Da
References
  1. Sano A, Munoz NM, Sano H, Choi J, Zhu X, Jacobs B, Leff AR: Inhibition of cPLA2 translocation and leukotriene C4 secretion by fluticasone propionate in exogenously activated human eosinophils. Am J Respir Crit Care Med. 1999 Jun;159(6):1903-9. [PubMed:10351938]
  2. Myo S, Zhu X, Myou S, Meliton AY, Liu J, Boetticher E, Lambertino AT, Xu C, Munoz NM, Leff AR: Additive blockade of beta 2-integrin adhesion of eosinophils by salmeterol and fluticasone propionate. Eur Respir J. 2004 Apr;23(4):511-7. [PubMed:15083746]
Kind
Protein
Organism
Human
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. Austin RJ, Maschera B, Walker A, Fairbairn L, Meldrum E, Farrow SN, Uings IJ: Mometasone furoate is a less specific glucocorticoid than fluticasone propionate. Eur Respir J. 2002 Dec;20(6):1386-92. [PubMed:12503693]
  2. 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
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. 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. Murai T, Reilly CA, Ward RM, Yost GS: The inhaled glucocorticoid fluticasone propionate efficiently inactivates cytochrome P450 3A5, a predominant lung P450 enzyme. Chem Res Toxicol. 2010 Aug 16;23(8):1356-64. doi: 10.1021/tx100124k. [PubMed:20707410]
Kind
Protein
Organism
Human
Pharmacological action
Unknown
Actions
Substrate
Inhibitor
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. Murai T, Reilly CA, Ward RM, Yost GS: The inhaled glucocorticoid fluticasone propionate efficiently inactivates cytochrome P450 3A5, a predominant lung P450 enzyme. Chem Res Toxicol. 2010 Aug 16;23(8):1356-64. doi: 10.1021/tx100124k. [PubMed:20707410]
Kind
Protein
Organism
Human
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
Human
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
Human
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. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [PubMed:17139284]
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. [PubMed:17016423]
Kind
Protein
Organism
Human
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. FDA reports [Link]
Kind
Protein
Organism
Human
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 13, 2005 07:24 / Updated on September 23, 2018 19:37