Fluticasone Furoate
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Also known as AlisadeAllermistArnuity elliptaAvamysEnnhaleFlonase sensimist allergy reliefFuramistFuroate de fluticasoneFuroato de fluticasonaGSK 685 698GSK-685968GSK685968GW-685698XGW685698XRelvar elliptaTrelegy elliptaVeramyst
Summary
Fluticasone Furoate (CHEMBL1676) is an approved small-molecule anti-allergic agent (ATC R01AD12); indicated across 10 conditions including chronic obstructive pulmonary disease and obstructive lung disease.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: R01AD12 (+1 more)
- Indications: 10 conditions
- Clinical trials: 99
- Chemistry: 538.6 Da · C27H29F3O6S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1676 |
| Name | Fluticasone Furoate |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 9854489 |
| ChEBI | CHEBI:74899 |
| ATC | R01AD12, R03BA09 |
| Molecular formula | C27H29F3O6S |
| Molecular weight | 538.6 |
| InChIKey | XTULMSXFIHGYFS-VLSRWLAYSA-N |
SMILES: C[C@@H]1C[C@H]2[C@@H]3C[C@@H](C4=CC(=O)C=C[C@@]4([C@]3([C@H](C[C@@]2([C@]1(C(=O)SCF)OC(=O)C5=CC=CO5)C)O)F)C)F
IUPAC name: [(6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-17-(fluoromethylsulfanylcarbonyl)-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-17-yl] furan-2-carboxylate
ChEBI definition: A trifluorinated corticosteroid that consists of 6α,9-difluoro-11β,17α-dihydroxy-17β-{[(fluoromethyl)sulfanyl]carbonyl}-16-methyl-3-oxoandrosta-1,4-diene bearing a 2-furoyl substituent at position 17. Used in combination with vilanterol trifenate for treatment of bronchospasm associated with chronic obstructive pulmonary disease.
Pharmacological roles (ChEBI): anti-allergic agent, prodrug, anti-asthmatic drug.
Also known as: Alisade, Allermist, Arnuity ellipta, Avamys, Ennhale, Flonase sensimist allergy relief, Fluticasone furoate, Furamist, Furoate de fluticasone, Furoato de fluticasona, GSK 685 698, GSK-685968
Patent coverage: 485 distinct patent families (1,493 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Androgen receptor, Mineralocorticoid receptor, Glucocorticoid receptor, Progesterone receptor, Cannabinoid receptor 1, Prostaglandin G/H synthase 1, Androgen receptor.
Bioactivity
ChEMBL activities: 13 potent at pChembl ≥ 5 of 15 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| NR3C1 | 10.4 | IC50 | 0.04 | nM | CHEMBL_ACT_2715553 |
| NR3C1 | 9.4 | EC50 | 0.4 | nM | CHEMBL_ACT_18503379 |
| NR3C1 | 9.31 | EC50 | 0.49 | nM | CHEMBL_ACT_6390732 |
| NR3C1 | 9.29 | Ki | 0.51 | nM | CHEMBL_ACT_18503310 |
| NR3C1 | 9.1 | IC50 | 0.8 | nM | CHEMBL_ACT_18141197 |
| PGR | 8.52 | AC50 | 3 | nM | CHEMBL_ACT_25204799 |
| PGR | 7.68 | IC50 | 21 | nM | CHEMBL_ACT_18141196 |
| NR3C1 | 7.33 | AC50 | 47 | nM | CHEMBL_ACT_25176337 |
| AR | 6.89 | AC50 | 130 | nM | CHEMBL_ACT_25203866 |
| NR3C2 | 6.78 | IC50 | 166 | nM | CHEMBL_ACT_18141205 |
| PGR | 6.76 | AC50 | 173 | nM | CHEMBL_ACT_25223459 |
| P15207 | 5.73 | IC50 | 1880 | nM | CHEMBL_ACT_18141201 |
| PTGS1 | 5 | AC50 | 9890 | nM | CHEMBL_ACT_25206662 |
Target pathways
No target-pathway data for this drug (no mapped target genes).
Indications & clinical
Indications
10 indications (7 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| chronic obstructive pulmonary disease | 4 | MONDO:0005002 | EFO:0000341 |
| obstructive lung disease | 4 | MONDO:0002267 | HP:0006536 |
| seasonal allergic rhinitis | 4 | MONDO:0005324 | EFO:0003956 |
| perennial allergic rhinitis | 4 | MONDO:0024332 | EFO:1001417 |
| allergic rhinitis | 4 | MONDO:0011786 | EFO:0005854 |
| asthma | 4 | MONDO:0004979 | MONDO:0004979 |
| vasomotor rhinitis | 3 | MONDO:0006004 | EFO:0007533 |
| rhinitis | 3 | MONDO:0003014 | EFO:0008521 |
| severe acute respiratory syndrome | 3 | MONDO:0005091 | MONDO:0100096 |
1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 99.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 39 |
| PHASE4 | 23 |
| PHASE2 | 15 |
| PHASE1 | 12 |
| Not specified | 9 |
| PHASE1/PHASE2 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT06372496 | PHASE4 | ACTIVE_NOT_RECRUITING | Pragmatic Open - Label Randomized Clinical Trial of FF/UMEC/VI vs Non-ellipta Usual Care ICS-LABA for Adult Participants With Uncontrolled Asthma |
| NCT00435461 | PHASE4 | COMPLETED | Fluticasone Furoate Nasal Spray Versus Oral Fexofenadine |
| NCT00473915 | PHASE4 | COMPLETED | Intranasal Steroids and the Nasal Ocular Response |
| NCT00502775 | PHASE4 | COMPLETED | Fluticasone Furoate Nasal Spray Versus Oral Fexofenadine |
| NCT00584987 | PHASE4 | COMPLETED | Intranasal Steroids and Oxymetazoline in Allergic Rhinitis |
| NCT00603044 | PHASE4 | COMPLETED | Mechanism of Action of Fluticasone Furoate in Childhood Obstructive Sleep Apnea Syndrome |
| NCT00791973 | PHASE4 | COMPLETED | Effect of Veramyst on the Nasal and Ocular Symptoms of the Early Reaction to Nasal Challenge With Allergen |
| NCT01013701 | PHASE4 | TERMINATED | Compare the Effects of Fluticasone Furoate Nasal Spray vs Placebo in Patients With Nasal Polypoid Disease |
| NCT01957150 | PHASE4 | COMPLETED | Study Evaluating the Effect of Fluticasone Furoate/ Vilanterol (FF/VI) Inhalation Powder Compared With Vilanterol (VI) Inhalation Powder on Bone Mineral Density (BMD) in Subjects With Chronic Obstructive Pulmonary Disease (COPD). |
| NCT02730351 | PHASE4 | COMPLETED | Crossover Study Comparing Fluticasone Furoate (FF)/Vilanterol (VI) Once Daily Versus Fluticasone Propionate (FP) Twice Daily in Subjects With Asthma and Exercise-Induced Bronchoconstriction (EIB) |
| NCT02889809 | PHASE4 | COMPLETED | Effects of a Orally Inhaled Fluticasone Furoate on Growth Velocity in Prepubertal, Paediatric Subjects With Asthma Over a Year |
| NCT03152149 | PHASE4 | COMPLETED | INvestigating COPD Outcomes, Genomics and Neutrophilic Inflammation With Tiotropium and Olodaterol |
| NCT03315000 | PHASE4 | COMPLETED | Effect of Vilanterol on Methacholine Challenge Results |
| NCT03363191 | PHASE4 | WITHDRAWN | The Efficacy of Fluticasone Furoate/Vilanterol Versus (vs) Fluticasone Furoate on Asthma |
| NCT03898466 | PHASE4 | COMPLETED | Effect of Fluticasone Furoate on Methacholine Challenge |
| NCT03949842 | PHASE4 | WITHDRAWN | Legend: TRELEGY Real World Chronic Obstructive Pulmonary Disease (COPD) Effectiveness Study |
| NCT04606394 | PHASE4 | COMPLETED | Peak Inspiratory Flow and Dry Powder Inhaler Performance in COPD |
| NCT04671355 | PHASE4 | WITHDRAWN | TRIMBOW® and RELVAR® on Lung Stiffness Reduction Assessed Through Forced Oscillation Technique in Patients With COPD |
| NCT05292053 | PHASE4 | COMPLETED | Outcomes of Once-Daily ICS/LABA/LAMA + PRN Respiratory Therapy Treatments in Hospitalized Patients With COPD Exacerbations |
| NCT05342558 | PHASE4 | COMPLETED | Efficacy and Safety of ICS/LABA vs. LAMA/LABA in Patients With Different COPD Phenotypes. |
| NCT05651750 | PHASE4 | UNKNOWN | Medical vs Surgical Treatment in OSA Among Children |
| NCT06282861 | PHASE4 | TERMINATED | ANTES B+ Clinical Trial |
| NCT06905483 | PHASE4 | COMPLETED | Comparative Effects of Triple Inhaled Therapy With Budesonide/Glycopyrronium/Formoterol Versus Fluticasone Furoate/Umeclidinium/Vilanterol on Small Airway Disease in COPD Patients: A Randomized Crossover Study |
| NCT00103454 | PHASE3 | COMPLETED | A Study To Evaluate The Efficacy And Safety Of A Once-Daily Investigational Nasal Spray In Adults And Adolescents With Perennial Allergic Rhinitis (PAR). |
| NCT00107757 | PHASE3 | COMPLETED | Seasonal Allergic Rhinitis In Pediatric Subjects |
| NCT00108914 | PHASE3 | COMPLETED | Perennial Allergic Rhinitis Study In Pediatric Subjects |
| NCT00109486 | PHASE3 | COMPLETED | Safety Study To Assess Growth In Children With Seasonal Allergic And/Or Perennial Allergic Rhinitis Treated With GW685698X Aqueous Nasal Spray Or Placebo Nasal Spray |
| NCT00115622 | PHASE3 | COMPLETED | Study In Adults And Adolescents With Seasonal Allergic Rhinitis |
| NCT00117325 | PHASE3 | COMPLETED | Study Of Adults And Adolescents With Vasomotor Rhinitis |
| NCT00118703 | PHASE3 | COMPLETED | Once-Daily Investigational Nasal Spray In Adults And Adolescents With Vasomotor Rhinitis |
| NCT00224523 | PHASE3 | COMPLETED | Long Term Safety Of GW685698X Via Nasal Biopsy |
| NCT00225823 | PHASE3 | COMPLETED | Study In Adults And Adolescents With Seasonal Allergic Rhinitis. |
| NCT01072149 | PHASE3 | COMPLETED | A Study to Evaluate the Efficacy, Safety, Tolerability, Pharmacokinetic (PK), and Pharmacodynamic (PD) Profiles of 3 Doses of Fluticasone Furoate (FF)/GW642444 Inhalation Powder at the End of a 28-day Treatment Period in Subjects With Chronic Obstructive Pulmonary Disease (COPD) Compared to Placebo |
| NCT01086384 | PHASE3 | COMPLETED | Asthma Exacerbation Study |
| NCT01134042 | PHASE3 | COMPLETED | Study HZA106829: Efficacy/Safety Study of Fluticasone Furoate/Vilanterol (GW642444) in Adult and Adolescent Asthmatics |
| NCT01147848 | PHASE3 | COMPLETED | HZA113091 Efficacy and Safety of Fluticasone Furoate/Vilanterol (GW642444) in Adults and Adolescents |
| NCT01159912 | PHASE3 | COMPLETED | Evaluating the Efficacy and Safety of Fluticasone Furoate Inhalation Powder in the Treatment of Asthma in Adults and Adolescents |
| NCT01165138 | PHASE3 | COMPLETED | Study HZA106827: Efficacy/Safety Study of Fluticasone Furoate/Vilanterol (GW642444) in Adult and Adolescent Asthmatics |
| NCT01279057 | PHASE3 | COMPLETED | A Study Comparing Two Fluticasone Furoate Nasal Sprays in the Relief of the Signs and Symptoms of Seasonal Allergic Rhinitis |
| NCT01313676 | PHASE3 | COMPLETED | Study to Evaluate the Effect of Fluticasone Furoate/Vilanterol on Survival in Subjects With Chronic Obstructive Pulmonary Disease |
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
No competitor molecules sharing a primary target (ChEMBL phase ≥2 or PubChem drug-class).