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fluticasone furoate 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
	4554	397864-44-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: fluticasone furoate avamys veramyst	Fluticasone furoate is a synthetic trifluorinated corticosteroid with anti‑inflammatory activity. Fluticasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor. The precise mechanism of corticosteroid action on asthma is not known. Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation. These anti-inflammatory actions of corticosteroids contribute to their efficacy in asthma. Molecular weight: 538.58 Formula: C27H29F3O6S CLOGP: 4.26 LIPINSKI: 1 HAC: 6 HDO: 1 TPSA: 93.81 ALOGS: -4.09 ROTB: 6 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

fluticasone furoate
avamys
veramyst

Fluticasone furoate is a synthetic trifluorinated corticosteroid with anti‑inflammatory activity. Fluticasone furoate has been shown in vitro to exhibit a binding affinity for the human glucocorticoid receptor. The precise mechanism of corticosteroid action on asthma is not known. Inflammation is an important component in the pathogenesis of asthma. Corticosteroids have been shown to have a wide range of actions on multiple cell types (e.g., mast cells, eosinophils, neutrophils, macrophages, lymphocytes) and mediators (e.g., histamine, eicosanoids, leukotrienes, cytokines) involved in inflammation. These anti-inflammatory actions of corticosteroids contribute to their efficacy in asthma.

Molecular weight: 538.58
Formula: C27H29F3O6S
CLOGP: 4.26
LIPINSKI: 1
HAC: 6
HDO: 1
TPSA: 93.81
ALOGS: -4.09
ROTB: 6

Status: ONP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.20	mg	N
0.11	mg	N
0.60	mg	Inhal.aerosol
0.60	mg	Inhal.powder
1.50	mg	Inhal.solution

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	4.95 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	13.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	10.60 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	0.14 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K
BA (Bioavailability)	0.01 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

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Approvals:

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Date	Agency	Company
April 22, 2009	PMDA	GlaxoSmithKline K.K.
April 27, 2007	FDA	GLAXOSMITHKLINE
Jan. 11, 2008	EMA	GlaxoSmithKline (Ireland) Limited

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FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Macular degeneration	770.62	18.23	278	16913	24098	63447733
Asthma	528.59	18.23	363	16828	127198	63344633
Wheezing	421.70	18.23	283	16908	95312	63376519
Obstructive airways disorder	409.64	18.23	168	17023	20531	63451300
Full blood count abnormal	311.37	18.23	158	17033	31559	63440272
Nasal congestion	245.99	18.23	176	17015	65484	63406347
Therapeutic product effect incomplete	232.24	18.23	223	16968	124833	63346998
Blepharospasm	199.01	18.23	71	17120	5925	63465906
Gastrooesophageal reflux disease	195.58	18.23	180	17011	95459	63376372
Sleep disorder due to a general medical condition	169.00	18.23	77	17114	12111	63459720

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Asthma	307.30	20.80	168	8570	42488	34905705
Wheezing	230.76	20.80	138	8600	41264	34906929
Appendicolith	176.23	20.80	70	8668	8531	34939662
Appendicitis	139.74	20.80	70	8668	14737	34933456
Nasal polyps	127.03	20.80	40	8698	2463	34945730
Stress	106.99	20.80	76	8662	30271	34917922
Nasal congestion	105.81	20.80	68	8670	22989	34925204
Cardiogenic shock	101.62	20.80	70	8668	26548	34921645
Ventricular fibrillation	93.88	20.80	63	8675	22891	34925302
Therapeutic product effect incomplete	89.97	20.80	85	8653	50456	34897737

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Asthma	698.69	16.54	454	22812	134641	79586481
Wheezing	585.63	16.54	385	22881	116279	79604843
Obstructive airways disorder	426.26	16.54	200	23066	31259	79689863
Full blood count abnormal	358.73	16.54	193	23073	40281	79680841
Nasal congestion	339.01	16.54	234	23032	76318	79644804
Therapeutic product effect incomplete	294.44	16.54	278	22988	141367	79579755
Sleep disorder due to a general medical condition	222.20	16.54	100	23166	14177	79706945
Chronic sinusitis	195.62	16.54	89	23177	12937	79708185
Nasal polyps	183.46	16.54	72	23194	7255	79713867
Dyspnoea	174.35	16.54	596	22670	856429	78864693

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	D07AC17	DERMATOLOGICALS CORTICOSTEROIDS, DERMATOLOGICAL PREPARATIONS CORTICOSTEROIDS, PLAIN Corticosteroids, potent (group III)
ATC	R01AD08	RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Corticosteroids
ATC	R01AD12	RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Corticosteroids
ATC	R01AD58	RESPIRATORY SYSTEM NASAL PREPARATIONS DECONGESTANTS AND OTHER NASAL PREPARATIONS FOR TOPICAL USE Corticosteroids
ATC	R03AK06	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC	R03AK10	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC	R03AK11	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC	R03AL08	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03BA05	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Glucocorticoids
ATC	R03BA09	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Glucocorticoids

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
Chronic obstructive lung disease	indication	13645005	DOID:3083
Allergic rhinitis	indication	61582004
Chronic bronchitis	indication	63480004	DOID:6132
Pulmonary emphysema	indication	87433001
Asthma	indication	195967001	DOID:2841
Chronic Non-Allergic Rhinitis	indication
Mycosis	contraindication	3218000	DOID:1564
Ocular hypertension	contraindication	4210003	DOID:9282
Epistaxis	contraindication	12441001
Measles	contraindication	14189004	DOID:8622

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	11.49	acidic

Orange Book patent data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
0.05MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 12, 2023	RX	POWDER	INHALATION	7439393	May 21, 2025	MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS AGED 5 YEARS AND OLDER. RECOMMENDED DOSAGES: BREO 100/25 OR 200/25 AGES 18 YEARS AND OLDER; BREO 100/25 AGES 12-17 YEARS, AND BREO 50/25, AGES 5-11 YEARS
0.05MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 12, 2023	RX	POWDER	INHALATION	8511304	June 14, 2027	MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS AGED 5 YEARS AND OLDER. RECOMMENDED DOSAGES: BREO 100/25 OR 200/25 AGES 18 YEARS AND OLDER; BREO 100/25 AGES 12-17 YEARS, AND BREO 50/25, AGES 5-11 YEARS
0.05MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 12, 2023	RX	POWDER	INHALATION	11116721	Feb. 26, 2029	MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS AGED 5 YEARS AND OLDER. RECOMMENDED DOSAGES: BREO 100/25 OR 200/25 AGES 18 YEARS AND OLDER; BREO 100/25 AGES 12-17 YEARS, AND BREO 50/25, AGES 5-11 YEARS
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	RE44874	March 23, 2023	FOR THE LONG-TERM, ONCE-DAILY MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH COPD, INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA, ALSO TO REDUCE EXACERBATIONS OF COPD IN PATIENTS WITH A HISTORY OF EXACERBATIONS
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	RE44874	March 23, 2023	INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	7439393	May 21, 2025	INDICATED FOR LONG-TERM, ONCE-DAILY MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PTS WITH COPD, INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA, ALSO TO REDUCE EXACERBATIONS OF COPD IN PTS WITH A HISTORY OF EXACERBATIONS
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	7439393	May 21, 2025	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING BRONCHITIS AND/OR EMPHYSEMA
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	7439393	May 21, 2025	INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	7439393	May 21, 2025	INDICATED FOR THE ONCE-DAILY TREATMENT OF ASTHMA IN PATIENTS 18 YEARS AND OLDER
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	7439393	May 21, 2025	MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS AGED 5 YEARS AND OLDER. RECOMMENDED DOSAGES: BREO 100/25 OR 200/25 AGES 18 YEARS AND OLDER; BREO 100/25 AGES 12-17 YEARS, AND BREO 50/25, AGES 5-11 YEARS

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Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
0.05MG/INH	ARNUITY ELLIPTA	GLAXOSMITHKLINE	N205625	May 17, 2018	RX	POWDER	INHALATION	March 1, 2026	INFORMATION ADDED TO SECTION 8.4 OF THE LABELING TO INCLUDE THE RESULT OFSTUDY HZA114971
0.05MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 12, 2023	RX	POWDER	INHALATION	May 13, 2026	NEW STRENGTH
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	May 13, 2026	NEW PATIENT POPULATION
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	Sept. 9, 2023	MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 9, 2020	RX	POWDER	INHALATION	Sept. 9, 2023	NEW STRENGTH

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Glucocorticoid receptor	Nuclear hormone receptor	P04150	GCR_HUMAN	AGONIST	IC50	10.12	CHEMBL	CHEMBL
Mineralocorticoid receptor	Nuclear hormone receptor	P08235	MCR_HUMAN		IC50	6.83	CHEMBL
Progesterone receptor	Nuclear hormone receptor	P06401	PRGR_HUMAN		IC50	7.68	CHEMBL
Androgen receptor	Transcription factor		ANDR_RAT		IC50	5.73	CHEMBL
Glucocorticoid receptor	Transcription factor		GCR_RAT		IC50	8.30	CHEMBL

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External reference:

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ID	Source
GW6	PDB_CHEM_ID
004952	NDDF
012173	NDDF
108632003	SNOMEDCT_US
10892	IUPHAR_LIGAND_ID
109674	MMSL
23848	MMSL
397192001	SNOMEDCT_US
4020529	VANDF
4026165	VUID

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0874	POWDER	100 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0874	POWDER	100 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0874	POWDER	100 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0876	POWDER	200 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0876	POWDER	200 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0876	POWDER	200 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0888	POWDER	50 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0888	POWDER	50 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Arnuity Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0888	POWDER	50 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0859	POWDER	100 ug	RESPIRATORY (INHALATION)	NDA	27 sections

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