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

Stem definition	Drug id	CAS RN
bronchodilators, phenethylamine derivatives	4799	503068-34-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: GW642444X vilanterol Breo Ellipta vilanterol trifenatate GW642444M	Vilanterol is a long-acting beta2-adrenergic agonist. The clinical relevance of this in vitro finding is unknown. Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, there are also beta2-receptors in the human heart comprising 10% to 50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2-agonists may have cardiac effects. The pharmacologic effects of beta2-adrenergic agonist drugs, including vilanterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells. Molecular weight: 486.43 Formula: C24H33Cl2NO5 CLOGP: 3.19 LIPINSKI: 0 HAC: 6 HDO: 4 TPSA: 91.18 ALOGS: -5.61 ROTB: 16 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

GW642444X
vilanterol
Breo Ellipta
vilanterol trifenatate
GW642444M

Vilanterol is a long-acting beta2-adrenergic agonist. The clinical relevance of this in vitro finding is unknown. Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, there are also beta2-receptors in the human heart comprising 10% to 50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2-agonists may have cardiac effects. The pharmacologic effects of beta2-adrenergic agonist drugs, including vilanterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibition of release of mediators of immediate hypersensitivity from cells, especially from mast cells.

Molecular weight: 486.43
Formula: C24H33Cl2NO5
CLOGP: 3.19
LIPINSKI: 0
HAC: 6
HDO: 4
TPSA: 91.18
ALOGS: -5.61
ROTB: 16

Status: ONP

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

Drug dosage:

None

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	2.38 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	25.70 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.06 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.40 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Nov. 13, 2013	EMA	GlaxoSmithKline (Ireland) Limited
May 10, 2013	FDA	GLAXO GRP LTD

FDA Adverse Event Reporting System (Female)

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
Lactose intolerance	89.66	47.41	18	963	2960	63485081
Obstructive airways disorder	67.41	47.41	21	960	20678	63467363
Asthma	59.63	47.41	32	949	127529	63360512
Hydronephrosis	57.51	47.41	16	965	10646	63477395
Sneezing	57.29	47.41	18	963	18200	63469841
Eye pruritus	56.85	47.41	18	963	18653	63469388
Haemoptysis	56.80	47.41	20	961	28706	63459335
Lacrimation increased	55.08	47.41	18	963	20613	63467428
Full blood count abnormal	54.86	47.41	20	961	31697	63456344
Subclavian vein thrombosis	54.34	47.41	11	970	1879	63486162
Wheezing	50.36	47.41	26	955	95569	63392472

FDA Adverse Event Reporting System (Male)

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
Appendicolith	436.51	110.32	108	2801	8493	34945529
Appendicitis	378.34	110.32	108	2801	14699	34939323
Cardiogenic shock	315.94	110.32	108	2801	26510	34927512
Stress	305.88	110.32	109	2800	30238	34923784
Ventricular fibrillation	263.88	110.32	91	2818	22863	34931159
Ascites	260.50	110.32	109	2800	46462	34907560
Blood phosphorus increased	255.13	110.32	69	2840	7652	34946370
Abdominal distension	233.47	110.32	108	2801	58384	34895638
Multiple organ dysfunction syndrome	205.84	110.32	108	2801	76458	34877564
Hyponatraemia	200.82	110.32	109	2800	82582	34871440
General physical health deterioration	156.63	110.32	109	2800	128160	34825862
Constipation	150.16	110.32	109	2800	136873	34817149
Dry mouth	149.70	110.32	65	2844	30100	34923922
Abdominal pain	135.06	110.32	110	2799	163508	34790514
Sepsis	127.06	110.32	107	2802	166454	34787568

FDA Adverse Event Reporting System (Geriatric)

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
Appendicolith	491.20	65.36	107	3685	8444	79732152
Appendicitis	396.68	65.36	107	3685	20687	79719909
Cardiogenic shock	322.66	65.36	107	3685	41807	79698789
Ventricular fibrillation	279.97	65.36	90	3702	31836	79708760
Blood phosphorus increased	273.21	65.36	69	3723	10278	79730318
Ascites	264.58	65.36	108	3684	75454	79665142
Stress	262.51	65.36	109	3683	79503	79661093
Abdominal distension	216.98	65.36	108	3684	119542	79621054
Multiple organ dysfunction syndrome	213.51	65.36	107	3685	120139	79620457
Hyponatraemia	176.87	65.36	108	3684	177740	79562856
Constipation	170.96	65.36	126	3666	282924	79457672
Sepsis	167.35	65.36	122	3670	269306	79471290
Abdominal pain	151.46	65.36	134	3658	389435	79351161
General physical health deterioration	134.22	65.36	108	3684	275130	79465466
Blood uric acid increased	118.29	65.36	38	3754	13322	79727274
Dry mouth	117.96	65.36	65	3727	87954	79652642
Myasthenia gravis	114.74	65.36	35	3757	10364	79730232
Lactose intolerance	73.78	65.36	18	3774	2312	79738284
Analgesic therapy	65.54	65.36	14	3778	995	79739601

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	R03AK10	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with corticosteroids or other drugs, excl. anticholinergics
ATC	R03AL03	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
ATC	R03AL08	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
FDA MoA	N0000009922	Adrenergic beta2-Agonists
FDA EPC	N0000175779	beta2-Adrenergic Agonist
CHEBI has role	CHEBI:35522	beta-adrenergic agonists
CHEBI has role	CHEBI:35523	bronchodilator

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

Disease	Relation	SNOMED_ID	DOID
Chronic obstructive lung disease	indication	13645005	DOID:3083
Chronic bronchitis	indication	63480004	DOID:6132
Pulmonary emphysema	indication	87433001
Asthma	indication	195967001	DOID:2841

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	10.07	acidic
pKa2	9.28	Basic

Orange Book patent data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Patent number	Patent expiration date	Patent use
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	ANORO ELLIPTA	GLAXOSMITHKLINE	N203975	Dec. 18, 2013	RX	POWDER	INHALATION	RE44874	March 23, 2023	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
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
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	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 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	RE44874	March 23, 2023	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	RE44874	March 23, 2023	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA; AND ASTHMA
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 9, 2020	RX	POWDER	INHALATION	RE44874	March 23, 2023	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA; AND ASTHMA
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	ANORO ELLIPTA	GLAXOSMITHKLINE	N203975	Dec. 18, 2013	RX	POWDER	INHALATION	8309572	April 27, 2025	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	8309572	April 27, 2025	METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 9, 2020	RX	POWDER	INHALATION	8309572	April 27, 2025	METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	ANORO ELLIPTA	GLAXOSMITHKLINE	N203975	Dec. 18, 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 CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
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
0.1MG/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
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	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
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	RX	POWDER	INHALATION	7439393	May 21, 2025	INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	RX	POWDER	INHALATION	7439393	May 21, 2025	INDICATED FOR THE ONCE-DAILY TREATMENT OF ASTHMA IN PATIENTS 18 YEARS AND OLDER
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	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
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	7439393	May 21, 2025	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	7439393	May 21, 2025	MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS 18 YRS AND OLDER, OR CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 9, 2020	RX	POWDER	INHALATION	7439393	May 21, 2025	MAINTENANCE TREATMENT OF ASTHMA IN PATIENTS 18 YRS AND OLDER, OR CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	ANORO ELLIPTA	GLAXOSMITHKLINE	N203975	Dec. 18, 2013	RX	POWDER	INHALATION	8183257	July 27, 2025	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	8183257	July 27, 2025	METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA INHALATION
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	8183257	July 27, 2025	METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 9, 2020	RX	POWDER	INHALATION	8183257	July 27, 2025	METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	ANORO ELLIPTA	GLAXOSMITHKLINE	N203975	Dec. 18, 2013	RX	POWDER	INHALATION	8511304	June 14, 2027	INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA.
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
0.1MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	May 10, 2013	RX	POWDER	INHALATION	8511304	June 14, 2027	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	8511304	June 14, 2027	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 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	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
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	RX	POWDER	INHALATION	8511304	June 14, 2027	INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	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
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	8511304	June 14, 2027	METHOD OF DISPENSING A COMBINATION MEDICAMENT PRODUCT FROM CLAIMED DELIVERY DEVICE, FOR EXAMPLE FOR THE TREATMENT OF ASTHMA OR COPD
0.2MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 9, 2020	RX	POWDER	INHALATION	8511304	June 14, 2027	METHOD OF DISPENSING A COMBINATION MEDICAMENT PRODUCT FROM CLAIMED DELIVERY DEVICE, FOR EXAMPLE FOR THE TREATMENT OF ASTHMA OR COPD
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	11116721	Feb. 26, 2029	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	11116721	Feb. 26, 2029	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	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
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	RX	POWDER	INHALATION	11116721	Feb. 26, 2029	INDICATED FOR THE ONCE-DAILY INHALED TREATMENT FOR ASTHMA IN ADULTS AGED 18 YEARS AND OLDER
0.2MG/INH;EQ 0.025MG BASE/INH	BREO ELLIPTA	GLAXO GRP LTD	N204275	April 30, 2015	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
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	ANORO ELLIPTA	GLAXOSMITHKLINE	N203975	Dec. 18, 2013	RX	POWDER	INHALATION	11090294	Nov. 29, 2030	MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD)
0.1MG/INH;EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	TRELEGY ELLIPTA	GLAXOSMITHKLINE	N209482	Sept. 18, 2017	RX	POWDER	INHALATION	11090294	Nov. 29, 2030	MAINTENANCE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) COMPRISING THE ONCE PER DAY ADMINISTRATION OF TRELEGY ELLIPTA, 100 MCG FLUTICASONE FUROATE/62.5 MCG UMECLIDINIUM/25 MCG VILANTEROL

Orange Book exclusivity data (new drug applications)

Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
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
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

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	AGONIST	EC50	9.40	WOMBAT-PK	CHEMBL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		EC50	6.40	WOMBAT-PK
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		EC50	6.10	WOMBAT-PK

External reference:

ID	Source
D09696	KEGG_DRUG
4032565	VUID
N0000188266	NUI
503070-58-4	SECONDARY_CAS_RN
4032565	VANDF
CHEBI:75037	CHEBI
CHEMBL1198857	ChEMBL_ID
CHEMBL1084647	ChEMBL_ID
C550468	MESH_SUPPLEMENTAL_RECORD_UI
7353	IUPHAR_LIGAND_ID
9198	INN_ID
DB09082	DRUGBANK_ID
028LZY775B	UNII
1424883	RXNORM
203032	MMSL
29456	MMSL
29954	MMSL
d08099	MMSL
015022	NDDF
015023	NDDF
702408004	SNOMEDCT_US
702409007	SNOMEDCT_US
720194004	SNOMEDCT_US
C2935023	UMLSCUI
CHEMBL1084172	ChEMBL_ID
10184665	PUBCHEM_CID

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0859	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0859	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0859	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Anoro Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0869	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Anoro Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0869	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Anoro Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0869	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0882	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0882	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0882	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0887	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0887	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0887	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0893	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0893	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0893	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0916	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Fluticasone Furoate and Vilanterol	HUMAN PRESCRIPTION DRUG LABEL	2	66993-135	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA authorized generic	26 sections
Fluticasone Furoate and Vilanterol	HUMAN PRESCRIPTION DRUG LABEL	2	66993-135	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA authorized generic	26 sections
Fluticasone Furoate and Vilanterol	HUMAN PRESCRIPTION DRUG LABEL	2	66993-136	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA authorized generic	26 sections
Fluticasone Furoate and Vilanterol	HUMAN PRESCRIPTION DRUG LABEL	2	66993-136	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA authorized generic	26 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	70518-2028	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Breo Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	70518-2028	POWDER	25 ug	RESPIRATORY (INHALATION)	NDA	27 sections