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

Stem definition	Drug id	CAS RN
muscarinic receptors agonists/antagonists	4816	869113-09-7

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: incruse umeclidinium GSK573719A umeclidinium bromide	a long-acting antimuscarinic agent with similar affinity to the subtypes of muscarinic receptors M1 to M5, in the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation Molecular weight: 428.60 Formula: C29H34NO2 CLOGP: 1.60 LIPINSKI: 0 HAC: 3 HDO: 1 TPSA: 29.46 ALOGS: -7.38 ROTB: 8 Status: ONP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

incruse
umeclidinium
GSK573719A
umeclidinium bromide

a long-acting antimuscarinic agent with similar affinity to the subtypes of muscarinic receptors M1 to M5, in the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation

Molecular weight: 428.60
Formula: C29H34NO2
CLOGP: 1.60
LIPINSKI: 0
HAC: 3
HDO: 1
TPSA: 29.46
ALOGS: -7.38
ROTB: 8

Status: ONP

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

Drug dosage:

Dose	Unit	Route
55	mcg	Inhal.powder

ADMET properties:

Property	Value	Reference
Vd (Volume of distribution)	1.23 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	35.95 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.11 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	19 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Dec. 18, 2013	FDA	GLAXOSMITHKLINE
July 4, 2014	PMDA	GLAXOSMITHKLINE K.K.

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
Wheezing	369.62	23.30	172	6204	61875	50536873
Obstructive airways disorder	291.40	23.30	99	6277	15553	50583195
Asthma	256.48	23.30	152	6224	89185	50509563
Nasal polyps	228.32	23.30	55	6321	2499	50596249
Full blood count abnormal	194.17	23.30	82	6294	23306	50575442
Cough	172.32	23.30	180	6196	241084	50357664
Sleep disorder due to a general medical condition	166.55	23.30	54	6322	7317	50591431
Dyspnoea	151.45	23.30	256	6120	547352	50051396
Sputum discoloured	149.09	23.30	58	6318	13337	50585411
Therapeutic product effect incomplete	139.16	23.30	105	6271	91410	50507338
Productive cough	113.85	23.30	75	6301	52619	50546129
Asthma-chronic obstructive pulmonary disease overlap syndrome	108.05	23.30	22	6354	453	50598295
Salpingo-oophorectomy unilateral	105.20	23.30	22	6354	519	50598229
Sputum increased	101.35	23.30	27	6349	1840	50596908
Sinusitis fungal	100.80	23.30	25	6351	1281	50597467
Osteoporosis	99.66	23.30	65	6311	44814	50553934
Respiratory symptom	98.99	23.30	28	6348	2386	50596362
Loss of personal independence in daily activities	96.81	23.30	76	6300	69974	50528774
Dyspnoea exertional	94.17	23.30	66	6310	51167	50547581
Hiatus hernia	94.04	23.30	46	6330	18298	50580450
Embolism venous	93.28	23.30	27	6349	2498	50596250
Total lung capacity increased	93.26	23.30	21	6355	706	50598042
Gastrooesophageal reflux disease	93.07	23.30	77	6299	76351	50522397
Female genital tract fistula	83.36	23.30	27	6349	3639	50595109
Diastolic dysfunction	81.08	23.30	29	6347	5273	50593475
Emphysema	72.45	23.30	31	6345	9062	50589686
Venous pressure jugular increased	71.19	23.30	16	6360	533	50598215
Chronic obstructive pulmonary disease	69.55	23.30	56	6320	53379	50545369
Kyphosis	69.31	23.30	21	6355	2274	50596474
Oedema peripheral	63.08	23.30	88	6288	157873	50440875
Chronic sinusitis	62.69	23.30	25	6351	6120	50592628
Rhinitis allergic	62.20	23.30	26	6350	7174	50591574
Chest discomfort	61.95	23.30	67	6309	92655	50506093
Disease recurrence	59.56	23.30	35	6341	20046	50578702
Tricuspid valve incompetence	59.44	23.30	30	6346	12740	50586008
Bronchiectasis	59.40	23.30	28	6348	10255	50588493
Diverticulum	55.53	23.30	27	6349	10587	50588161
Sarcoidosis	53.23	23.30	21	6355	4996	50593752
Eczema	53.10	23.30	34	6342	22668	50576080
Rectal prolapse	52.80	23.30	16	6360	1733	50597015
Hysterectomy	50.29	23.30	23	6353	7867	50590881
Iron deficiency anaemia	49.03	23.30	29	6347	16805	50581943
Upper-airway cough syndrome	48.52	23.30	23	6353	8527	50590221
Pneumococcal infection	47.98	23.30	11	6365	401	50598347
Sleep apnoea syndrome	46.74	23.30	32	6344	23836	50574912
Bundle branch block left	45.57	23.30	20	6356	6210	50592538
Cardiac murmur	43.46	23.30	23	6353	10761	50587987
Sputum purulent	43.26	23.30	12	6364	951	50597797
Lung neoplasm malignant	40.76	23.30	25	6351	15459	50583289
Candida infection	40.16	23.30	29	6347	23494	50575254
Osteoarthritis	39.66	23.30	46	6330	68560	50530188
Chorea	39.35	23.30	12	6364	1328	50597420
Tooth injury	34.17	23.30	10	6366	961	50597787
Nicotine dependence	33.32	23.30	9	6367	646	50598102
Blood test abnormal	31.65	23.30	19	6357	11300	50587448
Secondary immunodeficiency	28.02	23.30	9	6367	1179	50597569
Fungal infection	27.98	23.30	26	6350	29939	50568809
Pulmonary embolism	25.69	23.30	46	6330	101658	50497090
Pneumonia respiratory syncytial viral	24.22	23.30	7	6369	643	50598105
Respiratory gas exchange disorder	23.59	23.30	6	6370	340	50598408

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
Asthma	373.81	34.60	164	5526	33685	29535152
Wheezing	328.31	34.60	149	5541	33091	29535746
Obstructive airways disorder	323.61	34.60	109	5581	10907	29557930
Therapeutic product effect incomplete	322.63	34.60	155	5535	39150	29529687
Full blood count abnormal	244.00	34.60	96	5594	14917	29553920
Bronchial wall thickening	220.39	34.60	49	5641	1003	29567834
Appendicolith	197.27	34.60	57	5633	3423	29565414
Pulmonary function test abnormal	168.05	34.60	45	5645	2037	29566800
Right atrial hypertrophy	157.19	34.60	33	5657	509	29568328
Appendicitis	145.54	34.60	57	5633	8722	29560115
Bronchiectasis	135.25	34.60	50	5640	6535	29562302
Bronchial secretion retention	132.39	34.60	33	5657	1120	29567717
Right ventricular hypertrophy	132.17	34.60	33	5657	1128	29567709
Loss of personal independence in daily activities	126.87	34.60	72	5618	25368	29543469
Obstruction	115.61	34.60	33	5657	1893	29566944
Aortic valve stenosis	111.16	34.60	33	5657	2175	29566662
Cardiogenic shock	105.70	34.60	58	5632	19132	29549705
Cough	104.59	34.60	125	5565	126602	29442235
Productive cough	103.28	34.60	68	5622	31191	29537646
Stress	96.93	34.60	57	5633	21433	29547404
Dyspnoea	94.84	34.60	199	5491	326533	29242304
Diastolic dysfunction	84.31	34.60	33	5657	5031	29563806
Sleep disorder due to a general medical condition	83.89	34.60	29	5661	3117	29565720
Intervertebral disc degeneration	83.07	34.60	33	5657	5231	29563606
Chest X-ray abnormal	82.29	34.60	30	5660	3764	29565073
Ascites	69.44	34.60	57	5633	36562	29532275
Pulmonary function test decreased	68.84	34.60	27	5663	4136	29564701
Sleep apnoea syndrome	67.28	34.60	42	5648	17557	29551280
Blood test abnormal	66.90	34.60	29	5661	5720	29563117
Abdominal distension	64.02	34.60	60	5630	45851	29522986
Osteoporosis	63.29	34.60	34	5656	10735	29558102
Blood immunoglobulin E increased	59.96	34.60	20	5670	1927	29566910
Benign prostatic hyperplasia	57.92	34.60	33	5657	11677	29557160
Pleural thickening	57.03	34.60	13	5677	298	29568539
Hypoacusis	56.58	34.60	35	5655	14388	29554449
Hyponatraemia	52.80	34.60	65	5625	67568	29501269
Gout	49.12	34.60	34	5656	16877	29551960
Eosinophil count increased	48.21	34.60	25	5665	7344	29561493
Inspiratory capacity abnormal	46.45	34.60	9	5681	90	29568747
Breath sounds abnormal	46.02	34.60	22	5668	5435	29563402
Gastrooesophageal reflux disease	45.49	34.60	42	5648	31454	29537383
Multiple organ dysfunction syndrome	45.02	34.60	58	5632	63058	29505779
Ocular discomfort	42.83	34.60	15	5675	1674	29567163
Chest discomfort	42.16	34.60	48	5642	45935	29522902
Ventricular fibrillation	41.73	34.60	30	5660	15803	29553034
Iron deficiency	41.08	34.60	17	5673	2988	29565849
Dyspnoea exertional	40.26	34.60	42	5648	36448	29532389
Constipation	38.09	34.60	74	5616	114086	29454751
Asthma-chronic obstructive pulmonary disease overlap syndrome	36.93	34.60	11	5679	732	29568105

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
Obstructive airways disorder	559.25	23.66	192	10797	22993	64464750
Wheezing	557.07	23.66	272	10717	80307	64407436
Asthma	452.47	23.66	250	10739	94975	64392768
Full blood count abnormal	357.34	23.66	148	10841	29609	64458134
Therapeutic product effect incomplete	309.79	23.66	202	10787	103280	64384463
Cough	234.50	23.66	272	10717	301876	64185867
Appendicolith	199.60	23.66	56	10933	3413	64484330
Productive cough	197.31	23.66	134	10855	73069	64414674
Bronchial wall thickening	192.21	23.66	48	10941	1859	64485884
Bronchiectasis	182.08	23.66	74	10915	14066	64473677
Pulmonary function test abnormal	177.15	23.66	50	10939	3114	64484629
Nasal polyps	174.78	23.66	51	10938	3578	64484165
Dyspnoea	172.42	23.66	377	10612	718297	63769446
Diastolic dysfunction	162.52	23.66	60	10929	8815	64478928
Right atrial hypertrophy	160.96	23.66	33	10956	512	64487231
Loss of personal independence in daily activities	156.72	23.66	116	10873	72338	64415405
Osteoporosis	155.42	23.66	94	10895	41986	64445757
Sleep disorder due to a general medical condition	141.01	23.66	53	10936	8181	64479562
Sputum discoloured	140.31	23.66	66	10923	17790	64469953
Gastrooesophageal reflux disease	136.27	23.66	113	10876	83030	64404713
Right ventricular hypertrophy	131.90	23.66	33	10956	1287	64486456
Asthma-chronic obstructive pulmonary disease overlap syndrome	126.90	23.66	31	10958	1094	64486649
Appendicitis	124.93	23.66	56	10933	13513	64474230
Dyspnoea exertional	120.36	23.66	100	10889	73630	64414113
Sleep apnoea syndrome	116.24	23.66	69	10920	29763	64457980
Bronchial secretion retention	110.67	23.66	33	10956	2494	64485249
Obstruction	102.51	23.66	33	10956	3215	64484528
Blood test abnormal	99.09	23.66	47	10942	12896	64474847
Aortic valve stenosis	91.40	23.66	33	10956	4547	64483196
Chest discomfort	90.38	23.66	105	10884	116001	64371742
Salpingo-oophorectomy unilateral	89.44	23.66	20	10969	476	64487267
Respiratory symptom	84.16	23.66	28	10961	3025	64484718
Cardiogenic shock	81.67	23.66	57	10932	32370	64455373
Sinusitis fungal	77.85	23.66	23	10966	1683	64486060
Total lung capacity increased	77.27	23.66	19	10970	689	64487054
Female genital tract fistula	75.76	23.66	25	10964	2633	64485110
Upper-airway cough syndrome	73.79	23.66	34	10955	8736	64479007
Hiatus hernia	72.13	23.66	44	10945	19913	64467830
Sputum increased	71.82	23.66	26	10963	3609	64484134
Chest X-ray abnormal	69.33	23.66	30	10959	6651	64481092
Benign prostatic hyperplasia	69.29	23.66	33	10956	9132	64478611
Embolism venous	68.97	23.66	25	10964	3482	64484261
Chronic obstructive pulmonary disease	68.65	23.66	72	10917	70976	64416767
Intervertebral disc degeneration	60.83	23.66	34	10955	13086	64474657
Pulmonary function test decreased	60.53	23.66	27	10962	6434	64481309
Ascites	60.19	23.66	63	10926	61938	64425805
Eczema	56.27	23.66	44	10945	29676	64458067
Stress	56.08	23.66	60	10929	60474	64427269
Kyphosis	54.42	23.66	19	10970	2374	64485369
Venous pressure jugular increased	53.17	23.66	16	10973	1247	64486496
Blood immunoglobulin E increased	52.50	23.66	21	10968	3823	64483920
Chronic sinusitis	48.61	23.66	23	10966	6269	64481474
Rectal prolapse	48.25	23.66	16	10973	1710	64486033
Abdominal distension	46.81	23.66	69	10920	95925	64391818
Hypoacusis	46.18	23.66	37	10952	25830	64461913
Rhinitis allergic	46.01	23.66	24	10965	8054	64479689
Gout	45.58	23.66	34	10955	21379	64466364
Hysterectomy	43.67	23.66	20	10969	5065	64482678
Emphysema	43.25	23.66	28	10961	14041	64473702
Eosinophil count increased	43.17	23.66	28	10961	14084	64473659
Inspiratory capacity abnormal	41.99	23.66	8	10981	83	64487660
Sputum purulent	40.92	23.66	13	10976	1213	64486530
Multiple organ dysfunction syndrome	39.84	23.66	66	10923	101347	64386396
Tricuspid valve incompetence	38.45	23.66	28	10961	16975	64470768
Diverticulum	37.49	23.66	25	10964	13173	64474570
Sinusitis	37.33	23.66	79	10910	145849	64341894
Pneumococcal infection	37.16	23.66	11	10978	810	64486933
Sarcoidosis	37.13	23.66	19	10970	6127	64481616
Oedema peripheral	36.61	23.66	98	10891	210219	64277524
Drug interaction	35.49	23.66	9	10980	362074	64125669
Breath sounds abnormal	35.32	23.66	23	10966	11646	64476097
Cardiac failure congestive	34.92	23.66	72	10917	130508	64357235
Disease recurrence	32.33	23.66	33	10956	31477	64456266
Iron deficiency anaemia	32.20	23.66	28	10961	21861	64465882
Ventricular fibrillation	32.07	23.66	29	10960	23831	64463912
Chorea	31.09	23.66	12	10977	1988	64485755
Bundle branch block left	30.92	23.66	20	10969	10014	64477729
Pleural thickening	30.86	23.66	13	10976	2697	64485046
Iron deficiency	28.98	23.66	17	10972	7160	64480583
Systolic dysfunction	28.78	23.66	13	10976	3189	64484554
Toxicity to various agents	28.75	23.66	13	10976	363500	64124243
Nicotine dependence	28.70	23.66	9	10980	805	64486938
Osteoarthritis	28.68	23.66	44	10945	63292	64424451
Bronchial hyperreactivity	28.44	23.66	12	10977	2500	64485243
Cardiac murmur	28.34	23.66	20	10969	11543	64476200
Drug ineffective	27.92	23.66	64	10925	840183	63647560
Tooth injury	27.86	23.66	10	10979	1353	64486390
Diaphragmatic disorder	27.41	23.66	10	10979	1418	64486325
Constipation	26.85	23.66	93	10896	229244	64258499
Hyponatraemia	26.68	23.66	70	10919	148269	64339474
Bronchopulmonary aspergillosis allergic	26.17	23.66	10	10979	1612	64486131
Ocular discomfort	26.02	23.66	13	10976	3986	64483757
Asthenia	25.91	23.66	21	10968	428023	64059720
Seasonal allergy	25.81	23.66	19	10970	11707	64476036
Neutropenia	25.39	23.66	5	10984	239619	64248124
Lung neoplasm malignant	24.85	23.66	24	10965	21424	64466319

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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
ATC	R03BB07	RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Anticholinergics
FDA MoA	N0000175370	Cholinergic Antagonists
FDA EPC	N0000175574	Anticholinergic
CHEBI has role	CHEBI:48876	muscarinic antagonists

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

None

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 0.0625MG 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.
EQ 62.5MCG BASE/INH	INCRUSE ELLIPTA	GLAXO GRP ENGLAND	N205382	April 30, 2014	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.
0.1MG/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.
EQ 62.5MCG BASE/INH	INCRUSE ELLIPTA	GLAXO GRP ENGLAND	N205382	April 30, 2014	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.
0.1MG/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
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
EQ 0.0625MG BASE/INH;EQ 0.025MG BASE/INH	ANORO ELLIPTA	GLAXOSMITHKLINE	N203975	Dec. 18, 2013	RX	POWDER	INHALATION	June 9, 2022	ADDITIONAL INFORMATION ADDED TO THE LABELING BASED ON SAFETY AND EFFICACY DATA FROM THE IMPACT TRIAL
EQ 62.5MCG BASE/INH	INCRUSE ELLIPTA	GLAXO GRP ENGLAND	N205382	April 30, 2014	RX	POWDER	INHALATION	June 9, 2022	ADDITIONAL INFORMATION ADDED TO THE LABELING BASED ON SAFETY AND EFFICACY DATA FROM THE IMPACT TRIAL
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

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Muscarinic acetylcholine receptor M3	GPCR	P20309	ACM3_HUMAN	ANTAGONIST	Ki	10.22	SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M4	GPCR	P08173	ACM4_HUMAN	ANTAGONIST	Ki	10.30	IUPHAR
Muscarinic acetylcholine receptor M5	GPCR	P08912	ACM5_HUMAN	ANTAGONIST	Ki	9.90	IUPHAR
Muscarinic acetylcholine receptor M1	GPCR	P11229	ACM1_HUMAN		Ki	9.80	SCIENTIFIC LITERATURE
Muscarinic acetylcholine receptor M2	GPCR	P08172	ACM2_HUMAN		Ki	9.82	SCIENTIFIC LITERATURE

External reference:

ID	Source
D10180	KEGG_DRUG
4033108	VANDF
4033109	VANDF
CHEBI:79040	CHEBI
CHEMBL1187833	ChEMBL_ID
C573971	MESH_SUPPLEMENTAL_RECORD_UI
7354	IUPHAR_LIGAND_ID
DB09076	DRUGBANK_ID
GE2T1418SV	UNII
11519070	PUBCHEM_CID
1487512	RXNORM
d08187	MMSL
015344	NDDF
015345	NDDF
706898002	SNOMEDCT_US
706899005	SNOMEDCT_US
715611006	SNOMEDCT_US
C3661274	UMLSCUI
CHEMBL523299	ChEMBL_ID
9551	INN_ID
869185-19-3	SECONDARY_CAS_RN

Pharmaceutical products:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Anoro Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0869	POWDER	62.50 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Incruse Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0873	AEROSOL, POWDER	62.50 ug	ORAL	NDA	27 sections
Incruse Ellipta	HUMAN PRESCRIPTION DRUG LABEL	1	0173-0873	AEROSOL, POWDER	62.50 ug	ORAL	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0887	POWDER	62.50 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0887	POWDER	62.50 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0893	POWDER	62.50 ug	RESPIRATORY (INHALATION)	NDA	27 sections
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0893	POWDER	62.50 ug	RESPIRATORY (INHALATION)	NDA	27 sections