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
BA (Bioavailability)	0.13 %	Kawashima H, Watanabe R, Esaki T, Kuroda M, Nagao C, Natsume-Kitatani Y, Ohashi R, Komura H, Mizuguchi K

Approvals:

Date	Agency	Company
Dec. 18, 2013	FDA	GLAXOSMITHKLINE
July 4, 2014	PMDA	GLAXOSMITHKLINE K.K.
March 20, 2017	EMA	GlaxoSmithKline Trading Services Limited

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	454.97	23.08	238	8981	95357	63384446
Nasal polyps	394.13	23.08	104	9115	5935	63473868
Asthma	327.80	23.08	213	9006	127348	63352455
Obstructive airways disorder	315.13	23.08	117	9102	20582	63459221
Asthma-chronic obstructive pulmonary disease overlap syndrome	253.24	23.08	59	9160	2002	63477801
Total lung capacity increased	236.23	23.08	57	9162	2253	63477550
Full blood count abnormal	225.33	23.08	104	9115	31613	63448190
Cough	177.64	23.08	215	9004	292528	63187275
Gastrooesophageal reflux disease	175.38	23.08	130	9089	95509	63384294
Sarcoidosis	172.74	23.08	57	9162	7065	63472738
Sputum discoloured	166.12	23.08	69	9150	16278	63463525
Sleep disorder due to a general medical condition	164.03	23.08	63	9156	12125	63467678
Rhinitis allergic	162.78	23.08	62	9157	11665	63468138
Dyspnoea	161.53	23.08	318	8901	660995	62818808
Chronic obstructive pulmonary disease	158.92	23.08	104	9115	62582	63417221
Bronchiectasis	150.20	23.08	64	9155	16078	63463725
Therapeutic product effect incomplete	148.71	23.08	132	9087	124924	63354879
Cardiac murmur	139.72	23.08	59	9160	14493	63465310
Salpingo-oophorectomy unilateral	133.90	23.08	30	9189	851	63478952
Dyspnoea exertional	126.49	23.08	89	9130	60213	63419590
Sinusitis fungal	126.43	23.08	33	9186	1798	63478005
Sputum increased	125.90	23.08	35	9184	2424	63477379
Respiratory symptom	119.54	23.08	36	9183	3311	63476492
Embolism venous	117.29	23.08	35	9184	3119	63476684
Lung neoplasm malignant	116.75	23.08	57	9162	19576	63460227
Productive cough	115.93	23.08	86	9133	63122	63416681
Oedema peripheral	106.26	23.08	134	9085	189377	63290426
Hiatus hernia	105.83	23.08	55	9164	21539	63458264
Hypomania	104.43	23.08	38	9181	6292	63473511
Osteoporosis	100.64	23.08	76	9143	57262	63422541
Diastolic dysfunction	99.92	23.08	37	9182	6434	63473369
Jaundice cholestatic	95.46	23.08	37	9182	7287	63472516
Loss of personal independence in daily activities	94.84	23.08	92	9127	97198	63382605
Emphysema	90.72	23.08	40	9179	10898	63468905
Female genital tract fistula	87.34	23.08	35	9184	7524	63472279
Schizophrenia	84.50	23.08	37	9182	9915	63469888
Diverticulum	74.85	23.08	36	9183	11955	63467848
Tricuspid valve incompetence	73.81	23.08	38	9181	14583	63465220
Chest discomfort	73.35	23.08	85	9134	109884	63369919
Eczema	68.44	23.08	48	9171	32243	63447560
Venous pressure jugular increased	68.13	23.08	16	9203	561	63479242
Hysterectomy	66.91	23.08	31	9188	9468	63470335
Disease recurrence	64.90	23.08	44	9175	27986	63451817
Kyphosis	64.27	23.08	21	9198	2519	63477284
Chronic sinusitis	63.74	23.08	33	9186	12810	63466993
Iron deficiency anaemia	62.74	23.08	38	9181	19931	63459872
Candida infection	59.74	23.08	42	9177	28309	63451494
Pneumonia	58.84	23.08	172	9047	456595	63023208
Psychotic disorder	56.30	23.08	39	9180	25673	63454130
Sleep apnoea syndrome	54.16	23.08	40	9179	29093	63450710
Sputum purulent	48.96	23.08	14	9205	1073	63478730
Rectal prolapse	48.58	23.08	16	9203	1967	63477836
Pneumococcal infection	45.34	23.08	11	9208	444	63479359
Cholelithiasis	43.61	23.08	42	9177	43883	63435920
Bundle branch block left	40.47	23.08	20	9199	7039	63472764
Nicotine dependence	40.37	23.08	11	9208	706	63479097
Hepatotoxicity	39.79	23.08	37	9182	37004	63442799
Blood bilirubin increased	39.70	23.08	37	9182	37103	63442700
Upper-airway cough syndrome	39.17	23.08	23	9196	11395	63468408
Chorea	35.40	23.08	12	9207	1612	63478191
Fungal infection	34.25	23.08	34	9185	36840	63442963
Osteoarthritis	33.43	23.08	54	9165	95289	63384514
Secondary immunodeficiency	33.24	23.08	11	9208	1372	63478431
Impaired quality of life	32.76	23.08	22	9197	13761	63466042
Tooth injury	29.95	23.08	10	9209	1282	63478521
Swelling	29.29	23.08	3	9216	275375	63204428
Pain	29.24	23.08	39	9180	740589	62739214
Radioallergosorbent test positive	27.99	23.08	5	9214	42	63479761
Drug ineffective	27.93	23.08	70	9149	1044695	62435108
Gastroenteritis bacterial	26.96	23.08	7	9212	373	63479430
Pulmonary embolism	26.78	23.08	55	9164	116629	63363174
Respiratory gas exchange disorder	26.64	23.08	7	9212	391	63479412
Deep vein thrombosis	24.78	23.08	44	9175	83756	63396047
Rheumatoid arthritis	24.03	23.08	4	9215	253815	63225988
Pneumonia respiratory syncytial viral	23.84	23.08	8	9211	1042	63478761
Blood test abnormal	23.66	23.08	19	9200	15610	63464193
Alopecia	23.20	23.08	10	9209	337526	63142277

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	502.64	38.14	240	9219	42416	34905056
Obstructive airways disorder	446.55	38.14	165	9294	15329	34932143
Wheezing	433.63	38.14	215	9244	41187	34906285
Therapeutic product effect incomplete	404.31	38.14	219	9240	50322	34897150
Appendicolith	348.30	38.14	118	9341	8483	34938989
Full blood count abnormal	307.92	38.14	133	9326	18535	34928937
Appendicitis	285.86	38.14	118	9341	14689	34932783
Bronchial wall thickening	266.36	38.14	64	9395	1304	34946168
Cardiogenic shock	225.45	38.14	120	9339	26498	34920974
Pulmonary function test abnormal	216.35	38.14	62	9397	2548	34944924
Right atrial hypertrophy	211.31	38.14	48	9411	757	34946715
Stress	210.71	38.14	120	9339	30227	34917245
Right ventricular hypertrophy	180.56	38.14	48	9411	1486	34945986
Bronchial secretion retention	180.50	38.14	48	9411	1488	34945984
Loss of personal independence in daily activities	180.20	38.14	112	9347	33067	34914405
Ventricular fibrillation	165.29	38.14	93	9366	22861	34924611
Bronchiectasis	162.01	38.14	70	9389	9731	34937741
Ascites	161.39	38.14	119	9340	46452	34901020
Aortic valve stenosis	153.68	38.14	48	9411	2655	34944817
Obstruction	153.40	38.14	48	9411	2671	34944801
Abdominal distension	149.78	38.14	125	9334	58367	34889105
Blood phosphorus increased	143.72	38.14	60	9399	7661	34939811
Productive cough	131.81	38.14	97	9362	37716	34909756
Chest X-ray abnormal	127.08	38.14	47	9412	4351	34943121
Cough	123.63	38.14	176	9283	149964	34797508
Hyponatraemia	119.97	38.14	129	9330	82562	34864910
Sleep disorder due to a general medical condition	115.74	38.14	46	9413	5175	34942297
Diastolic dysfunction	114.57	38.14	48	9411	6179	34941293
Intervertebral disc degeneration	113.18	38.14	48	9411	6369	34941103
Multiple organ dysfunction syndrome	112.02	38.14	120	9339	76446	34871026
Dyspnoea	100.42	38.14	274	9185	376508	34570964
Iron deficiency	94.06	38.14	40	9419	5341	34942131
Osteoporosis	84.87	38.14	49	9410	12619	34934853
Sleep apnoea syndrome	84.29	38.14	58	9401	20263	34927209
Blood immunoglobulin E increased	83.95	38.14	30	9429	2516	34944956
Constipation	81.02	38.14	138	9321	136844	34810628
Hypoacusis	78.36	38.14	51	9408	16250	34931222
Blood test abnormal	78.07	38.14	38	9421	6933	34940539
Benign prostatic hyperplasia	76.24	38.14	48	9411	14447	34933025
General physical health deterioration	72.91	38.14	127	9332	128142	34819330
Bronchopulmonary aspergillosis allergic	72.21	38.14	21	9438	908	34946564
Pulmonary function test decreased	70.79	38.14	32	9427	4943	34942529
Dry mouth	70.00	38.14	61	9398	30104	34917368
Myasthenia gravis	69.32	38.14	35	9424	6905	34940567
Gout	68.39	38.14	50	9409	19203	34928269
Eosinophil count increased	67.86	38.14	37	9422	8535	34938937
Abdominal pain	67.10	38.14	141	9318	163477	34783995
Chronic obstructive pulmonary disease	65.07	38.14	73	9386	48845	34898627
Blood uric acid increased	63.86	38.14	37	9422	9587	34937885
Gastrooesophageal reflux disease	59.92	38.14	62	9397	37862	34909610
Inspiratory capacity abnormal	57.85	38.14	12	9447	120	34947352
Factor V Leiden mutation	55.12	38.14	11	9448	89	34947383
Pleural thickening	54.72	38.14	14	9445	371	34947101
Diaphragmatic disorder	53.54	38.14	18	9441	1257	34946215
Ocular discomfort	51.50	38.14	20	9439	2114	34945358
Sepsis	50.00	38.14	127	9332	166434	34781038
Asthma-chronic obstructive pulmonary disease overlap syndrome	45.60	38.14	16	9443	1271	34946201
Multiple allergies	44.90	38.14	20	9439	2983	34944489
Chest discomfort	44.79	38.14	64	9395	54466	34893006
Coagulation factor deficiency	44.47	38.14	10	9449	150	34947322
Drug therapy	43.57	38.14	15	9444	1126	34946346
Breath sounds abnormal	41.82	38.14	25	9434	6856	34940616
Vasculitis	41.61	38.14	30	9429	11266	34936206
Analgesic therapy	41.56	38.14	14	9445	984	34946488
Blood cholesterol increased	40.66	38.14	38	9421	20505	34926967

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
Wheezing	722.04	24.59	396	16921	116268	79610803
Obstructive airways disorder	709.51	24.59	264	17053	31195	79695876
Asthma	613.35	24.59	375	16942	134720	79592351
Full blood count abnormal	453.71	24.59	206	17111	40268	79686803
Therapeutic product effect incomplete	388.87	24.59	288	17029	141357	79585714
Appendicolith	370.00	24.59	117	17200	8434	79718637
Nasal polyps	315.95	24.59	100	17217	7227	79719844
Bronchiectasis	292.68	24.59	127	17190	22259	79704812
Appendicitis	268.68	24.59	117	17200	20677	79706394
Asthma-chronic obstructive pulmonary disease overlap syndrome	262.50	24.59	72	17245	3149	79723922
Cough	251.38	24.59	351	16966	366438	79360633
Bronchial wall thickening	224.36	24.59	61	17256	2580	79724491
Productive cough	222.95	24.59	171	17146	88160	79638911
Gastrooesophageal reflux disease	222.83	24.59	183	17134	104063	79623008
Pulmonary function test abnormal	218.50	24.59	66	17251	4078	79722993
Right atrial hypertrophy	212.56	24.59	46	17271	725	79726346
Diastolic dysfunction	208.35	24.59	81	17236	10730	79716341
Total lung capacity increased	204.22	24.59	55	17262	2243	79724828
Chronic obstructive pulmonary disease	197.43	24.59	157	17160	85262	79641809
Loss of personal independence in daily activities	196.36	24.59	169	17148	102411	79624660
Cardiogenic shock	196.36	24.59	119	17198	41795	79685276
Dyspnoea	188.20	24.59	505	16812	856520	78870551
Sleep disorder due to a general medical condition	183.31	24.59	80	17237	14197	79712874
Right ventricular hypertrophy	178.11	24.59	46	17271	1591	79725480
Osteoporosis	170.92	24.59	120	17197	53992	79673079
Sputum discoloured	159.83	24.59	83	17234	21660	79705411
Ventricular fibrillation	153.01	24.59	92	17225	31834	79695237
Ascites	151.71	24.59	128	17189	75434	79651637
Obstruction	146.62	24.59	50	17267	4560	79722511
Stress	141.90	24.59	126	17191	79486	79647585
Blood phosphorus increased	139.43	24.59	60	17257	10287	79716784
Sleep apnoea syndrome	139.28	24.59	91	17226	36387	79690684
Bronchial secretion retention	136.37	24.59	46	17271	4058	79723013
Dyspnoea exertional	136.04	24.59	128	17189	86945	79640126
Sarcoidosis	134.66	24.59	55	17262	8280	79718791
Rhinitis allergic	129.62	24.59	60	17257	12209	79714862
Respiratory symptom	129.40	24.59	46	17271	4745	79722326
Aortic valve stenosis	124.91	24.59	46	17271	5248	79721823
Abdominal distension	118.78	24.59	138	17179	119512	79607559
Salpingo-oophorectomy unilateral	113.35	24.59	28	17289	806	79726265
Cardiac murmur	106.61	24.59	57	17260	15767	79711304
Chest X-ray abnormal	103.88	24.59	45	17272	7838	79719233
Multiple organ dysfunction syndrome	101.89	24.59	128	17189	120118	79606953
Chest discomfort	101.49	24.59	137	17180	137907	79589164
Blood test abnormal	97.91	24.59	56	17261	17654	79709417
Sinusitis fungal	96.54	24.59	31	17286	2343	79724728
Benign prostatic hyperplasia	90.15	24.59	46	17271	11566	79715505
Sputum increased	86.87	24.59	34	17283	4579	79722492
Embolism venous	86.07	24.59	33	17284	4206	79722865
Hypomania	83.15	24.59	38	17279	7506	79719565
Intervertebral disc degeneration	79.54	24.59	47	17270	15738	79711333
Hiatus hernia	76.60	24.59	53	17264	23259	79703812
Iron deficiency	76.36	24.59	40	17277	10614	79716457
Female genital tract fistula	75.12	24.59	33	17284	5942	79721129
Lung neoplasm malignant	74.86	24.59	56	17261	27736	79699335
Hyponatraemia	71.59	24.59	134	17183	177714	79549357
Pulmonary function test decreased	70.39	24.59	34	17283	7603	79719468
Blood immunoglobulin E increased	69.17	24.59	31	17286	5851	79721220
Bronchopulmonary aspergillosis allergic	66.36	24.59	25	17292	3036	79724035
Jaundice cholestatic	65.93	24.59	37	17280	11247	79715824
Eczema	65.61	24.59	61	17256	40757	79686314
Oedema peripheral	65.51	24.59	159	17158	252129	79474942
Gout	64.73	24.59	49	17268	24700	79702371
Hypoacusis	64.45	24.59	53	17264	30097	79696974
Myasthenia gravis	63.22	24.59	35	17282	10364	79716707
Upper-airway cough syndrome	62.03	24.59	36	17281	11657	79715414
Blood uric acid increased	60.13	24.59	37	17280	13323	79713748
Eosinophil count increased	58.82	24.59	40	17277	17065	79710006
Hysterectomy	58.03	24.59	28	17289	6244	79720827
Schizophrenia	57.64	24.59	38	17279	15402	79711669
Inspiratory capacity abnormal	55.17	24.59	11	17306	113	79726958
Constipation	54.82	24.59	160	17157	282890	79444181
Emphysema	53.41	24.59	37	17280	16263	79710808
Toxicity to various agents	53.35	24.59	13	17304	421527	79305544
Diaphragmatic disorder	51.83	24.59	18	17299	1732	79725339
Venous pressure jugular increased	48.41	24.59	16	17301	1324	79725747
Kyphosis	47.75	24.59	19	17298	2672	79724399
Diverticulum	46.91	24.59	33	17284	14863	79712208
Drug interaction	46.66	24.59	16	17301	415167	79311904
Chronic sinusitis	46.07	24.59	31	17286	12995	79714076
Drug therapy	46.05	24.59	15	17302	1186	79725885
Drug ineffective	45.75	24.59	105	17212	1080808	78646263
Factor V Leiden mutation	45.00	24.59	10	17307	179	79726892
Tricuspid valve incompetence	44.97	24.59	36	17281	19676	79707395
Analgesic therapy	44.43	24.59	14	17303	995	79726076
Sputum purulent	44.34	24.59	15	17302	1334	79725737
Dry mouth	42.69	24.59	72	17245	87947	79639124
Asthenia	42.03	24.59	30	17287	511659	79215412
Rectal prolapse	40.82	24.59	16	17301	2162	79724909
Coagulation factor deficiency	40.72	24.59	9	17308	157	79726914
Sleep disorder therapy	40.12	24.59	13	17304	1011	79726060
Iron deficiency anaemia	38.63	24.59	37	17280	25635	79701436
Sepsis	37.40	24.59	136	17181	269292	79457779
Pain	36.99	24.59	60	17257	703742	79023329
Cardiac failure congestive	36.11	24.59	89	17228	142313	79584758
Arthralgia	35.76	24.59	43	17274	571760	79155311
Systolic dysfunction	35.29	24.59	17	17300	3778	79723293
Sinusitis	34.49	24.59	107	17210	195394	79531677
Neutropenia	34.24	24.59	10	17307	287700	79439371
Abdominal pain	33.45	24.59	170	17147	389399	79337672
General physical health deterioration	33.31	24.59	133	17184	275105	79451966
Nicotine dependence	32.89	24.59	11	17306	944	79726127
Pneumococcal infection	32.86	24.59	11	17306	947	79726124
Diarrhoea	31.46	24.59	93	17224	880396	78846675
Infusion related reaction	31.33	24.59	6	17311	230231	79496840
Seasonal allergy	31.26	24.59	27	17290	16379	79710692
Pulmonary vasculitis	31.20	24.59	10	17307	751	79726320
Coagulation factor V level abnormal	30.33	24.59	6	17311	59	79727012
Vasculitis	30.11	24.59	32	17285	25070	79702001
Breath sounds abnormal	29.84	24.59	26	17291	15958	79711113
Disease recurrence	29.69	24.59	42	17275	44067	79683004
Pleural thickening	29.68	24.59	14	17303	2968	79724103
Hyperphosphataemia	29.56	24.59	18	17299	6358	79720713
Bronchial hyperreactivity	29.43	24.59	14	17303	3026	79724045
Rheumatoid arthritis	29.30	24.59	5	17312	208465	79518606
Pyrexia	28.55	24.59	66	17251	678643	79048428
Candida infection	28.14	24.59	38	17279	38176	79688895
Multiple allergies	27.99	24.59	21	17296	10439	79716632
Musculoskeletal stiffness	27.42	24.59	3	17314	175005	79552066
Psychotic disorder	27.24	24.59	39	17278	41363	79685708
Thrombocytopenia	26.84	24.59	12	17305	265247	79461824
Radioallergosorbent test positive	26.09	24.59	5	17312	41	79727030
Chorea	26.08	24.59	12	17305	2405	79724666
Alopecia	25.81	24.59	9	17308	231346	79495725
Ocular discomfort	25.53	24.59	15	17302	4968	79722103
Restrictive pulmonary disease	25.27	24.59	12	17305	2583	79724488
Therapeutic product effect decreased	25.20	24.59	3	17314	163860	79563211
Drug abuse	24.96	24.59	3	17314	162688	79564383
Left ventricular hypertrophy	24.59	24.59	20	17297	11171	79715900

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
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
869185-19-3	SECONDARY_CAS_RN
4033108	VANDF
4033109	VANDF
CHEBI:79040	CHEBI
CHEMBL1187833	ChEMBL_ID
C573971	MESH_SUPPLEMENTAL_RECORD_UI
7354	IUPHAR_LIGAND_ID
DB09076	DRUGBANK_ID
GE2T1418SV	UNII
1487512	RXNORM
29953	MMSL
d08187	MMSL
015344	NDDF
015345	NDDF
706898002	SNOMEDCT_US
706899005	SNOMEDCT_US
715611006	SNOMEDCT_US
C3661274	UMLSCUI
CHEMBL523299	ChEMBL_ID
11519070	PUBCHEM_CID
9551	INN_ID

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
Anoro Ellipta	HUMAN PRESCRIPTION DRUG LABEL	2	0173-0869	POWDER	62.50 ug	RESPIRATORY (INHALATION)	NDA	27 sections
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	0173-0887	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
Trelegy Ellipta	HUMAN PRESCRIPTION DRUG LABEL	3	0173-0893	POWDER	62.50 ug	RESPIRATORY (INHALATION)	NDA	27 sections