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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:

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

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Approvals:

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

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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	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

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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
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

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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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
CHEBI has role	CHEBI:48876	muscarinic antagonists
FDA EPC	N0000175574	Anticholinergic
FDA MoA	N0000175370	Cholinergic Antagonists

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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
Chronic bronchitis	indication	63480004	DOID:6132
Pulmonary emphysema	indication	87433001
Asthma	indication	195967001	DOID:2841

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

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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
0.1MG/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
0.1MG/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
0.1MG/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
0.1MG/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
0.1MG/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
0.1MG/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
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

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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
0.1MG/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
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

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External reference:

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ID	Source
015344	NDDF
015345	NDDF
11519070	PUBCHEM_CID
1487512	RXNORM
29953	MMSL
4033108	VANDF
4033109	VANDF
706898002	SNOMEDCT_US
706899005	SNOMEDCT_US
715611006	SNOMEDCT_US

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Pharmaceutical products:

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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

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