Umeclidinium

Summary

Umeclidinium (CHEMBL1187833) is an approved small molecule targeting CHRM1, CHRM2, and CHRM3; indicated across 3 conditions including chronic obstructive pulmonary disease and asthma.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Small molecule
• Targets: 5 (CHRM1, CHRM2, CHRM3…)
• Indications: 3 conditions
• Clinical trials: 48
• Chemistry: 428.6 Da · C29H34NO2+

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1187833
Name	Umeclidinium
Type	Small molecule
Max phase	4
FDA approved	yes
PubChem CID	11519070
Molecular formula	C29H34NO2+
Molecular weight	428.6
InChIKey	FVTWTVQXNAJTQP-UHFFFAOYSA-N

SMILES: C1C[N+]2(CCC1(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)CCOCC5=CC=CC=C5

IUPAC name: diphenyl-[1-(2-phenylmethoxyethyl)-1-azoniabicyclo[2.2.2]octan-4-yl]methanol

Also known as: GSK-573719, GSK573719, Umeclidinium, Umeclidinium cation, Umeclidinium ion, UMECLIDINIUM, Umeclidinium (bromide), umeclidinium

Parent form; salt/anhydrous children: CHEMBL523299

Patent coverage: 427 distinct patent families (1,095 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
CHRM1	M1 receptor	Antagonist	9.8	0.2%	P11229
CHRM2	M2 receptor	Antagonist	9.82	0%	P08172
CHRM3	M3 receptor	Antagonist	10.22	0%	P20309
CHRM4	M4 receptor	Antagonist	10.3	1.6%	P08173
CHRM5	M5 receptor	Antagonist	9.9	0%	P08912

Broader ChEMBL bioactivity targets: 7 (assay-derived). Sample: Muscarinic acetylcholine receptor M2, Muscarinic acetylcholine receptor M1, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, Mu-type opioid receptor, Sodium-dependent dopamine transporter, 3’,5’-cyclic-AMP phosphodiesterase 4A.

Bioactivity

ChEMBL activities: 6 potent at pChembl ≥ 5 of 7 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
CHRM2	8.36	AC50	4.4	nM	CHEMBL_ACT_25196085
CHRM1	8.28	AC50	5.3	nM	CHEMBL_ACT_25210509
SLC6A4	6.52	AC50	301.7	nM	CHEMBL_ACT_25151676
SLC6A3	6.05	AC50	897.7	nM	CHEMBL_ACT_25125308
OPRM1	5.97	AC50	1073	nM	CHEMBL_ACT_25158524
SLC6A2	5.56	AC50	2727	nM	CHEMBL_ACT_25146349

Target pathways

Aggregated over 5 target gene(s): CHRM1, CHRM2, CHRM3, CHRM4, CHRM5.

Top Reactome pathways

17 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Signaling by GPCR	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Class A/1 (Rhodopsin-like receptors)	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Amine ligand-binding receptors	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
GPCR downstream signalling	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Muscarinic acetylcholine receptors	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
GPCR ligand binding	5	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
G alpha (q) signalling events	3	CHRM1, CHRM3, CHRM5
G alpha (i) signalling events	2	CHRM2, CHRM4
Metabolism	1	CHRM3
Integration of energy metabolism	1	CHRM3
Membrane Trafficking	1	CHRM2
Acetylcholine regulates insulin secretion	1	CHRM3
Regulation of insulin secretion	1	CHRM3
Vesicle-mediated transport	1	CHRM2
Cargo recognition for clathrin-mediated endocytosis	1	CHRM2
Clathrin-mediated endocytosis	1	CHRM2

Dominant GO biological processes

GO term	Targets
signal transduction	5
G protein-coupled receptor signaling pathway	5
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5
adenylate cyclase-inhibiting G protein-coupled acetylcholine receptor signaling pathway	5
G protein-coupled acetylcholine receptor signaling pathway	5
chemical synaptic transmission	5
phospholipase C-activating G protein-coupled acetylcholine receptor signaling pathway	3
nervous system development	3
acetylcholine receptor signaling pathway	3
regulation of locomotion	2
saliva secretion	2
regulation of smooth muscle contraction	2
phospholipase C-activating G protein-coupled receptor signaling pathway	1
neuromuscular synaptic transmission	1
positive regulation of monoatomic ion transport	1

Indications & clinical

Indications

3 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
chronic obstructive pulmonary disease	3	MONDO:0005002	EFO:0000341
asthma	2	MONDO:0004979	MONDO:0004979

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 48.

Phase distribution

Phase	Trials
PHASE3	19
PHASE2	9
PHASE1	9
PHASE4	8
Not specified	3

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06571942	PHASE4	RECRUITING	Effect of the Inhaled Triple Therapies Over the Small Airway in Biomass Exposure
NCT07133880	PHASE4	RECRUITING	Compare the Effects of Nebulizer Versus Inhaler Based Therapy for COPD Using Long-acting Bronchodilators
NCT02236611	PHASE4	COMPLETED	A 12-week Study to Evaluate the Efficacy and Safety of Umeclidinium 62.5 Microgram (mcg) Compared With Glycopyrronium 44 mcg in Subjects With Chronic Obstructive Pulmonary Disease (COPD)
NCT03611699	PHASE4	COMPLETED	Static Lung Hyperinflation and Sympathetic Nerve Activity-Associated Large Artery Stiffness in COPD Patients
NCT03949842	PHASE4	WITHDRAWN	Legend: TRELEGY Real World Chronic Obstructive Pulmonary Disease (COPD) Effectiveness Study
NCT04522596	PHASE4	UNKNOWN	Effect of Dual Bronchodilation With Umeclidinium/Vilanterol on Patients With COPD, Hyperinflation and Heart Failure
NCT05342558	PHASE4	COMPLETED	Efficacy and Safety of ICS/LABA vs. LAMA/LABA in Patients With Different COPD Phenotypes.
NCT06905483	PHASE4	COMPLETED	Comparative Effects of Triple Inhaled Therapy With Budesonide/Glycopyrronium/Formoterol Versus Fluticasone Furoate/Umeclidinium/Vilanterol on Small Airway Disease in COPD Patients: A Randomized Crossover Study
NCT01313637	PHASE3	COMPLETED	A 24-week Evaluation of GSK573719/Vilanterol (125/25mcg) and Components in COPD
NCT01316900	PHASE3	COMPLETED	24-week Trial Comparing GSK573719/GW642444 With GW642444 and With Tiotropium in Chronic Obstructive Pulmonary Disease
NCT01316913	PHASE3	COMPLETED	24-week Trial Comparing GSK573719/GW642444 With GSK573719 and With Tiotropium in Chronic Obstructive Pulmonary Disease
NCT01323660	PHASE3	COMPLETED	An Exercise Endurance Study to Evaluate the Effects of Treatment of Chronic Obstructive Pulmonary Disease (COPD) Patients With a Dual Bronchodilator: GSK573719/GW642444.Study B
NCT01328444	PHASE3	COMPLETED	An Exercise Endurance Study to Evaluate the Effects of Treatment of Chronic Obstructive Pulmonary Disease (COPD) Patients With a Dual Bronchodilator: GSK573719/GW642444. Study A
NCT01376388	PHASE3	COMPLETED	Long-term Safety Study for GSK573719/GW642444 in Japanese
NCT01387230	PHASE3	COMPLETED	Evaluate the Efficacy and Safety of GSK573719 Delivered Via a Novel Dry Powder Inhaler in Subjects With COPD
NCT01636713	PHASE3	COMPLETED	A 24-week Study to Evaluate the Efficacy and Safety of GSK573719/GW642444 125/25 mcg and 62.5/25mcg Inhalation Powder Compared With Placebo in Subjects With COPD
NCT01702363	PHASE3	COMPLETED	Long-term Safety Study for GSK573719 in Japanese
NCT01716520	PHASE3	COMPLETED	Cross-Over Study in Subjects With COPD, Evaluating Lung Function Response After Treatment With Once Daily Umeclidinium 62.5mcg, Vilanterol 25mcg, and Umeclidinium/Vilanterol 62.5/25mcg
NCT01777334	PHASE3	COMPLETED	The Purpose of This Study is to Evaluate the Spirometric Effect (Trough FEV1) of Umeclidinium/Vilanterol 62.5/25 mcg Once Daily Compared With Tiotriopium 18 mcg Once Daily Over a 24-week Treatment Period in Subjects With COPD
NCT01817764	PHASE3	COMPLETED	A Study to Compare the Efficacy and Safety of Umeclidinium/Vilanterol and Fluticasone Propionate/Salmeterol in Subjects With Chronic Obstructive Pulmonary Disease (COPD)
NCT01899742	PHASE3	COMPLETED	The Purpose of the This Study is to Evaluate the Spirometric Effect (Trough FEV1) of Umeclidinium/Vilanterol 62.5/25 mcg Once Daily Compared With Tiotropium 18mcg Once Daily Over a a 12-week Treatment Period in Subjects With COPD Who Continue to Have Symptoms on Tiotropium
NCT02014480	PHASE3	COMPLETED	A Cross-Over Study to Evaluate Lung Function Response After Treatment With Umeclidinium (UMEC) 62.5 Micrograms (mcg), Vilanterol (VI) 25 mcg, and Umeclidinium/Vilanterol (UMEC/VI) 62.5/25 mcg Once-Daily in Subjects With Chronic Obstructive Pulmonary Disease (COPD)
NCT02207829	PHASE3	COMPLETED	A 12-week Study to Evaluate the Efficacy and Safety of Umeclidinium Compared With Tiotropium in Subjects With Chronic Obstructive Pulmonary Disease
NCT02487446	PHASE3	COMPLETED	Efficacy and Safety Study of QVA149 in COPD Patients
NCT02487498	PHASE3	COMPLETED	Efficacy and Safety Study of Indacaterol Maleate/Glycopyrronium Bromide in Chronic Obstructive Pulmonary Disease (COPD) Patients.
NCT02731846	PHASE3	WITHDRAWN	A Study Comparing the Closed Triple Therapy, Open Triple Therapy and a Dual Therapy for Effect on Lung Function in Subjects With Chronic Obstructive Pulmonary Disease (COPD)
NCT03162055	PHASE3	COMPLETED	Efficacy and Safety of Glycopyrronium/Formoterol Fumarate Fixed-dose Combination Relative to Umeclidinium/Vilanterol Fixed-dose Combination Over 24 Weeks in Patients With Moderate to Very Severe Chronic Obstructive Pulmonary Disease
NCT07282886	PHASE2	RECRUITING	VENTURI (VENTilation Using Respiratory Imaging)
NCT00515502	PHASE2	COMPLETED	Safety Study Using GSK573719 And Tiotropium In Patients With Chronic Obstructive Pulmonary Disease
NCT00732472	PHASE2	COMPLETED	A Study to Assess the Safety and Tolerability of Once Daily Inhaled Doses of GSK573719 Made With Magnesium Stearate in Subjects With Chronic Obstructive Pulmonary Disease(COPD)for 7 Days
NCT01030965	PHASE2	COMPLETED	28-day Repeat Dose Study of GSK573719
NCT01372410	PHASE2	COMPLETED	A Randomized, Double Blind, Placebo Controlled, Incomplete Block, Crossover, Dose Ranging Study to Evaluate the Dose Response of GSK573719 Administered Once or Twice Daily Over 7 Days in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT01653483	PHASE2	WITHDRAWN	Aura Adolescent PK Study GSK2829332
NCT02563899	PHASE2	COMPLETED	Pharmacokinetic, Safety, Tolerability, and Clinical Effect of Topical Umeclidinium in Primary Axillary Hyperhidrosis
NCT02570165	PHASE2	COMPLETED	Dose-Finding Study of Batefenterol (GSK961081) Via Dry Powder Inhaler in Patients With Chronic Obstructive Pulmonary Disease (COPD)
NCT02673619	PHASE2	COMPLETED	A Study to Evaluate Clinical Effect, Pharmacokinetics , Safety, and Tolerability of Umeclidinium in Palmar Hyperhidrosis Subjects
NCT00475436	PHASE1	COMPLETED	A Single Centre Randomized Study Evaluating The Safety And Tolerability Of GSK573719 In Healthy Volunteers
NCT00976144	PHASE1	COMPLETED	Safety, Tolerability, Pharmacokinetic and Pharmacodynamic Effects of GSK573719 (LAMA) and GW642444 (LABA)Administered Individually and Concurrently in Healthy Japanese Subjects
NCT01013974	PHASE1	COMPLETED	A Study of GSK573719 in Healthy Japanese Male Subjects
NCT01110018	PHASE1	COMPLETED	GSK573719 IV Enabling Study

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No CPIC/DPWG dosing guideline or drug-level clinical/variant annotations in PharmGKB for this molecule.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

575 molecules share ≥1 primary target. Top 60 by shared-target count:

Molecule	Source	Status	Shared targets
ACLIDINIUM BROMIDE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CLOZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
GENTIAN VIOLET	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
Mavorixafor	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
OLANZAPINE	ChEMBL + PubChem	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ACETYLCHOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
AMIODARONE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
AMITRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
AMOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ATROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
BENZTROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
BETHANECHOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CARBACHOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CARBAMOYLCHOLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CHLOROQUINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CHLORPROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CINNARIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CLEMASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CLIDINIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CLOMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CYCLIZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
CYPROHEPTADINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DARIFENACIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DESLORATADINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DEXCHLORPHENIRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DICYCLOMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DIMENHYDRINATE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DIPHENHYDRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DIPHENIDOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
DOXEPIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
EBASTINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
GLYCOPYRRONIUM BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
HALOPERIDOL	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
HOMATROPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
HYDROXYCHLOROQUINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
IMIPRAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
IPRATROPIUM	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
KETOTIFEN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
LOXAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
MAPROTILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
MEPAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
METHSCOPOLAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
METHSCOPOLAMINE BROMIDE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
MIANSERIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
NORTRIPTYLINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
ORPHENADRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
OXYBUTYNIN	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PAROXETINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PERHEXILINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PILOCARPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PIRENZEPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PROCHLORPERAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PROMAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
PROMETHAZINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
QUETIAPINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
QUINACRINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
RISPERIDONE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
SCOPOLAMINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5
SERTRALINE	ChEMBL	Phase 4 (approved)	CHRM1, CHRM2, CHRM3, CHRM4, CHRM5