Identification

Name
Umeclidinium
Accession Number
DB09076
Type
Small Molecule
Groups
Approved
Description

Umeclidinium is a long-acting muscarinic antagonist (LAMA) used as maintenance treatment for symptoms of chronic obstructive pulmonary disease (COPD). It is available as a once-daily inhalation monotherapy or as a fixed-dose combination product with the long-acting beta2-agonist vilanterol. COPD is a progressive obstructive lung disease characterized by shortness of breath, cough, sputum production, and chronically poor airflow with a forced expiratory volume in 1 second (FEV1) of less than 80%. By blocking the M3 muscarinic receptor which is highly expressed in airway smooth muscle of the lungs, umeclidinium inhibits the binding of acetylcholine and thereby opens up the airways by preventing bronchoconstriction. Its use has been shown to provide clinically significant, sustained improvements in lung function.

Structure
Thumb
Synonyms
  • 1-[2-(benzyloxy)ethyl]-4-[hydroxy(diphenyl)methyl]-1-azoniabicyclo[2.2.2]octane
External IDs
GSK-573719 / GSK573719 / GSK573719A
Product Ingredients
IngredientUNIICASInChI Key
Umeclidinium bromide7AN603V4JV869113-09-7PEJHHXHHNGORMP-UHFFFAOYSA-M
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
IncrusePowder, metered55 μgRespiratory (inhalation)Glaxo Group Limited2014-04-28Not applicableEu
IncrusePowder, metered55 μgRespiratory (inhalation)Glaxo Group Limited2014-04-28Not applicableEu
IncrusePowder, metered55 μgRespiratory (inhalation)Glaxo Group Limited2014-04-28Not applicableEu
Incruse ElliptaPowder62.5 mcgRespiratory (inhalation)Glaxosmithkline Inc2015-04-27Not applicableCanada
Incruse ElliptaAerosol, powder62.5 ug/1OralGlaxosmithkline Inc2014-04-30Not applicableUs
Mixture Products
NameIngredientsDosageRouteLabellerMarketing StartMarketing End
AnoroUmeclidinium bromide (55 micrograms) + Vilanterol Trifenatate (22 micrograms)Powder, meteredRespiratory (inhalation)Glaxo Group Limited2014-05-08Not applicableEu
AnoroUmeclidinium bromide (55 micrograms) + Vilanterol Trifenatate (22 micrograms)Powder, meteredRespiratory (inhalation)Glaxo Group Limited2014-05-08Not applicableEu
AnoroUmeclidinium bromide (55 micrograms) + Vilanterol Trifenatate (22 micrograms)Powder, meteredRespiratory (inhalation)Glaxo Group Limited2014-05-08Not applicableEu
Anoro ElliptaUmeclidinium (62.5 mcg) + Vilanterol (25 mcg)PowderRespiratory (inhalation)Glaxosmithkline Inc2014-03-14Not applicableCanada
Anoro ElliptaUmeclidinium bromide (62.5 ug/1) + Vilanterol Trifenatate (25 ug/1)PowderRespiratory (inhalation)Glaxosmithkline Inc2014-01-31Not applicableUs
Trelegy ElliptaUmeclidinium bromide (62.5 ug/1) + Fluticasone furoate (100 ug/1) + Vilanterol Trifenatate (25 ug/1)PowderRespiratory (inhalation)Glaxosmithkline Inc2017-09-18Not applicableUs
Categories
UNII
GE2T1418SV
CAS number
869185-19-3
Weight
Average: 428.595
Monoisotopic: 428.258405759
Chemical Formula
C29H34NO2
InChI Key
FVTWTVQXNAJTQP-UHFFFAOYSA-N
InChI
InChI=1S/C29H34NO2/c31-29(26-12-6-2-7-13-26,27-14-8-3-9-15-27)28-16-19-30(20-17-28,21-18-28)22-23-32-24-25-10-4-1-5-11-25/h1-15,31H,16-24H2/q+1
IUPAC Name
1-[2-(benzyloxy)ethyl]-4-(hydroxydiphenylmethyl)-1-azabicyclo[2.2.2]octan-1-ium
SMILES
OC(C1=CC=CC=C1)(C1=CC=CC=C1)C12CC[N+](CCOCC3=CC=CC=C3)(CC1)CC2

Pharmacology

Indication

Indicated for the long-term, once-daily, maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD).

Structured Indications
Pharmacodynamics
Not Available
Mechanism of action

Umeclidinium is a long-acting, antimuscarinic agent, which is often referred to as an anticholinergic. It has similar affinity to the subtypes of muscarinic receptors M1 to M5. In the airways, it exhibits pharmacological effects through the inhibition of M3 receptor at the smooth muscle leading to bronchodilation.

TargetActionsOrganism
NMuscarinic acetylcholine receptor M1
antagonist
Human
AMuscarinic acetylcholine receptor M2
antagonist
Human
AMuscarinic acetylcholine receptor M3
antagonist
Human
NMuscarinic acetylcholine receptor M4
antagonist
Human
NMuscarinic acetylcholine receptor M5
antagonist
Human
Absorption

Cmax occurred at 5 to 15 minutes, with steady state concentrations arriving in 14 days with 1.8-fold accumulation.

Volume of distribution

Mean volume of distribution was 86 L.

Protein binding

89%

Metabolism

In vitro data showed that umeclidinium is primarily metabolized by the enzyme cytochrome P450 2D6 (CYP2D6) and is a substrate for the P-glycoprotein (P-gp) transporter. The primary metabolic routes for umeclidinium are oxidative (hydroxylation, Odealkylation) followed by conjugation (e.g., glucuronidation), resulting in a range of metabolites with either reduced pharmacological activity or for which the pharmacological activity has not been established. Systemic exposure to the metabolites is low.

Route of elimination

Following intravenous dosing with radiolabeled umeclidinium, mass balance showed 58% of the radiolabel in the feces and 22% in the urine.

Half life

The effective half-life after once daily dosing is 11 hours.

Clearance
Not Available
Toxicity

In clinical trials, the most common adverse effects of umeclidinium were nasopharyngitis, upper respiratory tract infection, cough, and arthralgia. Atrial fibrillation occurred in <1% of patients, but was more common among patients treated with umeclidinium than in those treated with placebo. Anticholinergics like umeclidinium should be used with caution in patients with narrow-angle glaucoma and in those with prostatic hyperplasia or bladder-neck obstruction. Inhaled medications can cause paradoxical bronchospasm, which can be fatal.

Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
AbirateroneThe serum concentration of Umeclidinium can be increased when it is combined with Abiraterone.Approved
AcetaminophenThe serum concentration of Umeclidinium can be increased when it is combined with Acetaminophen.Approved
AclidiniumUmeclidinium may increase the anticholinergic activities of Aclidinium.Approved
AfatinibThe serum concentration of Umeclidinium can be increased when it is combined with Afatinib.Approved
AlbendazoleThe serum concentration of Umeclidinium can be increased when it is combined with Albendazole.Approved, Vet Approved
AlcuroniumUmeclidinium may increase the anticholinergic activities of Alcuronium.Experimental
AldosteroneThe serum concentration of Umeclidinium can be decreased when it is combined with Aldosterone.Experimental, Investigational
AlectinibThe serum concentration of Umeclidinium can be increased when it is combined with Alectinib.Approved
AlfentanilThe serum concentration of Umeclidinium can be increased when it is combined with Alfentanil.Approved, Illicit
AmantadineThe serum concentration of Umeclidinium can be increased when it is combined with Amantadine.Approved
Aminohippuric acidThe serum concentration of Umeclidinium can be increased when it is combined with Aminohippuric acid.Approved, Investigational
AmiodaroneThe metabolism of Umeclidinium can be decreased when combined with Amiodarone.Approved, Investigational
AmitriptylineThe serum concentration of Umeclidinium can be increased when it is combined with Amitriptyline.Approved
AmlodipineThe serum concentration of Umeclidinium can be increased when it is combined with Amlodipine.Approved
AmprenavirThe serum concentration of Umeclidinium can be decreased when it is combined with Amprenavir.Approved
AmsacrineThe serum concentration of Umeclidinium can be increased when it is combined with Amsacrine.Approved
Anisotropine MethylbromideUmeclidinium may increase the anticholinergic activities of Anisotropine Methylbromide.Approved
ArtemetherThe metabolism of Umeclidinium can be decreased when combined with Artemether.Approved
AstemizoleThe serum concentration of Umeclidinium can be increased when it is combined with Astemizole.Approved, Withdrawn
AtazanavirThe serum concentration of Umeclidinium can be increased when it is combined with Atazanavir.Approved, Investigational
AtenololThe serum concentration of Umeclidinium can be increased when it is combined with Atenolol.Approved
AtomoxetineThe metabolism of Umeclidinium can be decreased when combined with Atomoxetine.Approved
AtorvastatinThe serum concentration of Umeclidinium can be increased when it is combined with Atorvastatin.Approved
AtracuriumUmeclidinium may increase the anticholinergic activities of Atracurium.Experimental, Investigational
Atracurium besylateUmeclidinium may increase the anticholinergic activities of Atracurium besylate.Approved
AtropineUmeclidinium may increase the anticholinergic activities of Atropine.Approved, Vet Approved
AzelastineThe serum concentration of Umeclidinium can be increased when it is combined with Azelastine.Approved
AzithromycinThe serum concentration of Umeclidinium can be increased when it is combined with Azithromycin.Approved
BenactyzineUmeclidinium may increase the anticholinergic activities of Benactyzine.Withdrawn
BenzatropineUmeclidinium may increase the anticholinergic activities of Benzatropine.Approved
BenzocaineThe serum concentration of Umeclidinium can be increased when it is combined with Benzocaine.Approved
BepridilThe serum concentration of Umeclidinium can be increased when it is combined with Bepridil.Approved, Withdrawn
BetaxololThe metabolism of Umeclidinium can be decreased when combined with Betaxolol.Approved
BiperidenUmeclidinium may increase the anticholinergic activities of Biperiden.Approved, Investigational
BoceprevirThe serum concentration of Umeclidinium can be increased when it is combined with Boceprevir.Approved, Withdrawn
BornaprineUmeclidinium may increase the anticholinergic activities of Bornaprine.Experimental
BosutinibThe serum concentration of Umeclidinium can be increased when it is combined with Bosutinib.Approved
BromocriptineThe serum concentration of Umeclidinium can be increased when it is combined with Bromocriptine.Approved, Investigational
BuprenorphineThe serum concentration of Umeclidinium can be increased when it is combined with Buprenorphine.Approved, Illicit, Investigational, Vet Approved
BupropionThe metabolism of Umeclidinium can be decreased when combined with Bupropion.Approved
BuspironeThe serum concentration of Umeclidinium can be increased when it is combined with Buspirone.Approved, Investigational
CabazitaxelThe serum concentration of Umeclidinium can be increased when it is combined with Cabazitaxel.Approved
CaffeineThe serum concentration of Umeclidinium can be increased when it is combined with Caffeine.Approved
CanagliflozinThe serum concentration of Umeclidinium can be increased when it is combined with Canagliflozin.Approved
Candesartan cilexetilThe serum concentration of Umeclidinium can be increased when it is combined with Candesartan.Approved
CaptoprilThe serum concentration of Umeclidinium can be increased when it is combined with Captopril.Approved
CarbamazepineThe serum concentration of Umeclidinium can be decreased when it is combined with Carbamazepine.Approved, Investigational
CarvedilolThe serum concentration of Umeclidinium can be increased when it is combined with Carvedilol.Approved, Investigational
CaspofunginThe serum concentration of Umeclidinium can be increased when it is combined with Caspofungin.Approved
CelecoxibThe metabolism of Umeclidinium can be decreased when combined with Celecoxib.Approved, Investigational
ChloroquineThe serum concentration of Umeclidinium can be increased when it is combined with Chloroquine.Approved, Vet Approved
ChlorphenoxamineUmeclidinium may increase the anticholinergic activities of Chlorphenoxamine.Withdrawn
ChlorpromazineThe serum concentration of Umeclidinium can be increased when it is combined with Chlorpromazine.Approved, Vet Approved
ChlorpropamideThe serum concentration of Umeclidinium can be increased when it is combined with Chlorpropamide.Approved
ChlorprothixeneThe serum concentration of Umeclidinium can be increased when it is combined with Chlorprothixene.Approved, Investigational, Withdrawn
CholecalciferolThe metabolism of Umeclidinium can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CholesterolThe serum concentration of Umeclidinium can be increased when it is combined with Cholesterol.Experimental, Investigational
Cholic AcidThe serum concentration of Umeclidinium can be decreased when it is combined with Cholic Acid.Approved
CilazaprilThe serum concentration of Umeclidinium can be increased when it is combined with Cilazapril.Approved
CimetidineThe serum concentration of Umeclidinium can be decreased when it is combined with Cimetidine.Approved
CinacalcetThe metabolism of Umeclidinium can be decreased when combined with Cinacalcet.Approved
CiprofloxacinThe serum concentration of Umeclidinium can be increased when it is combined with Ciprofloxacin.Approved, Investigational
CitalopramThe serum concentration of Umeclidinium can be increased when it is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Umeclidinium can be increased when it is combined with Clarithromycin.Approved
ClemastineThe metabolism of Umeclidinium can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Umeclidinium can be decreased when combined with Clobazam.Approved, Illicit
ClofazimineThe serum concentration of Umeclidinium can be increased when it is combined with Clofazimine.Approved, Investigational
ClomipramineThe serum concentration of Umeclidinium can be increased when it is combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe serum concentration of Umeclidinium can be decreased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineThe metabolism of Umeclidinium can be decreased when combined with Clozapine.Approved
CobicistatThe serum concentration of Umeclidinium can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Umeclidinium can be decreased when combined with Cocaine.Approved, Illicit
ColchicineThe serum concentration of Umeclidinium can be increased when it is combined with Colchicine.Approved
ColforsinThe serum concentration of Umeclidinium can be increased when it is combined with Colforsin.Experimental, Investigational
CrizotinibThe serum concentration of Umeclidinium can be increased when it is combined with Crizotinib.Approved
CyclopentolateUmeclidinium may increase the anticholinergic activities of Cyclopentolate.Approved
CyclophosphamideThe serum concentration of Umeclidinium can be increased when it is combined with Cyclophosphamide.Approved, Investigational
CyclosporineThe serum concentration of Umeclidinium can be decreased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
DaclatasvirThe serum concentration of Umeclidinium can be increased when it is combined with Daclatasvir.Approved
DactinomycinThe serum concentration of Umeclidinium can be increased when it is combined with Dactinomycin.Approved
DarifenacinUmeclidinium may increase the anticholinergic activities of Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Umeclidinium can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Umeclidinium can be increased when it is combined with Dasatinib.Approved, Investigational
DaunorubicinThe serum concentration of Umeclidinium can be decreased when it is combined with Daunorubicin.Approved
DelavirdineThe metabolism of Umeclidinium can be decreased when combined with Delavirdine.Approved
DesipramineThe serum concentration of Umeclidinium can be increased when it is combined with Desipramine.Approved
DesloratadineUmeclidinium may increase the anticholinergic activities of Desloratadine.Approved, Investigational
DexamethasoneThe serum concentration of Umeclidinium can be decreased when it is combined with Dexamethasone.Approved, Investigational, Vet Approved
DexetimideUmeclidinium may increase the anticholinergic activities of Dexetimide.Withdrawn
DextromethorphanThe serum concentration of Umeclidinium can be increased when it is combined with Dextromethorphan.Approved
DiclofenacThe serum concentration of Umeclidinium can be increased when it is combined with Diclofenac.Approved, Vet Approved
DicyclomineUmeclidinium may increase the anticholinergic activities of Dicyclomine.Approved
DigoxinThe serum concentration of Umeclidinium can be decreased when it is combined with Digoxin.Approved
DihydroergotamineThe serum concentration of Umeclidinium can be increased when it is combined with Dihydroergotamine.Approved
DiltiazemThe serum concentration of Umeclidinium can be increased when it is combined with Diltiazem.Approved
DiphenhydramineThe metabolism of Umeclidinium can be decreased when combined with Diphenhydramine.Approved
DipyridamoleThe serum concentration of Umeclidinium can be increased when it is combined with Dipyridamole.Approved
DosulepinThe metabolism of Umeclidinium can be decreased when combined with Dosulepin.Approved
DoxazosinThe serum concentration of Umeclidinium can be increased when it is combined with Doxazosin.Approved
DoxepinThe serum concentration of Umeclidinium can be increased when it is combined with Doxepin.Approved
DoxorubicinThe serum concentration of Umeclidinium can be decreased when it is combined with Doxorubicin.Approved, Investigational
DronabinolThe serum concentration of Umeclidinium can be increased when it is combined with Dronabinol.Approved, Illicit
DronedaroneThe serum concentration of Umeclidinium can be increased when it is combined with Dronedarone.Approved
DuloxetineThe metabolism of Umeclidinium can be decreased when combined with Duloxetine.Approved
ElbasvirThe serum concentration of Umeclidinium can be increased when it is combined with Elbasvir.Approved
EliglustatThe metabolism of Umeclidinium can be decreased when combined with Eliglustat.Approved
EmeproniumUmeclidinium may increase the anticholinergic activities of Emepronium.Experimental
EnalaprilThe serum concentration of Umeclidinium can be increased when it is combined with Enalapril.Approved, Vet Approved
EnasidenibThe serum concentration of Umeclidinium can be increased when it is combined with Enasidenib.Approved
EnzalutamideThe serum concentration of Umeclidinium can be increased when it is combined with Enzalutamide.Approved
ErgonovineThe serum concentration of Umeclidinium can be increased when it is combined with Ergonovine.Approved
ErgotamineThe serum concentration of Umeclidinium can be increased when it is combined with Ergotamine.Approved
ErythromycinThe serum concentration of Umeclidinium can be decreased when it is combined with Erythromycin.Approved, Vet Approved
EstramustineThe serum concentration of Umeclidinium can be increased when it is combined with Estramustine.Approved
EstriolThe serum concentration of Umeclidinium can be decreased when it is combined with Estriol.Approved, Investigational, Vet Approved
EstroneThe serum concentration of Umeclidinium can be decreased when it is combined with Estrone.Approved
EtanautineUmeclidinium may increase the anticholinergic activities of Etanautine.Experimental
EthopropazineUmeclidinium may increase the anticholinergic activities of Ethopropazine.Approved
EtoposideThe serum concentration of Umeclidinium can be increased when it is combined with Etoposide.Approved
EtravirineThe serum concentration of Umeclidinium can be increased when it is combined with Etravirine.Approved
EtybenzatropineUmeclidinium may increase the anticholinergic activities of Etybenzatropine.Experimental
FelodipineThe serum concentration of Umeclidinium can be increased when it is combined with Felodipine.Approved, Investigational
FentanylThe serum concentration of Umeclidinium can be increased when it is combined with Fentanyl.Approved, Illicit, Investigational, Vet Approved
FesoterodineUmeclidinium may increase the anticholinergic activities of Fesoterodine.Approved
FexofenadineThe serum concentration of Umeclidinium can be increased when it is combined with Fexofenadine.Approved
FidaxomicinThe serum concentration of Umeclidinium can be increased when it is combined with Fidaxomicin.Approved
FluconazoleThe serum concentration of Umeclidinium can be increased when it is combined with Fluconazole.Approved
FluoxetineThe metabolism of Umeclidinium can be decreased when combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe serum concentration of Umeclidinium can be increased when it is combined with Flupentixol.Approved, Withdrawn
FluphenazineThe serum concentration of Umeclidinium can be increased when it is combined with Fluphenazine.Approved
FlurazepamThe serum concentration of Umeclidinium can be increased when it is combined with Flurazepam.Approved, Illicit
FluvoxamineThe serum concentration of Umeclidinium can be increased when it is combined with Fluvoxamine.Approved, Investigational
GallamineUmeclidinium may increase the anticholinergic activities of Gallamine.Experimental
Gallamine TriethiodideUmeclidinium may increase the anticholinergic activities of Gallamine Triethiodide.Approved
GefitinibThe serum concentration of Umeclidinium can be increased when it is combined with Gefitinib.Approved, Investigational
GenisteinThe serum concentration of Umeclidinium can be increased when it is combined with Genistein.Investigational
GlecaprevirThe serum concentration of Umeclidinium can be increased when it is combined with Glecaprevir.Approved
GlyburideThe serum concentration of Umeclidinium can be increased when it is combined with Glyburide.Approved
GlycerinThe serum concentration of Umeclidinium can be increased when it is combined with Glycerin.Approved, Investigational
GlycopyrroniumUmeclidinium may increase the anticholinergic activities of Glycopyrronium.Approved, Investigational, Vet Approved
Gramicidin DThe serum concentration of Umeclidinium can be increased when it is combined with Gramicidin D.Approved
GrepafloxacinThe serum concentration of Umeclidinium can be increased when it is combined with Grepafloxacin.Investigational, Withdrawn
HaloperidolThe serum concentration of Umeclidinium can be increased when it is combined with Haloperidol.Approved
HexamethoniumUmeclidinium may increase the anticholinergic activities of Hexamethonium.Experimental
HomatropineUmeclidinium may increase the anticholinergic activities of Homatropine.Approved
HydrocortisoneThe serum concentration of Umeclidinium can be increased when it is combined with Hydrocortisone.Approved, Vet Approved
HyoscyamineUmeclidinium may increase the anticholinergic activities of Hyoscyamine.Approved
IdelalisibThe serum concentration of Umeclidinium can be increased when it is combined with Idelalisib.Approved
ImatinibThe serum concentration of Umeclidinium can be increased when it is combined with Imatinib.Approved
ImipramineThe serum concentration of Umeclidinium can be increased when it is combined with Imipramine.Approved
IndinavirThe serum concentration of Umeclidinium can be decreased when it is combined with Indinavir.Approved
IndomethacinThe serum concentration of Umeclidinium can be increased when it is combined with Indomethacin.Approved, Investigational
Ipratropium bromideUmeclidinium may increase the anticholinergic activities of Ipratropium bromide.Approved
IsavuconazoniumThe serum concentration of Umeclidinium can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsoniazidThe metabolism of Umeclidinium can be decreased when combined with Isoniazid.Approved
ItraconazoleThe serum concentration of Umeclidinium can be increased when it is combined with Itraconazole.Approved, Investigational
IvacaftorThe serum concentration of Umeclidinium can be increased when it is combined with Ivacaftor.Approved
IvermectinThe serum concentration of Umeclidinium can be increased when it is combined with Ivermectin.Approved, Vet Approved
KetamineThe serum concentration of Umeclidinium can be increased when it is combined with Ketamine.Approved, Vet Approved
KetoconazoleThe serum concentration of Umeclidinium can be increased when it is combined with Ketoconazole.Approved, Investigational
LansoprazoleThe serum concentration of Umeclidinium can be increased when it is combined with Lansoprazole.Approved, Investigational
LapatinibThe serum concentration of Umeclidinium can be increased when it is combined with Lapatinib.Approved, Investigational
LevofloxacinThe serum concentration of Umeclidinium can be increased when it is combined with Levofloxacin.Approved, Investigational
LevothyroxineThe serum concentration of Umeclidinium can be decreased when it is combined with Levothyroxine.Approved
LidocaineThe serum concentration of Umeclidinium can be increased when it is combined with Lidocaine.Approved, Vet Approved
LiothyronineThe serum concentration of Umeclidinium can be decreased when it is combined with Liothyronine.Approved, Vet Approved
LiotrixThe serum concentration of Umeclidinium can be decreased when it is combined with Liotrix.Approved
LisinoprilThe serum concentration of Umeclidinium can be increased when it is combined with Lisinopril.Approved, Investigational
LomitapideThe serum concentration of Umeclidinium can be increased when it is combined with Lomitapide.Approved
LoperamideThe serum concentration of Umeclidinium can be increased when it is combined with Loperamide.Approved
LopinavirThe metabolism of Umeclidinium can be decreased when combined with Lopinavir.Approved
LoratadineThe serum concentration of Umeclidinium can be increased when it is combined with Loratadine.Approved
LorcaserinThe metabolism of Umeclidinium can be decreased when combined with Lorcaserin.Approved
LosartanThe serum concentration of Umeclidinium can be increased when it is combined with Losartan.Approved
LovastatinThe serum concentration of Umeclidinium can be increased when it is combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Umeclidinium is combined with Loxapine.Approved
LumacaftorThe serum concentration of Umeclidinium can be decreased when it is combined with Lumacaftor.Approved
LumefantrineThe metabolism of Umeclidinium can be decreased when combined with Lumefantrine.Approved
ManidipineThe metabolism of Umeclidinium can be decreased when combined with Manidipine.Approved, Investigational
MaprotilineThe serum concentration of Umeclidinium can be increased when it is combined with Maprotiline.Approved
MazaticolUmeclidinium may increase the anticholinergic activities of Mazaticol.Experimental
MebendazoleThe serum concentration of Umeclidinium can be increased when it is combined with Mebendazole.Approved, Vet Approved
MecamylamineUmeclidinium may increase the anticholinergic activities of Mecamylamine.Approved
MefloquineThe serum concentration of Umeclidinium can be increased when it is combined with Mefloquine.Approved
Megestrol acetateThe serum concentration of Umeclidinium can be increased when it is combined with Megestrol acetate.Approved, Vet Approved
MeprobamateThe serum concentration of Umeclidinium can be increased when it is combined with Meprobamate.Approved, Illicit
MethadoneThe serum concentration of Umeclidinium can be increased when it is combined with Methadone.Approved
MethanthelineUmeclidinium may increase the anticholinergic activities of Methantheline.Approved, Investigational
MethotrimeprazineThe metabolism of Umeclidinium can be decreased when combined with Methotrimeprazine.Approved
MetixeneUmeclidinium may increase the anticholinergic activities of Metixene.Approved
MetoprololThe serum concentration of Umeclidinium can be increased when it is combined with Metoprolol.Approved, Investigational
MibefradilThe serum concentration of Umeclidinium can be increased when it is combined with Mibefradil.Investigational, Withdrawn
MiconazoleThe serum concentration of Umeclidinium can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MidazolamThe serum concentration of Umeclidinium can be decreased when it is combined with Midazolam.Approved, Illicit
MidostaurinThe metabolism of Umeclidinium can be decreased when combined with Midostaurin.Approved
MifepristoneThe serum concentration of Umeclidinium can be decreased when it is combined with Mifepristone.Approved, Investigational
MirabegronThe metabolism of Umeclidinium can be decreased when combined with Mirabegron.Approved
MitomycinThe serum concentration of Umeclidinium can be increased when it is combined with Mitomycin.Approved
MitoxantroneThe serum concentration of Umeclidinium can be decreased when it is combined with Mitoxantrone.Approved, Investigational
MorphineThe serum concentration of Umeclidinium can be increased when it is combined with Morphine.Approved, Investigational
NaltrexoneThe serum concentration of Umeclidinium can be increased when it is combined with Naltrexone.Approved, Investigational, Vet Approved
NaringeninThe serum concentration of Umeclidinium can be increased when it is combined with Naringenin.Experimental
NefazodoneThe serum concentration of Umeclidinium can be decreased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Umeclidinium can be decreased when it is combined with Nelfinavir.Approved
NeostigmineThe serum concentration of Umeclidinium can be increased when it is combined with Neostigmine.Approved, Vet Approved
NevirapineThe metabolism of Umeclidinium can be decreased when combined with Nevirapine.Approved
NicardipineThe serum concentration of Umeclidinium can be increased when it is combined with Nicardipine.Approved
NifedipineThe serum concentration of Umeclidinium can be decreased when it is combined with Nifedipine.Approved
NilotinibThe serum concentration of Umeclidinium can be increased when it is combined with Nilotinib.Approved, Investigational
NisoldipineThe serum concentration of Umeclidinium can be increased when it is combined with Nisoldipine.Approved
NitrazepamThe serum concentration of Umeclidinium can be increased when it is combined with Nitrazepam.Approved
NitrendipineThe serum concentration of Umeclidinium can be increased when it is combined with Nitrendipine.Approved, Investigational
NorethisteroneThe serum concentration of Umeclidinium can be decreased when it is combined with Norethisterone.Approved
OmeprazoleThe serum concentration of Umeclidinium can be increased when it is combined with Omeprazole.Approved, Investigational, Vet Approved
OrphenadrineUmeclidinium may increase the anticholinergic activities of Orphenadrine.Approved
OtiloniumUmeclidinium may increase the anticholinergic activities of Otilonium.Experimental, Investigational
OxitropiumUmeclidinium may increase the anticholinergic activities of Oxitropium.Investigational
OxybutyninUmeclidinium may increase the anticholinergic activities of Oxybutynin.Approved, Investigational
OxyphenoniumUmeclidinium may increase the anticholinergic activities of Oxyphenonium.Approved
P-NitrophenolThe serum concentration of Umeclidinium can be increased when it is combined with P-Nitrophenol.Experimental
PaclitaxelThe serum concentration of Umeclidinium can be increased when it is combined with Paclitaxel.Approved, Vet Approved
Palmitic AcidThe serum concentration of Umeclidinium can be increased when it is combined with Palmitic Acid.Approved, Experimental
PancuroniumUmeclidinium may increase the anticholinergic activities of Pancuronium.Approved
PanobinostatThe serum concentration of Umeclidinium can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe serum concentration of Umeclidinium can be increased when it is combined with Pantoprazole.Approved
ParoxetineThe metabolism of Umeclidinium can be decreased when combined with Paroxetine.Approved, Investigational
Peginterferon alfa-2bThe serum concentration of Umeclidinium can be decreased when it is combined with Peginterferon alfa-2b.Approved
PentoliniumUmeclidinium may increase the anticholinergic activities of Pentolinium.Approved
PerindoprilThe serum concentration of Umeclidinium can be increased when it is combined with Perindopril.Approved
PhenglutarimideUmeclidinium may increase the anticholinergic activities of Phenglutarimide.Experimental
PhenobarbitalThe serum concentration of Umeclidinium can be decreased when it is combined with Phenobarbital.Approved
PibrentasvirThe serum concentration of Umeclidinium can be increased when it is combined with Pibrentasvir.Approved
PimozideThe serum concentration of Umeclidinium can be increased when it is combined with Pimozide.Approved
PipecuroniumUmeclidinium may increase the anticholinergic activities of Pipecuronium.Approved
PirenzepineUmeclidinium may increase the anticholinergic activities of Pirenzepine.Approved
Platelet Activating FactorThe serum concentration of Umeclidinium can be decreased when it is combined with Platelet Activating Factor.Experimental
PonatinibThe serum concentration of Umeclidinium can be increased when it is combined with Ponatinib.Approved
PosaconazoleThe serum concentration of Umeclidinium can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PravastatinThe serum concentration of Umeclidinium can be increased when it is combined with Pravastatin.Approved
PrazosinThe serum concentration of Umeclidinium can be increased when it is combined with Prazosin.Approved
PrednisoneThe serum concentration of Umeclidinium can be increased when it is combined with Prednisone.Approved, Vet Approved
ProbenecidThe serum concentration of Umeclidinium can be increased when it is combined with Probenecid.Approved
ProcyclidineUmeclidinium may increase the anticholinergic activities of Procyclidine.Approved
ProgesteroneThe serum concentration of Umeclidinium can be decreased when it is combined with Progesterone.Approved, Vet Approved
PromazineThe metabolism of Umeclidinium can be decreased when combined with Promazine.Approved, Vet Approved
PromethazineThe serum concentration of Umeclidinium can be increased when it is combined with Promethazine.Approved
PropafenoneThe serum concentration of Umeclidinium can be increased when it is combined with Propafenone.Approved
PropanthelineUmeclidinium may increase the anticholinergic activities of Propantheline.Approved
PropiverineUmeclidinium may increase the anticholinergic activities of Propiverine.Approved, Investigational
PropranololThe serum concentration of Umeclidinium can be increased when it is combined with Propranolol.Approved, Investigational
ProtriptylineThe serum concentration of Umeclidinium can be increased when it is combined with Protriptyline.Approved
QuercetinThe serum concentration of Umeclidinium can be increased when it is combined with Quercetin.Experimental, Investigational
QuinacrineThe serum concentration of Umeclidinium can be increased when it is combined with Quinacrine.Approved, Investigational
QuinidineUmeclidinium may increase the anticholinergic activities of Quinidine.Approved
QuinineThe serum concentration of Umeclidinium can be increased when it is combined with Quinine.Approved
RanitidineThe serum concentration of Umeclidinium can be increased when it is combined with Ranitidine.Approved
RanolazineThe serum concentration of Umeclidinium can be increased when it is combined with Ranolazine.Approved, Investigational
ReboxetineThe serum concentration of Umeclidinium can be increased when it is combined with Reboxetine.Approved, Investigational
RegorafenibThe serum concentration of Umeclidinium can be increased when it is combined with Regorafenib.Approved
ReserpineThe serum concentration of Umeclidinium can be decreased when it is combined with Reserpine.Approved, Investigational
RifampicinThe serum concentration of Umeclidinium can be decreased when it is combined with Rifampicin.Approved
RilpivirineThe serum concentration of Umeclidinium can be increased when it is combined with Rilpivirine.Approved
RitonavirThe metabolism of Umeclidinium can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe serum concentration of Umeclidinium can be increased when it is combined with Rolapitant.Approved
RopiniroleThe metabolism of Umeclidinium can be decreased when combined with Ropinirole.Approved, Investigational
SaquinavirThe serum concentration of Umeclidinium can be decreased when it is combined with Saquinavir.Approved, Investigational
ScopolamineUmeclidinium may increase the anticholinergic activities of Scopolamine.Approved
Scopolamine butylbromideUmeclidinium may increase the anticholinergic activities of Scopolamine butylbromide.Approved, Vet Approved
SelegilineThe serum concentration of Umeclidinium can be increased when it is combined with Selegiline.Approved, Investigational, Vet Approved
SertralineThe serum concentration of Umeclidinium can be increased when it is combined with Sertraline.Approved
SimeprevirThe serum concentration of Umeclidinium can be increased when it is combined with Simeprevir.Approved
SimvastatinThe serum concentration of Umeclidinium can be increased when it is combined with Simvastatin.Approved
SirolimusThe serum concentration of Umeclidinium can be decreased when it is combined with Sirolimus.Approved, Investigational
SolifenacinUmeclidinium may increase the anticholinergic activities of Solifenacin.Approved
SorafenibThe serum concentration of Umeclidinium can be increased when it is combined with Sorafenib.Approved, Investigational
SpironolactoneThe serum concentration of Umeclidinium can be increased when it is combined with Spironolactone.Approved
St. John's WortThe serum concentration of Umeclidinium can be decreased when it is combined with St. John&#39;s Wort.Investigational, Nutraceutical
StaurosporineThe serum concentration of Umeclidinium can be increased when it is combined with Staurosporine.Experimental
StiripentolThe metabolism of Umeclidinium can be decreased when combined with Stiripentol.Approved
StreptozocinThe serum concentration of Umeclidinium can be decreased when it is combined with Streptozocin.Approved
SulfinpyrazoneThe serum concentration of Umeclidinium can be increased when it is combined with Sulfinpyrazone.Approved
SumatriptanThe serum concentration of Umeclidinium can be increased when it is combined with Sumatriptan.Approved, Investigational
SunitinibThe serum concentration of Umeclidinium can be increased when it is combined with Sunitinib.Approved, Investigational
TacrineThe serum concentration of Umeclidinium can be increased when it is combined with Tacrine.Investigational, Withdrawn
TacrolimusThe serum concentration of Umeclidinium can be decreased when it is combined with Tacrolimus.Approved, Investigational
TamoxifenThe serum concentration of Umeclidinium can be decreased when it is combined with Tamoxifen.Approved
Taurocholic AcidThe serum concentration of Umeclidinium can be increased when it is combined with Taurocholic Acid.Experimental
TelaprevirThe serum concentration of Umeclidinium can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelmisartanThe serum concentration of Umeclidinium can be increased when it is combined with Telmisartan.Approved, Investigational
TemsirolimusThe serum concentration of Umeclidinium can be increased when it is combined with Temsirolimus.Approved
TerazosinThe serum concentration of Umeclidinium can be increased when it is combined with Terazosin.Approved
TerbinafineThe metabolism of Umeclidinium can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TerfenadineThe serum concentration of Umeclidinium can be increased when it is combined with Terfenadine.Withdrawn
TesmilifeneThe serum concentration of Umeclidinium can be decreased when it is combined with Tesmilifene.Investigational
TestosteroneThe serum concentration of Umeclidinium can be increased when it is combined with Testosterone.Approved, Investigational
ThioridazineThe metabolism of Umeclidinium can be decreased when combined with Thioridazine.Approved, Withdrawn
TicagrelorThe serum concentration of Umeclidinium can be increased when it is combined with Ticagrelor.Approved
TiclopidineThe metabolism of Umeclidinium can be decreased when combined with Ticlopidine.Approved
TiotropiumUmeclidinium may increase the anticholinergic activities of Tiotropium.Approved
TipranavirThe metabolism of Umeclidinium can be decreased when combined with Tipranavir.Approved, Investigational
TolterodineUmeclidinium may increase the anticholinergic activities of Tolterodine.Approved, Investigational
TolvaptanThe serum concentration of Umeclidinium can be increased when it is combined with Tolvaptan.Approved
TranylcypromineThe metabolism of Umeclidinium can be decreased when combined with Tranylcypromine.Approved
TrazodoneThe serum concentration of Umeclidinium can be decreased when it is combined with Trazodone.Approved, Investigational
TrifluoperazineThe serum concentration of Umeclidinium can be increased when it is combined with Trifluoperazine.Approved
TriflupromazineThe serum concentration of Umeclidinium can be increased when it is combined with Triflupromazine.Approved, Vet Approved
TrihexyphenidylUmeclidinium may increase the anticholinergic activities of Trihexyphenidyl.Approved
TrimethaphanUmeclidinium may increase the anticholinergic activities of Trimethaphan.Approved, Investigational
TrimethoprimThe serum concentration of Umeclidinium can be decreased when it is combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe serum concentration of Umeclidinium can be increased when it is combined with Trimipramine.Approved
TroleandomycinThe serum concentration of Umeclidinium can be increased when it is combined with Troleandomycin.Approved
TropatepineUmeclidinium may increase the anticholinergic activities of Tropatepine.Experimental
TropicamideUmeclidinium may increase the anticholinergic activities of Tropicamide.Approved
TrospiumUmeclidinium may increase the anticholinergic activities of Trospium.Approved
TubocurarineUmeclidinium may increase the anticholinergic activities of Tubocurarine.Approved
VecuroniumUmeclidinium may increase the anticholinergic activities of Vecuronium.Approved
VelpatasvirThe serum concentration of Umeclidinium can be increased when it is combined with Velpatasvir.Approved
VenlafaxineThe serum concentration of Umeclidinium can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Umeclidinium can be decreased when it is combined with Verapamil.Approved
VinblastineThe serum concentration of Umeclidinium can be decreased when it is combined with Vinblastine.Approved
VincristineThe serum concentration of Umeclidinium can be decreased when it is combined with Vincristine.Approved, Investigational
VinorelbineThe serum concentration of Umeclidinium can be increased when it is combined with Vinorelbine.Approved, Investigational
VoxilaprevirThe serum concentration of Umeclidinium can be increased when it is combined with Voxilaprevir.Approved
ZimelidineThe serum concentration of Umeclidinium can be increased when it is combined with Zimelidine.Withdrawn
ZiprasidoneThe metabolism of Umeclidinium can be decreased when combined with Ziprasidone.Approved
Food Interactions
Not Available

References

General References
  1. Feldman GJ, Edin A: The combination of umeclidinium bromide and vilanterol in the management of chronic obstructive pulmonary disease: current evidence and future prospects. Ther Adv Respir Dis. 2013 Dec;7(6):311-9. doi: 10.1177/1753465813499789. Epub 2013 Sep 3. [PubMed:24004659]
  2. Decramer M, Maltais F, Feldman G, Brooks J, Harris S, Mehta R, Crater G: Bronchodilation of umeclidinium, a new long-acting muscarinic antagonist, in COPD patients. Respir Physiol Neurobiol. 2013 Jan 15;185(2):393-9. doi: 10.1016/j.resp.2012.08.022. Epub 2012 Sep 28. [PubMed:23026438]
  3. Tal-Singer R, Cahn A, Mehta R, Preece A, Crater G, Kelleher D, Pouliquen IJ: Initial assessment of single and repeat doses of inhaled umeclidinium in patients with chronic obstructive pulmonary disease: two randomised studies. Eur J Pharmacol. 2013 Feb 15;701(1-3):40-8. doi: 10.1016/j.ejphar.2012.12.019. Epub 2012 Dec 28. [PubMed:23276660]
  4. Trivedi R, Richard N, Mehta R, Church A: Umeclidinium in patients with COPD: a randomised, placebo-controlled study. Eur Respir J. 2014 Jan;43(1):72-81. doi: 10.1183/09031936.00033213. Epub 2013 Aug 15. [PubMed:23949963]
  5. Goyal N, Beerahee M, Kalberg C, Church A, Kilbride S, Mehta R: Population pharmacokinetics of inhaled umeclidinium and vilanterol in patients with chronic obstructive pulmonary disease. Clin Pharmacokinet. 2014 Jul;53(7):637-48. doi: 10.1007/s40262-014-0143-4. [PubMed:24756395]
  6. Scott LJ, Hair P: Umeclidinium/Vilanterol: first global approval. Drugs. 2014 Mar;74(3):389-95. doi: 10.1007/s40265-014-0186-8. [PubMed:24532124]
  7. Salmon M, Luttmann MA, Foley JJ, Buckley PT, Schmidt DB, Burman M, Webb EF, DeHaas CJ, Kotzer CJ, Barrett VJ, Slack RJ, Sarau HM, Palovich MR, Laine DI, Hay DW, Rumsey WL: Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70. doi: 10.1124/jpet.112.202051. Epub 2013 Feb 22. [PubMed:23435542]
External Links
KEGG Drug
D10180
PubChem Compound
11519070
PubChem Substance
347827824
ChemSpider
9693858
BindingDB
50267614
ChEBI
79041
ChEMBL
CHEMBL1187833
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Umeclidinium_bromide
ATC Codes
R03AL03 — Vilanterol and umeclidinium bromideR03BB07 — Umeclidinium bromide
AHFS Codes
  • 12:08.08 — Antimuscarinics Antispasmodics

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedOtherPulmonary Disease, Chronic Obstructive2
1CompletedPreventionHealthy Volunteers / Pulmonary Disease, Chronic Obstructive1
1CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD) / Pulmonary Disease, Chronic Obstructive1
1CompletedTreatmentPulmonary Disease, Chronic Obstructive3
2CompletedDiagnosticAsthma Bronchial1
2CompletedTreatmentHyperhidrosis2
2CompletedTreatmentPulmonary Disease, Chronic Obstructive6
2RecruitingDiagnosticChronic Obstructive Pulmonary Disease (COPD)1
2WithdrawnTreatmentAsthma Bronchial1
3Active Not RecruitingTreatmentChronic Obstructive Pulmonary Disease (COPD)1
3Active Not RecruitingTreatmentPulmonary Disease, Chronic Obstructive1
3CompletedOtherPulmonary Disease, Chronic Obstructive1
3CompletedTreatmentChronic Obstructive Pulmonary Disease (COPD)3
3CompletedTreatmentPulmonary Disease, Chronic Obstructive13
3WithdrawnTreatmentPulmonary Disease, Chronic Obstructive1
4CompletedTreatmentPulmonary Disease, Chronic Obstructive1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Powder, meteredRespiratory (inhalation)
PowderRespiratory (inhalation)
Powder, meteredRespiratory (inhalation)55 μg
Aerosol, powderOral62.5 ug/1
PowderRespiratory (inhalation)62.5 mcg
Prices
Not Available
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US5873360Yes1996-08-232016-08-23Us
US7439393No2002-09-112022-09-11Us
USRE44874No2003-03-232023-03-23Us
US8511304No2007-06-142027-06-14Us
US8161968No2008-02-052028-02-05Us
US8746242No2010-10-112030-10-11Us
US8113199No2007-10-232027-10-23Us
US7776895No2002-09-112022-09-11Us
US8534281No2009-08-102029-08-10Us
US8309572No2005-04-272025-04-27Us
US8183257No2005-07-272025-07-27Us
US7488827No2005-04-272025-04-27Us
US7498440No2005-04-272025-04-27Us
US8201556No2009-02-052029-02-05Us
US9333310No2007-10-022027-10-02Us
US9750726No2010-11-292030-11-29Us

Properties

State
Solid
Experimental Properties
Not Available
Predicted Properties
PropertyValueSource
Water Solubility1.94e-05 mg/mLALOGPS
logP2.88ALOGPS
logP0.68ChemAxon
logS-7.4ALOGPS
pKa (Strongest Acidic)13.04ChemAxon
pKa (Strongest Basic)-3.7ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count2ChemAxon
Hydrogen Donor Count1ChemAxon
Polar Surface Area29.46 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity141.75 m3·mol-1ChemAxon
Polarizability50.42 Å3ChemAxon
Number of Rings5ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterNoChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Predicted ADMET features
Not Available

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available

Taxonomy

Description
This compound belongs to the class of organic compounds known as diphenylmethanes. These are compounds containing a diphenylmethane moiety, which consists of a methane wherein two hydrogen atoms are replaced by two phenyl groups.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Diphenylmethanes
Direct Parent
Diphenylmethanes
Alternative Parents
Benzylethers / Quinuclidines / Aralkylamines / Piperidines / Tetraalkylammonium salts / Tertiary alcohols / Dialkyl ethers / Azacyclic compounds / Organopnictogen compounds / Organic salts
show 3 more
Substituents
Diphenylmethane / Benzylether / Quinuclidine / Aralkylamine / Piperidine / Tetraalkylammonium salt / Quaternary ammonium salt / Tertiary alcohol / Dialkyl ether / Ether
show 14 more
Molecular Framework
Aromatic heteropolycyclic compounds
External Descriptors
Not Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM1
Uniprot ID
P11229
Uniprot Name
Muscarinic acetylcholine receptor M1
Molecular Weight
51420.375 Da
References
  1. Salmon M, Luttmann MA, Foley JJ, Buckley PT, Schmidt DB, Burman M, Webb EF, DeHaas CJ, Kotzer CJ, Barrett VJ, Slack RJ, Sarau HM, Palovich MR, Laine DI, Hay DW, Rumsey WL: Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70. doi: 10.1124/jpet.112.202051. Epub 2013 Feb 22. [PubMed:23435542]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
G-protein coupled acetylcholine receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM2
Uniprot ID
P08172
Uniprot Name
Muscarinic acetylcholine receptor M2
Molecular Weight
51714.605 Da
References
  1. Salmon M, Luttmann MA, Foley JJ, Buckley PT, Schmidt DB, Burman M, Webb EF, DeHaas CJ, Kotzer CJ, Barrett VJ, Slack RJ, Sarau HM, Palovich MR, Laine DI, Hay DW, Rumsey WL: Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70. doi: 10.1124/jpet.112.202051. Epub 2013 Feb 22. [PubMed:23435542]
Kind
Protein
Organism
Human
Pharmacological action
Yes
Actions
Antagonist
General Function
Receptor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM3
Uniprot ID
P20309
Uniprot Name
Muscarinic acetylcholine receptor M3
Molecular Weight
66127.445 Da
References
  1. Salmon M, Luttmann MA, Foley JJ, Buckley PT, Schmidt DB, Burman M, Webb EF, DeHaas CJ, Kotzer CJ, Barrett VJ, Slack RJ, Sarau HM, Palovich MR, Laine DI, Hay DW, Rumsey WL: Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70. doi: 10.1124/jpet.112.202051. Epub 2013 Feb 22. [PubMed:23435542]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Guanyl-nucleotide exchange factor activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM4
Uniprot ID
P08173
Uniprot Name
Muscarinic acetylcholine receptor M4
Molecular Weight
53048.65 Da
References
  1. Salmon M, Luttmann MA, Foley JJ, Buckley PT, Schmidt DB, Burman M, Webb EF, DeHaas CJ, Kotzer CJ, Barrett VJ, Slack RJ, Sarau HM, Palovich MR, Laine DI, Hay DW, Rumsey WL: Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70. doi: 10.1124/jpet.112.202051. Epub 2013 Feb 22. [PubMed:23435542]
Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Antagonist
General Function
Phosphatidylinositol phospholipase c activity
Specific Function
The muscarinic acetylcholine receptor mediates various cellular responses, including inhibition of adenylate cyclase, breakdown of phosphoinositides and modulation of potassium channels through the...
Gene Name
CHRM5
Uniprot ID
P08912
Uniprot Name
Muscarinic acetylcholine receptor M5
Molecular Weight
60073.205 Da
References
  1. Salmon M, Luttmann MA, Foley JJ, Buckley PT, Schmidt DB, Burman M, Webb EF, DeHaas CJ, Kotzer CJ, Barrett VJ, Slack RJ, Sarau HM, Palovich MR, Laine DI, Hay DW, Rumsey WL: Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70. doi: 10.1124/jpet.112.202051. Epub 2013 Feb 22. [PubMed:23435542]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Steroid hydroxylase activity
Specific Function
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic...
Gene Name
CYP2D6
Uniprot ID
P10635
Uniprot Name
Cytochrome P450 2D6
Molecular Weight
55768.94 Da
References
  1. Feldman GJ, Edin A: The combination of umeclidinium bromide and vilanterol in the management of chronic obstructive pulmonary disease: current evidence and future prospects. Ther Adv Respir Dis. 2013 Dec;7(6):311-9. doi: 10.1177/1753465813499789. Epub 2013 Sep 3. [PubMed:24004659]

Transporters

Kind
Protein
Organism
Human
Pharmacological action
No
Actions
Substrate
General Function
Xenobiotic-transporting atpase activity
Specific Function
Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
Gene Name
ABCB1
Uniprot ID
P08183
Uniprot Name
Multidrug resistance protein 1
Molecular Weight
141477.255 Da
References
  1. Feldman GJ, Edin A: The combination of umeclidinium bromide and vilanterol in the management of chronic obstructive pulmonary disease: current evidence and future prospects. Ther Adv Respir Dis. 2013 Dec;7(6):311-9. doi: 10.1177/1753465813499789. Epub 2013 Sep 3. [PubMed:24004659]

Drug created on May 19, 2015 10:00 / Updated on November 14, 2017 08:12