Identification
- Summary
Umeclidinium is a long-acting muscarinic antagonist used as a long-term maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD).
- Brand Names
- Anoro, Anoro Ellipta, Incruse Ellipta, Trelegy Ellipta
- Generic Name
- Umeclidinium
- DrugBank Accession Number
- DB09076
- Background
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.
- Type
- Small Molecule
- Groups
- Approved
- Structure
Structure for Umeclidinium (DB09076)
- Weight
- Average: 428.595
Monoisotopic: 428.258405759 - Chemical Formula
- C29H34NO2
- Synonyms
- 1-[2-(benzyloxy)ethyl]-4-[hydroxy(diphenyl)methyl]-1-azoniabicyclo[2.2.2]octane
- Umeclidinium
- External IDs
- GSK-573719
- GSK573719
- GSK573719A
Pharmacology
- Indication
Indicated for the long-term, once-daily, maintenance treatment of airflow obstruction in patients with chronic obstructive pulmonary disease (COPD).8
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- Contraindications & Blackbox Warnings
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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.
Target Actions Organism AMuscarinic acetylcholine receptor M2 antagonistHumans AMuscarinic acetylcholine receptor M3 antagonistHumans NMuscarinic acetylcholine receptor M1 antagonistHumans NMuscarinic acetylcholine receptor M4 antagonistHumans NMuscarinic acetylcholine receptor M5 antagonistHumans - 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
- Adverse Effects
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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.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbatacept The metabolism of Umeclidinium can be increased when combined with Abatacept. Abemaciclib The serum concentration of Abemaciclib can be increased when it is combined with Umeclidinium. Abiraterone The metabolism of Umeclidinium can be decreased when combined with Abiraterone. Abrocitinib The serum concentration of Umeclidinium can be increased when it is combined with Abrocitinib. Acebutolol The metabolism of Umeclidinium can be decreased when combined with Acebutolol. Acetaminophen The metabolism of Umeclidinium can be decreased when combined with Acetaminophen. Aclidinium The risk or severity of adverse effects can be increased when Umeclidinium is combined with Aclidinium. Adagrasib The serum concentration of Umeclidinium can be increased when it is combined with Adagrasib. Adalimumab The metabolism of Umeclidinium can be increased when combined with Adalimumab. Adenosine The risk or severity of Tachycardia can be increased when Adenosine is combined with Umeclidinium. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Umeclidinium bromide 7AN603V4JV 869113-09-7 PEJHHXHHNGORMP-UHFFFAOYSA-M - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Incruse Ellipta Aerosol, powder 62.5 ug/1 Oral GlaxoSmithKline LLC 2014-04-30 Not applicable US 
Incruse Ellipta Powder, metered 55 mcg Respiratory (inhalation) Glaxo Smith Kline (Ireland) Limited 2016-09-08 Not applicable EU 
Incruse Ellipta Powder, metered 55 mcg Respiratory (inhalation) Glaxo Smith Kline (Ireland) Limited 2016-09-08 Not applicable EU Incruse Ellipta Powder 62.5 mcg / act Respiratory (inhalation) Glaxosmithkline Inc 2015-04-27 Not applicable Canada 
Incruse Ellipta Powder, metered 55 mcg Respiratory (inhalation) Glaxo Smith Kline (Ireland) Limited 2016-09-08 Not applicable EU Rolufta Ellipta 55 mcg Respiratory (inhalation) Glaxo Smith Kline Trading Services 2020-12-22 Not applicable EU Rolufta Ellipta 55 mcg Respiratory (inhalation) Glaxo Smith Kline Trading Services 2020-12-22 Not applicable EU Rolufta Ellipta 55 mcg Respiratory (inhalation) Glaxo Smith Kline Trading Services 2020-12-22 Not applicable EU - Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Anoro Umeclidinium bromide (55 micrograms) + Vilanterol trifenatate (22 micrograms) Powder, metered Respiratory (inhalation) Glaxo Smith Kline (Ireland) Limited 2016-09-08 Not applicable EU Anoro Umeclidinium bromide (55 micrograms) + Vilanterol trifenatate (22 micrograms) Powder, metered Respiratory (inhalation) Glaxo Smith Kline (Ireland) Limited 2016-09-08 Not applicable EU Anoro Umeclidinium bromide (55 micrograms) + Vilanterol trifenatate (22 micrograms) Powder, metered Respiratory (inhalation) Glaxo Smith Kline (Ireland) Limited 2016-09-08 Not applicable EU ANORO ELLIPTA Umeclidinium bromide (74.2 MCG) + Vilanterol trifenatate (40 MCG) Powder Respiratory (inhalation) บริษัท แกล็กโซสมิทไคล์น (ประเทศไทย) จำกัด 2017-08-11 Not applicable Thailand 
Anoro Ellipta Umeclidinium bromide (62.5 ug/1) + Vilanterol trifenatate (25 ug/1) Powder Respiratory (inhalation) GlaxoSmithKline LLC 2014-01-31 Not applicable US Anoro Ellipta Umeclidinium bromide (62.5 mcg / act) + Vilanterol trifenatate (25 mcg / act) Powder Respiratory (inhalation) Glaxosmithkline Inc 2014-03-14 Not applicable Canada ANORO ELLIPTA 62.5 MCG + 25 MCG KULLANIMA HAZIR INHALASYON TOZU, 3 X 30 DOZ Umeclidinium bromide (55 mcg) + Vilanterol trifenatate (22 mcg) Aerosol, powder Respiratory (inhalation) GLAXOSMİTHKLİNE İLAÇLARI SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey 
ANORO ELLIPTA 62.5 MCG + 25 MCG KULLANIMA HAZIR INHALASYON TOZU, 30 DOZ Umeclidinium bromide (55 mcg) + Vilanterol trifenatate (22 mcg) Aerosol, powder Respiratory (inhalation) GLAXOSMİTHKLİNE İLAÇLARI SAN. VE TİC. A.Ş. 2020-08-14 Not applicable Turkey ANORO ELLIPTA INHALATION POWDER 62.5 MCG/25 MCG Umeclidinium (62.5 mcg) + Vilanterol (25 mcg) Powder, metered Respiratory (inhalation) GLAXOSMITHKLINE PTE LTD 2015-08-28 Not applicable Singapore Elebrato Ellipta Umeclidinium bromide (55 mcg) + Fluticasone furoate (92 mcg) + Vilanterol trifenatate (22 mcg) Powder, metered Respiratory (inhalation) Glaxo Smith Kline Trading Services 2020-12-16 Not applicable EU
Categories
- ATC Codes
- R03AL08 — Vilanterol, umeclidinium bromide and fluticasone furoate
- R03AL — Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- R03AL — Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids
- R03A — ADRENERGICS, INHALANTS
- R03 — DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES
- R — RESPIRATORY SYSTEM
- Drug Categories
- Adrenergics, Inhalants
- Agents producing tachycardia
- Agents to Treat Airway Disease
- Anticholinergic Agents
- Antimuscarinics Antispasmodics
- Cytochrome P-450 CYP2D6 Substrates
- Cytochrome P-450 Substrates
- Drugs for Obstructive Airway Diseases
- Muscarinic Antagonists
- P-glycoprotein substrates
- Pulmonary Disease, Chronic Obstructive, drug therapy
- Chemical TaxonomyProvided by Classyfire
- 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
- Alcohol / Amine / Aralkylamine / Aromatic alcohol / Aromatic heteropolycyclic compound / Azacycle / Benzylether / Dialkyl ether / Diphenylmethane / Ether show 14 more
- Molecular Framework
- Aromatic heteropolycyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- GE2T1418SV
- CAS number
- 869185-19-3
- 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
References
- General References
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- 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. [Article]
- Scott LJ, Hair P: Umeclidinium/Vilanterol: first global approval. Drugs. 2014 Mar;74(3):389-95. doi: 10.1007/s40265-014-0186-8. [Article]
- 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. [Article]
- FDA Approved Drug Products: INCRUSE ELLIPTA (umeclidinium inhalation powder) for oral inhalation use [Link]
- External Links
- KEGG Drug
- D10180
- PubChem Compound
- 11519070
- PubChem Substance
- 347827824
- ChemSpider
- 9693858
- BindingDB
- 50267614
- 1487514
- ChEBI
- 79041
- ChEMBL
- CHEMBL1187833
- ZINC
- ZINC000034608502
- RxList
- RxList Drug Page
- Drugs.com
- Drugs.com Drug Page
- Wikipedia
- Umeclidinium_bromide
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Completed Basic Science Chronic Obstructive Pulmonary Disease (COPD) 1 4 Completed Treatment Chronic Obstructive Pulmonary Disease (COPD) 3 4 Not Yet Recruiting Treatment Chronic Obstructive Pulmonary Disease (COPD) 1 4 Recruiting Treatment Chronic Obstructive Pulmonary Disease (COPD) 1 4 Recruiting Treatment Chronic Obstructive Pulmonary Disease (COPD) / Heart Failure 1 4 Terminated Other Chronic Obstructive Pulmonary Disease (COPD) 1 4 Withdrawn Treatment Chronic Obstructive Pulmonary Disease (COPD) 1 3 Completed Other Chronic Obstructive Pulmonary Disease (COPD) 1 3 Completed Treatment Chronic Obstructive Pulmonary Disease (COPD) 23 3 Recruiting Treatment Chronic Obstructive Pulmonary Disease (COPD) / Non-Small Cell Lung Cancer (NSCLC) 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Powder, metered Respiratory (inhalation) 62.5 mcg Powder Oral; Respiratory (inhalation) 55 mcg Tablet Oral 62.5 mg Aerosol, powder Oral 62.5 ug/1 Powder Respiratory (inhalation) 62.5 mcg/1blister Powder Respiratory (inhalation) 62.5 mcg / act Powder, metered Respiratory (inhalation) 55 MCG Aerosol, powder Respiratory (inhalation) 62.5 mg Powder, metered Respiratory (inhalation) 62.5 mcg Powder Respiratory (inhalation) 55 mcg Aerosol, powder Respiratory (inhalation) 55 mcg Powder Respiratory (inhalation) Aerosol, powder Respiratory (inhalation) Powder, metered Respiratory (inhalation) - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5873360 Yes 1999-02-23 2016-08-23 US US7101866 No 2006-09-05 2021-08-03 US US7439393 No 2008-10-21 2022-09-11 US US6759398 No 2004-07-06 2021-08-03 US USRE44874 No 2014-04-29 2023-03-23 US US6537983 No 2003-03-25 2021-08-03 US US8511304 No 2013-08-20 2027-06-14 US US7629335 No 2009-12-08 2021-08-03 US US8161968 No 2012-04-24 2028-02-05 US US8746242 No 2014-06-10 2030-10-11 US US8113199 No 2012-02-14 2027-10-23 US US7776895 No 2010-08-17 2022-09-11 US US8534281 No 2013-09-17 2029-08-10 US US6878698 No 2005-04-12 2021-08-03 US US8309572 No 2012-11-13 2025-04-27 US US8183257 No 2012-05-22 2025-07-27 US US7488827 No 2009-02-10 2025-04-27 US US7498440 No 2009-03-03 2025-04-27 US US8201556 No 2012-06-19 2029-02-05 US US9333310 No 2016-05-10 2027-10-02 US US9750726 No 2017-09-05 2030-11-29 US US9750762 No 2017-09-05 2030-11-29 US US11090294 No 2021-08-17 2030-11-29 US
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 1.94e-05 mg/mL ALOGPS logP 2.88 ALOGPS logP 0.68 Chemaxon logS -7.4 ALOGPS pKa (Strongest Acidic) 13.04 Chemaxon pKa (Strongest Basic) -3.7 Chemaxon Physiological Charge 1 Chemaxon Hydrogen Acceptor Count 2 Chemaxon Hydrogen Donor Count 1 Chemaxon Polar Surface Area 29.46 Å2 Chemaxon Rotatable Bond Count 8 Chemaxon Refractivity 141.75 m3·mol-1 Chemaxon Polarizability 50.42 Å3 Chemaxon Number of Rings 5 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule Yes Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS Not Available
Targets
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- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Transporters
- Kind
- Protein
- Organism
- Humans
- 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
- 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. [Article]
Drug created at May 19, 2015 16:00 / Updated at March 21, 2023 17:58