Umeclidinium
Highest phase reached
Approved
Drug type
Small molecule
First approval year
2013
- First approval year
- 2013
- Listing at source
- Listed
- Highest phase reached
- Approved
- Drug type
- Small molecule
- Drug name
- Umeclidinium
- Molecular weight
- 428.6
- Structure (SMILES)
- OC(c1ccccc1)(c1ccccc1)C12CC[N+](CCOCc3ccccc3)(CC1)CC2
- gsk 573719
- GSK-573719
- gsk573719
- GSK573719
- GSK573719 (INHALATION POWDER)
- GSK573719 1000 μg
- GSK573719 125 mcg (one strip)
- GSK573719 125 mcg(two strips)
- GSK573719 125mcg
- GSK573719 250 μg
- GSK573719 250mcg
- GSK573719 500 μg
- GSK573719 500mcg
- GSK573719 62.5 mcg (one strip)
- GSK573719 62.5 mcg(two strips)
- umeclidinium
- Umeclidinium
- UMECLIDINIUM [USAN]
- UMECLIDINIUM [VANDF]
- Umeclidinium [WHO-DD]
- umeclidinium cation
- Umeclidinium cation
- umeclidinium ion
- Umeclidinium ion
- umeclidinium usan
And 2 more, listed on the interactive page.
- ATC classification codes
- R03BB07
- ChEMBL ID
- CHEMBL1187833
- InChIKey
- FVTWTVQXNAJTQP-UHFFFAOYSA-N
- PubChem compound IDs
- 11519070
- FDA ingredient codes (UNII)
- GE2T1418SV
- 869113-09-7
- 869185-19-3
- 1487512
- 1487514
- Applicant
- GLAXOSMITHKLINE
- Approval date
- 18 Dec 2013
- Application number
- NDA203975
- Status
- Authorised
- Status date
- 20 Mar 2017
- Authorisation date
- 20 Mar 2017
- Approved indications
- Rolufta is indicated as a maintenance bronchodilator treatment to relieve symptoms in adult patients with chronic obstructive pulmonary disease (COPD).
- Product number
- EMEA/H/C/004654
- Authorisation holder
- GlaxoSmithKline Trading Services Limited
- Priority medicines scheme
- No
- Generic
- No
- Biosimilar
- No
- Generic medicines
- 0
- Biosimilar medicines
- 0
- Advanced therapy
- No
- Conditional approval
- No
- Additional monitoring
- No
- Accelerated assessment
- No
- Exceptional circumstances
- No
Therapeutic areas
- Pulmonary Disease, Chronic Obstructive
European medicines record
- First in class
- No
- Orphan designation
- No
- Availability
- Prescription only
- Pharmacology name
- umeclidinium
- Type
- Synthetic organic
- Drug name stem
- -clidinium; -ium
- Approval recorded by Guide to Pharmacology
- Yes
Administration routes
- topical
- Action
- Antagonist
- Action type
- Antagonist
- Target
- M2 receptor
- Gene symbol
- CHRM2
- Protein identifier
- P08172
- Median affinity
- 9.82
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- M4 receptor
- Gene symbol
- CHRM4
- Protein identifier
- P08173
- Median affinity
- 10.3
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- M5 receptor
- Gene symbol
- CHRM5
- Protein identifier
- P08912
- Median affinity
- 9.9
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- M1 receptor
- Gene symbol
- CHRM1
- Protein identifier
- P11229
- Median affinity
- 9.8
- Affinity units
- pKi
- Action
- Antagonist
- Action type
- Antagonist
- Target
- M3 receptor
- Gene symbol
- CHRM3
- Protein identifier
- P20309
- Median affinity
- 10.22
- Affinity units
- pKi
Open Targets mechanisms
- Mechanism
- Muscarinic acetylcholine receptor M3 antagonist
- Action type
- Antagonist
- Target
- Muscarinic acetylcholine receptor M3
- Action type
- Antagonist
- Gene symbol
- CHRM4
- Protein identifier
- P08173
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Antagonist
- Gene symbol
- CHRM5
- Protein identifier
- P08912
- Organism
- Homo sapiens
- Target development level
- Clinical
- Action type
- Antagonist
- Gene symbol
- CHRM3
- Protein identifier
- P20309
- Organism
- Homo sapiens
- Target development level
- Clinical
- Condition
- Pulmonary Disease, Chronic Obstructive
- Highest recorded phase
- 3
- Condition identifier
- EFO:0000341
- Subject identifier
- D029424
- Condition
- Hyperhidrosis
- Highest recorded phase
- 2
- Condition identifier
- HP:0000975
- Subject identifier
- D006945
- Condition
- Asthma
- Highest recorded phase
- 2
- Condition identifier
- MONDO:0004979
- Subject identifier
- D001249
- Condition identifier
- EFO_0000341
- Condition identifier
- HP_0000975
- Highest recorded phase
- 1
- Condition identifier
- HP_0002094
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0004979
- Highest recorded phase
- 2
- Condition identifier
- MONDO_0004979
- Highest recorded phase
- 3
- Condition identifier
- MONDO_0005002
- Highest recorded phase
- 4
- Condition identifier
- MONDO_0005249
- Event
- angle closure glaucoma
- Reports
- 3
- Reporting signal score
- 8.19215
- Event
- asthma
- Reports
- 52
- Reporting signal score
- 143.291
- Event
- blood count abnormal
- Reports
- 19
- Reporting signal score
- 58.4348
- Event
- blood immunoglobulin e increased
- Reports
- 3
- Reporting signal score
- 9.41919
- Event
- blood test abnormal
- Reports
- 5
- Reporting signal score
- 11.3502
- Event
- bronchial wall thickening
- Reports
- 2
- Reporting signal score
- 8.12474
- Event
- bronchiectasis
- Reports
- 5
- Reporting signal score
- 13.6079
- Event
- bronchospasm
- Reports
- 8
- Reporting signal score
- 16.8602
- Event
- bronchospasm paradoxical
- Reports
- 3
- Reporting signal score
- 15.7172
- Event
- chest discomfort
- Reports
- 10
- Reporting signal score
- 9.6496
- Event
- choking
- Reports
- 4
- Reporting signal score
- 8.77955
- Event
- chronic obstructive pulmonary disease
- Reports
- 20
- Reporting signal score
- 48.1409
- Event
- cough
- Reports
- 41
- Reporting signal score
- 60.1426
- Event
- diarrhoea
- Reports
- 1
- Reporting signal score
- 7.12035
- Event
- dyspepsia
- Reports
- 10
- Reporting signal score
- 12.9626
- Event
- dyspnoea
- Reports
- 59
- Reporting signal score
- 65.3154
- Event
- dyspnoea exertional
- Reports
- 6
- Reporting signal score
- 7.84987
- Event
- gastrooesophageal reflux disease
- Reports
- 11
- Reporting signal score
- 15.8938
- Event
- glaucoma
- Reports
- 8
- Reporting signal score
- 19.4055
- Event
- halo vision
- Reports
- 3
- Reporting signal score
- 12.7882
- Event
- lethargy
- Reports
- 9
- Reporting signal score
- 10.4816
- Event
- loss of personal independence in daily activities
- Reports
- 5
- Reporting signal score
- 7.45475
- Event
- lung hyperinflation
- Reports
- 2
- Reporting signal score
- 7.82244
- Event
- mouth swelling
- Reports
- 4
- Reporting signal score
- 11.7295
- Event
- obstructive airways disorder
- Reports
- 17
- Reporting signal score
- 58.8277
And 15 more, listed on the interactive page.
- NCT00475436
- NCT00515502
- NCT00732472
- NCT00976144
- NCT01030965
- NCT01110018
- NCT01128634
- NCT01313637
- NCT01316887
- NCT01316900
- NCT01316913
- NCT01323660
- NCT01328444
- NCT01362257
- NCT01372410
- NCT01376388
- NCT01387230
- NCT01521377
- NCT01521390
- NCT01571999
- NCT01577680
- NCT01636713
- NCT01702363
- NCT01716520
- NCT01777334
And 16 more, listed on the interactive page.
- Dose
- 1 actuation (umeclidinium 62.5 mcg)
- Route
- Inhalation
- How often
- Once daily
- Do not use more than 1 time every 24 hours
- Use at the same time every day
- Hydrogen bond acceptors
- 2
- Hydrogen bond donors
- 1
- Polar surface area
- 29.46
- Calculated partition coefficient (ALogP)
- 5.14
- Calculated partition coefficient (XLogP)
- 4.7
- Prodrug
- No
- Chirality
- Achiral
- Inorganic
- No
- Rule-of-five violations
- 1
- Rotatable bonds
- 8
- Heavy atoms
- 32
- Molecular formula
- C29H34NO2+
- Monoisotopic mass
- 428.258954327
- Natural product
- Yes
- Recorded assays
- 54
- Active assays
- 14
- Confirmatory
- Other
Related records
Trials (149)
- 24-week Trial Comparing GSK573719/GW642444 With GSK573719 and With Tiotropium in Chronic Obstructive Pulmonary Disease
- 24-week Trial Comparing GSK573719/GW642444 With GW642444 and With Tiotropium in Chronic Obstructive Pulmonary Disease
- 28-day Repeat Dose Study of GSK573719
- A 24-week Evaluation of GSK573719/Vilanterol (125/25mcg) and Components in COPD
- 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
- A 6-month Study to Evaluate the Efficacy and Safety of Fluticasone Furoate (FF)/GW642444 Inhalation Powder in Subjects With Chronic Obstructive Pulmonary Disease (COPD)
- A Bioequivalence Study Between Fluticasone and Salmeterol vs. SERETIDE DISKUS® in Healthy Volunteers With Charcoal Blockade
- A Bioequivalence Study Between Fluticasone Propionate 100 mcg/Blister Oral Inhalation Powder/Respirent Pharmaceuticals vs. FLOVENT DISKUS® 100 mcg/Blister Oral Inhalation Powder /GSK in Healthy Volunteers Under Fasting Conditions
- A Bioequivalence Study Between Fluticasone Propionate 250 mcg/Blister Oral Inhalation Powder/Respirent Pharmaceuticals vs. FLOVENT DISKUS® 250 mcg/Blister Oral Inhalation Powder /GSK in Healthy Volunteers Under Fasting Conditions
- A Bioequivalence Study Between Fluticasone Salmeterol Xinafoate vs. SERETIDE DISKUS® in Healthy Volunteers With Charcoal Blockade (BREATH-PK250-CC)
- A Clinical Study Evaluating the Pharmacokinetics and Pharmacodynamics of HSK39004 Inhalation Suspension in COPD Patients
- A Clinical Study of TQC3721 Inhalation Powder in Patients With Chronic Obstructive Pulmonary Disease
- A Clinical Study to Evaluate the Safety, Tolerability and Pharmacokinetic Characteristics of RC010 Inhalation Powder in Healthy Participants
- A Clinical Study to Evaluate the Safety, Tolerability and Pharmacokinetic Profile of TQC3302 Inhalation Spray in Healthy Adult Subjects
- A Clinical Study to Investigate if a Single Dose of an Approved Drug Product (Glycopyrrolate Inhalation Solution) Reduces Trapped Air in the Lungs of Participants With Chronic Obstructive Pulmonary Disease.
- A Clinical Trial Comparing TQC3927 Inhaled Powder With Glycopyrronium Bromide and Formoterol Inhaled Aerosol (Biovoping® Lingchang®) for the Treatment of Chronic Obstructive Pulmonary Disease
- A Clinical Trial for Examining the Therapeutic Equivalence Between Fluticasone Propionate 100 mcg/Blister Oral Inhalation Powder/Respirent Pharmaceuticals vs. FLOVENT DISKUS® 100mcg/Blister Oral Inhalation Powder/GSK in Patients With Asthma
- A Clinical Trial of TQC3927 Powder for Inhalation in Chronic Obstructive Pulmonary Disease
- A Clinical Trial to Evaluate the Efficacy and Safety of HRS-9821 Inhalation Suspension in Patients With Moderate to Severe Chronic Obstructive Pulmonary Disease
- A Comparison of Totally Intravenous and Inhalation Anesthesia for Intraocular Pressure During Robot-Assisted Laparoscopic Radical Prostatectomy
In development for (2)
- Asthma Phase 2
- Chronic obstructive pulmonary disease Phase 3
Targets (1)
- CHRM3 Muscarinic acetylcholine receptor M3 antagonist