umeclidinium Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| muscarinic receptors agonists/antagonists | 4816 | 869113-09-7 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a long-acting antimuscarinic agent with similar affinity to the subtypes of muscarinic receptors M1 to M5, in the airways, it exhibits pharmacological effects through inhibition of M3 receptor at the smooth muscle leading to bronchodilation
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 55 | mcg | Inhal.powder |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 1.23 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 35.95 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.11 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 19 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Dec. 18, 2013 | FDA | GLAXOSMITHKLINE |
FDA Adverse Event Reporting System (Female)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Dyspnoea | 174.59 | 73.16 | 54 | 146 | 78679 | 2279206 |
| Cough | 154.98 | 73.16 | 41 | 159 | 33076 | 2324809 |
| Asthma | 152.13 | 73.16 | 33 | 167 | 11281 | 2346604 |
| Obstructive airways disorder | 138.17 | 73.16 | 22 | 178 | 1351 | 2356534 |
| Wheezing | 116.12 | 73.16 | 24 | 176 | 6360 | 2351525 |
| Nasal polyps | 115.92 | 73.16 | 15 | 185 | 201 | 2357684 |
| Respiratory symptom | 97.95 | 73.16 | 13 | 187 | 213 | 2357672 |
| Chronic obstructive pulmonary disease | 96.48 | 73.16 | 21 | 179 | 7056 | 2350829 |
| Sputum increased | 92.22 | 73.16 | 12 | 188 | 167 | 2357718 |
| Osteoporosis | 88.26 | 73.16 | 18 | 182 | 4396 | 2353489 |
| Chest discomfort | 86.31 | 73.16 | 22 | 178 | 14573 | 2343312 |
| Salpingo-oophorectomy unilateral | 84.97 | 73.16 | 9 | 191 | 14 | 2357871 |
| Embolism venous | 84.48 | 73.16 | 12 | 188 | 329 | 2357556 |
| Sinusitis fungal | 80.21 | 73.16 | 10 | 190 | 96 | 2357789 |
| Female genital tract fistula | 80.21 | 73.16 | 12 | 188 | 475 | 2357410 |
| Productive cough | 79.17 | 73.16 | 17 | 183 | 5304 | 2352581 |
| Emphysema | 77.56 | 73.16 | 13 | 187 | 1072 | 2356813 |
| Diastolic dysfunction | 76.93 | 73.16 | 12 | 188 | 628 | 2357257 |
| Sputum discoloured | 76.63 | 73.16 | 13 | 187 | 1153 | 2356732 |
| Hiatus hernia | 75.47 | 73.16 | 14 | 186 | 2070 | 2355815 |
FDA Adverse Event Reporting System (Male)
| MedDRA adverse event term | Likelihood ratio | Likelihood ratio threshold | Patients taking drug having adverse event | Patients taking drug not having adverse event | Patients not taking drug having adverse event | Patients not taking drug not having adverse event |
|---|---|---|---|---|---|---|
| Chronic obstructive pulmonary disease | 94.13 | 52.28 | 22 | 185 | 5931 | 1740643 |
| Asthma | 92.87 | 52.28 | 21 | 186 | 4883 | 1741691 |
| Dyspnoea | 84.69 | 52.28 | 33 | 174 | 52026 | 1694548 |
| Urinary retention | 59.67 | 52.28 | 15 | 192 | 5380 | 1741194 |
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R03AL03 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids |
| ATC | R03AL08 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids |
| ATC | R03BB07 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES OTHER DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES, INHALANTS Anticholinergics |
| CHEBI has role | CHEBI:48876 | muscarinic antagonist |
| FDA EPC | N0000175574 | Anticholinergic |
| FDA MoA | N0000175370 | Cholinergic Antagonists |
Drug Use (View source of the data)
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic obstructive lung disease | indication | 13645005 | DOID:3083 |
Acid dissociation constants calculated using MoKa v3.0.0
None
Orange Book patent data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Patent number | Patent expiration date | Patent use |
|---|---|---|---|---|---|---|---|---|---|---|
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | 6537983 | Aug. 3, 2021 | THE TREATMENT OF AN INFLAMMATORY DISORDER OF THE RESPIRATORY TRACT BY ONCE-PER-DAY ADMINISTRATION OF A PHARMACEUTICAL FORMULATION COMPRISING FLUTICASONE FUROATE AND A LONG-ACTING BETA2 ADRENORECEPTOR AGONIST |
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | 6759398 | Aug. 3, 2021 | THE TREATMENT OF AN INFLAMMATORY DISORDER OF THE RESPIRATORY TRACT BY ONCE-PER-DAY ADMINISTRATION OF A PHARMACEUTICAL FORMULATION COMPRISING FLUTICASONE FUROATE AND A LONG-ACTING BETA2 ADRENORECEPTOR AGONIST |
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | 6878698 | Aug. 3, 2021 | THE TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE BY ONCE-PER-DAY ADMINISTRATION OF A PHARMACEUTICAL FORMULATION COMPRISING FLUTICASONE FUROATE AND A LONG-ACTING BETA2 ADRENORECEPTOR |
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | 7101866 | Aug. 3, 2021 | USE OF FLUTICASONE FUROATE FOR THE TREATMENT OF AN INFLAMMATORY OR ALLERGIC CONDITIONS, INCLUDING CHRONIC OBSTRUCTIVE PULMONARY DISEASE |
| EQ 0.0625MG BASE/INH | ANORO ELLIPTA | GLAXOSMITHKLINE | N203975 | Dec. 18, 2013 | RX | POWDER | INHALATION | RE44874 | March 23, 2023 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA. |
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | RE44874 | March 23, 2023 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA |
| EQ 0.0625MG BASE/INH | ANORO ELLIPTA | GLAXOSMITHKLINE | N203975 | Dec. 18, 2013 | RX | POWDER | INHALATION | 8309572 | April 27, 2025 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA. |
| EQ 62.5MCG BASE/INH | INCRUSE ELLIPTA | GLAXO GRP ENGLAND | N205382 | April 30, 2014 | RX | POWDER | INHALATION | 8309572 | April 27, 2025 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA. |
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | 8309572 | April 27, 2025 | METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA TOPICAL APPLICATION |
| EQ 0.0625MG BASE/INH | ANORO ELLIPTA | GLAXOSMITHKLINE | N203975 | Dec. 18, 2013 | RX | POWDER | INHALATION | 7439393 | May 21, 2025 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA. |
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | 7439393 | May 21, 2025 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA |
| EQ 0.0625MG BASE/INH | ANORO ELLIPTA | GLAXOSMITHKLINE | N203975 | Dec. 18, 2013 | RX | POWDER | INHALATION | 8183257 | July 27, 2025 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA. |
| EQ 62.5MCG BASE/INH | INCRUSE ELLIPTA | GLAXO GRP ENGLAND | N205382 | April 30, 2014 | RX | POWDER | INHALATION | 8183257 | July 27, 2025 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA. |
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | 8183257 | July 27, 2025 | METHOD OF INHIBITING THE BINDING OF ACETYLCHOLINE TO AN ACETYLCHOLINE RECEPTOR IN THE RESPIRATORY TRACT OF A HUMAN, COMPRISING CONTACTING THE RECEPTOR WITH AN EFFECTIVE AMOUNT OF UMECLIDINIUM, VIA INHALATION |
| EQ 0.0625MG BASE/INH | ANORO ELLIPTA | GLAXOSMITHKLINE | N203975 | Dec. 18, 2013 | RX | POWDER | INHALATION | 8511304 | June 14, 2027 | INDICATED FOR THE LONG-TERM, ONCE-DAILY, MAINTENANCE TREATMENT OF AIRFLOW OBSTRUCTION IN PATIENTS WITH CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), INCLUDING CHRONIC BRONCHITIS AND/OR EMPHYSEMA. |
Orange Book exclusivity data (new drug applications)
| Formulation strength | Trade name | Applicant | Application number | Approval date | Type | Dose form | Route | Exclusivity date | Description |
|---|---|---|---|---|---|---|---|---|---|
| EQ 0.0625MG BASE/INH | TRELEGY ELLIPTA | GLAXOSMITHKLINE | N209482 | Sept. 18, 2017 | RX | POWDER | INHALATION | April 24, 2021 | REVISED INDICATION FOR FIXED-DOSE COMBINATION OF FLUTICASONE FUROATE, UMECLIDINIUM, AND VILANTEROL TO TREAT AIRFLOW OBSTRUCTION IN CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD) AND TO REDUCE COPD EXACERBATIONS IN PTS WITH HISTORY OF EXACERBATIONS |
| EQ 0.0625MG BASE/INH | ANORO ELLIPTA | GLAXOSMITHKLINE | N203975 | Dec. 18, 2013 | RX | POWDER | INHALATION | June 9, 2022 | ADDITIONAL INFORMATION ADDED TO THE LABELING BASED ON SAFETY AND EFFICACY DATA FROM THE IMPACT TRIAL |
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Muscarinic acetylcholine receptor M3 | GPCR | ANTAGONIST | Ki | 10.22 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Muscarinic acetylcholine receptor M2 | GPCR | Ki | 9.82 | SCIENTIFIC LITERATURE | |||||
| Muscarinic acetylcholine receptor M1 | GPCR | Ki | 9.80 | SCIENTIFIC LITERATURE | |||||
| Muscarinic acetylcholine receptor M4 | GPCR | ANTAGONIST | Ki | 10.30 | IUPHAR | ||||
| Muscarinic acetylcholine receptor M5 | GPCR | ANTAGONIST | Ki | 9.90 | IUPHAR |
External reference:
| ID | Source |
|---|---|
| D10180 | KEGG_DRUG |
| C3832899 | UMLSCUI |
| 7AN603V4JV | UNII |
| 9551 | INN_ID |
| 715611006 | SNOMEDCT_US |
| 1487514 | RXNORM |
| d08187 | MMSL |
| 015344 | NDDF |
| 4033108 | VANDF |
| 706898002 | SNOMEDCT_US |
| 11519070 | PUBCHEM_CID |
| CHEBI:79040 | CHEBI |
| CHEMBL523299 | ChEMBL_ID |
| CHEMBL1187833 | ChEMBL_ID |
| DB09076 | DRUGBANK_ID |
| C573971 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7354 | IUPHAR_LIGAND_ID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Anoro Ellipta | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0173-0869 | POWDER | 62.50 ug | RESPIRATORY (INHALATION) | NDA | 18 sections |
| Incruse Ellipta | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0173-0873 | AEROSOL, POWDER | 62.50 ug | ORAL | NDA | 19 sections |
| Trelegy Ellipta | HUMAN PRESCRIPTION DRUG LABEL | 3 | 0173-0887 | POWDER | 62.50 ug | RESPIRATORY (INHALATION) | NDA | 18 sections |