olodaterol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| bronchodilators, phenethylamine derivatives | 4814 | 868049-49-4 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
a long-acting beta2-adrenergic agonist (LABA), activation of beta2 receptors in the airways results in a stimulation of intracellular adenyl cyclase, an enzyme that mediates the synthesis of cyclic-3',5' adenosine monophosphate (cAMP), elevated levels of cAMP induce bronchodilation by relaxation of airway smooth muscle cells
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
| Dose | Unit | Route |
|---|---|---|
| 5 | mcg | Inhal.solution |
ADMET properties:
| Property | Value | Reference |
|---|---|---|
| Vd (Volume of distribution) | 15.85 L/kg | Lombardo F, Berellini G, Obach RS |
| CL (Clearance) | 12.45 mL/min/kg | Lombardo F, Berellini G, Obach RS |
| fu (Fraction unbound in plasma) | 0.40 % | Lombardo F, Berellini G, Obach RS |
| t_half (Half-life) | 22.10 hours | Lombardo F, Berellini G, Obach RS |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| July 31, 2014 | FDA | BOEHRINGER INGELHEIM |
FDA Adverse Event Reporting System (Female)
None
FDA Adverse Event Reporting System (Male)
None
FDA Adverse Event Reporting System (Geriatric)
| 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 |
|---|---|---|---|---|---|---|
| Wheezing | 45.70 | 35.53 | 21 | 615 | 116643 | 79627109 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| ATC | R03AC19 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Selective beta-2-adrenoreceptor agonists |
| ATC | R03AL06 | RESPIRATORY SYSTEM DRUGS FOR OBSTRUCTIVE AIRWAY DISEASES ADRENERGICS, INHALANTS Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids |
| FDA MoA | N0000009922 | Adrenergic beta2-Agonists |
| MeSH PA | D018927 | Anti-Asthmatic Agents |
| MeSH PA | D001993 | Bronchodilator Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| FDA EPC | N0000175779 | beta2-Adrenergic Agonist |
| CHEBI has role | CHEBI:35522 | beta-adrenergic agonists |
| CHEBI has role | CHEBI:35523 | bronchodilator |
Drug Use | Suggest Off label Use Form| |View source of the data|
| Disease | Relation | SNOMED_ID | DOID |
|---|---|---|---|
| Chronic obstructive lung disease | indication | 13645005 | DOID:3083 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 10.32 | acidic |
| pKa2 | 11.96 | acidic |
| pKa3 | 13.95 | acidic |
| pKa4 | 8.47 | Basic |
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 0.0025MG BASE/INH | STRIVERDI RESPIMAT | BOEHRINGER INGELHEIM | N203108 | July 31, 2014 | RX | SPRAY, METERED | INHALATION | 8044046 | Nov. 10, 2023 | TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), CHRONIC BRONCHITIS OR EMPHYSEMA |
| EQ 0.0025MG BASE/INH;EQ 0.0025MG BASE/INH | STIOLTO RESPIMAT | BOEHRINGER INGELHEIM | N206756 | May 21, 2015 | RX | SPRAY, METERED | INHALATION | 8044046 | Nov. 10, 2023 | TREATMENT OF COPD |
| EQ 0.0025MG BASE/INH | STRIVERDI RESPIMAT | BOEHRINGER INGELHEIM | N203108 | July 31, 2014 | RX | SPRAY, METERED | INHALATION | 7220742 | May 12, 2025 | TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), CHRONIC BRONCHITIS OR EMPHYSEMA |
| EQ 0.0025MG BASE/INH | STRIVERDI RESPIMAT | BOEHRINGER INGELHEIM | N203108 | July 31, 2014 | RX | SPRAY, METERED | INHALATION | 8034809 | May 12, 2025 | TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), CHRONIC BRONCHITIS OR EMPHYSEMA |
| EQ 0.0025MG BASE/INH;EQ 0.0025MG BASE/INH | STIOLTO RESPIMAT | BOEHRINGER INGELHEIM | N206756 | May 21, 2015 | RX | SPRAY, METERED | INHALATION | 7220742 | May 12, 2025 | TREATMENT OF RESPIRATORY COMPLAINTS |
| EQ 0.0025MG BASE/INH;EQ 0.0025MG BASE/INH | STIOLTO RESPIMAT | BOEHRINGER INGELHEIM | N206756 | May 21, 2015 | RX | SPRAY, METERED | INHALATION | 8034809 | May 12, 2025 | TREATMENT OF COPD |
| EQ 0.0025MG BASE/INH | STRIVERDI RESPIMAT | BOEHRINGER INGELHEIM | N203108 | July 31, 2014 | RX | SPRAY, METERED | INHALATION | 7396341 | Oct. 10, 2026 | TREATMENT OF CHRONIC OBSTRUCTIVE PULMONARY DISEASE (COPD), CHRONIC BRONCHITIS OR EMPHYSEMA |
Orange Book exclusivity data (new drug applications)
None
Bioactivity Summary:
| Target | Class | Pharos | UniProt | Action | Type | Activity value (-log[M]) | Mechanism action | Bioact source | MoA source |
|---|---|---|---|---|---|---|---|---|---|
| Beta-2 adrenergic receptor | GPCR | ANTAGONIST | Ki | 9.14 | SCIENTIFIC LITERATURE | SCIENTIFIC LITERATURE | |||
| Beta-1 adrenergic receptor | GPCR | Ki | 7.33 | SCIENTIFIC LITERATURE | |||||
| Beta-3 adrenergic receptor | GPCR | Ki | 5.26 | SCIENTIFIC LITERATURE |
External reference:
| ID | Source |
|---|---|
| D10020 | KEGG_DRUG |
| 4033628 | VUID |
| N0000190930 | NUI |
| 869477-96-3 | SECONDARY_CAS_RN |
| 4033628 | VANDF |
| 4033629 | VANDF |
| CHEBI:82700 | CHEBI |
| DZQ | PDB_CHEM_ID |
| CHEMBL605846 | ChEMBL_ID |
| C549647 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7543 | IUPHAR_LIGAND_ID |
| 9174 | INN_ID |
| DB09080 | DRUGBANK_ID |
| VD2YSN1AFD | UNII |
| 1546059 | RXNORM |
| 220486 | MMSL |
| 30305 | MMSL |
| d08261 | MMSL |
| 015412 | NDDF |
| 015413 | NDDF |
| 704459002 | SNOMEDCT_US |
| 704460007 | SNOMEDCT_US |
| 715600003 | SNOMEDCT_US |
| C2934193 | UMLSCUI |
| CHEMBL2105743 | ChEMBL_ID |
| 11504295 | PUBCHEM_CID |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| Stiolto Respimat | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0597-0155 | SPRAY, METERED | 2.74 ug | RESPIRATORY (INHALATION) | NDA | 31 sections |
| Stiolto Respimat | HUMAN PRESCRIPTION DRUG LABEL | 2 | 0597-0155 | SPRAY, METERED | 2.74 ug | RESPIRATORY (INHALATION) | NDA | 31 sections |
| Striverdi Respimat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0597-0192 | SPRAY, METERED | 2.50 ug | RESPIRATORY (INHALATION) | NDA | 31 sections |
| Striverdi Respimat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0597-0192 | SPRAY, METERED | 2.50 ug | RESPIRATORY (INHALATION) | NDA | 31 sections |