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olodaterol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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 |
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.881 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 13.521 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.259 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 4.102 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 31.520 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 62.720 | % | High | 1 |
| herg | hERG pIC50 | 4.483 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 5.212 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 34.198 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 40.670 | % | High | 1 |
| kinase-safety-class | ACVR2B,AXL,BRAF,CAMK2D,CDK5,CDK9,EIF2AK3,ERBB2,GRK2,ITK,MAPK7,PDK1,PDK2,PDK4,PRKDC,TEK,TGFBR1 | 17 | |||
| kinase-selectivity-class | AXL,GRK2 | 2 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 2.183 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 2.742 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 71.121 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 37.920 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 4.603 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 52.650 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.009 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 52.360 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 80.580 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 39.070 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 810.961 | uM | High | 1 |
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 | 50.84 | 32.58 | 29 | 842 | 255201 | 110333227 |
| Asthma-chronic obstructive pulmonary disease overlap syndrome | 37.84 | 32.58 | 9 | 862 | 6335 | 110582093 |
| Total lung capacity increased | 34.41 | 32.58 | 8 | 863 | 5104 | 110583324 |
| Dyspnoea | 33.41 | 32.58 | 42 | 829 | 1106830 | 109481598 |
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 | D001993 | Bronchodilator Agents |
| MeSH PA | D018373 | Peripheral Nervous System Agents |
| MeSH PA | D018927 | Anti-Asthmatic Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| FDA EPC | N0000175779 | beta2-Adrenergic Agonist |
| CHEBI has role | CHEBI:35522 | β-adrenergic agonist |
| CHEBI has role | CHEBI:35523 | bronchodilator agent |
| CHEBI has role | CHEBI:65023 | anti-asthmatic agent |
Related Drugs by ATC class:
R03AC Selective beta-2-adrenoreceptor agonists 17 drugs
R03AL Adrenergics in combination with anticholinergics incl. triple combinations with corticosteroids 14 drugs
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)
None
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 |
| 4033628 | VANDF |
| 4033629 | VANDF |
| CHEBI:82700 | CHEBI |
| DZQ | PDB_CHEM_ID |
| CHEMBL605846 | ChEMBL_ID |
| CHEMBL2105743 | ChEMBL_ID |
| C549647 | MESH_SUPPLEMENTAL_RECORD_UI |
| 7543 | IUPHAR_LIGAND_ID |
| 869477-96-3 | SECONDARY_CAS_RN |
| 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 |
| 9174 | INN_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 |
| Striverdi Respimat | HUMAN PRESCRIPTION DRUG LABEL | 1 | 0597-0192 | SPRAY, METERED | 2.50 ug | RESPIRATORY (INHALATION) | NDA | 31 sections |