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arformoterol 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |
| Stem definition | Drug id | CAS RN |
|---|---|---|
| bronchodilators, phenethylamine derivatives | 4943 | 67346-49-0 |
Description:
| Molecule | Description |
|---|---|
|
Synonyms:
|
the (R,R)-enantiomer of formoterol, is a selective long-acting beta2-adrenergic receptor agonist (beta2-agonist) that has two-fold greater potency than racemic formoterol
Legend: OFP - off patent OFM - off market ONP - on patent |
Drug dosage:
None
ADMET properties:
None
Predicted pharmacokinetic/toxicological properties (PK-AZ):
| Property | Description | Value | Unit | Confidence | Similarity |
|---|---|---|---|---|---|
| azlogd74 | LogD at pH 7.4 | 0.557 | High | 1 | |
| caco2-efflux | Caco-2 efflux ratio (BA/AB) | 12.023 | High | 1 | |
| caco2-intrinsic-papp | Caco-2 intrinsic apparent permeability | 0.662 | 10^-6 cm/s | High | 1 |
| dh-clint | Dog hepatocyte intrinsic clearance | 4.864 | uL/min/10^6 cells | High | 1 |
| dppb | Dog plasma protein binding (% unbound) | 51.320 | % | High | 1 |
| fcs-ppb | Fetal calf serum protein binding (% unbound) | 56.690 | % | High | 1 |
| herg | hERG pIC50 | 4.404 | pIC50 | High | 1 |
| hh-clint | Human hepatocyte intrinsic clearance | 3.548 | uL/min/10^6 cells | High | 1 |
| hlm-clint | Human liver microsomal intrinsic clearance | 7.745 | uL/min/mg protein | High | 1 |
| hppb | Human plasma protein binding (% unbound) | 54.590 | % | High | 1 |
| kinase-safety-class | ACVR2A,ACVR2B,AKT2,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EGFR,EIF2AK3,EPHB4,ERBB2,GRK2,GRK3,IGF1R,ITK,JAK2,JAK3,KDR,KIT,MAP2K6,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MTOR,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIM2,PLK1,PRKCD,PRKDC,SIK2,SIK3,STK33,SYK,TEK,TGFBR1,TTK,ZAP70 | 51 | |||
| kinase-selectivity-class | AXL,BRAF,EIF2AK3,EPHB4,ERBB2,GRK2,MAP2K6,SIK2,STK33,TEK | 10 | |||
| mdck-mdr1-bcrp-efflux | MDCK-MDR1-BCRP efflux ratio | 4.285 | High | 1 | |
| mdck-mdr1-efflux | MDCK-MDR1 efflux ratio | 3.327 | High | 1 | |
| mh-clint | Mouse hepatocyte intrinsic clearance | 59.156 | High | 1 | |
| mppb | Mouse plasma protein binding (% unbound) | 51.320 | High | 1 | |
| nih-mdck-mdr1-efflux | NIH MDCK-MDR1 efflux ratio | 5.212 | High | 1 | |
| pfas-class | PFAS structural alert (1 = True, 0 = False) | 0 | |||
| pppb | Pig plasma protein binding (% unbound) | 63.740 | % | High | 1 |
| rat-kpuu-brain | Rat brain Kpuu | 0.031 | % | High | 1 |
| rh-clint | Rat hepatocyte intrinsic clearance | 29.648 | uL/min/10^6 cells | High | 1 |
| rh-fuinc | Rat hepatocyte fraction unbound in incubation | 84.720 | % | High | 1 |
| rppb | Rat plasma protein binding (% unbound) | 50.630 | % | High | 1 |
| solubility-dd | Solubility at pH 7.4 in DMSO | 891.251 | uM | High | 1 |
Approvals:
| Date | Agency | Company | Orphan |
|---|---|---|---|
| Oct. 6, 2006 | FDA | SUNOVION |
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 |
|---|---|---|---|---|---|---|
| Chronic obstructive pulmonary disease | 80.55 | 26.64 | 36 | 1789 | 73793 | 90552829 |
| Dyspnoea | 47.42 | 26.64 | 72 | 1753 | 880883 | 89745739 |
| Pneumonia | 35.40 | 26.64 | 53 | 1772 | 638006 | 89988616 |
| Bronchitis | 34.86 | 26.64 | 27 | 1798 | 152900 | 90473722 |
| Cough | 31.71 | 26.64 | 38 | 1787 | 368924 | 90257698 |
| Death | 29.77 | 26.64 | 41 | 1784 | 456510 | 90170112 |
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 |
|---|---|---|---|---|---|---|
| Dyspnoea | 76.11 | 31.31 | 64 | 748 | 442557 | 42177966 |
| Chronic obstructive pulmonary disease | 43.42 | 31.31 | 22 | 790 | 63092 | 42557431 |
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 |
|---|---|---|---|---|---|---|
| Chronic obstructive pulmonary disease | 105.49 | 23.90 | 50 | 2342 | 109108 | 110477799 |
| Dyspnoea | 72.57 | 23.90 | 103 | 2289 | 1106769 | 109480138 |
| Pneumonia | 39.62 | 23.90 | 69 | 2323 | 876645 | 109710262 |
| Bronchitis | 32.49 | 23.90 | 27 | 2365 | 157005 | 110429902 |
| Death | 25.19 | 23.90 | 50 | 2342 | 698819 | 109888088 |
| Acute respiratory failure | 24.56 | 23.90 | 17 | 2375 | 75243 | 110511664 |
FDA Adverse Event Reporting System (Pediatric)
None
Pharmacologic Action:
| Source | Code | Description |
|---|---|---|
| FDA MoA | N0000009922 | Adrenergic beta2-Agonists |
| MeSH PA | D000318 | Adrenergic beta-Agonists |
| MeSH PA | D001993 | Bronchodilator Agents |
| MeSH PA | D018377 | Neurotransmitter Agents |
| MeSH PA | D018663 | Adrenergic Agents |
| MeSH PA | D018927 | Anti-Asthmatic Agents |
| MeSH PA | D019141 | Respiratory System Agents |
| MeSH PA | D058666 | Adrenergic beta-2 Receptor Agonists |
| 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:49167 | anti-asthmatic drug |
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 |
| Chronic bronchitis | indication | 63480004 | DOID:6132 |
| Pulmonary emphysema | indication | 87433001 |
🐶 Veterinary Drug Use
None
🐶 Veterinary products
None
Acid dissociation constants calculated using MoKa v3.0.0
| Dissociation level | Dissociation constant | Type (acidic/basic) |
|---|---|---|
| pKa1 | 9.23 | acidic |
| pKa2 | 12.47 | acidic |
| pKa3 | 8.49 | 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 | AGONIST | Kd | 8.54 | SCIENTIFIC LITERATURE | DRUG LABEL | |||
| Beta-3 adrenergic receptor | GPCR | EC50 | 7.60 | CHEMBL | |||||
| Beta-1 adrenergic receptor | GPCR | AGONIST | Kd | 6.95 | SCIENTIFIC LITERATURE | ||||
| Beta-2 adrenergic receptor | GPCR | EC50 | 9.90 | CHEMBL |
External reference:
| ID | Source |
|---|---|
| F91H02EBWT | UNII |
| D02981 | KEGG_DRUG |
| 4026108 | VUID |
| N0000176102 | NUI |
| 200815-49-2 | SECONDARY_CAS_RN |
| 4026108 | VANDF |
| 4026109 | VANDF |
| C0969589 | UMLSCUI |
| CHEBI:408174 | CHEBI |
| H98 | PDB_CHEM_ID |
| CHEMBL1363 | ChEMBL_ID |
| 3083544 | PUBCHEM_CID |
| DB01274 | DRUGBANK_ID |
| CHEMBL1951071 | ChEMBL_ID |
| CHEMBL3989798 | ChEMBL_ID |
| D000068759 | MESH_DESCRIPTOR_UI |
| 8398 | INN_ID |
| 7479 | IUPHAR_LIGAND_ID |
| 304962 | RXNORM |
| 347152 | MMSL |
| 88699 | MMSL |
| d05893 | MMSL |
| 011766 | NDDF |
| 011767 | NDDF |
| 423317005 | SNOMEDCT_US |
| 423347007 | SNOMEDCT_US |
| 427097003 | SNOMEDCT_US |
| F91H02EBWT | INXIGHT DRUGS |
Pharmaceutical products:
| Product | Category | Ingredients | NDC | Form | Quantity | Route | Marketing | Label |
|---|---|---|---|---|---|---|---|---|
| BROVANA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 27437-055 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | NDA | 28 sections |
| BROVANA | HUMAN PRESCRIPTION DRUG LABEL | 1 | 27437-060 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | NDA | 28 sections |
| Arformoterol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 42571-464 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 26 sections |
| arformoterol tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 43598-777 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 31 sections |
| Arformoterol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 50742-395 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 24 sections |
| Arformoterol Tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 60687-770 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 29 sections |
| Arformoterol tartrate | Human Prescription Drug Label | 1 | 62332-633 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 27 sections |
| Arformoterol Tartrate | Human Prescription Drug Label | 1 | 62756-277 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 30 sections |
| arformoterol tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 69097-168 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 27 sections |
| Arformoterol Tartrate Inhalation | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70436-151 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 24 sections |
| Arformoterol tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70748-175 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 27 sections |
| arformoterol tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 70756-612 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 25 sections |
| Arformoterol tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72266-259 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 20 sections |
| arformoterol tartrate | HUMAN PRESCRIPTION DRUG LABEL | 1 | 72603-208 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 25 sections |
| Arformoterol Tartrate Inhalation | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73043-052 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 24 sections |
| Arformoterol Tartrate Inhalation Solution | HUMAN PRESCRIPTION DRUG LABEL | 1 | 73289-0072 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 31 sections |
| Arformoterol Tartrate Inhalation Solution | HUMAN PRESCRIPTION DRUG LABEL | 1 | 76204-026 | SOLUTION | 15 ug | RESPIRATORY (INHALATION) | ANDA | 32 sections |