arformoterol Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
bronchodilators, phenethylamine derivatives 4943 67346-49-0

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • arformoterol
  • arformoterol tartrate
  • brovana
  • CGP-25827A
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
  • Molecular weight: 344.41
  • Formula: C19H24N2O4
  • CLOGP: 1.26
  • LIPINSKI: 0
  • HAC: 6
  • HDO: 4
  • TPSA: 90.82
  • ALOGS: -3.92
  • ROTB: 8

  • Status: ONP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

None

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Oct. 6, 2006 FDA SUNOVION

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Chronic obstructive pulmonary disease 99.89 28.14 43 1281 57590 46627148
Dyspnoea 52.24 28.14 68 1256 515480 46169258
Pneumonia 35.38 28.14 48 1276 376272 46308466

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Chronic obstructive pulmonary disease 94.17 33.38 36 628 46090 29905724
Dyspnoea 62.49 33.38 54 610 333241 29618573

Pharmacologic Action:

SourceCodeDescription
FDA MoA N0000009922 Adrenergic beta2-Agonists
FDA EPC N0000175779 beta2-Adrenergic Agonist
MeSH PA D018663 Adrenergic Agents
MeSH PA D000322 Adrenergic Agonists
MeSH PA D058666 Adrenergic beta-2 Receptor Agonists
MeSH PA D000318 Adrenergic beta-Agonists
MeSH PA D018927 Anti-Asthmatic Agents
MeSH PA D001993 Bronchodilator Agents
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D019141 Respiratory System Agents
CHEBI has role CHEBI:35522 beta-adrenergic receptor agonist
CHEBI has role CHEBI:35523 bronchodilator agents
CHEBI has role CHEBI:49167 anti-asthmatic agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Chronic obstructive lung disease indication 13645005 DOID:3083
Chronic bronchitis indication 63480004 DOID:6132
Pulmonary emphysema indication 87433001

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (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:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Beta-2 adrenergic receptor GPCR AGONIST Kd 8.54 SCIENTIFIC LITERATURE DRUG LABEL
Beta-1 adrenergic receptor GPCR AGONIST Kd 6.95 SCIENTIFIC LITERATURE
Beta-3 adrenergic receptor GPCR EC50 7.60 CHEMBL
Beta-2 adrenergic receptor GPCR EC50 9.90 CHEMBL

External reference:

IDSource
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
CHEMBL1951071 ChEMBL_ID
CHEMBL1200811 ChEMBL_ID
CHEMBL3989798 ChEMBL_ID
DB01274 DRUGBANK_ID
D000068759 MESH_DESCRIPTOR_UI
3083544 PUBCHEM_CID
8398 INN_ID
7479 IUPHAR_LIGAND_ID
304962 RXNORM
88699 MMSL
d05893 MMSL
011766 NDDF
011767 NDDF
423317005 SNOMEDCT_US
423347007 SNOMEDCT_US
427097003 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Brovana HUMAN PRESCRIPTION DRUG LABEL 1 63402-911 SOLUTION 15 ug RESPIRATORY (INHALATION) NDA 32 sections
ARFORMOTEROL TARTRATE HUMAN PRESCRIPTION DRUG LABEL 1 68462-833 SOLUTION 15 ug RESPIRATORY (INHALATION) ANDA 27 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 23 sections
Arformoterol Tartrate HUMAN PRESCRIPTION DRUG LABEL 1 70748-257 SOLUTION 15 ug RESPIRATORY (INHALATION) NDA authorized generic 27 sections