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Identification
NameFormoterol
Accession NumberDB00983  (APRD00641)
TypeSmall Molecule
GroupsApproved, Investigational
DescriptionFormoterol is a long-acting (12 hours) beta2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD). Inhaled formoterol works like other beta2-agonists, causing bronchodilatation through relaxation of the smooth muscle in the airway so as to treat the exacerbation of asthma.
Structure
Thumb
Synonyms
2'-Hydroxy-5'-(1-hydroxy-2-((P-methoxy-alpha-methylphenethyl)amino)ethyl)formanilide
2'-Hydroxy-5'-{1-hydroxy-2-[(P-methoxy-alpha-methylphenethyl)amino]ethyl}formanilide
Formoterolum
N-[2-Hydroxy-5-(1-hydroxy-2-{[2-(4-methoxyphenyl)-1-methylethyl]amino}ethyl)phenyl]formamide
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
ForadilCapsule12 ug/1Respiratory (inhalation)Physicians Total Care, Inc.2004-05-28Not applicableUs
ForadilCapsule12 ug/1Respiratory (inhalation)Merck Sharp & Dohme Corp.2001-02-162017-01-31Us
ForadilCapsule12 ug/1Respiratory (inhalation)Merck Sharp & Dohme Corp.2001-02-162017-01-31Us
Foradil Dry Powder Capsules for InhalationCapsule12 mcgRespiratory (inhalation)Novartis Pharmaceuticals Canada Inc1997-07-08Not applicableCanada
Oxeze TurbuhalerPowder12 mcgRespiratory (inhalation)Astrazeneca Canada Inc1998-03-12Not applicableCanada
Oxeze TurbuhalerPowder6 mcgRespiratory (inhalation)Astrazeneca Canada Inc1998-03-12Not applicableCanada
PerforomistSolution20 ug/2mLRespiratory (inhalation)Mylan Specialty L.P.2007-10-01Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International Brands
NameCompany
ForadileNot Available
Oxis TurbuhalerNot Available
Brand mixtures
NameLabellerIngredients
Bevespi AerosphereAstra Zeneca Pharmaceuticals Lp
Duaklir GenuairAstrazeneca Canada Inc
DuleraMerck Sharp & Dohme Corp.
SymbicortAstra Zeneca Lp
Symbicort 100 TurbuhalerAstrazeneca Canada Inc
Symbicort 200 TurbuhalerAstrazeneca Canada Inc
Symbicort Forte TurbuhalerAstrazeneca Canada Inc
ZenhaleMerck Canada Inc
Salts
Name/CASStructureProperties
Formoterol fumarate
ThumbNot applicableDBSALT001371
Formoterol fumarate dihydrate
Thumb
  • InChI Key: PAANKGSMSCGEOJ-FJGATTJMSA-N
  • Monoisotopic Mass: 496.205695238
  • Average Mass: 496.513
DBSALT001072
Categories
UNII5ZZ84GCW8B
CAS number73573-87-2
WeightAverage: 344.4049
Monoisotopic: 344.173607266
Chemical FormulaC19H24N2O4
InChI KeyBPZSYCZIITTYBL-UHFFFAOYSA-N
InChI
InChI=1S/C19H24N2O4/c1-13(9-14-3-6-16(25-2)7-4-14)20-11-19(24)15-5-8-18(23)17(10-15)21-12-22/h3-8,10,12-13,19-20,23-24H,9,11H2,1-2H3,(H,21,22)
IUPAC Name
N-[2-hydroxy-5-(1-hydroxy-2-{[1-(4-methoxyphenyl)propan-2-yl]amino}ethyl)phenyl]formamide
SMILES
COC1=CC=C(CC(C)NCC(O)C2=CC(NC=O)=C(O)C=C2)C=C1
Pharmacology
IndicationFor use as long-term maintenance treatment of asthma in patients 6 years of age and older with reversible obstructive airways disease, including patients with symptoms of nocturnal asthma, who are using optimal corticosteroid treatment and experiencing regular or frequent breakthrough symptoms requiring use of a short-acting bronchodilator. Not indicated for asthma that can be successfully managed with occasional use of an inhaled, short-acting beta2-adrenergic agonist. Also used for the prevention of exercise-induced bronchospasm, as well as long-term treatment of bronchospasm associated with COPD.
Structured Indications
PharmacodynamicsFormoterol is a long-acting selective beta2-adrenergic receptor agonist (beta2-agonist). Inhaled formoterol fumarate acts locally in the lung as a bronchodilator. In vitro studies have shown that formoterol has more than 200-fold greater agonist activity at beta2-receptors than at beta1- receptors. Although beta2-receptors are the predominant adrenergic receptors in bronchial smooth muscle and beta1-receptors are the predominant receptors in the heart, there are also beta2-receptors in the human heart comprising 10%-50% of the total beta-adrenergic receptors. The precise function of these receptors has not been established, but they raise the possibility that even highly selective beta2- agonists may have cardiac effects.
Mechanism of actionThe pharmacologic effects of beta2-adrenoceptor agonist drugs, including formoterol, are at least in part attributable to stimulation of intracellular adenyl cyclase, the enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3', 5'-adenosine monophosphate (cyclic AMP). Increased cyclic AMP levels cause relaxation of bronchial smooth muscle and inhibits the release of pro-inflammatory mast-cell mediators such as histamine and leukotrienes. Formoterol also inhibits histamine-induced plasma albumin extravasation in anesthetized guinea pigs and inhibits allergen-induced eosinophil influx in dogs with airway hyper-responsiveness. The relevance of these in vitro and animal findings to humans is unknown.
TargetKindPharmacological actionActionsOrganismUniProt ID
Beta-2 adrenergic receptorProteinyes
agonist
HumanP07550 details
Related Articles
AbsorptionRapidly absorbed into plasma following administration by oral inhalation. It is likely that the majority of the inhaled formoterol delivered is swallowed and then absorbed from the gastrointestinal tract.
Volume of distributionNot Available
Protein bindingThe binding of formoterol to human plasma proteins in vitro was 61%-64% at concentrations from 0.1 to 100 ng/mL. Binding to human serum albumin in vitro was 31%-38% over a range of 5 to 500 ng/mL. The concentrations of formoterol used to assess the plasma protein binding were higher than those achieved in plasma following inhalation of a single 120 µg dose.
Metabolism

Metabolized primarily by direct glucuronidation at either the phenolic or aliphatic hydroxyl group and O-demethylation followed by glucuronide conjugation at either phenolic hydroxyl groups. Minor pathways involve sulfate conjugation of formoterol and deformylation followed by sulfate conjugation. The most prominent pathway involves direct conjugation at the phenolic hydroxyl group. The second major pathway involves O-demethylation followed by conjugation at the phenolic 2'-hydroxyl group. Four cytochrome P450 isozymes (CYP2D6, CYP2C19, CYP2C9 and CYP2A6) are involved in the O-demethylation of formoterol.

Route of eliminationFollowing inhalation of a 12 mcg or 24 mcg dose by 16 patients with asthma, about 10% and 15%-18% of the total dose was excreted in the urine as unchanged formoterol and direct conjugates of formoterol, respectively.
Half life10 hours
Clearance
  • Renal cl=150 mL/min [Healty subjects receiving oral administration of 80 mcg]
ToxicityAn overdosage is likely to lead to effects that are typical of ß2-adrenergic stimulants: nausea, vomiting, headache, tremor, somnolence, palpitations, tachycardia, ventricular arrhythmias, metabolic acidosis, hypokalemia, hyperglycemia.
Affected organisms
  • Humans and other mammals
PathwaysNot Available
SNP Mediated EffectsNot Available
SNP Mediated Adverse Drug ReactionsNot Available
Interactions
Drug Interactions
DrugInteractionDrug group
7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINEThe risk or severity of adverse effects can be increased when 7,8-DICHLORO-1,2,3,4-TETRAHYDROISOQUINOLINE is combined with Formoterol.Experimental
AbirateroneThe serum concentration of Formoterol can be increased when it is combined with Abiraterone.Approved
AcebutololAcebutolol may decrease the bronchodilatory activities of Formoterol.Approved
AlfuzosinAlfuzosin may decrease the vasoconstricting activities of Formoterol.Approved, Investigational
AlprenololAlprenolol may decrease the bronchodilatory activities of Formoterol.Approved, Withdrawn
Ambroxol acefyllinateThe risk or severity of adverse effects can be increased when Ambroxol acefyllinate is combined with Formoterol.Experimental
AmineptineThe risk or severity of adverse effects can be increased when Amineptine is combined with Formoterol.Illicit, Withdrawn
AminophyllineThe risk or severity of adverse effects can be increased when Aminophylline is combined with Formoterol.Approved
AmiodaroneFormoterol may increase the QTc-prolonging activities of Amiodarone.Approved, Investigational
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Formoterol.Approved
AnagrelideFormoterol may increase the QTc-prolonging activities of Anagrelide.Approved
AprepitantThe metabolism of Formoterol can be increased when combined with Aprepitant.Approved, Investigational
ArmodafinilThe metabolism of Formoterol can be decreased when combined with Armodafinil.Approved, Investigational
Arsenic trioxideFormoterol may increase the QTc-prolonging activities of Arsenic trioxide.Approved, Investigational
ArtemetherFormoterol may increase the QTc-prolonging activities of Artemether.Approved
AsenapineFormoterol may increase the QTc-prolonging activities of Asenapine.Approved
AtenololAtenolol may decrease the bronchodilatory activities of Formoterol.Approved
AtomoxetineAtomoxetine may increase the tachycardic activities of Formoterol.Approved
AtosibanThe risk or severity of adverse effects can be increased when Formoterol is combined with Atosiban.Approved
AzithromycinFormoterol may increase the QTc-prolonging activities of Azithromycin.Approved
BedaquilineFormoterol may increase the QTc-prolonging activities of Bedaquiline.Approved
BendroflumethiazideFormoterol may increase the hypokalemic activities of Bendroflumethiazide.Approved
BenmoxinThe risk or severity of adverse effects can be increased when Benmoxin is combined with Formoterol.Withdrawn
Benzylpenicilloyl PolylysineFormoterol may decrease effectiveness of Benzylpenicilloyl Polylysine as a diagnostic agent.Approved
BetahistineThe therapeutic efficacy of Formoterol can be decreased when used in combination with Betahistine.Approved
BetaxololThe metabolism of Formoterol can be decreased when combined with Betaxolol.Approved
BisoprololBisoprolol may decrease the bronchodilatory activities of Formoterol.Approved
BopindololBopindolol may decrease the bronchodilatory activities of Formoterol.Approved
BortezomibThe metabolism of Formoterol can be decreased when combined with Bortezomib.Approved, Investigational
BromocriptineBromocriptine may increase the hypertensive activities of Formoterol.Approved, Investigational
BucindololBucindolol may decrease the vasoconstricting activities of Formoterol.Investigational
BumetanideFormoterol may increase the hypokalemic activities of Bumetanide.Approved
BupranololBupranolol may decrease the bronchodilatory activities of Formoterol.Approved
BupropionThe metabolism of Formoterol can be decreased when combined with Bupropion.Approved
CabergolineCabergoline may increase the hypertensive activities of Formoterol.Approved
CaffeineThe risk or severity of adverse effects can be increased when Caffeine is combined with Formoterol.Approved
CapecitabineThe metabolism of Formoterol can be decreased when combined with Capecitabine.Approved, Investigational
CarbamazepineThe metabolism of Formoterol can be increased when combined with Carbamazepine.Approved, Investigational
CaroxazoneThe risk or severity of adverse effects can be increased when Caroxazone is combined with Formoterol.Withdrawn
CarteololCarteolol may decrease the bronchodilatory activities of Formoterol.Approved
CarvedilolCarvedilol may decrease the vasoconstricting activities of Formoterol.Approved, Investigational
CelecoxibThe metabolism of Formoterol can be decreased when combined with Celecoxib.Approved, Investigational
CeliprololCeliprolol may decrease the bronchodilatory activities of Formoterol.Approved, Investigational
CeritinibThe serum concentration of Formoterol can be increased when it is combined with Ceritinib.Approved
ChloramphenicolThe metabolism of Formoterol can be decreased when combined with Chloramphenicol.Approved, Vet Approved
ChloroquineFormoterol may increase the QTc-prolonging activities of Chloroquine.Approved, Vet Approved
ChlorothiazideFormoterol may increase the hypokalemic activities of Chlorothiazide.Approved, Vet Approved
ChlorpromazineFormoterol may increase the QTc-prolonging activities of Chlorpromazine.Approved, Vet Approved
ChlorthalidoneFormoterol may increase the hypokalemic activities of Chlorthalidone.Approved
CholecalciferolThe metabolism of Formoterol can be decreased when combined with Cholecalciferol.Approved, Nutraceutical
CimetidineThe metabolism of Formoterol can be decreased when combined with Cimetidine.Approved
CinacalcetThe metabolism of Formoterol can be decreased when combined with Cinacalcet.Approved
CiprofloxacinFormoterol may increase the QTc-prolonging activities of Ciprofloxacin.Approved, Investigational
CisaprideFormoterol may increase the QTc-prolonging activities of Cisapride.Approved, Investigational, Withdrawn
CitalopramFormoterol may increase the QTc-prolonging activities of Citalopram.Approved
ClarithromycinFormoterol may increase the QTc-prolonging activities of Clarithromycin.Approved
ClemastineThe metabolism of Formoterol can be decreased when combined with Clemastine.Approved
ClobazamThe metabolism of Formoterol can be decreased when combined with Clobazam.Approved, Illicit
ClomipramineThe metabolism of Formoterol can be decreased when combined with Clomipramine.Approved, Vet Approved
ClotrimazoleThe metabolism of Formoterol can be decreased when combined with Clotrimazole.Approved, Vet Approved
ClozapineFormoterol may increase the QTc-prolonging activities of Clozapine.Approved
CobicistatThe serum concentration of Formoterol can be increased when it is combined with Cobicistat.Approved
CocaineThe metabolism of Formoterol can be decreased when combined with Cocaine.Approved, Illicit
CrizotinibFormoterol may increase the QTc-prolonging activities of Crizotinib.Approved
CyclobenzaprineThe risk or severity of adverse effects can be increased when Cyclobenzaprine is combined with Formoterol.Approved
CyclosporineThe metabolism of Formoterol can be decreased when combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Formoterol can be decreased when it is combined with Dabrafenib.Approved
DarifenacinThe metabolism of Formoterol can be decreased when combined with Darifenacin.Approved, Investigational
DarunavirThe serum concentration of Formoterol can be increased when it is combined with Darunavir.Approved
DelavirdineThe metabolism of Formoterol can be decreased when combined with Delavirdine.Approved
DesfluraneDesflurane may increase the arrhythmogenic activities of Formoterol.Approved
DesipramineThe metabolism of Formoterol can be decreased when combined with Desipramine.Approved
DesvenlafaxineDesvenlafaxine may increase the tachycardic activities of Formoterol.Approved
DihydroergotamineDihydroergotamine may increase the hypertensive activities of Formoterol.Approved
DiphenhydramineThe metabolism of Formoterol can be decreased when combined with Diphenhydramine.Approved
DisopyramideFormoterol may increase the QTc-prolonging activities of Disopyramide.Approved
DofetilideFormoterol may increase the QTc-prolonging activities of Dofetilide.Approved
DolasetronFormoterol may increase the QTc-prolonging activities of Dolasetron.Approved
DomperidoneFormoterol may increase the QTc-prolonging activities of Domperidone.Approved, Investigational, Vet Approved
DosulepinThe risk or severity of adverse effects can be increased when Dosulepin is combined with Formoterol.Approved
DoxazosinDoxazosin may decrease the vasoconstricting activities of Formoterol.Approved
DoxepinThe risk or severity of adverse effects can be increased when Doxepin is combined with Formoterol.Approved
DronedaroneFormoterol may increase the QTc-prolonging activities of Dronedarone.Approved
DroperidolFormoterol may increase the QTc-prolonging activities of Droperidol.Approved, Vet Approved
DuloxetineDuloxetine may increase the tachycardic activities of Formoterol.Approved
DyphyllineThe risk or severity of adverse effects can be increased when Dyphylline is combined with Formoterol.Approved
EfavirenzThe metabolism of Formoterol can be decreased when combined with Efavirenz.Approved, Investigational
EliglustatFormoterol may increase the QTc-prolonging activities of Eliglustat.Approved
EnfluraneEnflurane may increase the arrhythmogenic activities of Formoterol.Approved, Vet Approved
Ergoloid mesylateErgoloid mesylate may increase the hypertensive activities of Formoterol.Approved
ErgonovineErgonovine may increase the hypertensive activities of Formoterol.Approved
ErgotamineErgotamine may increase the hypertensive activities of Formoterol.Approved
ErythromycinFormoterol may increase the QTc-prolonging activities of Erythromycin.Approved, Vet Approved
EscitalopramFormoterol may increase the QTc-prolonging activities of Escitalopram.Approved, Investigational
Eslicarbazepine acetateThe metabolism of Formoterol can be decreased when combined with Eslicarbazepine acetate.Approved
EsmirtazapineThe risk or severity of adverse effects can be increased when Esmirtazapine is combined with Formoterol.Investigational
EsmololEsmolol may decrease the bronchodilatory activities of Formoterol.Approved
EsomeprazoleThe metabolism of Formoterol can be decreased when combined with Esomeprazole.Approved, Investigational
Etacrynic acidFormoterol may increase the hypokalemic activities of Etacrynic acid.Approved
EtravirineThe metabolism of Formoterol can be decreased when combined with Etravirine.Approved
FlecainideFormoterol may increase the QTc-prolonging activities of Flecainide.Approved, Withdrawn
FloxuridineThe metabolism of Formoterol can be decreased when combined with Floxuridine.Approved
FluconazoleThe metabolism of Formoterol can be decreased when combined with Fluconazole.Approved
FluorouracilThe metabolism of Formoterol can be decreased when combined with Fluorouracil.Approved
FluoxetineFormoterol may increase the QTc-prolonging activities of Fluoxetine.Approved, Vet Approved
FlupentixolFormoterol may increase the QTc-prolonging activities of Flupentixol.Approved, Withdrawn
FluvastatinThe metabolism of Formoterol can be decreased when combined with Fluvastatin.Approved
FluvoxamineThe metabolism of Formoterol can be decreased when combined with Fluvoxamine.Approved, Investigational
FosphenytoinThe metabolism of Formoterol can be increased when combined with Fosphenytoin.Approved
FurazolidoneThe risk or severity of adverse effects can be increased when Furazolidone is combined with Formoterol.Approved, Vet Approved
FurosemideFormoterol may increase the hypokalemic activities of Furosemide.Approved, Vet Approved
Gadobenic acidFormoterol may increase the QTc-prolonging activities of Gadobenic acid.Approved
GemfibrozilThe metabolism of Formoterol can be decreased when combined with Gemfibrozil.Approved
GemifloxacinFormoterol may increase the QTc-prolonging activities of Gemifloxacin.Approved, Investigational
GoserelinFormoterol may increase the QTc-prolonging activities of Goserelin.Approved
GranisetronFormoterol may increase the QTc-prolonging activities of Granisetron.Approved, Investigational
HaloperidolFormoterol may increase the QTc-prolonging activities of Haloperidol.Approved
HalothaneHalothane may increase the arrhythmogenic activities of Formoterol.Approved, Vet Approved
HydracarbazineThe risk or severity of adverse effects can be increased when Hydracarbazine is combined with Formoterol.Approved
HydrochlorothiazideFormoterol may increase the hypokalemic activities of Hydrochlorothiazide.Approved, Vet Approved
HydroflumethiazideFormoterol may increase the hypokalemic activities of Hydroflumethiazide.Approved
IbutilideFormoterol may increase the QTc-prolonging activities of Ibutilide.Approved
IloperidoneFormoterol may increase the QTc-prolonging activities of Iloperidone.Approved
ImipramineThe metabolism of Formoterol can be decreased when combined with Imipramine.Approved
IndapamideFormoterol may increase the hypokalemic activities of Indapamide.Approved
IndinavirThe metabolism of Formoterol can be decreased when combined with Indinavir.Approved
IndoraminIndoramin may decrease the vasoconstricting activities of Formoterol.Withdrawn
IproclozideThe risk or severity of adverse effects can be increased when Iproclozide is combined with Formoterol.Withdrawn
IproniazidThe risk or severity of adverse effects can be increased when Iproniazid is combined with Formoterol.Withdrawn
IrbesartanThe metabolism of Formoterol can be decreased when combined with Irbesartan.Approved, Investigational
IsocarboxazidThe risk or severity of adverse effects can be increased when Isocarboxazid is combined with Formoterol.Approved
IsofluraneIsoflurane may increase the arrhythmogenic activities of Formoterol.Approved, Vet Approved
IsoniazidThe metabolism of Formoterol can be decreased when combined with Isoniazid.Approved
KetoconazoleThe metabolism of Formoterol can be decreased when combined with Ketoconazole.Approved, Investigational
LabetalolLabetalol may decrease the vasoconstricting activities of Formoterol.Approved
LeflunomideThe metabolism of Formoterol can be decreased when combined with Leflunomide.Approved, Investigational
LenvatinibFormoterol may increase the QTc-prolonging activities of Lenvatinib.Approved
LeuprolideFormoterol may increase the QTc-prolonging activities of Leuprolide.Approved, Investigational
LevofloxacinFormoterol may increase the QTc-prolonging activities of Levofloxacin.Approved, Investigational
LevomilnacipranLevomilnacipran may increase the tachycardic activities of Formoterol.Approved
LopinavirFormoterol may increase the QTc-prolonging activities of Lopinavir.Approved
LorcaserinThe metabolism of Formoterol can be decreased when combined with Lorcaserin.Approved
LosartanThe metabolism of Formoterol can be decreased when combined with Losartan.Approved
LovastatinThe metabolism of Formoterol can be decreased when combined with Lovastatin.Approved, Investigational
LoxapineThe risk or severity of adverse effects can be increased when Formoterol is combined with Loxapine.Approved
LuliconazoleThe serum concentration of Formoterol can be increased when it is combined with Luliconazole.Approved
LumacaftorThe serum concentration of Formoterol can be decreased when it is combined with Lumacaftor.Approved
LumefantrineFormoterol may increase the QTc-prolonging activities of Lumefantrine.Approved
MebanazineThe risk or severity of adverse effects can be increased when Mebanazine is combined with Formoterol.Withdrawn
MethadoneFormoterol may increase the QTc-prolonging activities of Methadone.Approved
MethotrimeprazineThe metabolism of Formoterol can be decreased when combined with Methotrimeprazine.Approved
MethoxyfluraneMethoxyflurane may increase the arrhythmogenic activities of Formoterol.Approved, Vet Approved
MethyclothiazideFormoterol may increase the hypokalemic activities of Methyclothiazide.Approved
Methylene blueThe risk or severity of adverse effects can be increased when Methylene blue is combined with Formoterol.Investigational
MetolazoneFormoterol may increase the hypokalemic activities of Metolazone.Approved
MetoprololThe metabolism of Formoterol can be decreased when combined with Metoprolol.Approved, Investigational
MifepristoneThe serum concentration of Formoterol can be increased when it is combined with Mifepristone.Approved, Investigational
MilnacipranMilnacipran may increase the tachycardic activities of Formoterol.Approved
MinaprineThe risk or severity of adverse effects can be increased when Minaprine is combined with Formoterol.Approved
MirabegronThe metabolism of Formoterol can be decreased when combined with Mirabegron.Approved
MirtazapineThe risk or severity of adverse effects can be increased when Mirtazapine is combined with Formoterol.Approved
MoclobemideThe metabolism of Formoterol can be decreased when combined with Moclobemide.Approved
ModafinilThe metabolism of Formoterol can be decreased when combined with Modafinil.Approved, Investigational
MoxifloxacinFormoterol may increase the QTc-prolonging activities of Moxifloxacin.Approved, Investigational
NadololNadolol may decrease the bronchodilatory activities of Formoterol.Approved
NebivololNebivolol may decrease the bronchodilatory activities of Formoterol.Approved, Investigational
NelfinavirThe metabolism of Formoterol can be decreased when combined with Nelfinavir.Approved
NevirapineThe metabolism of Formoterol can be decreased when combined with Nevirapine.Approved
NialamideThe risk or severity of adverse effects can be increased when Nialamide is combined with Formoterol.Withdrawn
NicardipineThe metabolism of Formoterol can be decreased when combined with Nicardipine.Approved
NicotineThe metabolism of Formoterol can be decreased when combined with Nicotine.Approved
NilotinibFormoterol may increase the QTc-prolonging activities of Nilotinib.Approved, Investigational
Nitrous oxideNitrous oxide may increase the arrhythmogenic activities of Formoterol.Approved, Vet Approved
NortriptylineThe risk or severity of adverse effects can be increased when Nortriptyline is combined with Formoterol.Approved
OctamoxinThe risk or severity of adverse effects can be increased when Octamoxin is combined with Formoterol.Withdrawn
OfloxacinFormoterol may increase the QTc-prolonging activities of Ofloxacin.Approved
OmeprazoleThe metabolism of Formoterol can be decreased when combined with Omeprazole.Approved, Investigational, Vet Approved
OndansetronFormoterol may increase the QTc-prolonging activities of Ondansetron.Approved
OpipramolThe risk or severity of adverse effects can be increased when Opipramol is combined with Formoterol.Investigational
OxprenololOxprenolol may decrease the bronchodilatory activities of Formoterol.Approved
PaliperidoneFormoterol may increase the QTc-prolonging activities of Paliperidone.Approved
PanobinostatThe serum concentration of Formoterol can be increased when it is combined with Panobinostat.Approved, Investigational
PantoprazoleThe metabolism of Formoterol can be decreased when combined with Pantoprazole.Approved
PargylineThe risk or severity of adverse effects can be increased when Pargyline is combined with Formoterol.Approved
ParoxetineThe metabolism of Formoterol can be decreased when combined with Paroxetine.Approved, Investigational
PazopanibFormoterol may increase the QTc-prolonging activities of Pazopanib.Approved
Peginterferon alfa-2bThe serum concentration of Formoterol can be decreased when it is combined with Peginterferon alfa-2b.Approved
PenbutololPenbutolol may decrease the bronchodilatory activities of Formoterol.Approved, Investigational
PentamidineFormoterol may increase the QTc-prolonging activities of Pentamidine.Approved
PentobarbitalThe metabolism of Formoterol can be increased when combined with Pentobarbital.Approved, Vet Approved
PerflutrenFormoterol may increase the QTc-prolonging activities of Perflutren.Approved
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Formoterol.Approved
PheniprazineThe risk or severity of adverse effects can be increased when Pheniprazine is combined with Formoterol.Withdrawn
PhenobarbitalThe metabolism of Formoterol can be increased when combined with Phenobarbital.Approved
PhenoxypropazineThe risk or severity of adverse effects can be increased when Phenoxypropazine is combined with Formoterol.Withdrawn
PhenytoinThe metabolism of Formoterol can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideFormoterol may increase the QTc-prolonging activities of Pimozide.Approved
PindololPindolol may decrease the bronchodilatory activities of Formoterol.Approved
PiretanideFormoterol may increase the hypokalemic activities of Piretanide.Experimental
PirlindoleThe risk or severity of adverse effects can be increased when Pirlindole is combined with Formoterol.Approved
PivhydrazineThe risk or severity of adverse effects can be increased when Pivhydrazine is combined with Formoterol.Withdrawn
PolythiazideFormoterol may increase the hypokalemic activities of Polythiazide.Approved
PrazosinPrazosin may decrease the vasoconstricting activities of Formoterol.Approved
PrimaquineFormoterol may increase the QTc-prolonging activities of Primaquine.Approved
PrimidoneThe metabolism of Formoterol can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideFormoterol may increase the QTc-prolonging activities of Procainamide.Approved
PromazineFormoterol may increase the QTc-prolonging activities of Promazine.Approved, Vet Approved
PropafenoneFormoterol may increase the QTc-prolonging activities of Propafenone.Approved
PropranololPropranolol may decrease the bronchodilatory activities of Formoterol.Approved, Investigational
ProtriptylineThe risk or severity of adverse effects can be increased when Protriptyline is combined with Formoterol.Approved
PyrimethamineThe metabolism of Formoterol can be decreased when combined with Pyrimethamine.Approved, Vet Approved
QuetiapineFormoterol may increase the QTc-prolonging activities of Quetiapine.Approved
QuinethazoneFormoterol may increase the hypokalemic activities of Quinethazone.Approved
QuinidineFormoterol may increase the QTc-prolonging activities of Quinidine.Approved
QuinineFormoterol may increase the QTc-prolonging activities of Quinine.Approved
RanolazineThe metabolism of Formoterol can be decreased when combined with Ranolazine.Approved, Investigational
RasagilineThe risk or severity of adverse effects can be increased when Rasagiline is combined with Formoterol.Approved
RifampicinThe metabolism of Formoterol can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Formoterol can be increased when combined with Rifapentine.Approved
RitonavirThe metabolism of Formoterol can be decreased when combined with Ritonavir.Approved, Investigational
RolapitantThe metabolism of Formoterol can be decreased when combined with Rolapitant.Approved
RopiniroleThe metabolism of Formoterol can be decreased when combined with Ropinirole.Approved, Investigational
SafrazineThe risk or severity of adverse effects can be increased when Safrazine is combined with Formoterol.Withdrawn
SaquinavirFormoterol may increase the QTc-prolonging activities of Saquinavir.Approved, Investigational
SecobarbitalThe metabolism of Formoterol can be increased when combined with Secobarbital.Approved, Vet Approved
SelegilineThe risk or severity of adverse effects can be increased when Selegiline is combined with Formoterol.Approved, Investigational, Vet Approved
SertralineThe metabolism of Formoterol can be decreased when combined with Sertraline.Approved
SevofluraneSevoflurane may increase the arrhythmogenic activities of Formoterol.Approved, Vet Approved
SildenafilThe metabolism of Formoterol can be decreased when combined with Sildenafil.Approved, Investigational
SilodosinSilodosin may decrease the vasoconstricting activities of Formoterol.Approved
SorafenibThe metabolism of Formoterol can be decreased when combined with Sorafenib.Approved, Investigational
SotalolSotalol may decrease the bronchodilatory activities of Formoterol.Approved
SpironolactoneSpironolactone may decrease the vasoconstricting activities of Formoterol.Approved
StiripentolThe metabolism of Formoterol can be decreased when combined with Stiripentol.Approved
SulfadiazineThe metabolism of Formoterol can be decreased when combined with Sulfadiazine.Approved, Vet Approved
SulfamethoxazoleThe metabolism of Formoterol can be decreased when combined with Sulfamethoxazole.Approved
SulfisoxazoleThe metabolism of Formoterol can be decreased when combined with Sulfisoxazole.Approved, Vet Approved
TamsulosinTamsulosin may decrease the vasoconstricting activities of Formoterol.Approved, Investigational
TelavancinFormoterol may increase the QTc-prolonging activities of Telavancin.Approved
TelithromycinFormoterol may increase the QTc-prolonging activities of Telithromycin.Approved
TerazosinTerazosin may decrease the vasoconstricting activities of Formoterol.Approved
TerbinafineThe metabolism of Formoterol can be decreased when combined with Terbinafine.Approved, Investigational, Vet Approved
TetrabenazineFormoterol may increase the QTc-prolonging activities of Tetrabenazine.Approved
TheophyllineThe risk or severity of adverse effects can be increased when Theophylline is combined with Formoterol.Approved
ThioridazineFormoterol may increase the QTc-prolonging activities of Thioridazine.Approved
TianeptineThe risk or severity of adverse effects can be increased when Tianeptine is combined with Formoterol.Approved
TicagrelorThe metabolism of Formoterol can be decreased when combined with Ticagrelor.Approved
TiclopidineThe metabolism of Formoterol can be decreased when combined with Ticlopidine.Approved
TimololTimolol may decrease the bronchodilatory activities of Formoterol.Approved
TipranavirThe metabolism of Formoterol can be decreased when combined with Tipranavir.Approved, Investigational
TolbutamideThe metabolism of Formoterol can be decreased when combined with Tolbutamide.Approved
ToloxatoneThe risk or severity of adverse effects can be increased when Toloxatone is combined with Formoterol.Approved
TopiramateThe metabolism of Formoterol can be decreased when combined with Topiramate.Approved
TorasemideFormoterol may increase the hypokalemic activities of Torasemide.Approved
ToremifeneFormoterol may increase the QTc-prolonging activities of Toremifene.Approved, Investigational
Trans-2-PhenylcyclopropylamineThe risk or severity of adverse effects can be increased when Trans-2-Phenylcyclopropylamine is combined with Formoterol.Experimental
TranylcypromineThe metabolism of Formoterol can be decreased when combined with Tranylcypromine.Approved
TrichlormethiazideFormoterol may increase the hypokalemic activities of Trichlormethiazide.Approved, Vet Approved
TrimazosinTrimazosin may decrease the vasoconstricting activities of Formoterol.Experimental
TrimethoprimThe metabolism of Formoterol can be decreased when combined with Trimethoprim.Approved, Vet Approved
TrimipramineThe risk or severity of adverse effects can be increased when Trimipramine is combined with Formoterol.Approved
Valproic AcidThe metabolism of Formoterol can be decreased when combined with Valproic Acid.Approved, Investigational
ValsartanThe metabolism of Formoterol can be decreased when combined with Valsartan.Approved, Investigational
VandetanibFormoterol may increase the QTc-prolonging activities of Vandetanib.Approved
VemurafenibFormoterol may increase the QTc-prolonging activities of Vemurafenib.Approved
VenlafaxineVenlafaxine may increase the tachycardic activities of Formoterol.Approved
VoriconazoleThe metabolism of Formoterol can be decreased when combined with Voriconazole.Approved, Investigational
ZafirlukastThe metabolism of Formoterol can be decreased when combined with Zafirlukast.Approved, Investigational
ZiprasidoneFormoterol may increase the QTc-prolonging activities of Ziprasidone.Approved
ZuclopenthixolFormoterol may increase the QTc-prolonging activities of Zuclopenthixol.Approved, Investigational
Food InteractionsNot Available
References
Synthesis Reference

Jan W. Trofast, Edib Jakupovic, Katarina L. Mansson, “Process for preparing formoterol and related compounds.” U.S. Patent US5434304, issued August, 1992.

US5434304
General References
  1. Bartow RA, Brogden RN: Formoterol. An update of its pharmacological properties and therapeutic efficacy in the management of asthma. Drugs. 1998 Feb;55(2):303-22. [PubMed:9506248 ]
  2. Cheer SM, Scott LJ: Formoterol: a review of its use in chronic obstructive pulmonary disease. Am J Respir Med. 2002;1(4):285-300. [PubMed:14720051 ]
  3. Steiropoulos P, Tzouvelekis A, Bouros D: Formoterol in the management of chronic obstructive pulmonary disease. Int J Chron Obstruct Pulmon Dis. 2008;3(2):205-15. [PubMed:18686730 ]
  4. Faulds D, Hollingshead LM, Goa KL: Formoterol. A review of its pharmacological properties and therapeutic potential in reversible obstructive airways disease. Drugs. 1991 Jul;42(1):115-37. [PubMed:1718682 ]
  5. Op't Holt TB: Inhaled beta agonists. Respir Care. 2007 Jul;52(7):820-32. [PubMed:17594727 ]
External Links
ATC CodesR03AK11R03AL05R03AK07R03AK08R03AC13R03AK09
AHFS Codes
  • 12:12.08.12
PDB EntriesNot Available
FDA labelDownload (1.48 MB)
MSDSDownload (36.2 KB)
ADMET
Predicted ADMET features
PropertyValueProbability
Human Intestinal Absorption+0.8991
Blood Brain Barrier-0.8026
Caco-2 permeable-0.6916
P-glycoprotein substrateSubstrate0.747
P-glycoprotein inhibitor INon-inhibitor0.8773
P-glycoprotein inhibitor IINon-inhibitor0.8561
Renal organic cation transporterNon-inhibitor0.8818
CYP450 2C9 substrateNon-substrate0.714
CYP450 2D6 substrateNon-substrate0.7086
CYP450 3A4 substrateSubstrate0.5556
CYP450 1A2 substrateNon-inhibitor0.6609
CYP450 2C9 inhibitorNon-inhibitor0.907
CYP450 2D6 inhibitorInhibitor0.8931
CYP450 2C19 inhibitorInhibitor0.8994
CYP450 3A4 inhibitorNon-inhibitor0.8757
CYP450 inhibitory promiscuityLow CYP Inhibitory Promiscuity0.8442
Ames testNon AMES toxic0.7517
CarcinogenicityNon-carcinogens0.8704
BiodegradationNot ready biodegradable0.992
Rat acute toxicity2.4047 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Weak inhibitor0.9611
hERG inhibition (predictor II)Non-inhibitor0.6602
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Novartis pharmaceuticals corp
  • Dey pharma lp
Packagers
Dosage forms
FormRouteStrength
Powder, meteredRespiratory (inhalation)
CapsuleRespiratory (inhalation)12 ug/1
CapsuleRespiratory (inhalation)12 mcg
PowderRespiratory (inhalation)12 mcg
PowderRespiratory (inhalation)6 mcg
SolutionRespiratory (inhalation)20 ug/2mL
AerosolRespiratory (inhalation)
PowderRespiratory (inhalation)
Aerosol, meteredRespiratory (inhalation)
Prices
Unit descriptionCostUnit
Formoterol fumarate powder1346.4USD g
Foradil Aerolizer 60 12 mcg capsule Box170.72USD box
Foradil aerolizer 12 mcg cap2.83USD each
Foradil 12 mcg Capsule0.88USD capsule
Oxeze Turbuhaler 12 mcg/dose Metered Inhalation Powder0.82USD dose
Oxeze Turbuhaler 6 mcg/dose Metered Inhalation Powder0.61USD dose
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US6068832 No1997-08-272017-08-27Us
US6123924 No1997-09-262017-09-26Us
US6182655 No1996-12-052016-12-05Us
US6488027 No1999-03-082019-03-08Us
US6667344 No2001-06-222021-06-22Us
US6814953 No2001-06-222021-06-22Us
US6887459 No2000-11-282020-11-28Us
US7067502 No2000-05-212020-05-21Us
US7348362 No2001-06-222021-06-22Us
US7367333 No1998-11-112018-11-11Us
US7462645 No2001-06-222021-06-22Us
US7566705 No2000-05-212020-05-21Us
US7587988 No2006-04-102026-04-10Us
US7759328 No2003-01-292023-01-29Us
US7897646 No1998-09-092018-09-09Us
US7967011 No2001-08-112021-08-11Us
US8143239 No2003-01-292023-01-29Us
US8387615 No2004-11-102024-11-10Us
US8461211 No1998-09-092018-09-09Us
US8528545 No2008-10-162028-10-16Us
US8575137 No2003-01-292023-01-29Us
US8616196 No2009-04-072029-04-07Us
US8623922 No2001-06-222021-06-22Us
US8875699 No2004-11-102024-11-10Us
Properties
StateSolid
Experimental Properties
PropertyValueSource
water solubilitySlightly (as fumarate salt)Not Available
logP2.2Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0416 mg/mLALOGPS
logP1.91ALOGPS
logP1.06ChemAxon
logS-3.9ALOGPS
pKa (Strongest Acidic)8.61ChemAxon
pKa (Strongest Basic)9.81ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count5ChemAxon
Hydrogen Donor Count4ChemAxon
Polar Surface Area90.82 Å2ChemAxon
Rotatable Bond Count8ChemAxon
Refractivity97.87 m3·mol-1ChemAxon
Polarizability36.56 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
Spectra
Spectrum TypeDescriptionSplash Key
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, PositiveNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 10V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 20V, NegativeNot Available
Predicted LC-MS/MSPredicted LC-MS/MS Spectrum - 40V, NegativeNot Available
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as amphetamines and derivatives. These are organic compounds containing or derived from 1-phenylpropan-2-amine.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassPhenethylamines
Direct ParentAmphetamines and derivatives
Alternative Parents
Substituents
  • Amphetamine or derivatives
  • Phenylpropane
  • Methoxybenzene
  • Phenol ether
  • Anisole
  • Aralkylamine
  • Phenol
  • Alkyl aryl ether
  • Secondary carboxylic acid amide
  • Secondary alcohol
  • 1,2-aminoalcohol
  • Secondary amine
  • Ether
  • Secondary aliphatic amine
  • Carboxylic acid derivative
  • Carboxylic acid amide
  • Hydrocarbon derivative
  • Aromatic alcohol
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Alcohol
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External DescriptorsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
agonist
General Function:
Protein homodimerization activity
Specific Function:
Beta-adrenergic receptors mediate the catecholamine-induced activation of adenylate cyclase through the action of G proteins. The beta-2-adrenergic receptor binds epinephrine with an approximately 30-fold greater affinity than it does norepinephrine.
Gene Name:
ADRB2
Uniprot ID:
P07550
Molecular Weight:
46458.32 Da
References
  1. Handley DA, Senanayake CH, Dutczak W, Benovic JL, Walle T, Penn RB, Wilkinson HS, Tanoury GJ, Andersson RG, Johansson F, Morley J: Biological actions of formoterol isomers. Pulm Pharmacol Ther. 2002;15(2):135-45. [PubMed:12090787 ]
  2. Scola AM, Chong LK, Suvarna SK, Chess-Williams R, Peachell PT: Desensitisation of mast cell beta2-adrenoceptor-mediated responses by salmeterol and formoterol. Br J Pharmacol. 2004 Jan;141(1):163-71. Epub 2003 Dec 8. [PubMed:14662724 ]
  3. Ryall JG, Sillence MN, Lynch GS: Systemic administration of beta2-adrenoceptor agonists, formoterol and salmeterol, elicit skeletal muscle hypertrophy in rats at micromolar doses. Br J Pharmacol. 2006 Mar;147(6):587-95. [PubMed:16432501 ]
  4. Lofdahl CG, Svedmyr N: Formoterol fumarate, a new beta 2-adrenoceptor agonist. Acute studies of selectivity and duration of effect after inhaled and oral administration. Allergy. 1989 May;44(4):264-71. [PubMed:2544117 ]
  5. Kompa AR, Molenaar P, Summers RJ: Beta-adrenoceptor regulation and functional responses in the guinea-pig following chronic administration of the long-acting beta 2-adrenoceptor agonist formoterol. Naunyn Schmiedebergs Arch Pharmacol. 1995 Jun;351(6):576-88. [PubMed:7675115 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  7. Bartow RA, Brogden RN: Formoterol. An update of its pharmacological properties and therapeutic efficacy in the management of asthma. Drugs. 1998 Feb;55(2):303-22. [PubMed:9506248 ]
  8. Cheer SM, Scott LJ: Formoterol: a review of its use in chronic obstructive pulmonary disease. Am J Respir Med. 2002;1(4):285-300. [PubMed:14720051 ]
  9. Steiropoulos P, Tzouvelekis A, Bouros D: Formoterol in the management of chronic obstructive pulmonary disease. Int J Chron Obstruct Pulmon Dis. 2008;3(2):205-15. [PubMed:18686730 ]
  10. Faulds D, Hollingshead LM, Goa KL: Formoterol. A review of its pharmacological properties and therapeutic potential in reversible obstructive airways disease. Drugs. 1991 Jul;42(1):115-37. [PubMed:1718682 ]
  11. Op't Holt TB: Inhaled beta agonists. Respir Care. 2007 Jul;52(7):820-32. [PubMed:17594727 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants.
Gene Name:
CYP2D6
Uniprot ID:
P10635
Molecular Weight:
55768.94 Da
References
  1. Somers GI, Lindsay N, Lowdon BM, Jones AE, Freathy C, Ho S, Woodrooffe AJ, Bayliss MK, Manchee GR: A comparison of the expression and metabolizing activities of phase I and II enzymes in freshly isolated human lung parenchymal cells and cryopreserved human hepatocytes. Drug Metab Dispos. 2007 Oct;35(10):1797-805. Epub 2007 Jul 12. [PubMed:17627976 ]
  2. Zhang M, Fawcett JP, Kennedy JM, Shaw JP: Stereoselective glucuronidation of formoterol by human liver microsomes. Br J Clin Pharmacol. 2000 Feb;49(2):152-7. [PubMed:10671910 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
Gene Name:
CYP2C19
Uniprot ID:
P33261
Molecular Weight:
55930.545 Da
References
  1. Somers GI, Lindsay N, Lowdon BM, Jones AE, Freathy C, Ho S, Woodrooffe AJ, Bayliss MK, Manchee GR: A comparison of the expression and metabolizing activities of phase I and II enzymes in freshly isolated human lung parenchymal cells and cryopreserved human hepatocytes. Drug Metab Dispos. 2007 Oct;35(10):1797-805. Epub 2007 Jul 12. [PubMed:17627976 ]
  2. Zhang M, Fawcett JP, Kennedy JM, Shaw JP: Stereoselective glucuronidation of formoterol by human liver microsomes. Br J Clin Pharmacol. 2000 Feb;49(2):152-7. [PubMed:10671910 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenyto...
Gene Name:
CYP2C9
Uniprot ID:
P11712
Molecular Weight:
55627.365 Da
References
  1. Somers GI, Lindsay N, Lowdon BM, Jones AE, Freathy C, Ho S, Woodrooffe AJ, Bayliss MK, Manchee GR: A comparison of the expression and metabolizing activities of phase I and II enzymes in freshly isolated human lung parenchymal cells and cryopreserved human hepatocytes. Drug Metab Dispos. 2007 Oct;35(10):1797-805. Epub 2007 Jul 12. [PubMed:17627976 ]
  2. Zhang M, Fawcett JP, Kennedy JM, Shaw JP: Stereoselective glucuronidation of formoterol by human liver microsomes. Br J Clin Pharmacol. 2000 Feb;49(2):152-7. [PubMed:10671910 ]
Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Steroid hydroxylase activity
Specific Function:
Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.
Gene Name:
CYP2A6
Uniprot ID:
P11509
Molecular Weight:
56501.005 Da
References
  1. Somers GI, Lindsay N, Lowdon BM, Jones AE, Freathy C, Ho S, Woodrooffe AJ, Bayliss MK, Manchee GR: A comparison of the expression and metabolizing activities of phase I and II enzymes in freshly isolated human lung parenchymal cells and cryopreserved human hepatocytes. Drug Metab Dispos. 2007 Oct;35(10):1797-805. Epub 2007 Jul 12. [PubMed:17627976 ]
  2. Zhang M, Fawcett JP, Kennedy JM, Shaw JP: Stereoselective glucuronidation of formoterol by human liver microsomes. Br J Clin Pharmacol. 2000 Feb;49(2):152-7. [PubMed:10671910 ]
Comments
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Drug created on June 13, 2005 07:24 / Updated on December 07, 2016 02:39