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Identification
NameFormoterol
Accession NumberDB00983  (APRD00641)
TypeSmall Molecule
GroupsApproved, Investigational
Description

Formoterol 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)Merck Sharp & Dohme Corp.2001-02-16Not applicableUs
Foradilcapsule12 ug/1respiratory (inhalation)Physicians Total Care, Inc.2004-05-28Not applicableUs
Foradilcapsule12 ug/1respiratory (inhalation)Merck Sharp & Dohme Corp.2001-02-16Not applicableUs
Foradil Dry Powder Capsules for Inhalationcapsule12 mcginhalationNovartis Pharmaceuticals Canada Inc1997-07-08Not applicableCanada
Oxeze Turbuhalerpowder6 mcginhalationAstrazeneca Canada Inc1998-03-12Not applicableCanada
Oxeze Turbuhalerpowder12 mcginhalationAstrazeneca 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
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 KeyInChIKey=BPZSYCZIITTYBL-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
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
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.
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.
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
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 (metered dose)inhalation
Aerosolrespiratory (inhalation)
Capsulerespiratory (inhalation)12 ug/1
Capsuleinhalation12 mcg
Powderinhalation12 mcg
Powderinhalation6 mcg
Solutionrespiratory (inhalation)20 ug/2mL
Powderinhalation
Aerosol, metered doseinhalation
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
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 CodesR03AK07R03AK11R03AL05R03AK08R03AK09R03AC13
AHFS Codes
  • 12:12.08.12
PDB EntriesNot Available
FDA labelDownload (1.48 MB)
MSDSDownload (36.2 KB)
Interactions
Drug Interactions
Drug
AcebutololThe risk or severity of adverse effects can be increased when Acebutolol is combined with Formoterol.
AcetaminophenThe risk or severity of adverse effects can be increased when Formoterol is combined with Acetaminophen.
Acetylsalicylic acidThe risk or severity of adverse effects can be increased when Formoterol is combined with Acetylsalicylic acid.
AminophyllineThe risk or severity of adverse effects can be increased when Aminophylline is combined with Formoterol.
AmitriptylineThe risk or severity of adverse effects can be increased when Amitriptyline is combined with Formoterol.
AmphetamineThe risk or severity of adverse effects can be increased when Formoterol is combined with Amphetamine.
ArformoterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Arformoterol.
ArmodafinilThe risk or severity of adverse effects can be increased when Formoterol is combined with Armodafinil.
ArticaineThe risk or severity of adverse effects can be increased when Formoterol is combined with Articaine.
AtomoxetineAtomoxetine may increase the tachycardic activities of Formoterol.
AtosibanThe risk or severity of adverse effects can be increased when Formoterol is combined with Atosiban.
BenzphetamineThe risk or severity of adverse effects can be increased when Formoterol is combined with Benzphetamine.
BetahistineThe therapeutic efficacy of Formoterol can be decreased when used in combination with Betahistine.
ButalbitalThe risk or severity of adverse effects can be increased when Formoterol is combined with Butalbital.
CaffeineThe risk or severity of adverse effects can be increased when Caffeine is combined with Formoterol.
ChlorphentermineThe risk or severity of adverse effects can be increased when Chlorphentermine is combined with Formoterol.
CitalopramFormoterol may increase the QTc-prolonging activities of Citalopram.
ClenbuterolThe risk or severity of adverse effects can be increased when Clenbuterol is combined with Formoterol.
CocaineThe risk or severity of adverse effects can be increased when Formoterol is combined with Cocaine.
DesfluraneDesflurane may increase the arrhythmogenic activities of Formoterol.
DexmethylphenidateThe risk or severity of adverse effects can be increased when Formoterol is combined with Dexmethylphenidate.
DextroamphetamineThe risk or severity of adverse effects can be increased when Formoterol is combined with Dextroamphetamine.
DiethylpropionThe risk or severity of adverse effects can be increased when Formoterol is combined with Diethylpropion.
DihydrocodeineThe risk or severity of adverse effects can be increased when Formoterol is combined with Dihydrocodeine.
DipivefrinThe risk or severity of adverse effects can be increased when Formoterol is combined with Dipivefrin.
DobutamineThe risk or severity of adverse effects can be increased when Formoterol is combined with Dobutamine.
DofetilideFormoterol may increase the QTc-prolonging activities of Dofetilide.
DopamineThe risk or severity of adverse effects can be increased when Dopamine is combined with Formoterol.
DoxapramThe risk or severity of adverse effects can be increased when Formoterol is combined with Doxapram.
DoxofyllineThe risk or severity of adverse effects can be increased when Formoterol is combined with Doxofylline.
DronabinolDronabinol may increase the tachycardic activities of Formoterol.
DyphyllineThe risk or severity of adverse effects can be increased when Dyphylline is combined with Formoterol.
EphedrineThe risk or severity of adverse effects can be increased when Formoterol is combined with Ephedrine.
EpinephrineThe risk or severity of adverse effects can be increased when Formoterol is combined with Epinephrine.
EsmololEsmolol may decrease the activities of Formoterol.
FenoterolThe risk or severity of adverse effects can be increased when Fenoterol is combined with Formoterol.
Fluticasone PropionateThe risk or severity of adverse effects can be increased when Formoterol is combined with Fluticasone Propionate.
GoserelinFormoterol may increase the QTc-prolonging activities of Goserelin.
IndacaterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Indacaterol.
IobenguaneThe therapeutic efficacy of Iobenguane can be decreased when used in combination with Formoterol.
Ipratropium bromideThe risk or severity of adverse effects can be increased when Formoterol is combined with Ipratropium bromide.
IsofluraneIsoflurane may increase the arrhythmogenic activities of Formoterol.
IsomethepteneThe risk or severity of adverse effects can be increased when Formoterol is combined with Isometheptene.
IsoprenalineThe risk or severity of adverse effects can be increased when Isoprenaline is combined with Formoterol.
LabetalolThe risk or severity of adverse effects can be increased when Labetalol is combined with Formoterol.
LeuprolideFormoterol may increase the QTc-prolonging activities of Leuprolide.
LevonordefrinThe risk or severity of adverse effects can be increased when Formoterol is combined with Levonordefrin.
LinezolidLinezolid may increase the hypertensive activities of Formoterol.
LisdexamfetamineThe risk or severity of adverse effects can be increased when Formoterol is combined with Lisdexamfetamine.
LoxapineThe risk or severity of adverse effects can be increased when Formoterol is combined with Loxapine.
MephentermineThe risk or severity of adverse effects can be increased when Mephentermine is combined with Formoterol.
MepivacaineThe risk or severity of adverse effects can be increased when Formoterol is combined with Mepivacaine.
MetaraminolThe risk or severity of adverse effects can be increased when Metaraminol is combined with Formoterol.
MethamphetamineThe risk or severity of adverse effects can be increased when Methamphetamine is combined with Formoterol.
MethoxamineThe risk or severity of adverse effects can be increased when Methoxamine is combined with Formoterol.
MethylphenidateThe risk or severity of adverse effects can be increased when Formoterol is combined with Methylphenidate.
MidodrineThe risk or severity of adverse effects can be increased when Formoterol is combined with Midodrine.
MifepristoneMifepristone may increase the QTc-prolonging activities of Formoterol.
ModafinilThe risk or severity of adverse effects can be increased when Formoterol is combined with Modafinil.
NabiloneNabilone may increase the tachycardic activities of Formoterol.
NadololNadolol may decrease the activities of Formoterol.
NaphazolineThe risk or severity of adverse effects can be increased when Naphazoline is combined with Formoterol.
NorepinephrineThe risk or severity of adverse effects can be increased when Formoterol is combined with Norepinephrine.
OlodaterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Olodaterol.
OrciprenalineThe risk or severity of adverse effects can be increased when Orciprenaline is combined with Formoterol.
OxymetazolineThe risk or severity of adverse effects can be increased when Formoterol is combined with Oxymetazoline.
PhendimetrazineThe risk or severity of adverse effects can be increased when Formoterol is combined with Phendimetrazine.
PhenelzineThe risk or severity of adverse effects can be increased when Phenelzine is combined with Formoterol.
PheniramineThe risk or severity of adverse effects can be increased when Formoterol is combined with Pheniramine.
PhenmetrazineThe risk or severity of adverse effects can be increased when Phenmetrazine is combined with Formoterol.
PhentermineThe risk or severity of adverse effects can be increased when Formoterol is combined with Phentermine.
PhenylephrineThe risk or severity of adverse effects can be increased when Formoterol is combined with Phenylephrine.
PhenylpropanolamineThe risk or severity of adverse effects can be increased when Phenylpropanolamine is combined with Formoterol.
PirbuterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Pirbuterol.
PropylhexedrineThe risk or severity of adverse effects can be increased when Formoterol is combined with Propylhexedrine.
PseudoephedrineThe risk or severity of adverse effects can be increased when Formoterol is combined with Pseudoephedrine.
RacepinephrineThe risk or severity of adverse effects can be increased when Formoterol is combined with Racepinephrine.
RitodrineThe risk or severity of adverse effects can be increased when Ritodrine is combined with Formoterol.
SalbutamolThe risk or severity of adverse effects can be increased when Formoterol is combined with Salbutamol.
SalmeterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Salmeterol.
SevofluraneSevoflurane may increase the arrhythmogenic activities of Formoterol.
Tedizolid PhosphateTedizolid Phosphate may increase the hypertensive activities of Formoterol.
TerbutalineThe risk or severity of adverse effects can be increased when Formoterol is combined with Terbutaline.
TheophyllineThe risk or severity of adverse effects can be increased when Theophylline is combined with Formoterol.
TorasemideFormoterol may increase the hypokalemic activities of Torasemide.
TranylcypromineThe risk or severity of adverse effects can be increased when Tranylcypromine is combined with Formoterol.
TrichlormethiazideFormoterol may increase the hypokalemic activities of Trichlormethiazide.
TriprolidineThe risk or severity of adverse effects can be increased when Formoterol is combined with Triprolidine.
VilanterolThe risk or severity of adverse effects can be increased when Formoterol is combined with Vilanterol.
Food InteractionsNot 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 ]
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Drug created on June 13, 2005 07:24 / Updated on August 24, 2016 01:52