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Identification
NameDofetilide
Accession NumberDB00204  (APRD00367)
TypeSmall Molecule
GroupsApproved
Description

Dofetilide is a class III antiarrhythmic agent that is approved by the Food and Drug Administration (FDA) for the maintenance of sinus rhythm in individuals prone to the formation of atrial fibrillation and flutter, and for the chemical cardioversion to sinus rhythm from atrial fibrillation and flutter. [Wikipedia]

Structure
Thumb
Synonyms
SynonymLanguageCode
beta-((P-Methanesulfonamidophenethyl)methylamino)methanesulfono-P-phenetidideNot AvailableNot Available
DofetilidaSpanishINN
DofetilideNot AvailableNot Available
DofetilidumLatinINN
TikosynNot AvailableNot Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Tikosyncapsule.125 mgoralPfizer Laboratories Div Pfizer Inc1999-10-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Tikosyncapsule.25 mgoralPfizer Laboratories Div Pfizer Inc1999-10-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Tikosyncapsule.5 mgoralPfizer Laboratories Div Pfizer Inc1999-10-01Not AvailableUs 0a2ef1ad1c84951dc1392a8bbe1f3cb241c91ed59e44ad8268635315440d978c
Generic Prescription ProductsNot Available
Over the Counter ProductsNot Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
CAS number115256-11-6
WeightAverage: 441.565
Monoisotopic: 441.139212369
Chemical FormulaC19H27N3O5S2
InChI KeyIXTMWRCNAAVVAI-UHFFFAOYSA-N
InChI
InChI=1S/C19H27N3O5S2/c1-22(13-12-16-4-6-17(7-5-16)20-28(2,23)24)14-15-27-19-10-8-18(9-11-19)21-29(3,25)26/h4-11,20-21H,12-15H2,1-3H3
IUPAC Name
N-[4-(2-{[2-(4-methanesulfonamidophenyl)ethyl](methyl)amino}ethoxy)phenyl]methanesulfonamide
SMILES
CN(CCOC1=CC=C(NS(C)(=O)=O)C=C1)CCC1=CC=C(NS(C)(=O)=O)C=C1
Taxonomy
DescriptionThis compound belongs to the class of organic compounds known as sulfanilides. These are organic aromatic compounds containing a sulfanilide moiety, with the general structure RS(=O)(=O)NC1=CC=CC=C1.
KingdomOrganic compounds
Super ClassBenzenoids
ClassBenzene and substituted derivatives
Sub ClassSulfanilides
Direct ParentSulfanilides
Alternative Parents
Substituents
  • Sulfanilide
  • Phenethylamine
  • Phenol ether
  • Aralkylamine
  • Alkyl aryl ether
  • Aminosulfonyl compound
  • Sulfonyl
  • Sulfonic acid derivative
  • Sulfonamide
  • Tertiary aliphatic amine
  • Tertiary amine
  • Ether
  • Hydrocarbon derivative
  • Organosulfur compound
  • Organooxygen compound
  • Organonitrogen compound
  • Amine
  • Aromatic homomonocyclic compound
Molecular FrameworkAromatic homomonocyclic compounds
External Descriptors
Pharmacology
IndicationFor the maintenance of normal sinus rhythm (delay in time to recurrence of atrial fibrillation/atrial flutter [AF/AFl]) in patients with atrial fibrillation/atrial flutter of greater than one week duration who have been converted to normal sinus rhythm
PharmacodynamicsDofetilide is an antiarrhythmic drug with Class III (cardiac action potential duration prolonging) properties and is indicated for the maintenance of normal sinus rhythm. Dofetilide increases the monophasic action potential duration in a predictable, concentration-dependent manner, primarily due to delayed repolarization. At concentrations covering several orders of magnitude, Dofetilide blocks only IKr with no relevant block of the other repolarizing potassium currents (e.g., IKs, IK1). At clinically relevant concentrations, Dofetilide has no effect on sodium channels (associated with Class I effect), adrenergic alpha-receptors, or adrenergic beta-receptors.
Mechanism of actionThe mechanism of action of Dofetilide is a blockade of the cardiac ion channel carrying the rapid component of the delayed rectifier potassium current, IKr. This inhibition of potassium channels results in a prolongation of action potential duration and the effective refractory period of accessory pathways (both anterograde and retrograde conduction in the accessory pathway).
Absorption>90%
Volume of distribution
  • 3 L/kg
Protein binding60% -70%
Metabolism

Hepatic

Route of eliminationNot Available
Half life10 hours
ClearanceNot Available
ToxicityNot Available
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+0.9924
Blood Brain Barrier+0.9179
Caco-2 permeable-0.6257
P-glycoprotein substrateSubstrate0.6018
P-glycoprotein inhibitor IInhibitor0.6848
P-glycoprotein inhibitor IINon-inhibitor0.7391
Renal organic cation transporterNon-inhibitor0.7308
CYP450 2C9 substrateNon-substrate0.7572
CYP450 2D6 substrateNon-substrate0.9116
CYP450 3A4 substrateSubstrate0.6699
CYP450 1A2 substrateNon-inhibitor0.6359
CYP450 2C9 substrateNon-inhibitor0.5189
CYP450 2D6 substrateNon-inhibitor0.7709
CYP450 2C19 substrateInhibitor0.544
CYP450 3A4 substrateNon-inhibitor0.7715
CYP450 inhibitory promiscuityHigh CYP Inhibitory Promiscuity0.6823
Ames testNon AMES toxic0.6193
CarcinogenicityNon-carcinogens0.6038
BiodegradationNot ready biodegradable1.0
Rat acute toxicity2.5430 LD50, mol/kg Not applicable
hERG inhibition (predictor I)Strong inhibitor0.8119
hERG inhibition (predictor II)Inhibitor0.8258
Pharmacoeconomics
Manufacturers
  • Pfizer pharmaceuticals production corp ltd
Packagers
Dosage forms
FormRouteStrength
Capsuleoral.125 mg
Capsuleoral.25 mg
Capsuleoral.5 mg
Prices
Unit descriptionCostUnit
Tikosyn 250 mcg capsule3.64USD capsule
Tikosyn 125 mcg capsule3.63USD capsule
Tikosyn 500 mcg capsule3.61USD capsule
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only.
Patents
CountryPatent NumberApprovedExpires (estimated)
United States49593661992-09-252012-09-25
United States61243631998-10-092018-10-09
Properties
StateSolid
Experimental Properties
PropertyValueSource
logP2.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0198 mg/mLALOGPS
logP2.17ALOGPS
logP0.24ChemAxon
logS-4.3ALOGPS
pKa (Strongest Acidic)10.15ChemAxon
pKa (Strongest Basic)8.99ChemAxon
Physiological Charge1ChemAxon
Hydrogen Acceptor Count6ChemAxon
Hydrogen Donor Count2ChemAxon
Polar Surface Area104.81 Å2ChemAxon
Rotatable Bond Count9ChemAxon
Refractivity113.27 m3·mol-1ChemAxon
Polarizability46.03 Å3ChemAxon
Number of Rings2ChemAxon
Bioavailability1ChemAxon
Rule of FiveYesChemAxon
Ghose FilterYesChemAxon
Veber's RuleYesChemAxon
MDDR-like RuleYesChemAxon
Spectra
Mass Spec (NIST)Not Available
SpectraNot Available
References
Synthesis Reference

DrugSyn.org

US4959366
General Reference
  1. Lenz TL, Hilleman DE: Dofetilide, a new class III antiarrhythmic agent. Pharmacotherapy. 2000 Jul;20(7):776-86. Pubmed
  2. Lenz TL, Hilleman DE: Dofetilide: A new antiarrhythmic agent approved for conversion and/or maintenance of atrial fibrillation/atrial flutter. Drugs Today (Barc). 2000 Nov;36(11):759-71. Pubmed
  3. Torp-Pedersen C, Moller M, Bloch-Thomsen PE, Kober L, Sandoe E, Egstrup K, Agner E, Carlsen J, Videbaek J, Marchant B, Camm AJ: Dofetilide in patients with congestive heart failure and left ventricular dysfunction. Danish Investigations of Arrhythmia and Mortality on Dofetilide Study Group. N Engl J Med. 1999 Sep 16;341(12):857-65. Pubmed
External Links
ATC CodesC01BD04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (1.45 MB)
MSDSNot Available
Interactions
Drug Interactions
Drug
AbirateroneCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
AcetaminophenCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
AcetazolamideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
AmilorideMay increase the serum concentration of Dofetilide.
AmlodipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
AnastrozoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
AprepitantCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
AtorvastatinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
AzelastineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
Azilsartan medoxomilThiazide Diuretics may enhance the QTc-prolonging effect of Dofetilide. Thiazide Diuretics may increase the serum concentration of Dofetilide.
BendroflumethiazideThiazide Diuretics may enhance the QTc-prolonging effect of Dofetilide. Thiazide Diuretics may increase the serum concentration of Dofetilide.
BicalutamideCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
BiotinCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
BoceprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
BromocriptineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
BumetanideLoop Diuretics may enhance the QTc-prolonging effect of Dofetilide.
ButalbitalCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
CanagliflozinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
CarfilzomibCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
ChlorothiazideThiazide Diuretics may enhance the QTc-prolonging effect of Dofetilide. Thiazide Diuretics may increase the serum concentration of Dofetilide.
ChlorthalidoneThiazide Diuretics may enhance the QTc-prolonging effect of Dofetilide. Thiazide Diuretics may increase the serum concentration of Dofetilide.
ChlorzoxazoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
CimetidineMay increase the serum concentration of Dofetilide. This is likely via inhibition of dofetilide renal tubular secretion (primarily) and inhibition of dofetilide metabolism.
ClemastineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
ClotrimazoleCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
CocaineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
ConivaptanCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
CrofelemerCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
CyclophosphamideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
Cyproterone acetateCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DalfopristinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DanazolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DarifenacinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DarunavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
DelavirdineCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
DesogestrelCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DiazepamCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DihydrocodeineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DihydroergotamineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DiltiazemCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
DisulfiramCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DocetaxelCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DolutegravirMay increase the serum concentration of Dofetilide.
DoxycyclineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
DrospirenoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
EntacaponeCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
ErgotamineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
Ethacrynic acidLoop Diuretics may enhance the QTc-prolonging effect of Dofetilide.
Ethinyl EstradiolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
EthynodiolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
EtoposideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
FelodipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
FentanylCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
FingolimodMay enhance the arrhythmogenic effect of Antiarrhythmic Agents (Class III).
Fluticasone PropionateCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
FluvastatinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
FluvoxamineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
FosamprenavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
FosaprepitantCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
FurosemideLoop Diuretics may enhance the QTc-prolonging effect of Dofetilide.
GlyburideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
Glycerol PhenylbutyrateCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
HydralazineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
HydrochlorothiazideThiazide Diuretics may enhance the QTc-prolonging effect of Dofetilide. Thiazide Diuretics may increase the serum concentration of Dofetilide.
IfosfamideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
IndapamideThiazide Diuretics may enhance the QTc-prolonging effect of Dofetilide. Thiazide Diuretics may increase the serum concentration of Dofetilide.
IndinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
IrbesartanCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
IsavuconazoniumCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
IsomethepteneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
IsoniazidCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
ItraconazoleAntifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Dofetilide.
IvacaftorCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
LamotrigineMay increase the serum concentration of Dofetilide.
LansoprazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
LomitapideCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
LomustineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
LosartanCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
LovastatinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
LurasidoneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
Megestrol acetateMegestrol may increase the serum concentration of Dofetilide.
MestranolCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
MetforminMay increase the serum concentration of Dofetilide.
MethimazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
MethyclothiazideThiazide Diuretics may enhance the QTc-prolonging effect of Dofetilide. Thiazide Diuretics may increase the serum concentration of Dofetilide.
MethylprednisoloneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
MetolazoneThiazide Diuretics may enhance the QTc-prolonging effect of Dofetilide. Thiazide Diuretics may increase the serum concentration of Dofetilide.
MicafunginCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
MidazolamCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
MifepristoneMay enhance the QTc-prolonging effect of Highest Risk QTc-Prolonging Agents.
MitoxantroneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
ModafinilCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
NefazodoneCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
NelfinavirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
NevirapineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
NifedipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
NisoldipineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
NizatidineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
NorelgestrominCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
OmeprazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
OrphenadrineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
OspemifeneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
OxybutyninCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
PilocarpineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
PosaconazoleAntifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Dofetilide.
PravastatinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
ProchlorperazineMay increase the serum concentration of Dofetilide.
ProgesteroneCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
PropafenoneMay enhance the arrhythmogenic effect of Antiarrhythmic Agents (Class III).
QuinupristinCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
RabeprazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
SaquinavirMay enhance the arrhythmogenic effect of Dofetilide. Saquinavir may increase the serum concentration of Dofetilide.
SelegilineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
SildenafilCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
SirolimusCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
Sodium phenylbutyrateCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
SulconazoleCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
SulfamethoxazoleTrimethoprim may decrease the excretion of Dofetilide.
TelaprevirCYP3A4 Inhibitors (Strong) may increase the serum concentration of Dofetilide.
TemsirolimusCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
TeniposideCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
TetracyclineCYP3A4 Inhibitors (Moderate) may increase the serum concentration of Dofetilide.
TiclopidineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
TolvaptanCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
TorasemideLoop Diuretics may enhance the QTc-prolonging effect of Dofetilide.
TranylcypromineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
TriamtereneMay increase the serum concentration of Dofetilide.
TrimethoprimMay decrease the excretion of Dofetilide.
VerapamilMay increase the serum concentration of Dofetilide.
VinblastineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
VincristineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
VinorelbineCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
VoriconazoleAntifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Dofetilide.
ZafirlukastCYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide.
Food InteractionsNot Available

Targets

1. Potassium voltage-gated channel subfamily H member 2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Potassium voltage-gated channel subfamily H member 2 Q12809 Details

References:

  1. Lees-Miller JP, Duan Y, Teng GQ, Duff HJ: Molecular determinant of high-affinity dofetilide binding to HERG1 expressed in Xenopus oocytes: involvement of S6 sites. Mol Pharmacol. 2000 Feb;57(2):367-74. Pubmed
  2. Overholt JL, Ficker E, Yang T, Shams H, Bright GR, Prabhakar NR: HERG-Like potassium current regulates the resting membrane potential in glomus cells of the rabbit carotid body. J Neurophysiol. 2000 Mar;83(3):1150-7. Pubmed
  3. Finlayson K, Pennington AJ, Kelly JS: [3H]dofetilide binding in SHSY5Y and HEK293 cells expressing a HERG-like K+ channel? Eur J Pharmacol. 2001 Feb 2;412(3):203-12. Pubmed
  4. Finlayson K, Turnbull L, January CT, Sharkey J, Kelly JS: [3H]dofetilide binding to HERG transfected membranes: a potential high throughput preclinical screen. Eur J Pharmacol. 2001 Oct 26;430(1):147-8. Pubmed
  5. Ficker E, Jarolimek W, Brown AM: Molecular determinants of inactivation and dofetilide block in ether a-go-go (EAG) channels and EAG-related K(+) channels. Mol Pharmacol. 2001 Dec;60(6):1343-8. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  7. Ficker E, Jarolimek W, Kiehn J, Baumann A, Brown AM: Molecular determinants of dofetilide block of HERG K+ channels. Circ Res. 1998 Feb 23;82(3):386-95. Pubmed
  8. Kang J, Chen XL, Wang H, Ji J, Cheng H, Incardona J, Reynolds W, Viviani F, Tabart M, Rampe D: Discovery of a small molecule activator of the human ether-a-go-go-related gene (HERG) cardiac K+ channel. Mol Pharmacol. 2005 Mar;67(3):827-36. Epub 2004 Nov 17. Pubmed

2. Potassium channel subfamily K member 2

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
Potassium channel subfamily K member 2 O95069 Details

References:

  1. Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. Pubmed
  2. Imming P, Sinning C, Meyer A: Drugs, their targets and the nature and number of drug targets. Nat Rev Drug Discov. 2006 Oct;5(10):821-34. Pubmed
  3. Roukoz H, Saliba W: Dofetilide: a new class III antiarrhythmic agent. Expert Rev Cardiovasc Ther. 2007 Jan;5(1):9-19. Pubmed

3. ATP-sensitive inward rectifier potassium channel 12

Kind: protein

Organism: Human

Pharmacological action: yes

Actions: inhibitor

Components

Name UniProt ID Details
ATP-sensitive inward rectifier potassium channel 12 Q14500 Details

References:

  1. Kiehn J, Wible B, Lacerda AE, Brown AM: Mapping the block of a cloned human inward rectifier potassium channel by dofetilide. Mol Pharmacol. 1996 Aug;50(2):380-7. Pubmed

Enzymes

1. Cytochrome P450 3A4

Kind: protein

Organism: Human

Pharmacological action: unknown

Actions: substrate

Components

Name UniProt ID Details
Cytochrome P450 3A4 P08684 Details

References:

  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

Comments
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Drug created on June 13, 2005 07:24 / Updated on October 08, 2013 14:23