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Identification
NameDofetilide
Accession NumberDB00204  (APRD00367)
TypeSmall Molecule
GroupsApproved
DescriptionDofetilide 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
beta-((P-Methanesulfonamidophenethyl)methylamino)methanesulfono-P-phenetidide
Dofetilida
Dofetilide
Dofetilidum
Tikosyn
External Identifiers Not Available
Approved Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Tikosyncapsule.125 mg/1oralPfizer Laboratories Div Pfizer Inc1999-10-01Not applicableUs
Tikosyncapsule.25 mg/1oralPfizer Laboratories Div Pfizer Inc1999-10-01Not applicableUs
Tikosyncapsule.5 mg/1oralPfizer Laboratories Div Pfizer Inc1999-10-01Not applicableUs
Approved Generic Prescription ProductsNot Available
Approved Over the Counter ProductsNot Available
Unapproved/Other Products Not Available
International BrandsNot Available
Brand mixturesNot Available
SaltsNot Available
Categories
UNIIR4Z9X1N2ND
CAS number115256-11-6
WeightAverage: 441.565
Monoisotopic: 441.139212369
Chemical FormulaC19H27N3O5S2
InChI KeyInChIKey=IXTMWRCNAAVVAI-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).
Related Articles
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 inhibitorNon-inhibitor0.5189
CYP450 2D6 inhibitorNon-inhibitor0.7709
CYP450 2C19 inhibitorInhibitor0.544
CYP450 3A4 inhibitorNon-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
ADMET data is predicted using admetSAR, a free tool for evaluating chemical ADMET properties. (23092397 )
Pharmacoeconomics
Manufacturers
  • Pfizer pharmaceuticals production corp ltd
Packagers
Dosage forms
FormRouteStrength
Capsuleoral.125 mg/1
Capsuleoral.25 mg/1
Capsuleoral.5 mg/1
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
Patent NumberPediatric ExtensionApprovedExpires (estimated)
US4959366 No1992-09-252012-09-25Us
US6124363 No1998-10-092018-10-09Us
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
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

DrugSyn.org

US4959366
General References
  1. Lenz TL, Hilleman DE: Dofetilide, a new class III antiarrhythmic agent. Pharmacotherapy. 2000 Jul;20(7):776-86. [PubMed:10907968 ]
  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:12845335 ]
  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:10486417 ]
External Links
ATC CodesC01BD04
AHFS CodesNot Available
PDB EntriesNot Available
FDA labelDownload (1.45 MB)
MSDSNot Available
Interactions
Drug Interactions
Drug
2-HYDROXY-1,4-NAPHTHOQUINONEThe metabolism of Dofetilide can be decreased when combined with 2-HYDROXY-1,4-NAPHTHOQUINONE.
2-mercaptobenzothiazoleThe metabolism of Dofetilide can be decreased when combined with 2-mercaptobenzothiazole.
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Dofetilide.
AlprazolamThe serum concentration of Dofetilide can be increased when it is combined with Alprazolam.
AmantadineAmantadine may increase the QTc-prolonging activities of Dofetilide.
AmilorideThe serum concentration of Dofetilide can be increased when it is combined with Amiloride.
AmiodaroneDofetilide may increase the QTc-prolonging activities of Amiodarone.
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Dofetilide.
AmlodipineThe serum concentration of Dofetilide can be increased when it is combined with Amlodipine.
AmorolfineThe metabolism of Dofetilide can be decreased when combined with Amorolfine.
AmoxapineAmoxapine may increase the QTc-prolonging activities of Dofetilide.
Amphotericin BThe metabolism of Dofetilide can be decreased when combined with Amphotericin B.
AN2690The metabolism of Dofetilide can be decreased when combined with AN2690.
AnagrelideDofetilide may increase the QTc-prolonging activities of Anagrelide.
AnidulafunginThe metabolism of Dofetilide can be decreased when combined with Anidulafungin.
ApomorphineApomorphine may increase the QTc-prolonging activities of Dofetilide.
AprepitantThe serum concentration of Dofetilide can be increased when it is combined with Aprepitant.
ArformoterolArformoterol may increase the QTc-prolonging activities of Dofetilide.
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Dofetilide.
Arsenic trioxideDofetilide may increase the QTc-prolonging activities of Arsenic trioxide.
ArtemetherThe metabolism of Dofetilide can be decreased when combined with Artemether.
ArtemetherDofetilide may increase the QTc-prolonging activities of Artemether.
AsenapineDofetilide may increase the QTc-prolonging activities of Asenapine.
AtazanavirThe serum concentration of Dofetilide can be increased when it is combined with Atazanavir.
AtomoxetineThe serum concentration of Dofetilide can be increased when it is combined with Atomoxetine.
AtorvastatinThe serum concentration of Dofetilide can be increased when it is combined with Atorvastatin.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Dofetilide.
Bafilomycin A1The metabolism of Dofetilide can be decreased when combined with Bafilomycin A1.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Dofetilide.
BendroflumethiazideBendroflumethiazide may increase the QTc-prolonging activities of Dofetilide.
Benzoic AcidThe metabolism of Dofetilide can be decreased when combined with Benzoic Acid.
BexaroteneThe serum concentration of Dofetilide can be decreased when it is combined with Bexarotene.
BicalutamideThe serum concentration of Dofetilide can be increased when it is combined with Bicalutamide.
BifonazoleThe metabolism of Dofetilide can be decreased when combined with Bifonazole.
BoceprevirThe serum concentration of Dofetilide can be increased when it is combined with Boceprevir.
BortezomibThe serum concentration of Dofetilide can be increased when it is combined with Bortezomib.
BosentanThe serum concentration of Dofetilide can be decreased when it is combined with Bosentan.
BumetanideBumetanide may increase the QTc-prolonging activities of Dofetilide.
BuserelinBuserelin may increase the QTc-prolonging activities of Dofetilide.
ButenafineThe metabolism of Dofetilide can be decreased when combined with Butenafine.
ButoconazoleThe metabolism of Dofetilide can be decreased when combined with Butoconazole.
CandicidinThe metabolism of Dofetilide can be decreased when combined with Candicidin.
CarbamazepineThe metabolism of Dofetilide can be increased when combined with Carbamazepine.
CaspofunginThe metabolism of Dofetilide can be decreased when combined with Caspofungin.
CeritinibCeritinib may increase the QTc-prolonging activities of Dofetilide.
CeruleninThe metabolism of Dofetilide can be decreased when combined with Cerulenin.
ChloroquineChloroquine may increase the QTc-prolonging activities of Dofetilide.
ChlorothiazideChlorothiazide may increase the QTc-prolonging activities of Dofetilide.
ChloroxineThe metabolism of Dofetilide can be decreased when combined with Chloroxine.
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Dofetilide.
ChlorthalidoneChlorthalidone may increase the QTc-prolonging activities of Dofetilide.
CiclopiroxThe metabolism of Dofetilide can be decreased when combined with Ciclopirox.
CilostazolThe serum concentration of Dofetilide can be increased when it is combined with Cilostazol.
CimetidineThe serum concentration of Dofetilide can be increased when it is combined with Cimetidine.
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Dofetilide.
CisaprideDofetilide may increase the QTc-prolonging activities of Cisapride.
CitalopramDofetilide may increase the QTc-prolonging activities of Citalopram.
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Dofetilide.
ClemastineThe serum concentration of Dofetilide can be increased when it is combined with Clemastine.
ClomipramineClomipramine may increase the QTc-prolonging activities of Dofetilide.
ClotrimazoleThe metabolism of Dofetilide can be decreased when combined with Clotrimazole.
ClozapineClozapine may increase the QTc-prolonging activities of Dofetilide.
CobicistatThe serum concentration of Dofetilide can be increased when it is combined with Cobicistat.
ConivaptanThe serum concentration of Dofetilide can be increased when it is combined with Conivaptan.
CrizotinibCrizotinib may increase the QTc-prolonging activities of Dofetilide.
CyclosporineThe metabolism of Dofetilide can be decreased when combined with Cyclosporine.
DabrafenibThe serum concentration of Dofetilide can be decreased when it is combined with Dabrafenib.
DalfopristinThe serum concentration of Dofetilide can be increased when it is combined with Dalfopristin.
DanazolThe serum concentration of Dofetilide can be increased when it is combined with Danazol.
DarunavirThe serum concentration of Dofetilide can be increased when it is combined with Darunavir.
DasatinibThe serum concentration of Dofetilide can be increased when it is combined with Dasatinib.
Decanoic AcidThe metabolism of Dofetilide can be decreased when combined with Decanoic Acid.
DeferasiroxThe serum concentration of Dofetilide can be decreased when it is combined with Deferasirox.
DegarelixDegarelix may increase the QTc-prolonging activities of Dofetilide.
DelavirdineThe serum concentration of Dofetilide can be increased when it is combined with Delavirdine.
DesfluraneDesflurane may increase the QTc-prolonging activities of Dofetilide.
DesipramineDesipramine may increase the QTc-prolonging activities of Dofetilide.
DexamethasoneThe serum concentration of Dofetilide can be decreased when it is combined with Dexamethasone.
DihydroergotamineThe serum concentration of Dofetilide can be increased when it is combined with Dihydroergotamine.
DiltiazemThe serum concentration of Dofetilide can be increased when it is combined with Diltiazem.
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Dofetilide.
DisopyramideDofetilide may increase the QTc-prolonging activities of Disopyramide.
DolasetronDolasetron may increase the QTc-prolonging activities of Dofetilide.
DolutegravirThe serum concentration of Dofetilide can be increased when it is combined with Dolutegravir.
DomperidoneDofetilide may increase the QTc-prolonging activities of Domperidone.
DoxepinDoxepin may increase the QTc-prolonging activities of Dofetilide.
DoxycyclineThe serum concentration of Dofetilide can be increased when it is combined with Doxycycline.
DronedaroneDofetilide may increase the QTc-prolonging activities of Dronedarone.
DroperidolDroperidol may increase the QTc-prolonging activities of Dofetilide.
EconazoleThe metabolism of Dofetilide can be decreased when combined with Econazole.
EfavirenzThe serum concentration of Dofetilide can be decreased when it is combined with Efavirenz.
EfinaconazoleThe metabolism of Dofetilide can be decreased when combined with Efinaconazole.
EliglustatDofetilide may increase the QTc-prolonging activities of Eliglustat.
EnzalutamideThe serum concentration of Dofetilide can be decreased when it is combined with Enzalutamide.
EribulinEribulin may increase the QTc-prolonging activities of Dofetilide.
ErythromycinErythromycin may increase the QTc-prolonging activities of Dofetilide.
EscitalopramDofetilide may increase the QTc-prolonging activities of Escitalopram.
Eslicarbazepine acetateThe serum concentration of Dofetilide can be decreased when it is combined with Eslicarbazepine acetate.
Etacrynic acidEtacrynic acid may increase the QTc-prolonging activities of Dofetilide.
EtravirineThe serum concentration of Dofetilide can be decreased when it is combined with Etravirine.
EzogabineEzogabine may increase the QTc-prolonging activities of Dofetilide.
FamotidineFamotidine may increase the QTc-prolonging activities of Dofetilide.
FelbamateFelbamate may increase the QTc-prolonging activities of Dofetilide.
FingolimodFingolimod may increase the arrhythmogenic activities of Dofetilide.
FlecainideFlecainide may increase the QTc-prolonging activities of Dofetilide.
FluconazoleThe metabolism of Dofetilide can be decreased when combined with Fluconazole.
FlucytosineThe metabolism of Dofetilide can be decreased when combined with Flucytosine.
FluoxetineDofetilide may increase the QTc-prolonging activities of Fluoxetine.
FlupentixolDofetilide may increase the QTc-prolonging activities of Flupentixol.
FluvoxamineThe serum concentration of Dofetilide can be increased when it is combined with Fluvoxamine.
FormoterolFormoterol may increase the QTc-prolonging activities of Dofetilide.
FosamprenavirThe serum concentration of Dofetilide can be increased when it is combined with Fosamprenavir.
FosaprepitantThe serum concentration of Dofetilide can be increased when it is combined with Fosaprepitant.
FoscarnetFoscarnet may increase the QTc-prolonging activities of Dofetilide.
FosphenytoinThe metabolism of Dofetilide can be increased when combined with Fosphenytoin.
FurosemideFurosemide may increase the QTc-prolonging activities of Dofetilide.
Fusidic AcidThe serum concentration of Dofetilide can be increased when it is combined with Fusidic Acid.
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Dofetilide.
GalantamineGalantamine may increase the QTc-prolonging activities of Dofetilide.
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Dofetilide.
Glycerol PhenylbutyrateThe serum concentration of Dofetilide can be increased when it is combined with Glycerol Phenylbutyrate.
GlyphosateThe metabolism of Dofetilide can be decreased when combined with Glyphosate.
GoserelinGoserelin may increase the QTc-prolonging activities of Dofetilide.
GranisetronGranisetron may increase the QTc-prolonging activities of Dofetilide.
GriseofulvinThe metabolism of Dofetilide can be decreased when combined with Griseofulvin.
HaloperidolHaloperidol may increase the QTc-prolonging activities of Dofetilide.
HaloproginThe metabolism of Dofetilide can be decreased when combined with Haloprogin.
HexetidineThe metabolism of Dofetilide can be decreased when combined with Hexetidine.
HistrelinHistrelin may increase the QTc-prolonging activities of Dofetilide.
HydrochlorothiazideHydrochlorothiazide may increase the QTc-prolonging activities of Dofetilide.
HydroflumethiazideHydroflumethiazide may increase the QTc-prolonging activities of Dofetilide.
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Dofetilide.
IbandronateIbandronate may increase the QTc-prolonging activities of Dofetilide.
IbutilideDofetilide may increase the QTc-prolonging activities of Ibutilide.
IdelalisibThe serum concentration of Dofetilide can be increased when it is combined with Idelalisib.
IloperidoneDofetilide may increase the QTc-prolonging activities of Iloperidone.
ImatinibThe serum concentration of Dofetilide can be increased when it is combined with Imatinib.
ImipramineImipramine may increase the QTc-prolonging activities of Dofetilide.
IndacaterolIndacaterol may increase the QTc-prolonging activities of Dofetilide.
IndapamideIndapamide may increase the QTc-prolonging activities of Dofetilide.
IndinavirThe serum concentration of Dofetilide can be increased when it is combined with Indinavir.
IsavuconazoniumThe serum concentration of Dofetilide can be increased when it is combined with Isavuconazonium.
IsoconazoleThe metabolism of Dofetilide can be decreased when combined with Isoconazole.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Dofetilide.
IsoniazidThe serum concentration of Dofetilide can be increased when it is combined with Isoniazid.
IsradipineThe serum concentration of Dofetilide can be increased when it is combined with Isradipine.
ItraconazoleThe metabolism of Dofetilide can be decreased when combined with Itraconazole.
IvabradineIvabradine may increase the QTc-prolonging activities of Dofetilide.
IvacaftorThe serum concentration of Dofetilide can be increased when it is combined with Ivacaftor.
KetoconazoleThe metabolism of Dofetilide can be decreased when combined with Ketoconazole.
LamotrigineThe serum concentration of Dofetilide can be increased when it is combined with Lamotrigine.
LapatinibThe serum concentration of Dofetilide can be increased when it is combined with Lapatinib.
LenvatinibLenvatinib may increase the QTc-prolonging activities of Dofetilide.
LeuprolideLeuprolide may increase the QTc-prolonging activities of Dofetilide.
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Dofetilide.
LidocaineLidocaine may increase the arrhythmogenic activities of Dofetilide.
LithiumLithium may increase the QTc-prolonging activities of Dofetilide.
LomitapideThe serum concentration of Dofetilide can be increased when it is combined with Lomitapide.
LopinavirDofetilide may increase the QTc-prolonging activities of Lopinavir.
LovastatinThe serum concentration of Dofetilide can be increased when it is combined with Lovastatin.
LuliconazoleThe serum concentration of Dofetilide can be increased when it is combined with Luliconazole.
LumefantrineDofetilide may increase the QTc-prolonging activities of Lumefantrine.
LurasidoneThe serum concentration of Dofetilide can be increased when it is combined with Lurasidone.
MaprotilineMaprotiline may increase the QTc-prolonging activities of Dofetilide.
MefloquineMefloquine may increase the QTc-prolonging activities of Dofetilide.
Megestrol acetateThe serum concentration of Dofetilide can be increased when it is combined with Megestrol acetate.
MetforminThe serum concentration of Dofetilide can be increased when it is combined with Metformin.
MethadoneMethadone may increase the QTc-prolonging activities of Dofetilide.
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Dofetilide.
MethyclothiazideMethyclothiazide may increase the QTc-prolonging activities of Dofetilide.
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Dofetilide.
MetolazoneMetolazone may increase the QTc-prolonging activities of Dofetilide.
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Dofetilide.
MevastatinThe metabolism of Dofetilide can be decreased when combined with Mevastatin.
MicafunginThe metabolism of Dofetilide can be decreased when combined with Micafungin.
MiconazoleThe metabolism of Dofetilide can be decreased when combined with Miconazole.
MifepristoneMifepristone may increase the QTc-prolonging activities of Dofetilide.
MiltefosineThe metabolism of Dofetilide can be decreased when combined with Miltefosine.
MirabegronMirabegron may increase the QTc-prolonging activities of Dofetilide.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Dofetilide.
MitotaneThe serum concentration of Dofetilide can be decreased when it is combined with Mitotane.
ModafinilThe serum concentration of Dofetilide can be decreased when it is combined with Modafinil.
MoexiprilMoexipril may increase the QTc-prolonging activities of Dofetilide.
MonensinThe metabolism of Dofetilide can be decreased when combined with Monensin.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Dofetilide.
MyxothiazolThe metabolism of Dofetilide can be decreased when combined with Myxothiazol.
NafcillinThe serum concentration of Dofetilide can be decreased when it is combined with Nafcillin.
NaftifineThe metabolism of Dofetilide can be decreased when combined with Naftifine.
NatamycinThe metabolism of Dofetilide can be decreased when combined with Natamycin.
NefazodoneThe serum concentration of Dofetilide can be increased when it is combined with Nefazodone.
NelfinavirThe serum concentration of Dofetilide can be increased when it is combined with Nelfinavir.
NetupitantThe serum concentration of Dofetilide can be increased when it is combined with Netupitant.
NevirapineThe serum concentration of Dofetilide can be increased when it is combined with Nevirapine.
NicardipineThe serum concentration of Dofetilide can be increased when it is combined with Nicardipine.
NilotinibDofetilide may increase the QTc-prolonging activities of Nilotinib.
NitroxolineThe metabolism of Dofetilide can be decreased when combined with Nitroxoline.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Dofetilide.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Dofetilide.
NystatinThe metabolism of Dofetilide can be decreased when combined with Nystatin.
OctreotideOctreotide may increase the QTc-prolonging activities of Dofetilide.
OfloxacinOfloxacin may increase the QTc-prolonging activities of Dofetilide.
OlanzapineOlanzapine may increase the QTc-prolonging activities of Dofetilide.
OlaparibThe serum concentration of Dofetilide can be increased when it is combined with Olaparib.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Dofetilide.
OndansetronOndansetron may increase the QTc-prolonging activities of Dofetilide.
OsimertinibThe serum concentration of Dofetilide can be increased when it is combined with Osimertinib.
OxiconazoleThe metabolism of Dofetilide can be decreased when combined with Oxiconazole.
OxytocinOxytocin may increase the QTc-prolonging activities of Dofetilide.
pafuramidineThe metabolism of Dofetilide can be decreased when combined with pafuramidine.
PalbociclibThe serum concentration of Dofetilide can be increased when it is combined with Palbociclib.
PaliperidoneDofetilide may increase the QTc-prolonging activities of Paliperidone.
PanobinostatPanobinostat may increase the QTc-prolonging activities of Dofetilide.
ParoxetineParoxetine may increase the QTc-prolonging activities of Dofetilide.
PasireotidePasireotide may increase the QTc-prolonging activities of Dofetilide.
PazopanibPazopanib may increase the QTc-prolonging activities of Dofetilide.
PentamidineThe metabolism of Dofetilide can be decreased when combined with Pentamidine.
PentobarbitalThe metabolism of Dofetilide can be increased when combined with Pentobarbital.
PerflutrenPerflutren may increase the QTc-prolonging activities of Dofetilide.
PhenobarbitalThe metabolism of Dofetilide can be increased when combined with Phenobarbital.
PhenytoinThe metabolism of Dofetilide can be increased when combined with Phenytoin.
PimozideDofetilide may increase the QTc-prolonging activities of Pimozide.
PiretanidePiretanide may increase the QTc-prolonging activities of Dofetilide.
PolythiazidePolythiazide may increase the QTc-prolonging activities of Dofetilide.
PosaconazoleThe metabolism of Dofetilide can be decreased when combined with Posaconazole.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Dofetilide.
PrimidoneThe metabolism of Dofetilide can be increased when combined with Primidone.
ProcainamideDofetilide may increase the QTc-prolonging activities of Procainamide.
ProchlorperazineThe serum concentration of Dofetilide can be increased when it is combined with Prochlorperazine.
PromazinePromazine may increase the QTc-prolonging activities of Dofetilide.
PromethazinePromethazine may increase the QTc-prolonging activities of Dofetilide.
PropafenonePropafenone may increase the arrhythmogenic activities of Dofetilide.
PropofolThe serum concentration of Dofetilide can be increased when it is combined with Propofol.
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Dofetilide.
QuetiapineDofetilide may increase the QTc-prolonging activities of Quetiapine.
QuinethazoneQuinethazone may increase the QTc-prolonging activities of Dofetilide.
QuinidineDofetilide may increase the QTc-prolonging activities of Quinidine.
QuinineDofetilide may increase the QTc-prolonging activities of Quinine.
QuinupristinThe serum concentration of Dofetilide can be increased when it is combined with Quinupristin.
RadicicolThe metabolism of Dofetilide can be decreased when combined with Radicicol.
RanolazineThe serum concentration of Dofetilide can be increased when it is combined with Ranolazine.
RifabutinThe metabolism of Dofetilide can be increased when combined with Rifabutin.
RifampicinThe metabolism of Dofetilide can be increased when combined with Rifampicin.
RifapentineThe metabolism of Dofetilide can be increased when combined with Rifapentine.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Dofetilide.
RisperidoneRisperidone may increase the QTc-prolonging activities of Dofetilide.
RitonavirThe serum concentration of Dofetilide can be increased when it is combined with Ritonavir.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Dofetilide.
Salicylhydroxamic AcidThe metabolism of Dofetilide can be decreased when combined with Salicylhydroxamic Acid.
Salicylic acidThe metabolism of Dofetilide can be decreased when combined with Salicylic acid.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Dofetilide.
SaquinavirSaquinavir may increase the arrhythmogenic activities of Dofetilide.
SertaconazoleThe metabolism of Dofetilide can be decreased when combined with Sertaconazole.
SertralineSertraline may increase the QTc-prolonging activities of Dofetilide.
SevofluraneSevoflurane may increase the QTc-prolonging activities of Dofetilide.
SildenafilThe serum concentration of Dofetilide can be increased when it is combined with Sildenafil.
SiltuximabThe serum concentration of Dofetilide can be decreased when it is combined with Siltuximab.
SimeprevirThe serum concentration of Dofetilide can be increased when it is combined with Simeprevir.
SinefunginThe metabolism of Dofetilide can be decreased when combined with Sinefungin.
SirolimusThe metabolism of Dofetilide can be decreased when combined with Sirolimus.
SolifenacinSolifenacin may increase the QTc-prolonging activities of Dofetilide.
SorafenibSorafenib may increase the QTc-prolonging activities of Dofetilide.
SotalolDofetilide may increase the QTc-prolonging activities of Sotalol.
St. John's WortThe serum concentration of Dofetilide can be decreased when it is combined with St. John's Wort.
StiripentolThe serum concentration of Dofetilide can be increased when it is combined with Stiripentol.
SulconazoleThe metabolism of Dofetilide can be decreased when combined with Sulconazole.
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Dofetilide.
SulfisoxazoleSulfisoxazole may increase the QTc-prolonging activities of Dofetilide.
SunitinibSunitinib may increase the QTc-prolonging activities of Dofetilide.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Dofetilide.
TavaboroleThe metabolism of Dofetilide can be decreased when combined with Tavaborole.
TelaprevirThe serum concentration of Dofetilide can be increased when it is combined with Telaprevir.
TelavancinTelavancin may increase the QTc-prolonging activities of Dofetilide.
TelithromycinTelithromycin may increase the QTc-prolonging activities of Dofetilide.
TerbinafineThe metabolism of Dofetilide can be decreased when combined with Terbinafine.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Dofetilide.
TerconazoleThe metabolism of Dofetilide can be decreased when combined with Terconazole.
TetrabenazineDofetilide may increase the QTc-prolonging activities of Tetrabenazine.
ThioridazineDofetilide may increase the QTc-prolonging activities of Thioridazine.
ThiothixeneThiothixene may increase the QTc-prolonging activities of Dofetilide.
ThymolThe metabolism of Dofetilide can be decreased when combined with Thymol.
TicagrelorThe serum concentration of Dofetilide can be increased when it is combined with Ticagrelor.
TiclopidineThe serum concentration of Dofetilide can be increased when it is combined with Ticlopidine.
TioconazoleThe metabolism of Dofetilide can be decreased when combined with Tioconazole.
TizanidineTizanidine may increase the QTc-prolonging activities of Dofetilide.
TocilizumabThe serum concentration of Dofetilide can be decreased when it is combined with Tocilizumab.
TolnaftateThe metabolism of Dofetilide can be decreased when combined with Tolnaftate.
TolterodineTolterodine may increase the QTc-prolonging activities of Dofetilide.
TorasemideTorasemide may increase the QTc-prolonging activities of Dofetilide.
ToremifeneDofetilide may increase the QTc-prolonging activities of Toremifene.
TrazodoneTrazodone may increase the QTc-prolonging activities of Dofetilide.
TreprostinilTreprostinil may increase the QTc-prolonging activities of Dofetilide.
TriamtereneThe serum concentration of Dofetilide can be increased when it is combined with Triamterene.
TrichlormethiazideTrichlormethiazide may increase the QTc-prolonging activities of Dofetilide.
TrimethoprimTrimethoprim may decrease the excretion rate of Dofetilide which could result in a lower serum level and potentially a reduction in efficacy.
TrimetrexateThe metabolism of Dofetilide can be decreased when combined with Trimetrexate.
TrimipramineTrimipramine may increase the QTc-prolonging activities of Dofetilide.
TriptorelinTriptorelin may increase the QTc-prolonging activities of Dofetilide.
VandetanibDofetilide may increase the QTc-prolonging activities of Vandetanib.
VardenafilVardenafil may increase the QTc-prolonging activities of Dofetilide.
VemurafenibDofetilide may increase the QTc-prolonging activities of Vemurafenib.
VenlafaxineThe serum concentration of Dofetilide can be increased when it is combined with Venlafaxine.
VerapamilThe serum concentration of Dofetilide can be increased when it is combined with Verapamil.
VilanterolVilanterol may increase the QTc-prolonging activities of Dofetilide.
VoriconazoleThe metabolism of Dofetilide can be decreased when combined with Voriconazole.
VorinostatVorinostat may increase the QTc-prolonging activities of Dofetilide.
ZiprasidoneDofetilide may increase the QTc-prolonging activities of Ziprasidone.
ZuclopenthixolDofetilide may increase the QTc-prolonging activities of Zuclopenthixol.
Food InteractionsNot Available

Targets

Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Voltage-gated potassium channel activity involved in ventricular cardiac muscle cell action potential repolarization
Specific Function:
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr). Isoforms USO have no channel activity by themself, but modulates channel characteristics by forming heterotetramers with other isoforms which are r...
Gene Name:
KCNH2
Uniprot ID:
Q12809
Molecular Weight:
126653.52 Da
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:10648647 ]
  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:10712445 ]
  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:11166283 ]
  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:11698075 ]
  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:11723241 ]
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. [PubMed:11752352 ]
  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:9486667 ]
  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:15548764 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Potassium ion leak channel activity
Specific Function:
Ion channel that contributes to passive transmembrane potassium transport (PubMed:23169818). Reversibly converts between a voltage-insensitive potassium leak channel and a voltage-dependent outward rectifying potassium channel in a phosphorylation-dependent manner (PubMed:11319556). In astrocytes, forms mostly heterodimeric potassium channels with KCNK1, with only a minor proportion of function...
Gene Name:
KCNK2
Uniprot ID:
O95069
Molecular Weight:
47092.215 Da
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:17139284 ]
  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:17016423 ]
  3. Roukoz H, Saliba W: Dofetilide: a new class III antiarrhythmic agent. Expert Rev Cardiovasc Ther. 2007 Jan;5(1):9-19. [PubMed:17187453 ]
Kind
Protein
Organism
Human
Pharmacological action
yes
Actions
inhibitor
General Function:
Inward rectifier potassium channel activity
Specific Function:
Inward rectifying potassium channel that is activated by phosphatidylinositol 4,5-bisphosphate and that probably participates in controlling the resting membrane potential in electrically excitable cells. Probably participates in establishing action potential waveform and excitability of neuronal and muscle tissues. Inward rectifier potassium channels are characterized by a greater tendency to ...
Gene Name:
KCNJ12
Uniprot ID:
Q14500
Molecular Weight:
49000.6 Da
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:8700146 ]

Enzymes

Kind
Protein
Organism
Human
Pharmacological action
unknown
Actions
substrate
General Function:
Vitamin d3 25-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 performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiot...
Gene Name:
CYP3A4
Uniprot ID:
P08684
Molecular Weight:
57342.67 Da
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. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [PubMed:19934256 ]
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Drug created on June 13, 2005 07:24 / Updated on September 29, 2016 02:25