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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
beta-((P-Methanesulfonamidophenethyl)methylamino)methanesulfono-P-phenetidide
Dofetilida
Dofetilide
Dofetilidum
Tikosyn
External Identifiers Not Available
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
Tikosyncapsule.125 mg/1oralPfizer Laboratories Div Pfizer Inc1999-10-012016-04-23Us
Tikosyncapsule.5 mg/1oralPfizer Laboratories Div Pfizer Inc1999-10-012016-04-23Us
Tikosyncapsule.25 mg/1oralPfizer Laboratories Div Pfizer Inc1999-10-012016-04-23Us
Generic Prescription ProductsNot Available
Over the Counter ProductsNot 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
SpectraNot 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
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.
AmoxapineAmoxapine may increase the QTc-prolonging activities of Dofetilide.
AnagrelideDofetilide may increase the QTc-prolonging activities of Anagrelide.
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.
ArtemetherDofetilide may increase the QTc-prolonging activities of Artemether.
AsenapineDofetilide may increase the QTc-prolonging activities of Asenapine.
AtazanavirAtazanavir may increase the QTc-prolonging activities of Dofetilide.
AtomoxetineAtomoxetine may increase the QTc-prolonging activities of Dofetilide.
AtorvastatinThe serum concentration of Dofetilide can be increased when it is combined with Atorvastatin.
AzithromycinAzithromycin may increase the QTc-prolonging activities of Dofetilide.
BedaquilineBedaquiline may increase the QTc-prolonging activities of Dofetilide.
BicalutamideThe serum concentration of Dofetilide can be increased when it is combined with Bicalutamide.
BoceprevirThe serum concentration of Dofetilide can be increased when it is combined with Boceprevir.
BortezomibBortezomib may increase the QTc-prolonging activities of Dofetilide.
BosutinibBosutinib may increase the QTc-prolonging activities of Dofetilide.
BumetanideBumetanide may increase the QTc-prolonging activities of Dofetilide.
BuserelinBuserelin may increase the QTc-prolonging activities of Dofetilide.
CeritinibCeritinib may increase the QTc-prolonging activities of Dofetilide.
ChloroquineChloroquine may increase the QTc-prolonging activities of Dofetilide.
ChlorothiazideChlorothiazide may increase the QTc-prolonging activities of Dofetilide.
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Dofetilide.
ChlorthalidoneChlorthalidone may increase the QTc-prolonging activities of Dofetilide.
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.
CitalopramCitalopram may increase the QTc-prolonging activities of Dofetilide.
ClarithromycinClarithromycin may increase the QTc-prolonging activities of Dofetilide.
ClomipramineClomipramine may increase the QTc-prolonging activities of Dofetilide.
ClotrimazoleThe serum concentration of Dofetilide can be increased when it is 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 serum concentration of Dofetilide can be increased when it is combined with Cyclosporine.
DabrafenibDabrafenib may increase the QTc-prolonging activities of Dofetilide.
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.
DasatinibDasatinib may increase the QTc-prolonging activities of Dofetilide.
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.
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.
DronedaroneDofetilide may increase the QTc-prolonging activities of Dronedarone.
DroperidolDroperidol may increase the QTc-prolonging activities of Dofetilide.
EliglustatDofetilide may increase the QTc-prolonging activities of Eliglustat.
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.
Etacrynic acidEthacrynic acid may increase the QTc-prolonging activities of Dofetilide.
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 serum concentration of Dofetilide can be increased when it is combined with Fluconazole.
FluoxetineDofetilide may increase the QTc-prolonging activities of Fluoxetine.
FlupentixolDofetilide may increase the QTc-prolonging activities of Flupentixol.
Fluticasone PropionateFluticasone Propionate may increase the QTc-prolonging activities of Dofetilide.
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.
FosphenytoinFosphenytoin may increase the QTc-prolonging activities of Dofetilide.
FurosemideFurosemide may increase the QTc-prolonging activities of Dofetilide.
Gadobenic acidGadobenate Dimeglumine 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.
GoserelinGoserelin may increase the QTc-prolonging activities of Dofetilide.
GranisetronGranisetron may increase the QTc-prolonging activities of Dofetilide.
HaloperidolHaloperidol may increase the QTc-prolonging activities of Dofetilide.
HistrelinHistrelin may increase the QTc-prolonging activities of Dofetilide.
HydrochlorothiazideHydrochlorothiazide 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.
IsofluraneIsoflurane may increase the QTc-prolonging activities of Dofetilide.
IsoniazidThe serum concentration of Dofetilide can be increased when it is combined with Isoniazid.
IsradipineIsradipine may increase the QTc-prolonging activities of Dofetilide.
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.
LapatinibLapatinib may increase the QTc-prolonging activities of Dofetilide.
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.
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.
MifepristoneMifepristone may increase the QTc-prolonging activities of Dofetilide.
MirabegronMirabegron may increase the QTc-prolonging activities of Dofetilide.
MirtazapineMirtazapine may increase the QTc-prolonging activities of Dofetilide.
MoexiprilMoexipril may increase the QTc-prolonging activities of Dofetilide.
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Dofetilide.
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.
NicardipineNicardipine may increase the QTc-prolonging activities of Dofetilide.
NilotinibDofetilide may increase the QTc-prolonging activities of Nilotinib.
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Dofetilide.
NortriptylineNortriptyline may increase the QTc-prolonging activities of Dofetilide.
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.
OlodaterolOlodaterol may increase the QTc-prolonging activities of Dofetilide.
OndansetronOndansetron may increase the QTc-prolonging activities of Dofetilide.
OsimertinibOsimertinib may increase the QTc-prolonging activities of Dofetilide.
OxytocinOxytocin may increase the QTc-prolonging activities of Dofetilide.
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.
PentamidinePentamidine may increase the QTc-prolonging activities of Dofetilide.
PerflutrenPerflutren may increase the QTc-prolonging activities of Dofetilide.
PimozideDofetilide may increase the QTc-prolonging activities of Pimozide.
PosaconazoleThe metabolism of Dofetilide can be decreased when combined with Posaconazole.
PrimaquinePrimaquine may increase the QTc-prolonging activities of Dofetilide.
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.
PropofolPropofol may increase the QTc-prolonging activities of Dofetilide.
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Dofetilide.
QuetiapineDofetilide may increase the QTc-prolonging activities of Quetiapine.
QuinidineDofetilide may increase the QTc-prolonging activities of Quinidine.
QuinineDofetilide may increase the QTc-prolonging activities of Quinine.
RanolazineRanolazine may increase the QTc-prolonging activities of Dofetilide.
RilpivirineRilpivirine may increase the QTc-prolonging activities of Dofetilide.
RisperidoneRisperidone may increase the QTc-prolonging activities of Dofetilide.
RitonavirRitonavir may increase the QTc-prolonging activities of Dofetilide.
SalbutamolSalbutamol may increase the QTc-prolonging activities of Dofetilide.
SalmeterolSalmeterol may increase the QTc-prolonging activities of Dofetilide.
SaquinavirSaquinavir may increase the arrhythmogenic activities of Dofetilide.
SertralineSertraline may increase the QTc-prolonging activities of Dofetilide.
SevofluraneSevoflurane may increase the QTc-prolonging activities of Dofetilide.
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.
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.
TacrolimusTacrolimus may increase the QTc-prolonging activities of Dofetilide.
TamoxifenTamoxifen may increase the QTc-prolonging activities of Dofetilide.
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.
TerbutalineTerbutaline may increase the QTc-prolonging activities of Dofetilide.
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.
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.
TizanidineTizanidine may increase the QTc-prolonging activities of Dofetilide.
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.
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.
VenlafaxineVenlafaxine may increase the QTc-prolonging activities of Dofetilide.
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 May 06, 2016 02:27