Identification

Name
Dofetilide
Accession Number
DB00204  (APRD00367)
Type
Small Molecule
Groups
Approved, Investigational
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.

Structure
Thumb
Synonyms
  • beta-((p-Methanesulfonamidophenethyl)methylamino)methanesulfono-p-phenetidide
  • Dofetilida
  • Dofetilidum
External IDs
UK-68,798 / UK-68798
Product Images
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DofetilideCapsule.5 mg/1OralGreenstone, Llc2016-05-01Not applicableUs
DofetilideCapsule.25 mg/1OralGreenstone, Llc2016-05-01Not applicableUs
DofetilideCapsule.125 mg/1OralGreenstone, Llc1999-10-01Not applicableUs
TikosynCapsule.5 mg/1OralAvera Mc Kennan Hospital2016-03-28Not applicableUs
TikosynCapsule.125 mg/1OralPfizer Laboratories Div Pfizer Inc.1999-10-01Not applicableUs
TikosynCapsule.5 mg/1OralPfizer Laboratories Div Pfizer Inc.1999-10-01Not applicableUs
TikosynCapsule.25 mg/1OralAvera Mc Kennan Hospital2016-07-29Not applicableUs
TikosynCapsule.25 mg/1OralPfizer Laboratories Div Pfizer Inc.1999-10-01Not applicableUs00069 5810 60 nlmimage10 213e90f4
TikosynCapsule.125 mg/1OralAvera Mc Kennan Hospital2016-06-28Not applicableUs
Generic Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
DofetilideCapsule500 ug/1OralSigma Pharm Laboratories, Llc2018-05-21Not applicableUs
DofetilideCapsule.5 mg/1OralMayne Pharma2016-06-07Not applicableUs
DofetilideCapsule.5 mg/1OralBionpharma Inc.2018-04-11Not applicableUs
DofetilideCapsule.125 mg/1OralMayne Pharma2016-06-07Not applicableUs
DofetilideCapsule250 ug/1OralSigma Pharm Laboratories, Llc2018-05-21Not applicableUs
DofetilideCapsule.25 mg/1OralBionpharma Inc.2018-04-11Not applicableUs
DofetilideCapsule.25 mg/1OralMayne Pharma2016-06-07Not applicableUs
DofetilideCapsule125 ug/1OralSigma Pharm Laboratories, Llc2018-05-21Not applicableUs
DofetilideCapsule.125 mg/1OralBionpharma Inc.2018-04-11Not applicableUs
Categories
UNII
R4Z9X1N2ND
CAS number
115256-11-6
Weight
Average: 441.565
Monoisotopic: 441.139212369
Chemical Formula
C19H27N3O5S2
InChI Key
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

Pharmacology

Indication

For 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

Associated Conditions
Pharmacodynamics

Dofetilide 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 action

The 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).

TargetActionsOrganism
APotassium voltage-gated channel subfamily H member 2
inhibitor
Human
APotassium channel subfamily K member 2
inhibitor
Human
AATP-sensitive inward rectifier potassium channel 12
inhibitor
Human
Absorption

>90%

Volume of distribution
  • 3 L/kg
Protein binding

60% -70%

Metabolism

Hepatic

Route of elimination
Not Available
Half life

10 hours

Clearance
Not Available
Toxicity
Not Available
Affected organisms
  • Humans and other mammals
Pathways
Not Available
Pharmacogenomic Effects/ADRs
Not Available

Interactions

Drug Interactions
DrugInteractionDrug group
2-HYDROXY-1,4-NAPHTHOQUINONEThe serum concentration of Dofetilide can be increased when it is combined with 2-HYDROXY-1,4-NAPHTHOQUINONE.Experimental
2-mercaptobenzothiazoleThe serum concentration of Dofetilide can be increased when it is combined with 2-mercaptobenzothiazole.Vet Approved
Acetyl sulfisoxazoleThe serum concentration of Dofetilide can be increased when it is combined with Acetyl sulfisoxazole.Approved, Vet Approved
AlfuzosinAlfuzosin may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
AmantadineAmantadine may increase the QTc-prolonging activities of Dofetilide.Approved
AmilorideThe serum concentration of Dofetilide can be increased when it is combined with Amiloride.Approved
AmiodaroneThe serum concentration of Dofetilide can be increased when it is combined with Amiodarone.Approved, Investigational
AmitriptylineAmitriptyline may increase the QTc-prolonging activities of Dofetilide.Approved
AmorolfineThe serum concentration of Dofetilide can be increased when it is combined with Amorolfine.Approved, Investigational
AmoxapineAmoxapine may increase the QTc-prolonging activities of Dofetilide.Approved
Amphotericin BThe serum concentration of Dofetilide can be increased when it is combined with Amphotericin B.Approved, Investigational
AnagrelideThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Anagrelide.Approved
AnidulafunginThe serum concentration of Dofetilide can be increased when it is combined with Anidulafungin.Approved, Investigational
ApalutamideThe serum concentration of Dofetilide can be decreased when it is combined with Apalutamide.Approved, Investigational
ApomorphineApomorphine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
AprepitantThe serum concentration of Dofetilide can be increased when it is combined with Aprepitant.Approved, Investigational
ArformoterolArformoterol may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
AripiprazoleAripiprazole may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
Arsenic trioxideThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Arsenic trioxide.Approved, Investigational
ArtemetherThe serum concentration of Dofetilide can be increased when it is combined with Artemether.Approved
AsenapineThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Asenapine.Approved
AtazanavirThe serum concentration of Dofetilide can be increased when it is combined with Atazanavir.Approved, Investigational
AtomoxetineThe serum concentration of Dofetilide can be increased when it is combined with Atomoxetine.Approved
AzithromycinAzithromycin may increase the QTc-prolonging activities of Dofetilide.Approved
AzosemideThe risk or severity of QTc prolongation, torsade de pointes, hypokalemia, hypomagnesemia, and cardiac arrest can be increased when Azosemide is combined with Dofetilide.Investigational
Bafilomycin A1The serum concentration of Dofetilide can be increased when it is combined with Bafilomycin A1.Experimental
BedaquilineBedaquiline may increase the QTc-prolonging activities of Dofetilide.Approved
BendroflumethiazideBendroflumethiazide may increase the QTc-prolonging activities of Dofetilide.Approved
Benzoic AcidThe serum concentration of Dofetilide can be increased when it is combined with Benzoic Acid.Approved, Investigational
BenzthiazideBenzthiazide may increase the QTc-prolonging activities of Dofetilide.Approved
BifonazoleThe serum concentration of Dofetilide can be increased when it is combined with Bifonazole.Approved, Investigational
BoceprevirThe serum concentration of Dofetilide can be increased when it is combined with Boceprevir.Approved, Withdrawn
BortezomibThe serum concentration of Dofetilide can be increased when it is combined with Bortezomib.Approved, Investigational
BosentanThe serum concentration of Dofetilide can be decreased when it is combined with Bosentan.Approved, Investigational
Brefeldin AThe serum concentration of Dofetilide can be increased when it is combined with Brefeldin A.Experimental
BumetanideThe risk or severity of QTc prolongation, torsade de pointes, hypokalemia, hypomagnesemia, and cardiac arrest can be increased when Bumetanide is combined with Dofetilide.Approved
BuserelinBuserelin may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
ButenafineThe serum concentration of Dofetilide can be increased when it is combined with Butenafine.Approved
ButoconazoleThe serum concentration of Dofetilide can be increased when it is combined with Butoconazole.Approved
CandicidinThe serum concentration of Dofetilide can be increased when it is combined with Candicidin.Withdrawn
Capric acidThe serum concentration of Dofetilide can be increased when it is combined with Capric acid.Experimental
CarbamazepineThe metabolism of Dofetilide can be increased when combined with Carbamazepine.Approved, Investigational
CaspofunginThe serum concentration of Dofetilide can be increased when it is combined with Caspofungin.Approved
CeritinibThe serum concentration of Dofetilide can be increased when it is combined with Ceritinib.Approved
CeruleninThe serum concentration of Dofetilide can be increased when it is combined with Cerulenin.Approved
ChloroquineChloroquine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational, Vet Approved
ChlorothiazideChlorothiazide may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
ChloroxineThe serum concentration of Dofetilide can be increased when it is combined with Chloroxine.Approved
ChlorpromazineChlorpromazine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational, Vet Approved
ChlorthalidoneChlorthalidone may increase the QTc-prolonging activities of Dofetilide.Approved
CiclopiroxThe serum concentration of Dofetilide can be increased when it is combined with Ciclopirox.Approved, Investigational
CimetidineThe serum concentration of Dofetilide can be increased when it is combined with Cimetidine.Approved, Investigational
CiprofloxacinCiprofloxacin may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
CisaprideThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Cisapride.Approved, Investigational, Withdrawn
CitalopramThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Citalopram.Approved
ClarithromycinThe serum concentration of Dofetilide can be increased when it is combined with Clarithromycin.Approved
ClemastineThe serum concentration of Dofetilide can be increased when it is combined with Clemastine.Approved, Investigational
ClomipramineClomipramine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational, Vet Approved
ClotrimazoleThe serum concentration of Dofetilide can be increased when it is combined with Clotrimazole.Approved, Vet Approved
ClozapineClozapine may increase the QTc-prolonging activities of Dofetilide.Approved
CobicistatThe serum concentration of Dofetilide can be increased when it is combined with Cobicistat.Approved
ConivaptanThe serum concentration of Conivaptan can be increased when it is combined with Dofetilide.Approved, Investigational
CordycepinThe serum concentration of Dofetilide can be increased when it is combined with Cordycepin.Investigational
CrizotinibThe serum concentration of Dofetilide can be increased when it is combined with Crizotinib.Approved
CurcuminThe serum concentration of Dofetilide can be increased when it is combined with Curcumin.Approved, Investigational
CyclopenthiazideCyclopenthiazide may increase the QTc-prolonging activities of Dofetilide.Experimental
CyclosporineThe serum concentration of Dofetilide can be increased when it is combined with Cyclosporine.Approved, Investigational, Vet Approved
DabrafenibThe serum concentration of Dofetilide can be decreased when it is combined with Dabrafenib.Approved, Investigational
DarunavirThe serum concentration of Dofetilide can be increased when it is combined with Darunavir.Approved
DasatinibThe serum concentration of Dofetilide can be increased when it is combined with Dasatinib.Approved, Investigational
DeferasiroxThe serum concentration of Dofetilide can be decreased when it is combined with Deferasirox.Approved, Investigational
DegarelixDegarelix may increase the QTc-prolonging activities of Dofetilide.Approved
DelamanidDofetilide may increase the QTc-prolonging activities of Delamanid.Approved, Investigational
DelavirdineThe serum concentration of Dofetilide can be increased when it is combined with Delavirdine.Approved
DesfluraneDesflurane may increase the QTc-prolonging activities of Dofetilide.Approved
DesipramineDesipramine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
DeutetrabenazineDofetilide may increase the QTc-prolonging activities of Deutetrabenazine.Approved, Investigational
DichloropheneThe serum concentration of Dofetilide can be increased when it is combined with Dichlorophene.Vet Approved
DihydroergotamineThe serum concentration of Dofetilide can be increased when it is combined with Dihydroergotamine.Approved, Investigational
DiltiazemThe serum concentration of Dofetilide can be increased when it is combined with Diltiazem.Approved, Investigational
DiphenhydramineDiphenhydramine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
DisopyramideThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Disopyramide.Approved
DolasetronDolasetron may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
DolutegravirThe serum concentration of Dofetilide can be increased when it is combined with Dolutegravir.Approved
DomperidoneThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Domperidone.Approved, Investigational, Vet Approved
DoxepinDoxepin may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
DoxycyclineThe serum concentration of Dofetilide can be increased when it is combined with Doxycycline.Approved, Investigational, Vet Approved
DronedaroneThe serum concentration of Dofetilide can be increased when it is combined with Dronedarone.Approved
DroperidolDroperidol may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
EconazoleThe serum concentration of Dofetilide can be increased when it is combined with Econazole.Approved
EfinaconazoleThe serum concentration of Dofetilide can be increased when it is combined with Efinaconazole.Approved
EliglustatThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Eliglustat.Approved
EnzalutamideThe serum concentration of Dofetilide can be decreased when it is combined with Enzalutamide.Approved
EpitizideEpitizide may increase the QTc-prolonging activities of Dofetilide.Experimental
EribulinEribulin may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
ErythromycinThe serum concentration of Dofetilide can be increased when it is combined with Erythromycin.Approved, Investigational, Vet Approved
EscitalopramThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Escitalopram.Approved, Investigational
Etacrynic acidThe risk or severity of QTc prolongation, torsade de pointes, hypokalemia, hypomagnesemia, and cardiac arrest can be increased when Etacrynic acid is combined with Dofetilide.Approved, Investigational
EzogabineEzogabine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
FamotidineFamotidine may increase the QTc-prolonging activities of Dofetilide.Approved
FelbamateFelbamate may increase the QTc-prolonging activities of Dofetilide.Approved
FenticonazoleThe serum concentration of Dofetilide can be increased when it is combined with Fenticonazole.Experimental
FingolimodFingolimod may increase the arrhythmogenic activities of Dofetilide.Approved, Investigational
FlecainideFlecainide may increase the QTc-prolonging activities of Dofetilide.Approved, Withdrawn
FluconazoleThe serum concentration of Dofetilide can be increased when it is combined with Fluconazole.Approved, Investigational
FlucytosineThe serum concentration of Dofetilide can be increased when it is combined with Flucytosine.Approved, Investigational
FluoxetineThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Fluoxetine.Approved, Vet Approved
FlupentixolThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Flupentixol.Approved, Investigational, Withdrawn
FlutrimazoleThe serum concentration of Dofetilide can be increased when it is combined with Flutrimazole.Experimental
FluvoxamineThe serum concentration of Dofetilide can be increased when it is combined with Fluvoxamine.Approved, Investigational
FormoterolFormoterol may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
FosamprenavirThe serum concentration of Dofetilide can be increased when it is combined with Fosamprenavir.Approved
FosaprepitantThe serum concentration of Dofetilide can be increased when it is combined with Fosaprepitant.Approved
FoscarnetFoscarnet may increase the QTc-prolonging activities of Dofetilide.Approved
FosphenytoinThe metabolism of Dofetilide can be increased when combined with Fosphenytoin.Approved, Investigational
FurosemideThe risk or severity of QTc prolongation, torsade de pointes, hypokalemia, hypomagnesemia, and cardiac arrest can be increased when Furosemide is combined with Dofetilide.Approved, Vet Approved
Fusidic AcidThe serum concentration of Dofetilide can be increased when it is combined with Fusidic Acid.Approved, Investigational
Gadobenic acidGadobenic acid may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
GalantamineGalantamine may increase the QTc-prolonging activities of Dofetilide.Approved
GemifloxacinGemifloxacin may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
GlyphosateThe serum concentration of Dofetilide can be increased when it is combined with Glyphosate.Experimental
GoserelinGoserelin may increase the QTc-prolonging activities of Dofetilide.Approved
GranisetronGranisetron may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
GriseofulvinThe serum concentration of Dofetilide can be increased when it is combined with Griseofulvin.Approved, Investigational, Vet Approved
HachimycinThe serum concentration of Dofetilide can be increased when it is combined with Hachimycin.Experimental
HaloperidolHaloperidol may increase the QTc-prolonging activities of Dofetilide.Approved
HaloproginThe serum concentration of Dofetilide can be increased when it is combined with Haloprogin.Approved, Withdrawn
HexetidineThe serum concentration of Dofetilide can be increased when it is combined with Hexetidine.Approved, Investigational
HistrelinHistrelin may increase the QTc-prolonging activities of Dofetilide.Approved
HydrochlorothiazideHydrochlorothiazide may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
HydroflumethiazideHydroflumethiazide may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
HydroxyzineHydroxyzine may increase the QTc-prolonging activities of Dofetilide.Approved
IbandronateIbandronate may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
IbutilideThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Ibutilide.Approved
IdelalisibThe serum concentration of Dofetilide can be increased when it is combined with Idelalisib.Approved
IloperidoneThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Iloperidone.Approved
ImatinibThe serum concentration of Dofetilide can be increased when it is combined with Imatinib.Approved
ImipramineImipramine may increase the QTc-prolonging activities of Dofetilide.Approved
IndacaterolIndacaterol may increase the QTc-prolonging activities of Dofetilide.Approved
IndapamideIndapamide may increase the QTc-prolonging activities of Dofetilide.Approved
IndinavirThe serum concentration of Dofetilide can be increased when it is combined with Indinavir.Approved
IsavuconazoleThe serum concentration of Dofetilide can be increased when it is combined with Isavuconazole.Approved, Investigational
IsavuconazoniumThe serum concentration of Dofetilide can be increased when it is combined with Isavuconazonium.Approved, Investigational
IsoconazoleThe serum concentration of Dofetilide can be increased when it is combined with Isoconazole.Approved
IsofluraneIsoflurane may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
IsradipineThe serum concentration of Dofetilide can be increased when it is combined with Isradipine.Approved, Investigational
ItraconazoleThe serum concentration of Dofetilide can be increased when it is combined with Itraconazole.Approved, Investigational
IvabradineDofetilide may increase the QTc-prolonging activities of Ivabradine.Approved
IvacaftorThe serum concentration of Dofetilide can be increased when it is combined with Ivacaftor.Approved
KetoconazoleThe serum concentration of Dofetilide can be increased when it is combined with Ketoconazole.Approved, Investigational
LamotrigineThe serum concentration of Dofetilide can be increased when it is combined with Lamotrigine.Approved, Investigational
LapatinibLapatinib may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
LenvatinibLenvatinib may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
LeuprolideLeuprolide may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
LevofloxacinLevofloxacin may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
LidocaineLidocaine may increase the arrhythmogenic activities of Dofetilide.Approved, Vet Approved
LithiumLithium may increase the QTc-prolonging activities of Dofetilide.Approved
LopinavirThe serum concentration of Dofetilide can be increased when it is combined with Lopinavir.Approved
LorpiprazoleThe serum concentration of Dofetilide can be increased when it is combined with Lorpiprazole.Approved
LovastatinThe serum concentration of Dofetilide can be increased when it is combined with Lovastatin.Approved, Investigational
LuliconazoleThe serum concentration of Dofetilide can be increased when it is combined with Luliconazole.Approved
LumacaftorThe metabolism of Dofetilide can be increased when combined with Lumacaftor.Approved
LumefantrineThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Lumefantrine.Approved
MacimorelinDofetilide may increase the QTc-prolonging activities of Macimorelin.Approved, Investigational
MaprotilineMaprotiline may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
MefloquineMefloquine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
Megestrol acetateThe serum concentration of Dofetilide can be increased when it is combined with Megestrol acetate.Approved, Investigational, Vet Approved
MepartricinThe serum concentration of Dofetilide can be increased when it is combined with Mepartricin.Experimental
MetforminThe serum concentration of Dofetilide can be increased when it is combined with Metformin.Approved
MethadoneMethadone may increase the QTc-prolonging activities of Dofetilide.Approved
MethotrimeprazineMethotrimeprazine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
MethyclothiazideMethyclothiazide may increase the QTc-prolonging activities of Dofetilide.Approved
MetoclopramideMetoclopramide may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
MetolazoneMetolazone may increase the QTc-prolonging activities of Dofetilide.Approved
MetronidazoleMetronidazole may increase the QTc-prolonging activities of Dofetilide.Approved
MevastatinThe serum concentration of Dofetilide can be increased when it is combined with Mevastatin.Experimental
MicafunginThe serum concentration of Dofetilide can be increased when it is combined with Micafungin.Approved, Investigational
MiconazoleThe serum concentration of Dofetilide can be increased when it is combined with Miconazole.Approved, Investigational, Vet Approved
MifepristoneDofetilide may increase the QTc-prolonging activities of Mifepristone.Approved, Investigational
MiltefosineThe serum concentration of Dofetilide can be increased when it is combined with Miltefosine.Approved, Investigational
MirabegronMirabegron may increase the QTc-prolonging activities of Dofetilide.Approved
MirtazapineMirtazapine may increase the QTc-prolonging activities of Dofetilide.Approved
MitotaneThe serum concentration of Dofetilide can be decreased when it is combined with Mitotane.Approved
MoexiprilMoexipril may increase the QTc-prolonging activities of Dofetilide.Approved
MonensinThe serum concentration of Dofetilide can be increased when it is combined with Monensin.Vet Approved
MoxifloxacinMoxifloxacin may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
MyxothiazolThe serum concentration of Dofetilide can be increased when it is combined with Myxothiazol.Experimental
NaftifineThe serum concentration of Dofetilide can be increased when it is combined with Naftifine.Approved
NatamycinThe serum concentration of Dofetilide can be increased when it is combined with Natamycin.Approved
NefazodoneThe serum concentration of Dofetilide can be increased when it is combined with Nefazodone.Approved, Withdrawn
NelfinavirThe serum concentration of Dofetilide can be increased when it is combined with Nelfinavir.Approved
NetupitantThe serum concentration of Dofetilide can be increased when it is combined with Netupitant.Approved, Investigational
NevirapineThe serum concentration of Dofetilide can be increased when it is combined with Nevirapine.Approved
NicardipineNicardipine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
NifuratelThe serum concentration of Dofetilide can be increased when it is combined with Nifuratel.Experimental
Nikkomycin ZThe serum concentration of Dofetilide can be increased when it is combined with Nikkomycin Z.Investigational
NilotinibThe serum concentration of Dofetilide can be increased when it is combined with Nilotinib.Approved, Investigational
NitroxolineThe serum concentration of Dofetilide can be increased when it is combined with Nitroxoline.Approved
NorfloxacinNorfloxacin may increase the QTc-prolonging activities of Dofetilide.Approved
NortriptylineNortriptyline may increase the QTc-prolonging activities of Dofetilide.Approved
NystatinThe serum concentration of Dofetilide can be increased when it is combined with Nystatin.Approved, Vet Approved
OctreotideOctreotide may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
OfloxacinOfloxacin may increase the QTc-prolonging activities of Dofetilide.Approved
OlanzapineOlanzapine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
OlaparibThe serum concentration of Dofetilide can be increased when it is combined with Olaparib.Approved
OlodaterolOlodaterol may increase the QTc-prolonging activities of Dofetilide.Approved
OmoconazoleThe serum concentration of Dofetilide can be increased when it is combined with Omoconazole.Experimental
OndansetronOndansetron may increase the QTc-prolonging activities of Dofetilide.Approved
OsimertinibThe serum concentration of Dofetilide can be increased when it is combined with Osimertinib.Approved
OxiconazoleThe serum concentration of Dofetilide can be increased when it is combined with Oxiconazole.Approved
OxytocinOxytocin may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
PafuramidineThe serum concentration of Dofetilide can be increased when it is combined with Pafuramidine.Investigational
PalbociclibThe serum concentration of Dofetilide can be increased when it is combined with Palbociclib.Approved, Investigational
PaliperidoneThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Paliperidone.Approved
PanobinostatPanobinostat may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
ParoxetineParoxetine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
PasireotidePasireotide may increase the QTc-prolonging activities of Dofetilide.Approved
PazopanibPazopanib may increase the QTc-prolonging activities of Dofetilide.Approved
PentamidineThe serum concentration of Dofetilide can be increased when it is combined with Pentamidine.Approved, Investigational
PentobarbitalThe metabolism of Dofetilide can be increased when combined with Pentobarbital.Approved, Investigational, Vet Approved
PerflutrenPerflutren may increase the QTc-prolonging activities of Dofetilide.Approved
PhenobarbitalThe metabolism of Dofetilide can be increased when combined with Phenobarbital.Approved, Investigational
PhenytoinThe metabolism of Dofetilide can be increased when combined with Phenytoin.Approved, Vet Approved
PimozideThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Pimozide.Approved
PiretanideThe risk or severity of QTc prolongation, torsade de pointes, hypokalemia, hypomagnesemia, and cardiac arrest can be increased when Piretanide is combined with Dofetilide.Approved
PitolisantThe serum concentration of Dofetilide can be decreased when it is combined with Pitolisant.Approved, Investigational
PolythiazidePolythiazide may increase the QTc-prolonging activities of Dofetilide.Approved
PosaconazoleThe serum concentration of Dofetilide can be increased when it is combined with Posaconazole.Approved, Investigational, Vet Approved
PrimaquinePrimaquine may increase the QTc-prolonging activities of Dofetilide.Approved
PrimidoneThe metabolism of Dofetilide can be increased when combined with Primidone.Approved, Vet Approved
ProcainamideThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Procainamide.Approved
ProchlorperazineThe serum concentration of Dofetilide can be increased when it is combined with Prochlorperazine.Approved, Vet Approved
PromazinePromazine may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
PromethazinePromethazine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
PropafenonePropafenone may increase the arrhythmogenic activities of Dofetilide.Approved
PropofolPropofol may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational, Vet Approved
ProtriptylineProtriptyline may increase the QTc-prolonging activities of Dofetilide.Approved
PyrrolnitrinThe serum concentration of Dofetilide can be increased when it is combined with Pyrrolnitrin.Experimental
QuetiapineThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Quetiapine.Approved
QuinethazoneQuinethazone may increase the QTc-prolonging activities of Dofetilide.Approved
QuinidineThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Quinidine.Approved, Investigational
QuinineThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Quinine.Approved
RadicicolThe serum concentration of Dofetilide can be increased when it is combined with Radicicol.Experimental
RanolazineThe serum concentration of Dofetilide can be increased when it is combined with Ranolazine.Approved, Investigational
RibociclibThe risk or severity of QTc prolongation can be increased when Ribociclib is combined with Dofetilide.Approved, Investigational
RifabutinThe metabolism of Dofetilide can be increased when combined with Rifabutin.Approved, Investigational
RifampicinThe metabolism of Dofetilide can be increased when combined with Rifampicin.Approved
RifapentineThe metabolism of Dofetilide can be increased when combined with Rifapentine.Approved, Investigational
RilpivirineRilpivirine may increase the QTc-prolonging activities of Dofetilide.Approved
RisperidoneRisperidone may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
RitonavirRitonavir may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
RucaparibThe serum concentration of Dofetilide can be increased when it is combined with Rucaparib.Approved, Investigational
SalbutamolSalbutamol may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
Salicylhydroxamic AcidThe serum concentration of Dofetilide can be increased when it is combined with Salicylhydroxamic Acid.Experimental
Salicylic acidThe serum concentration of Dofetilide can be increased when it is combined with Salicylic acid.Approved, Investigational, Vet Approved
SalmeterolSalmeterol may increase the QTc-prolonging activities of Dofetilide.Approved
SaquinavirSaquinavir may increase the arrhythmogenic activities of Dofetilide.Approved, Investigational
SarilumabThe therapeutic efficacy of Dofetilide can be decreased when used in combination with Sarilumab.Approved, Investigational
SertaconazoleThe serum concentration of Dofetilide can be increased when it is combined with Sertaconazole.Approved, Investigational
SertralineSertraline may increase the QTc-prolonging activities of Dofetilide.Approved
SevofluraneSevoflurane may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
SildenafilThe serum concentration of Dofetilide can be increased when it is combined with Sildenafil.Approved, Investigational
SiltuximabThe serum concentration of Dofetilide can be decreased when it is combined with Siltuximab.Approved, Investigational
SimeprevirThe serum concentration of Dofetilide can be increased when it is combined with Simeprevir.Approved
SinefunginThe serum concentration of Dofetilide can be increased when it is combined with Sinefungin.Experimental
SirolimusThe serum concentration of Dofetilide can be increased when it is combined with Sirolimus.Approved, Investigational
SolifenacinSolifenacin may increase the QTc-prolonging activities of Dofetilide.Approved
SorafenibSorafenib may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
SotalolThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Sotalol.Approved
St. John's WortThe serum concentration of Dofetilide can be decreased when it is combined with St. John's Wort.Approved, Investigational, Nutraceutical
StiripentolThe serum concentration of Dofetilide can be increased when it is combined with Stiripentol.Approved
SulconazoleThe serum concentration of Dofetilide can be increased when it is combined with Sulconazole.Approved
SulfamethoxazoleSulfamethoxazole may increase the QTc-prolonging activities of Dofetilide.Approved
SulfisoxazoleThe serum concentration of Dofetilide can be increased when it is combined with Sulfisoxazole.Approved, Vet Approved
SunitinibSunitinib may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
TamoxifenTamoxifen may increase the QTc-prolonging activities of Dofetilide.Approved
TavaboroleThe serum concentration of Dofetilide can be increased when it is combined with Tavaborole.Approved, Investigational
TelaprevirThe serum concentration of Dofetilide can be increased when it is combined with Telaprevir.Approved, Withdrawn
TelavancinTelavancin may increase the QTc-prolonging activities of Dofetilide.Approved
TelithromycinThe serum concentration of Dofetilide can be increased when it is combined with Telithromycin.Approved
TerbinafineThe serum concentration of Dofetilide can be increased when it is combined with Terbinafine.Approved, Investigational, Vet Approved
TerbutalineTerbutaline may increase the QTc-prolonging activities of Dofetilide.Approved
TerconazoleThe serum concentration of Dofetilide can be increased when it is combined with Terconazole.Approved
TetrabenazineThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Tetrabenazine.Approved, Investigational
ThioridazineThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Thioridazine.Approved, Withdrawn
ThiothixeneThiothixene may increase the QTc-prolonging activities of Dofetilide.Approved
ThymolThe serum concentration of Dofetilide can be increased when it is combined with Thymol.Approved
TiclopidineThe serum concentration of Dofetilide can be increased when it is combined with Ticlopidine.Approved
TioconazoleThe serum concentration of Dofetilide can be increased when it is combined with Tioconazole.Approved
TizanidineTizanidine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
TocilizumabThe serum concentration of Dofetilide can be decreased when it is combined with Tocilizumab.Approved
TolciclateThe serum concentration of Dofetilide can be increased when it is combined with Tolciclate.Experimental
TolnaftateThe serum concentration of Dofetilide can be increased when it is combined with Tolnaftate.Approved, Investigational, Vet Approved
TolterodineTolterodine may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
TorasemideThe risk or severity of QTc prolongation, torsade de pointes, hypokalemia, hypomagnesemia, and cardiac arrest can be increased when Torasemide is combined with Dofetilide.Approved
ToremifeneThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Toremifene.Approved, Investigational
TrazodoneTrazodone may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
TreprostinilTreprostinil may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
TriamtereneThe serum concentration of Dofetilide can be increased when it is combined with Triamterene.Approved
TrichlormethiazideTrichlormethiazide may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
TrimethoprimTrimethoprim may decrease the excretion rate of Dofetilide which could result in a higher serum level.Approved, Vet Approved
TrimetrexateThe serum concentration of Dofetilide can be increased when it is combined with Trimetrexate.Approved, Investigational
TrimipramineTrimipramine may increase the QTc-prolonging activities of Dofetilide.Approved
TriptorelinTriptorelin may increase the QTc-prolonging activities of Dofetilide.Approved, Vet Approved
VandetanibThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Vandetanib.Approved
VardenafilVardenafil may increase the QTc-prolonging activities of Dofetilide.Approved
VemurafenibThe risk or severity of QTc prolongation can be increased when Vemurafenib is combined with Dofetilide.Approved
VenlafaxineThe serum concentration of Dofetilide can be increased when it is combined with Venlafaxine.Approved
VerapamilThe serum concentration of Dofetilide can be increased when it is combined with Verapamil.Approved
VilanterolVilanterol may increase the QTc-prolonging activities of Dofetilide.Approved
VoriconazoleThe serum concentration of Dofetilide can be increased when it is combined with Voriconazole.Approved, Investigational
VorinostatVorinostat may increase the QTc-prolonging activities of Dofetilide.Approved, Investigational
WortmanninThe serum concentration of Dofetilide can be increased when it is combined with Wortmannin.Experimental
ZiprasidoneThe serum concentration of Dofetilide can be increased when it is combined with Ziprasidone.Approved
ZuclopenthixolThe risk or severity of QTc prolongation can be increased when Dofetilide is combined with Zuclopenthixol.Approved, Investigational
Food Interactions
Not Available

References

Synthesis Reference
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
Human Metabolome Database
HMDB0014349
KEGG Drug
D00647
KEGG Compound
C07751
PubChem Compound
71329
PubChem Substance
46509127
ChemSpider
64435
BindingDB
50031720
ChEBI
4681
ChEMBL
CHEMBL473
Therapeutic Targets Database
DAP000495
PharmGKB
PA449389
IUPHAR
2604
Guide to Pharmacology
GtP Drug Page
RxList
RxList Drug Page
Drugs.com
Drugs.com Drug Page
Wikipedia
Dofetilide
ATC Codes
C01BD04 — Dofetilide
FDA label
Download (1.45 MB)

Clinical Trials

Clinical Trials
PhaseStatusPurposeConditionsCount
1CompletedBasic ScienceDrug-induced QT Interval Prolongation / Pharmacodynamics / Pharmacokinetics1
1CompletedOtherDrug-induced QT Interval Prolongation / Pharmacodynamics / Pharmacokinetics1
1CompletedTreatmentDrug-induced Surface ECG Changes1
1CompletedTreatmentLong qt Syndrome1
3SuspendedTreatmentNonvalvular Atrial Fibrillation1
3TerminatedTreatmentHeart Failure, Unspecified / Nonvalvular Atrial Fibrillation1
4WithdrawnTreatmentNonvalvular Atrial Fibrillation1
Not AvailableCompletedTreatmentNonvalvular Atrial Fibrillation1
Not AvailableRecruitingNot AvailableLong qt Syndrome / Therapeutic Agent Toxicity1

Pharmacoeconomics

Manufacturers
  • Pfizer pharmaceuticals production corp ltd
Packagers
  • Pfizer Inc.
Dosage forms
FormRouteStrength
CapsuleOral125 ug/1
CapsuleOral250 ug/1
CapsuleOral500 ug/1
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)
US4959366No1992-09-252012-09-25Us
US6124363No1998-10-092018-10-09Us

Properties

State
Solid
Experimental Properties
PropertyValueSource
logP2.1Not Available
Predicted Properties
PropertyValueSource
Water Solubility0.0198 mg/mLALOGPS
logP2.17ALOGPS
logP0.24ChemAxon
logS-4.4ALOGPS
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 RuleNoChemAxon
MDDR-like RuleNoChemAxon
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)

Spectra

Mass Spec (NIST)
Not Available
Spectra
SpectrumSpectrum TypeSplash Key
Predicted GC-MS Spectrum - GC-MSPredicted GC-MSNot Available
Predicted MS/MS Spectrum - 10V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Positive (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 10V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 20V, Negative (Annotated)Predicted LC-MS/MSNot Available
Predicted MS/MS Spectrum - 40V, Negative (Annotated)Predicted LC-MS/MSNot Available
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-1610900000-368db21beef81a5319f4
MS/MS Spectrum - , positiveLC-MS/MSsplash10-0006-0300900000-47394a7ed027cb5ab3cf

Taxonomy

Description
This 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.
Kingdom
Organic compounds
Super Class
Benzenoids
Class
Benzene and substituted derivatives
Sub Class
Sulfanilides
Direct Parent
Sulfanilides
Alternative Parents
Phenethylamines / Phenoxy compounds / Phenol ethers / Aralkylamines / Alkyl aryl ethers / Organosulfonamides / Organic sulfonamides / Aminosulfonyl compounds / Trialkylamines / Organopnictogen compounds
show 2 more
Substituents
Sulfanilide / Phenethylamine / Phenoxy compound / Phenol ether / Alkyl aryl ether / Aralkylamine / Organic sulfonic acid amide / Organosulfonic acid amide / Organic sulfonic acid or derivatives / Organosulfonic acid or derivatives
show 15 more
Molecular Framework
Aromatic homomonocyclic compounds
External Descriptors
tertiary amino compound, aromatic ether, sulfonamide (CHEBI:4681)

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 ...
Gene Name
KCNH2
Uniprot ID
Q12809
Uniprot Name
Potassium voltage-gated channel subfamily H member 2
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...
Gene Name
KCNK2
Uniprot ID
O95069
Uniprot Name
Potassium channel subfamily K member 2
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...
Gene Name
KCNJ12
Uniprot ID
Q14500
Uniprot Name
ATP-sensitive inward rectifier potassium channel 12
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 react...
Gene Name
CYP3A4
Uniprot ID
P08684
Uniprot Name
Cytochrome P450 3A4
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]

Drug created on June 13, 2005 07:24 / Updated on June 02, 2018 06:31