dofetilide

Trade name: tikosyn

Small moleculeapproved

Approved

Oct 1, 1999

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. 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). Used 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. — NCATS

Clinical trial activity

10 trials · 12 clinical orgs · 20 marketing orgs

Phase 1
5
Phase 2
3
Phase 3
2
Phase 4
1

Earliest trial started Aug 1, 2003 (NCT00540787)

Timeline

1990s

  1. Oct 1, 1999

    Pfizer — Earliest FDA Approval

  2. Oct 1, 1999

    Pfizer — NDA Organization

2000s

  1. Jan 1, 2006

    Earliest Phase 3 Sponsor(trial)

2010s

  1. Jan 1, 2013

    Earliest Phase 1 Sponsor(trial)

  2. Jun 6, 2016

    Mayne Pharma — Marketing Organization

  3. Jun 6, 2016

    Dr. Reddy's Laboratories — Marketing Organization

  4. Mar 26, 2018

    Sigmapharm Laboratories — Marketing Organization

  5. Apr 10, 2018

    Bionpharma Inc — Marketing Organization

  6. Oct 9, 2018

    Par Pharmaceuticals — Marketing Organization

  7. Oct 9, 2018

    Sun Pharmaceuticals — Marketing Organization

  8. Oct 9, 2018

    Strides Pharma Science — Marketing Organization

  9. Jan 22, 2019

    Aurobindo Pharma — Marketing Organization

  10. Sep 27, 2019

    Wilshire Pharmaceuticals — Marketing Organization

  11. Dec 17, 2019

    Prinston Inc — Marketing Organization

  12. Dec 27, 2019

    RiconPharma — Marketing Organization

  13. Dec 27, 2019

    Novast Labs — Marketing Organization

2020s

  1. Jan 29, 2020

    MSN Laboratories — Marketing Organization

  2. Jun 19, 2020

    Accord Research — Marketing Organization

  3. Oct 14, 2021

    Granules India — Marketing Organization

  4. Apr 14, 2022

    Vgyaan — Marketing Organization

  5. Apr 14, 2022

    Nuvo Research Inc. — Marketing Organization

  6. Apr 14, 2022

    Apicore — Marketing Organization

  7. Apr 15, 2022

    Teva — Marketing Organization

Indications

Mechanism of action

Approval history

  • approvedOct 1, 1999

Chemistry & pharmacology

Loading structure…

SMILES

CN(CCOC1=CC=C(NS(C)(=O)=O)C=C1)CCC2=CC=C(NS(C)(=O)=O)C=C2
Mol. weight
441.565 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Black box warning

Sources

Also known as

  • 1-(4-methanesulfonamidophenoxy)-2-(n-(4-methanesulfonamidophenethyl)-n-methylamine)ethane
  • 1-mspmpe
  • beta-((p-methanesulfonamidophenethyl)methylamino)methanesulfono-p-phenetidide
  • beta-((p-methanesulfonamidophenethyl)methylamino)methanesulfono-p-phenetidide
  • dofetilida
  • dofetilida
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilide
  • dofetilidum
  • dofetilidum
  • dofetillide
  • tikosyn
  • tikosyn
  • tikosyn
  • tikosyn
  • tikosyn
  • uk 68798
  • uk 68798
  • uk 68798
  • uk 68798
  • uk 68798
  • uk 68798
  • uk-68798
  • uk-68798
  • uk-68,798
  • uk-68,798

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06096337N/ADec 15, 2023Boston Scientific Corporation, The Cleveland Clinic
NCT05906732Phase 1/Phase 2 (Phase 2)Mar 12, 2023Spaulding Clinical Research Inc., Thryv Therapeutics, Inc.
NCT04037397Phase 3Jul 22, 2019Biosense Webster, Inc., Texas Cardiac Arrhythmia Institute, University of Pennsylvania
NCT03070470Phase 1Mar 14, 2017Food and Drug Administration, Spaulding Clinical Research Inc.
NCT02365532Phase 1Feb 1, 2015Gilead Sciences
NCT02308748Phase 1May 1, 2014Food and Drug Administration, Spaulding Clinical Research Inc.
NCT01873950Phase 1May 1, 2013Food and Drug Administration, Spaulding Clinical Research Inc.
NCT00408200N/ANov 1, 2006University of Pennsylvania
NCT00392106Phase 3Apr 1, 2006Johns Hopkins University, ProRhythm, Inc., University of Oklahoma
NCT00540787Phase 4Aug 1, 2003Biosense Webster, Inc.
Showing 10 of 10 trials
Page 1 / 1

Organizations

Research & Development (12)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Spaulding Clinical Research Inc.For profit4022013
Food and Drug AdministrationGovernment3312013
Biosense Webster, Inc.For profit2122003
University of PennsylvaniaAcademic/Hospital2222006
Boston Scientific CorporationFor profit1112023
Gilead SciencesFor profit1112015
Johns Hopkins UniversityAcademic/Hospital1012006
ProRhythm, Inc.For profit1112006
Texas Cardiac Arrhythmia InstituteAcademic/Hospital1012019
The Cleveland ClinicAcademic/Hospital1012023
Thryv Therapeutics, Inc.For profit1112023
University of OklahomaAcademic/Hospital1012006
12 organizations
Page 1 / 1

Marketing (22)

OrganizationOrg typeRelationshipDate
Accord ResearchFor profitMKTGJun 19, 2020
ApicoreFor profitMKTGApr 14, 2022
Aurobindo PharmaFor profitMKTGJan 22, 2019
Bionpharma IncFor profitMKTGApr 10, 2018
Bionpharma IncFor profitSYNApr 10, 2018
Dr. Reddy's LaboratoriesFor profitMKTGJun 6, 2016
Granules IndiaFor profitMKTGOct 14, 2021
MSN LaboratoriesFor profitMKTGJan 29, 2020
Mayne PharmaFor profitMKTGJun 6, 2016
Novast LabsFor profitMKTGDec 27, 2019
Nuvo Research Inc.For profitMKTGApr 14, 2022
Par PharmaceuticalsFor profitMKTGOct 9, 2018
PfizerFor profitNDAOct 1, 1999
Prinston IncFor profitMKTGDec 17, 2019
RiconPharmaFor profitMKTGDec 27, 2019
Sigmapharm LaboratoriesFor profitMKTGMar 26, 2018
Strides Pharma ScienceFor profitMKTGOct 9, 2018
Sun PharmaceuticalsFor profitMKTGOct 9, 2018
Sun PharmaceuticalsFor profitSYNOct 9, 2018
TevaFor profitMKTGApr 15, 2022
VgyaanFor profitMKTGApr 14, 2022
Wilshire PharmaceuticalsFor profitMKTGSep 27, 2019