dofetilide
Trade name: tikosyn
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
Earliest trial started Aug 1, 2003 (NCT00540787)
Timeline
2000s
- Jan 1, 2006
Earliest Phase 3 Sponsor(trial)
2010s
- Jan 1, 2013
Earliest Phase 1 Sponsor(trial)
- Jun 6, 2016
Mayne Pharma — Marketing Organization
- Jun 6, 2016
Dr. Reddy's Laboratories — Marketing Organization
- Mar 26, 2018
Sigmapharm Laboratories — Marketing Organization
- Apr 10, 2018
Bionpharma Inc — Marketing Organization
- Oct 9, 2018
Par Pharmaceuticals — Marketing Organization
- Oct 9, 2018
Sun Pharmaceuticals — Marketing Organization
- Oct 9, 2018
Strides Pharma Science — Marketing Organization
- Jan 22, 2019
Aurobindo Pharma — Marketing Organization
- Sep 27, 2019
Wilshire Pharmaceuticals — Marketing Organization
- Dec 17, 2019
Prinston Inc — Marketing Organization
- Dec 27, 2019
RiconPharma — Marketing Organization
- Dec 27, 2019
Novast Labs — Marketing Organization
2020s
- Jan 29, 2020
MSN Laboratories — Marketing Organization
- Jun 19, 2020
Accord Research — Marketing Organization
- Oct 14, 2021
Granules India — Marketing Organization
- Apr 14, 2022
Vgyaan — Marketing Organization
- Apr 14, 2022
Nuvo Research Inc. — Marketing Organization
- Apr 14, 2022
Apicore — Marketing Organization
- Apr 15, 2022
Teva — Marketing Organization
Indications
Mechanism of action
- HERGBLOCKER
KCNH2 blocker
Approval history
- approvedOct 1, 1999
Chemistry & pharmacology
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
Sources
- WikipediaDofetilide ↗
- NCATSR4Z9X1N2ND ↗
- ChEMBLCHEMBL473 ↗
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 ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT06096337 | N/A | Dec 15, 2023 | Boston Scientific Corporation, The Cleveland Clinic |
| NCT05906732 | Phase 1/Phase 2 (Phase 2) | Mar 12, 2023 | Spaulding Clinical Research Inc., Thryv Therapeutics, Inc. |
| NCT04037397 | Phase 3 | Jul 22, 2019 | Biosense Webster, Inc., Texas Cardiac Arrhythmia Institute, University of Pennsylvania |
| NCT03070470 | Phase 1 | Mar 14, 2017 | Food and Drug Administration, Spaulding Clinical Research Inc. |
| NCT02365532 | Phase 1 | Feb 1, 2015 | Gilead Sciences |
| NCT02308748 | Phase 1 | May 1, 2014 | Food and Drug Administration, Spaulding Clinical Research Inc. |
| NCT01873950 | Phase 1 | May 1, 2013 | Food and Drug Administration, Spaulding Clinical Research Inc. |
| NCT00408200 | N/A | Nov 1, 2006 | University of Pennsylvania |
| NCT00392106 | Phase 3 | Apr 1, 2006 | Johns Hopkins University, ProRhythm, Inc., University of Oklahoma |
| NCT00540787 | Phase 4 | Aug 1, 2003 | Biosense Webster, Inc. |
Organizations
Research & Development (12)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Spaulding Clinical Research Inc. | For profit | 4 | 0 | 2 | 2013 |
| Food and Drug Administration | Government | 3 | 3 | 1 | 2013 |
| Biosense Webster, Inc. | For profit | 2 | 1 | 2 | 2003 |
| University of Pennsylvania | Academic/Hospital | 2 | 2 | 2 | 2006 |
| Boston Scientific Corporation | For profit | 1 | 1 | 1 | 2023 |
| Gilead Sciences | For profit | 1 | 1 | 1 | 2015 |
| Johns Hopkins University | Academic/Hospital | 1 | 0 | 1 | 2006 |
| ProRhythm, Inc. | For profit | 1 | 1 | 1 | 2006 |
| Texas Cardiac Arrhythmia Institute | Academic/Hospital | 1 | 0 | 1 | 2019 |
| The Cleveland Clinic | Academic/Hospital | 1 | 0 | 1 | 2023 |
| Thryv Therapeutics, Inc. | For profit | 1 | 1 | 1 | 2023 |
| University of Oklahoma | Academic/Hospital | 1 | 0 | 1 | 2006 |
Marketing (22)
| Organization | Org type | Relationship | Date |
|---|---|---|---|
| Accord Research | For profit | MKTG | Jun 19, 2020 |
| Apicore | For profit | MKTG | Apr 14, 2022 |
| Aurobindo Pharma | For profit | MKTG | Jan 22, 2019 |
| Bionpharma Inc | For profit | MKTG | Apr 10, 2018 |
| Bionpharma Inc | For profit | SYN | Apr 10, 2018 |
| Dr. Reddy's Laboratories | For profit | MKTG | Jun 6, 2016 |
| Granules India | For profit | MKTG | Oct 14, 2021 |
| MSN Laboratories | For profit | MKTG | Jan 29, 2020 |
| Mayne Pharma | For profit | MKTG | Jun 6, 2016 |
| Novast Labs | For profit | MKTG | Dec 27, 2019 |
| Nuvo Research Inc. | For profit | MKTG | Apr 14, 2022 |
| Par Pharmaceuticals | For profit | MKTG | Oct 9, 2018 |
| Pfizer | For profit | NDA | Oct 1, 1999 |
| Prinston Inc | For profit | MKTG | Dec 17, 2019 |
| RiconPharma | For profit | MKTG | Dec 27, 2019 |
| Sigmapharm Laboratories | For profit | MKTG | Mar 26, 2018 |
| Strides Pharma Science | For profit | MKTG | Oct 9, 2018 |
| Sun Pharmaceuticals | For profit | MKTG | Oct 9, 2018 |
| Sun Pharmaceuticals | For profit | SYN | Oct 9, 2018 |
| Teva | For profit | MKTG | Apr 15, 2022 |
| Vgyaan | For profit | MKTG | Apr 14, 2022 |
| Wilshire Pharmaceuticals | For profit | MKTG | Sep 27, 2019 |