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Tikosyn (Dofetilide)

Pfizer Inc. · FDA-approved approved Small molecule Quality 68/100

Blocks cardiac potassium channel IKr to prolong repolarization and delay arrhythmia recurrence.

Dofetilide (Tikosyn) is a selective Class III antiarrhythmic that blocks the IKr potassium channel to maintain normal sinus rhythm and convert atrial fibrillation/flutter. The drug demonstrates strong efficacy with >90% bioavailability and a 10-hour half-life, enabling convenient twice-daily dosing. Major safety concerns include dose-dependent torsade de pointes (0.8% in supraventricular arrhythmia patients, 3.3% in CHF patients) and numerous drug interactions via renal cation transport inhibition, requiring careful patient selection and baseline QT assessment. Dofetilide remains indicated for highly symptomatic AF/AFl patients despite life-threatening arrhythmia risks, with strict contraindications for long QT syndrome and severe renal impairment.

At a glance

Generic nameDofetilide
SponsorPfizer Inc.
Drug classVaughan Williams Class III antiarrhythmic
TargetIKr potassium channel (rapid component of delayed rectifier potassium current)
ModalitySmall molecule
Therapeutic areaCardiovascular
PhaseFDA-approved

Mechanism of action

Dofetilide is a Class III antiarrhythmic agent that selectively blocks the IKr potassium channel, which carries the rapid component of the delayed rectifier potassium current in cardiac tissue. At clinically relevant concentrations, dofetilide demonstrates selective blockade of IKr with no significant effects on other repolarizing potassium currents (IKs, IK1), sodium channels, or adrenergic receptors. This selective mechanism prolongs the cardiac action potential duration and refractory period, thereby delaying the recurrence of atrial fibrillation and atrial flutter in patients who have been converted to normal sinus rhythm.

Approved indications

Boxed warnings

Common side effects

Serious adverse events

Drug interactions

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