生物活性

• 描述Dofetilide is an antiarrhythmic drug that selectively inhibits the rapid component of the delayed rectifier potassium current. The administration of dofetilide may cause ventricular arrhythmias and torsade de pointes^[3]. Dofetilide preferentially blocks open (or activated) channels and that the fast inactivation may competitively slow the binding kinetics. Dofetilide acts as a slow-onset/slow-offset open channel blocker of this current at nanomolar concentrations^[4]. Dofetilide was found to be safe in patients after myocardial infarction and those with congestive heart failure and left ventricular systolic dysfunction (ejection fraction of less than 35%). Because dofetilide has about an 80% renal excretion, dose adjustment is required in patients with impaired renal function^[5].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00578617	-	-	Completed	-	-
  NCT00578617	Atrial Fibrillation ... more >> Arrhythmia Collapse <<	Not Applicable	Completed	-	United States, Alabama ... more >> Universtity of Alabama Hospital Birminham, Alabama, United States, 35233 United States, California Good Samaritan Hospital Los Angeles, California, United States, 90017 United States, Illinois Loyola University Maywood, Illinois, United States, 60626 United States, Iowa Mercy Medical Center Des Moines, Iowa, United States, 50314 United States, Maryland Johns Hopkins Hospital Baltimore, Maryland, United States, 21287 United States, Massachusetts Brigham and Womens Hospital Boston, Massachusetts, United States, 02115 United States, Minnesota Mayo Clinic Rochester, Minnesota, United States, 55902 United States, Ohio Ohio State University Medical Center Columbus, Ohio, United States, 43210 United States, Pennsylvania University of Pennsylvania Health Philadelphia, Pennsylvania, United States, 19104 United States, Utah Intermountain Medical Center Murray, Utah, United States, 84157 Collapse <<
  NCT00911508	Atrial Fibrillation ... more >> Arrhythmia Collapse <<	Not Applicable	Completed	-	-

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• 参考文献

• [1] Bauer A, Becker R, et al. Effects of the I(Kr)-blocking agent dofetilide and of the I(Ks)-blocking agent chromanol 293b on regional disparity of left ventricular repolarization in the intact canine heart. J Cardiovasc Pharmacol. 2002 Mar;39(3):460-7.

  [2] Kiehn J, Lacerda AE, et al. Molecular physiology and pharmacology of HERG. Single-channel currents and block by dofetilide. Circulation. 1996 Nov 15;94(10):2572-9.

  [3] Marcantoni I, Laratta R, Mascia G, et al. Dofetilide-Induced Microvolt T-Wave Alternans. Conf Proc IEEE Eng Med Biol Soc. 2019;2019:95-98

  [4] Snyders DJ, Chaudhary A. High affinity open channel block by dofetilide of HERG expressed in a human cell line. Mol Pharmacol. 1996;49(6):949-955

  [5] Shenasa F, Shenasa M. Dofetilide: Electrophysiologic Effect, Efficacy, and Safety in Patients with Cardiac Arrhythmias. Card Electrophysiol Clin. 2016;8(2):423-436

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