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Chemical Compound Review

Tikosyn     N-[4-[2-[methyl-[2-[4- (methylsulfonylamino...

Synonyms: Dofetilida, Dofetilide, Xelide, Dofetilidum, Dofetilide;, ...
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Disease relevance of Tikosyn


Psychiatry related information on Tikosyn


High impact information on Tikosyn


Chemical compound and disease context of Tikosyn


Biological context of Tikosyn

  • Influence of dofetilide on QT-interval duration and dispersion at various heart rates during exercise in humans [12].
  • The activating currents displayed inward rectification and deactivating current tails were voltage-dependent, saturated at >>+20 mV, and were highly sensitive to dofetilide (IC50 of 46.9 nM) [13].
  • To assess physiological significance, dofetilide-sensitive currents were recorded during application of simulated action potential clamps [14].
  • OBJECTIVES: To examine the pharmacokinetics and the relation between plasma concentrations of the new potassium channel blocker dofetilide and QTc prolongation on the surface electrocardiogram after oral and intravenous administration [15].
  • This pattern suggested that dofetilide preferentially blocks open (or activated) channels and that the fast inactivation may competitively slow the binding kinetics [16].

Anatomical context of Tikosyn


Associations of Tikosyn with other chemical compounds

  • Elevating [K+]o from 1 to 8 mmol/L increased the IC50 for dofetilide block from 2.7 +/- 0.9 to 79 +/- 32 nmol/L and for quinidine block from 0.4 +/- 0.1 to 3.8 +/- 1.2 mumol/L [21].
  • Thus, the serine in position HERG 620 may participate directly in dofetilide binding; however, an intact C-type inactivation process seems to be crucial for high-affinity drug binding [19].
  • HERG/I(Kr) channels are blocked selectively by class III antiarrhythmic methanesulfonanilide drugs such as dofetilide [22].
  • Corresponding baseline recording periods, Ch and C1, matched by time with Dh and D1 were selected from the control ECG recording in the absence of dofetilide [23].
  • Recent data show that maintenance of sinus rhythm after successful cardioversion is enhanced by the use of class III drugs including amiodarone and dofetilide [24].

Gene context of Tikosyn


Analytical, diagnostic and therapeutic context of Tikosyn


  1. Dofetilide for atrial fibrillation. Rubin, S.A. N. Engl. J. Med. (2000) [Pubmed]
  2. Dofetilide in patients with congestive heart failure and left ventricular dysfunction. Danish Investigations of Arrhythmia and Mortality on Dofetilide Study Group. Torp-Pedersen, C., Møller, M., Bloch-Thomsen, P.E., Køber, L., Sandøe, E., Egstrup, K., Agner, E., Carlsen, J., Videbaek, J., Marchant, B., Camm, A.J. N. Engl. J. Med. (1999) [Pubmed]
  3. Effect of dofetilide in patients with recent myocardial infarction and left-ventricular dysfunction: a randomised trial. Køber, L., Bloch Thomsen, P.E., Møller, M., Torp-Pedersen, C., Carlsen, J., Sandøe, E., Egstrup, K., Agner, E., Videbaek, J., Marchant, B., Camm, A.J. Lancet (2000) [Pubmed]
  4. Qtc interval as a guide to select those patients with congestive heart failure and reduced left ventricular systolic function who will benefit from antiarrhythmic treatment with dofetilide. Brendorp, B., Elming, H., Jun, L., Køber, L., Malik, M., Jensen, G.B., Torp-Pedersen, C. Circulation (2001) [Pubmed]
  5. In vivo identification of genes that modify ether-a-go-go-related gene activity in Caenorhabditis elegans may also affect human cardiac arrhythmia. Petersen, C.I., McFarland, T.R., Stepanovic, S.Z., Yang, P., Reiner, D.J., Hayashi, K., George, A.L., Roden, D.M., Thomas, J.H., Balser, J.R. Proc. Natl. Acad. Sci. U.S.A. (2004) [Pubmed]
  6. Electrophysiological effects of dofetilide in an in vitro model of "border zone" between normal and ischemic/reperfused myocardium. Rouet, R., Picard, S., Libersa, C., Ghadanfar, M., Alabaster, C., Gérard, J.L. Circulation (2000) [Pubmed]
  7. Comparison of intravenously administered dofetilide versus amiodarone in the acute termination of atrial fibrillation and flutter. A multicentre, randomized, double-blind, placebo-controlled study. Bianconi, L., Castro, A., Dinelli, M., Alboni, P., Pappalardo, A., Richiardi, E., Santini, M. Eur. Heart J. (2000) [Pubmed]
  8. Atrial flutter can be terminated by a class III antiarrhythmic drug but not by a class IC drug. Crijns, H.J., Van Gelder, I.C., Kingma, J.H., Dunselman, P.H., Gosselink, A.T., Lie, K.I. Eur. Heart J. (1994) [Pubmed]
  9. RSD1235 blocks late INa and suppresses early afterdepolarizations and torsades de pointes induced by class III agents. Orth, P.M., Hesketh, J.C., Mak, C.K., Yang, Y., Lin, S., Beatch, G.N., Ezrin, A.M., Fedida, D. Cardiovasc. Res. (2006) [Pubmed]
  10. Class III antiarrhythmic action by potassium channel blockade: dofetilide attenuates hypoxia induced electromechanical changes. Yang, T., Tande, P.M., Lathrop, D.A., Refsum, H. Cardiovasc. Res. (1992) [Pubmed]
  11. Dofetilide: a review of its use in atrial fibrillation and atrial flutter. McClellan, K.J., Markham, A. Drugs (1999) [Pubmed]
  12. Influence of dofetilide on QT-interval duration and dispersion at various heart rates during exercise in humans. Démolis, J.L., Funck-Brentano, C., Ropers, J., Ghadanfar, M., Nichols, D.J., Jaillon, P. Circulation (1996) [Pubmed]
  13. HL-1 cells: a cardiac muscle cell line that contracts and retains phenotypic characteristics of the adult cardiomyocyte. Claycomb, W.C., Lanson, N.A., Stallworth, B.S., Egeland, D.B., Delcarpio, J.B., Bahinski, A., Izzo, N.J. Proc. Natl. Acad. Sci. U.S.A. (1998) [Pubmed]
  14. Novel gain-of-function mechanism in K(+) channel-related long-QT syndrome: altered gating and selectivity in the HERG1 N629D mutant. Lees-Miller, J.P., Duan, Y., Teng, G.Q., Thorstad, K., Duff, H.J. Circ. Res. (2000) [Pubmed]
  15. Pharmacokinetic and pharmacodynamic modeling of the effects of oral and intravenous administrations of dofetilide on ventricular repolarization. Le Coz, F., Funck-Brentano, C., Morell, T., Ghadanfar, M.M., Jaillon, P. Clin. Pharmacol. Ther. (1995) [Pubmed]
  16. High affinity open channel block by dofetilide of HERG expressed in a human cell line. Snyders, D.J., Chaudhary, A. Mol. Pharmacol. (1996) [Pubmed]
  17. Ibutilide, a methanesulfonanilide antiarrhythmic, is a potent blocker of the rapidly activating delayed rectifier K+ current (IKr) in AT-1 cells. Concentration-, time-, voltage-, and use-dependent effects. Yang, T., Snyders, D.J., Roden, D.M. Circulation (1995) [Pubmed]
  18. Electrophysiological mechanisms in a canine model of erythromycin-associated long QT syndrome. Rubart, M., Pressler, M.L., Pride, H.P., Zipes, D.P. Circulation (1993) [Pubmed]
  19. Molecular determinants of dofetilide block of HERG K+ channels. Ficker, E., Jarolimek, W., Kiehn, J., Baumann, A., Brown, A.M. Circ. Res. (1998) [Pubmed]
  20. Effect of dofetilide on cardiac repolarization in patients with ventricular tachycardia. A study using simultaneous monophasic action potential recordings from two sites in the right ventricle. Yuan, S., Wohlfart, B., Rasmussen, H.S., Olsson, S., Blomström-Lundqvist, C. Eur. Heart J. (1994) [Pubmed]
  21. Extracellular potassium modulation of drug block of IKr. Implications for torsade de pointes and reverse use-dependence. Yang, T., Roden, D.M. Circulation (1996) [Pubmed]
  22. Molecular determinants of inactivation and dofetilide block in ether a-go-go (EAG) channels and EAG-related K(+) channels. Ficker, E., Jarolimek, W., Brown, A.M. Mol. Pharmacol. (2001) [Pubmed]
  23. Dynamic analysis of dofetilide-induced changes in ventricular repolarization. Lande, G., Maison-Blanche, P., Fayn, J., Ghadanfar, M., Coumel, P., Funck-Brentano, C. Clin. Pharmacol. Ther. (1998) [Pubmed]
  24. Current management of symptomatic atrial fibrillation. Channer, K.S. Drugs (2001) [Pubmed]
  25. Significance of metabolism in the disposition and action of the antidysrhythmic drug, dofetilide. In vitro studies and correlation with in vivo data. Walker, D.K., Alabaster, C.T., Congrave, G.S., Hargreaves, M.B., Hyland, R., Jones, B.C., Reed, L.J., Smith, D.A. Drug Metab. Dispos. (1996) [Pubmed]
  26. Molecular biology of the long QT syndrome: impact on management. Priori, S.G., Napolitano, C., Paganini, V., Cantù, F., Schwartz, P.J. Pacing and clinical electrophysiology : PACE. (1997) [Pubmed]
  27. Electrophysiological characterization of an alternatively processed ERG K+ channel in mouse and human hearts. Lees-Miller, J.P., Kondo, C., Wang, L., Duff, H.J. Circ. Res. (1997) [Pubmed]
  28. A molecular basis for the therapy of the long QT syndrome. Priori, S.G., Napolitano, C., Schwartz, P.J. Archives des maladies du coeur et des vaisseaux. (1996) [Pubmed]
  29. Cloned human inward rectifier K+ channel as a target for class III methanesulfonanilides. Kiehn, J., Wible, B., Ficker, E., Taglialatela, M., Brown, A.M. Circ. Res. (1995) [Pubmed]
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