Page last updated: 2024-10-26

e 4031 and Torsade de Pointes

e 4031 has been researched along with Torsade de Pointes in 19 studies

E 4031: class III anti-arrhythmia agent; structure given in UD

Research Excerpts

ExcerptRelevanceReference
"We examined the cellular and ionic mechanism for QT prolongation and subsequent Torsade de Pointes (TdP) and the effect of verapamil under conditions mimicking KCNQ1 (I(Ks) gene) defect linked to acquired long QT syndrome (LQTS)."7.73Cellular and ionic mechanism for drug-induced long QT syndrome and effectiveness of verapamil. ( Aiba, T; Ding, WG; Horie, M; Inagaki, M; Matsuura, H; Miyoshi, S; Noda, T; Shimizu, W; Sunagawa, K; Toyoda, F; Zankov, DP, 2005)
"We examined the cellular and ionic mechanism for QT prolongation and subsequent Torsade de Pointes (TdP) and the effect of verapamil under conditions mimicking KCNQ1 (I(Ks) gene) defect linked to acquired long QT syndrome (LQTS)."3.73Cellular and ionic mechanism for drug-induced long QT syndrome and effectiveness of verapamil. ( Aiba, T; Ding, WG; Horie, M; Inagaki, M; Matsuura, H; Miyoshi, S; Noda, T; Shimizu, W; Sunagawa, K; Toyoda, F; Zankov, DP, 2005)
"We analyzed torsadogenic and pharmacokinetic profile of E-4031 using chronic atrioventricular block dogs."1.48Analysis of torsadogenic and pharmacokinetic profile of E-4031 in dogs bridging the gap of information between in vitro proarrhythmia assay and clinical observation in human subjects. ( Ando, K; Chiba, K; Goto, A; Hagiwara-Nagasawa, M; Izumi-Nakaseko, H; Naito, AT; Sugiyama, A, 2018)
"Arrhythmic outcome was defined as Torsade de Pointes (TdP) in the animal models and early afterdepolarizations (EADs) in the cell models."1.38Comparison of the IKr blockers moxifloxacin, dofetilide and E-4031 in five screening models of pro-arrhythmia reveals lack of specificity of isolated cardiomyocytes. ( Beekman, JD; de Boer, TP; Duker, G; Houtman, MJ; Jonsson, MK; Nalos, L; Peschar, M; Rook, MB; Sartipy, P; Thomsen, MB; van der Heyden, MA; van der Nagel, R; van Veen, TA; Varkevisser, R; Vos, MA, 2012)
"Fluoxetine (Prozac) was more potent at blocking hERG 1a/1b than 1a channels, yielding a corresponding reduction in the safety margin."1.37hERG subunit composition determines differential drug sensitivity. ( Abi-Gerges, N; Holkham, H; Jones, EM; Pollard, CE; Robertson, GA; Valentin, JP, 2011)
"However, the cycle length of the arrhythmia with quinidine was longer than that for control ([mean +/- SEM] 194 +/- 12 vs."1.30Optical mapping of drug-induced polymorphic arrhythmias and torsade de pointes in the isolated rabbit heart. ( Asano, Y; Baxter, WT; Davidenko, JM; Gray, RA; Jalife, J, 1997)
"Tamoxifen is an antiestrogen drug commonly used to treat breast cancer and has been shown to cause prolongation of the electrocardiographic QT interval in humans."1.30The antiestrogen tamoxifen blocks the delayed rectifier potassium current, IKr, in rabbit ventricular myocytes. ( Ebert, SN; Katchman, A; Liu, XK; Woosley, RL, 1998)
" Agents were compared over dosage ranges that produced maximal increases in QTc interval and monophasic action potential duration (MAPD)."1.29Comparative assessment of ibutilide, D-sotalol, clofilium, E-4031, and UK-68,798 in a rabbit model of proarrhythmia. ( Brunden, MN; Buchanan, LV; Gibson, JK; Kabell, G, 1993)

Research

Studies (19)

TimeframeStudies, this research(%)All Research%
pre-19900 (0.00)18.7374
1990's4 (21.05)18.2507
2000's7 (36.84)29.6817
2010's8 (42.11)24.3611
2020's0 (0.00)2.80

Authors

AuthorsStudies
Wiśniowska, B1
Mendyk, A1
Fijorek, K1
Glinka, A1
Polak, S1
Goto, A1
Izumi-Nakaseko, H1
Hagiwara-Nagasawa, M1
Chiba, K1
Ando, K1
Naito, AT1
Sugiyama, A2
Wang, WL1
Zhang, SS1
Deng, J1
Zhao, JY1
Zhao, CQ1
Lin, L1
Zhang, CT1
Lv, JG1
Yamamoto, W1
Asakura, K1
Ando, H1
Taniguchi, T1
Ojima, A1
Uda, T1
Osada, T1
Hayashi, S1
Kasai, C1
Miyamoto, N1
Tashibu, H1
Yoshinaga, T1
Yamazaki, D1
Kanda, Y1
Sawada, K1
Sekino, Y1
Wu, L2
Rajamani, S1
Li, H2
January, CT1
Shryock, JC2
Belardinelli, L2
Abi-Gerges, N1
Holkham, H1
Jones, EM1
Pollard, CE1
Valentin, JP1
Robertson, GA1
Ma, J1
Wang, C1
Grandi, E1
Zhang, P1
Luo, A1
Bers, DM1
Nalos, L1
Varkevisser, R1
Jonsson, MK1
Houtman, MJ1
Beekman, JD1
van der Nagel, R1
Thomsen, MB1
Duker, G1
Sartipy, P1
de Boer, TP1
Peschar, M1
Rook, MB1
van Veen, TA1
van der Heyden, MA1
Vos, MA1
Said, TH1
Wilson, LD1
Jeyaraj, D1
Fossa, AA1
Rosenbaum, DS1
Choi, BR1
Burton, F1
Salama, G1
Fish, JM1
Di Diego, JM1
Nesterenko, V1
Antzelevitch, C2
Aiba, T1
Shimizu, W1
Inagaki, M1
Noda, T1
Miyoshi, S1
Ding, WG1
Zankov, DP1
Toyoda, F1
Matsuura, H1
Horie, M1
Sunagawa, K1
Michael, G2
Dempster, J1
Kane, KA2
Coker, SJ2
Buchanan, LV1
Kabell, G1
Brunden, MN1
Gibson, JK1
Asano, Y1
Davidenko, JM1
Baxter, WT1
Gray, RA1
Jalife, J1
Burashnikov, A1
Liu, XK1
Katchman, A1
Ebert, SN1
Woosley, RL1
Miyashita, T1
Kubota, I1
Yamaki, M1
Watanabe, T1
Yamauchi, S1
Tomoike, H1

Clinical Trials (1)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
A Randomized Trial of Tamoxifen Combined With Amphotericin B and Fluconazole for Cryptococcal Meningitis[NCT03112031]Phase 250 participants (Actual)Interventional2017-10-10Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]

Other Studies

19 other studies available for e 4031 and Torsade de Pointes

ArticleYear
Predictive model for L-type channel inhibition: multichannel block in QT prolongation risk assessment.
    Journal of applied toxicology : JAT, 2012, Volume: 32, Issue:10

    Topics: Artificial Intelligence; Calcium Channel Blockers; Calcium Channels, L-Type; Cell Line; Computationa

2012
Analysis of torsadogenic and pharmacokinetic profile of E-4031 in dogs bridging the gap of information between in vitro proarrhythmia assay and clinical observation in human subjects.
    Journal of pharmacological sciences, 2018, Volume: 137, Issue:2

    Topics: Animals; Anti-Arrhythmia Agents; Atrioventricular Block; Chronic Disease; Dogs; Dose-Response Relati

2018
KN-93, A CaMKII inhibitor, suppresses ventricular arrhythmia induced by LQT2 without decreasing TDR.
    Journal of Huazhong University of Science and Technology. Medical sciences = Hua zhong ke ji da xue xue bao. Yi xue Ying De wen ban = Huazhong keji daxue xuebao. Yixue Yingdewen ban, 2013, Volume: 33, Issue:5

    Topics: Action Potentials; Animals; Anti-Arrhythmia Agents; Arrhythmias, Cardiac; Benzylamines; Calcium-Calm

2013
Electrophysiological Characteristics of Human iPSC-Derived Cardiomyocytes for the Assessment of Drug-Induced Proarrhythmic Potential.
    PloS one, 2016, Volume: 11, Issue:12

    Topics: Cells, Cultured; Chromans; Cisapride; Electrophysiological Phenomena; Heart Rate; Humans; Induced Pl

2016
Reduction of repolarization reserve unmasks the proarrhythmic role of endogenous late Na(+) current in the heart.
    American journal of physiology. Heart and circulatory physiology, 2009, Volume: 297, Issue:3

    Topics: 4-Aminopyridine; Acetanilides; Action Potentials; Animals; Anti-Arrhythmia Agents; Barium Compounds;

2009
hERG subunit composition determines differential drug sensitivity.
    British journal of pharmacology, 2011, Volume: 164, Issue:2b

    Topics: Action Potentials; Arrhythmias, Cardiac; Cell Line, Transformed; Drug Evaluation, Preclinical; Ether

2011
Late sodium current contributes to the reverse rate-dependent effect of IKr inhibition on ventricular repolarization.
    Circulation, 2011, Apr-26, Volume: 123, Issue:16

    Topics: Acetanilides; Action Potentials; Animals; Anti-Arrhythmia Agents; Bradycardia; Disease Models, Anima

2011
Comparison of the IKr blockers moxifloxacin, dofetilide and E-4031 in five screening models of pro-arrhythmia reveals lack of specificity of isolated cardiomyocytes.
    British journal of pharmacology, 2012, Volume: 165, Issue:2

    Topics: Action Potentials; Animals; Anti-Arrhythmia Agents; Aza Compounds; Cell Line; Disease Models, Animal

2012
Transmural dispersion of repolarization as a preclinical marker of drug-induced proarrhythmia.
    Journal of cardiovascular pharmacology, 2012, Volume: 60, Issue:2

    Topics: Action Potentials; Animals; Bepridil; Dogs; Dose-Response Relationship, Drug; Electrocardiography; E

2012
Cytosolic Ca2+ triggers early afterdepolarizations and Torsade de Pointes in rabbit hearts with type 2 long QT syndrome.
    The Journal of physiology, 2002, Sep-01, Volume: 543, Issue:Pt 2

    Topics: Animals; Anti-Arrhythmia Agents; Artifacts; Calcium; Calcium Signaling; Cryosurgery; Cytosol; Female

2002
Epicardial activation of left ventricular wall prolongs QT interval and transmural dispersion of repolarization: implications for biventricular pacing.
    Circulation, 2004, May-04, Volume: 109, Issue:17

    Topics: Action Potentials; Animals; Anti-Arrhythmia Agents; Cardiac Pacing, Artificial; Cisapride; Computer

2004
Cellular and ionic mechanism for drug-induced long QT syndrome and effectiveness of verapamil.
    Journal of the American College of Cardiology, 2005, Jan-18, Volume: 45, Issue:2

    Topics: Action Potentials; Animals; Anti-Arrhythmia Agents; Calcium Channel Blockers; Cats; Chromans; Heart;

2005
Potentiation of E-4031-induced torsade de pointes by HMR1556 or ATX-II is not predicted by action potential short-term variability or triangulation.
    British journal of pharmacology, 2007, Volume: 152, Issue:8

    Topics: Action Potentials; Animals; Chromans; Cnidarian Venoms; Delayed Rectifier Potassium Channels; Dose-R

2007
Adrenaline reveals the torsadogenic effect of combined blockade of potassium channels in anaesthetized guinea pigs.
    British journal of pharmacology, 2008, Volume: 154, Issue:7

    Topics: Action Potentials; Animals; Chromans; Delayed Rectifier Potassium Channels; Dose-Response Relationsh

2008
Comparative assessment of ibutilide, D-sotalol, clofilium, E-4031, and UK-68,798 in a rabbit model of proarrhythmia.
    Journal of cardiovascular pharmacology, 1993, Volume: 22, Issue:4

    Topics: Animals; Anti-Arrhythmia Agents; Blood Pressure; Electrocardiography; Heart Conduction System; Heart

1993
Optical mapping of drug-induced polymorphic arrhythmias and torsade de pointes in the isolated rabbit heart.
    Journal of the American College of Cardiology, 1997, Mar-15, Volume: 29, Issue:4

    Topics: Action Potentials; Animals; Anti-Arrhythmia Agents; Arrhythmias, Cardiac; Electrocardiography; Heart

1997
Acceleration-induced action potential prolongation and early afterdepolarizations.
    Journal of cardiovascular electrophysiology, 1998, Volume: 9, Issue:9

    Topics: Action Potentials; Animals; Anti-Arrhythmia Agents; Calcium Channel Blockers; Disease Models, Animal

1998
The antiestrogen tamoxifen blocks the delayed rectifier potassium current, IKr, in rabbit ventricular myocytes.
    The Journal of pharmacology and experimental therapeutics, 1998, Volume: 287, Issue:3

    Topics: Animals; Anti-Arrhythmia Agents; Dose-Response Relationship, Drug; Estrogen Antagonists; Heart Ventr

1998
4-aminopyridine inhibits the occurrence of ventricular fibrillation but not ventricular tachycardia in the reperfused, P6olated rat heart.
    Japanese circulation journal, 2000, Volume: 64, Issue:8

    Topics: 4-Aminopyridine; Animals; Anti-Arrhythmia Agents; Blood Flow Velocity; Glyburide; Heart; Heart Rate;

2000